28/06/2016 From GENETICS to EPIGENETICS .. to Primary Prevention ERNESTO BURGIO ISDE Scientific Committee ECERI - European Cancer and Environment Research Institute Relative frequency of articles with epigenetic or epigenetics in their title David Haig Int. J. Epidemiol. 2012;41:13-16 Foreword 1 1 28/06/2016 The rate of increase of genome-scale publications addressing cancer genetics has become greater than that of publications in the same area focused on selected genes In the past 10 years, according to PubMed, 22 277 articles with the word obesity in the title have been published. If the search is extended to articles with obesity in the title or abstract, the number triples to 66 159 Lancet (2011) 378(9793):760 Number of New York Times articles mentioning obesity and related comorbidities 2 28/06/2016 A quick search for “Microbiome” in scienctific journals online demonstrates how significantly this field of research has been growing over the past ten years 3 28/06/2016 Published papers about endocrine disruptors between 1993 and november 2006 (Gies) Colborn, vom Saal, Soto (1993): EHP endocrine disruptors Fetal programming 3 Ontogeny 4 Developmental Plasticity Evolutionary Medicine Phylogeny 5 Devo-Evo Mismatch 6 7 2 Environment 1 From Genetics to Epigenetics Is there a Project ? XXI Century Epidemiological Transition La transizione epidemiologica del XX secolo: dalla genetica all'epigenetica ERNESTO BURGIO ISDE Scientific Committee ECERI - European Cancer and Environment Research Institute 4 28/06/2016 We are currently facing a paradigm shift in biomedicine For the last 50 years it was agreed to consider DNA as the code and the key project for the assembly of our phenotype. In the last ten years and especially since the appearance of the first molecular epigenetic studies we have begun to understand that the construction of the phenotype is the result of the interaction between the information coming from the environment and the information deeply inscribed inside the DNA thanks to a very complex molecular network surrounding DNA: the epigenome Therefore it can be argued that there is no stable change in our phenotype (both physiological and pathological) which is not - environmentally induced - modulated by the epigenome - conditioned by the DNA Other key concepts (obviously interdependent) are: - developmental plasticity - fetal programming allow ing us to understand how the fetus epigenetically program (for life) all its cells in a predictive and adaptive way responding to information coming from the environment (through the mother bias ) It is important to note that in this period incorrect information ( pollutants, endocrine disruptors ..) and /or discrepancies between the information that the baby receives before and after birth (mismatch) may create epigenetically bad programmed cells (including gametes), thus causing chronic diseases in adulthood or even in subsequent generations This theory (DOHaD Developmental Origins of Health and Disease) could help us to explain the current epidemiological transition .. 5 28/06/2016 The first keyword: Epigenetics Mitotic chromosome Heterochromatin to recognize in the study of epigenetics the most appropriate and powerful tool to build up a new systemic and molecular model of genome .. finally understood as a dynamic and fluid network which can interact inside itself and with the outside Euchromatin Interphase chromosomes Le Dogme Central de Crick: Une fois l'information a pénétré dans une protéine ne peut pas sortir à nouveau (one direction-linear flow of information) Pour citer le biologiste moléculaire Richard C. Strohmann : l'ère de Watson et Crick, qui a commencé comme une théorie du gène a évolué à tort dans une théorie et le paradigme de la vie: c'est a dire, dans une forme revivifiée et soigneusement moléculaire du déterminisme génétique 6 28/06/2016 From directing the fate of stem cells to determining how.. we grow, the genes in our body act in complex networks.. the whole Genome is a Complex and highly dynamic molecular Network of interacting Genes and non-codifying sequences.. and proteins ….Genes Know How to Network…BUT... http://news.sciencemag.org/sciencenow/2009/04/21-03.html Strohman R. , April 2001 Beyond genetic determinism IN FACT Genes need to be told to switch “off” and “on”: • Genes need to be told how much expression (protein) is required and where. • Genes need to be regulated – this regulation is not performed by DNA but by many other controls arranged in a complex network • DNA has been called the Book of Life by the Human Genome Project scientists, but many other biologists consider DNA to be simply a random collection of words from which a meaningful story of life may be assembled… • In order to assemble that meaningful story, a living cell uses a second informational system. (...) The key concept here is that these dynamic-epigenetic networks have a life of their own —they follow network-rules not specified by DNA In such a fluid and systemic model the epigenome (also defined by some scientists as the controlling software of the genome) behaves as a sort of compensation chamber - the specific place where the flow of information that comes from outside (environment and microenvironment) meets and interacts with the information encoded in the genes for millions years (the hardware) Rudolf Jaenisch- Whitehead Institute and Dept. of Biology, MIT, Cambridge, MA 7 28/06/2016 EMF The second keyword: Environment We may represent the environment as a continuous stream of information (simple: photons: individual packages of E = M = Information) or complex (organic molecules, viruses etc) interacting with our cells [membrane /transmembrane receptors, signal transduction proteins, nuclear receptors, genome (DNA + Epigenome)] forcing them to adapt TCDD Viruses 1 SYNERGISM !! 3 2 “FLUID EPI-GENOME” HERVs 4 Everyday levels matter At high levels… arsenic kills people At moderately low levels… it causes a range of diseases At truly low levels … it interferes with gene activation Many of these substances (Dioxins, Heavy Metals, Polycyclic aromatic Hydrocarbons) are dangerous for humans health at very low-every daydoses (which are very difficult to be assessed by the ordinary toxicological studies) Kaltreider et al. 2002 8 28/06/2016 Histone Tails are subject to a variety of covalent modifications Histone Code” hypothesis: modifications of the Histone tails act as marks read by other proteins to control the expression or replication of chromosomal regions E.g. generally, Histone Acetylation is associated with transcriptionally active genes Deacetylation is associated with inactive genes (= gene silencing) The “meeting-point” between the information coming from the environment and the information encoded in the DNA (hardware) is the epigenome (software): mimetic molecules (EDCs) and other pollutants or danger-signals induce the epigenome to change Histone Acetyltransferases; Histone Methyltransferases Histone Deacetylases. Histone Lysine Acetylation P H3-K9 Nuclear Receptor DNA Response Element H3-S10 Many toxicants cause rapid alterations in gene expression by activating protein kinase signaling cascades. The resulting rapid, defensive alterations in gene activity require the transmission of a signal directly to the histones present in the chromatin of stress response genes: within minutes of exposure the phosphorylation of serine 10 of histone H3 and the acetylation of lysines 9 and/or 14 take place ATP-dependent Nucleosome Remodeling Complex Chromatin itself is the direct target of many toxicants * … toxicant-induced perturbations in chromatin structure may precipitate adverse effects.. Forcing genome to change 9 28/06/2016 DNA methylation Covalent modification of the DNA is also important for gene silencing human cells. Most genes have GC rich areas of DNA in their promoter regions, referred to as CpG islands. Methylation of the C residues within the CpG islands leads to gene silencing 2 (highly unstable base) The presence of 5-methylcytosine leads to the silencing of genes in that local area of the chromosome 1 2 MT = DNA methyltransferase 3 HDAC = HistoneDeacetylase MeCP2 = Methyl-CpG-binding protein 10 28/06/2016 3 The emerging evidence indicates that microRNAs control the epigenetic states that underpin development…animals, particularly primates, have evolved plasticity in these RNA regulatory systems, especially in the brain. Thus, it appears that what was dismissed as 'junk' because it was not understood holds the key to understanding human evolution, development, and cognition (JS MATTICK) The third key word is fetal programming Polycyclic Aromatic Hydrocarbons (PAH) (Ultra)-fine particles Heavy Metals Benzene Dioxin and Dioxin-like molecules MATERNAL STRESS ONTOGENY this is not a generic concept, concerning the way in which the "genetic program" contained in DNA is translated, during the nine 1 months of the ontogenetic process, in a specific complex phenotype. on the contrary,this is a precise technical term that refers to the ability, and at the same time to the necessity, of embryo-fetal cells to define their epigenetic setting in adaptive (and predictive) response to the information coming from the mother and, through her, from the outer world. 2 3 11 28/06/2016 The actual genetic program of a particular individual is actually the product of nine months of epigenetic adaptive-predictive “formatting” of billions of cells).. 1 Cellular Differentiation: Epigentic process The fourth keyword is an developmental plasticity Nature 447, 425-432 (24 May 2007) Differentiation Fetal Programming PLASTICITY 2 epi-mutations This is the stage of life which is far more sensitive to information coming from the environment (particularly to maternal-fetal stress, to nutritional errors, to pollutants ..) This image clearly shows the "power" of the epigenome and the predominant role of environmental information in the phenotypic shaping of cells, tissues , organisms .. the huge phenotypic (morphofunctional) difference between a lymphocyte and a neuron is not due to DNA, which is virtually identical in the two cells , but to the manner in which the same genome has been utilized by the two cells, on the basis of the information (positional and environmental) received during the first months of life (for neuron in the first 2 years) and processed by the epigenetic networks 12 28/06/2016 Most studied disease/organ endpoints and associated toxicity endpoints. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4393755/figure/F3/ Phylogenesis of 4 billion years of molecular coevolution * (in particular, our DNA is the product of this long journey) .. Mismatch We should never forget that we are at the same time the product Devo-Evo Ontogeny Recapitulates (anticipates) Phylogeny Ontogenesis And of 9 months of an individual development our epigenome being the product of nine months of cellular and tissue programming (adaptive to an environment that is rapidly changing).. A major risk: the EDCs and other xenobiotics (not being the product of molecular coevolution) can interfere at this level, acting as pseudo-morphogens 13 28/06/2016 The key-term in this context is certainly primary prevention ..recently, the fetal programming mismatch theory has been transformed into the key-moodel theory of DOHAD.. Obesity/Metabolic Syndrome Cardiovascular Diseases Obesogens Ipertension DOHAD Multiorgan Effects of Endocrine Disruptors Pesticides In Vitro Fertilization Materno Fetal Stress OBESITY DIABESITY PANDEMICS Placenta: Prediction of Future Health Developmental Time Windows of Vulnerability Reproductive Diseases/Dysfunctions Semen Abnormalities Asthma and allergies Lung Development Neurobehavioral Deficits and Diseases CANCER Psychiatric Diseases 14 28/06/2016 Il termine Epidemia di Cancro non andrebbe usato. Ma non bisogna sottacere il fatto che oggi una persona su due nei paesi più avanzati è destinata a sviluppare una patologia neoplastica.. 15 28/06/2016 Thousands per Annum the significant increase in the Less Developed Countries & in young people all over the world demonstrates the limits of the SMT ( necessary link between aging &CA) 14000 14000 12000 12000 10000 10000 8000 8000 6000 6000 4000 4000 2000 2000 00 2002 2002 2005 2005 2010 2010 2015 2015 2020 2020 LessDeveloped Developed More MoreDeveloped Developed Less ENVIRONMENT > GENETICS L'ambiente sembra influenzare i tassi e il rischio di cancro molto più che non la "predisposizione genetica". E' possibile rendersene conto confrontando i tassi di incidenza del cancro in diversi paesi e verificando come questi cambino quando le persone si spostano da un paese all'altro 16 28/06/2016 TEN LEADING CAUSES OF DEATH (Children aged under 15 years) U.S. 2006 CAUSE OF DEATH RANK ALL CAUSES 1 2 3 4 5 6 7 8 9 10 Accidents (unintentional injuries) Cancer Congenital anomalies Assault (homicide) Heart diseases Intentional self-harm(suicide) Influenza & pneumonia Septicemia Chronic lower respiratory diseases Cerebrovascular disease All other causes NO. OF DEATHS %OF TOTAL DEATHS DEATHRATE* 10780 100.0 19.0 3868 1284 859 756 414 219 193 172 158 149 2708 35.9 11.9 8.0 7.0 3.8 2.0 1.8 1.6 1.5 1.4 25.1 6.8 2.3 1.5 1.3 0.7 0.4 0.3 0.3 0.3 0.3 - * Rates are per 100,000 population and age adjusted to the 2000 US standard population. Based on US Mortality Data, 2006, National 33 Center for Health Statistics, Centers for Disease Control and Prevention, 2009 Bisogna sempre considerare i dati epidemiologici nel medio-lungo termine, per non essere ingannati dalle inevitabili fluttuazioni. E 'evidente che i tassi di incidenza sono aumentati drasticamente negli ultimi 30 anni negli USA da 130 a 170-180 nuovi casi/anno per milione di abitanti (ed è importante notare che un incremento analogo si è verificato in molti paesi europei) 17 28/06/2016 A first draft of the report, published on the Lancet in 2004, demonstrated an annual increase of 1-1,5% for all cancers (with more marked increases in lymphomas, soft tissue sarcomas, tumours of the nervous system…) . But the most troubling was the increase - almost the double - for all cancers in the very first year of life (apparently due to transplacental or even trans-generational exposure) CA incidence in childhood and adolescence IN EUROPE ( 1970-1999) http://www-dep.iarc.fr/accis.htm latency mother Steliarova-Foucher E, Stiller C, Kaatsch P, Berrino F, Coebergh JW, Lacour B, Parkin M. Geographical patterns and time trends of cancer incidence and survival among children and adolescents in Europe since the 1970s (the ACCISproject): an epidemiological study. Lancet. 2004 Dec 11-17;364(9451):2097105 ..in the last 20 years (1978 e il 1997) the overall incidence rate has increased significantly with an average annual percentage change (AAPC) of 1,1% (> 2% in the first year; 1,3 % during adolescence). These data should not be underestimated for at least 4 reasons: 18 28/06/2016 Non può essere ridotto a fenomeno para-fisologico (accumulo di lesioni ossidative a carico del Dna) Rapporto AIRTUM 2008 - Tumori infantili. Incidenza, sopravvivenza, andamenti temporali (Epidemiologia & Prevenzione 2008; 32(3) Suppl 2: 1-112) • Periodo di osservazione 1998-2002 • Incidenza (nuovi casi l’anno). Nell’area coperta dai registri tumori i tassi d’incidenza della malattia sono i seguenti: bambini 0-14 anni: 175,4 casi per milione/anno ragazzi 15-19 anni: 270,3 casi per milione/anno • Il tasso di incidenza per tutti i tumori pediatrici in Italia è più alto di quello rilevato negli anni novanta negli Stati Uniti (158) e in Europa (140). Attualmente in Germania è 141, in Francia è 138 • Andamenti temporali (anni 0-14) tra il 1988 e il 2002 (tre quinquenni) si è osservato un aumento della frequenza del 2% annuo, passando da 146,9 casi periodo 1988-1992 a 176,0 casi nel periodo 1998-2002 19 28/06/2016 • L’incremento più consistente riguarda i bimbi sotto l’anno di età (+ 3,2%), seguiti da quelli tra 10 e 14 anni (+2,4%), mentre è simile negli altri due gruppi (+1,6% nella fascia di età 1-4 anni, +1,8% tra i 5 e i 9 anni). • I tre tumori più frequenti nei bambini sono tutti in aumento: • leucemie + 1,6% annuo; linfomi + 4,6% annuo; tumori del sistema nervoso centrale + 2,0% annuo • Un fenomeno simile è stato osservato in diversi Paesi, • ma… in Italia il cambiamento percentuale annuo risulta più alto che in Europa: per l’insieme di tutti i tumori (+2% vs 1,1%) per le leucemie (+1,6% vs 0,6%) per i tumori del sistema nervoso centrale (+2% vs 1,7%) per i linfomi (+4,6% vs 0,9%). • (Negli Stati Uniti il tasso per tutti i tumori non è aumentato in modo significativo (+0,6%), l’incremento delle leucemie è dello 0,4% e i tumori del SNC sono stabili (-0,1%)) Cancer des enfants: de la génétique à l'épigénétique (vers un paradigme épigénétique dans la carcinogenèse) ERNESTO BURGIO ECERI - European Cancer and Environment Research Institute (Bruxelles) ISDE Scientific Committee 20 28/06/2016 Depuis des décennies le modèle de la cancérogenèse est basée sur des mutations stochastiques de l'ADN (SMT) What is Cancer ? Foreword 1 Is cancer a Genetic Disease ? Dans ce modèle les cellules somatiques d'un tissu subissent une régression (commencent à dé-différencier) pour des raisons intrinsèques accidentelles (mutations/épi-mutations) What is Cancer ? Nous proposons que le cancer est plutôt une maladie de cellules souches tissulaires (par détournement des mécanismes homéostatiques qui régissent la réparation des tissus et l'autorenouvellement des cellules souches ) après stress épi-génomique prolongé Or is cancer a stem cell disease (proceeding by misappropriating homeostatic mechanisms that govern tissue repair and stem cell self-renewal) In this case Tissue Stem Cells (TSCs) - capable of proliferation and self-renewal - proliferate after prolonged epi-genomic stress 21 28/06/2016 The Somatic Mutation Theory of Carcinogenesis Nel corso della vita, le mutazioni genetiche casuali si trasmettono da una generazione cellulare all'altra e così si accumulano Nature What’s Cancer ? The revolution in cancer research can be summed up in a single sentence: cancer is, in essence, a genetic disease Alterations in three types of genes are responsible for tumorigenesis: oncogenes, tumor-suppressor genes and stability genes Unlike diseases such as cystic fibrosis or muscular dystrophy, wherein mutations in one gene can cause disease, no single gene defect 'causes' cancer. Mammalian cells have multiple safeguards to protect them against the potentially lethal effects of cancer gene mutations, and only when several genes are defective does an invasive cancer develop Vogelstein B, Kinzler KW. Cancer genes and the pathways they control Nat Med. 2004 Aug;10(8):789-99. 22 28/06/2016 Darwinian Evolution Through Random Mutation STEP 1 La delezione o la mutazione del gene APC in 5q21 è sufficiente perché il colon venga tappezzato di polipi adenomatosi; Il DNA diventa ipometilato ⇒nuove mutazioni STEP 2 Le mutazioni di K-RAS (K-RAS1 in 6p12-11 e K-RAS2 in 12p12) sono spesso coinvolte nella progressione degli adenomi da precoci a intermedi. STEP 3 Il presunto gene soppressore dei tumori coinvolto è DCC (“Deleted in Colon Cancer” → perdita di eterozigosi in 18q21.3). STEP 4 mutazioni gene oncosoppressore p53 (localizzato in 17p12-13). STEP 5 MutazionI del gene NM23-H1 (17q22) rendono il CA altamente invasivo/metastatico.. 23 28/06/2016 What’s Cancer ? We suggest that the vast catalogues of cancer cell genotypes is a manifestation of six essential alterations in cell physiology that collectively dictate malignant growth Tumor development proceeds via a process formally analogous to Darwinian evolution, in which a succession of stochastic mutations, each conferring one or another type of growth advantage, leads to the progressive conversion of normal human cells into CA-cells… 1 2 3 CA-cells have defects in regulatory circuits that govern normal cell proliferation and homeostasis… the vast catalog of CA-cell genotypes is a manifestation of six essential alterations in cell physiology that collectively dictate malignant growth: 4 5 6 Proliferazione indipendente da segnali di crescita Resistenza all’apoptosi Attivazione dell’angiogenesi Insensibilità ai segnali inibitori Tendenza a metastatizzare Riattivazione della telomerasi (e immortalizzazione) 48 D. Hanahan, & Weinberg, R. A. (2000) The Hallmarks of Cancer, Cell, Vol. 100, pp. 57-70 24 28/06/2016 2 6 5 6 2 1 4 P P 3a P 3 P 3b RTK Receptor Tyrosine Kinases - l'autosuffisance en signaux de croissance, - l'insensibilité au signaux inhibiteurs de la croissance, - la capacité à éviter l'apoptose, - la capacité de se répliquer indéfiniment, - l'induction de l'angiogenèse et - la capacité à former des métastases some benign tumours can weigh many kilograms at the time of diagnosis sustained angiogenesis is a feature of both benign and malignant tumours RB protein is deficient both in retinoblastoma, a malignant tumour of the eye, and in retinoma, a benign tumour of this organ. evasion of apoptosis has been implicated in the pathogenesis of malignant and benign tumours insensitivity to antigrowth signals and evasion of cell death also seem to be characteristic of both benign and malignant tumours five of the proposed hallmarks of cancer are also characteristic of benign tumours La seule caractéristique distinctive du cancer est la capacité à métastaser (qui n’est pas, comme nous le verrons, le résultat des mutations, mais la réactivation d'un programme génétique embryonnaire !!) 25 28/06/2016 J Clin Invest. 2009;119(6):1438–1449. La seule caractéristique fondamentale (hallmark) du cancer est sa tendance à la métastase qui n'est pas due à des mutations, mais à la réactivation d'un programme embryonnaire, la transition épithélialemésenchymateuse (EMT) qui permet aux cellules foetales de l'embryon de migrer vers leur destination finale dans les divers tissus Les inducteurs de EMT sont bloqués chez l'adulte.. Mais ils sont activées dans la fibrose d'organes et dans les fases invasives des cancers The GWAS efforts are certainly creating bigger haystacks … In a recent editorial on Nature Heidi Ledford stated that the millions of genetic sequences and SNPs accumulated in an attempt to decipher the genetics of cancer have built giant haystacks in which researchers have gone lost … The full genome sequence of a lung cancer cell line, for example, yielded 22,910 point mutations, only 134 of which were in protein-coding regions 26 28/06/2016 Looking for that Needle in a Haystack Roughly 75 cancer genomes have been sequenced to some extent and published; researchers expect to have several hundred completed sequences by the end of the year. The efforts are certainly creating bigger haystacks. Circa 75 genomi neoplastici sono stati sequenziati ... i ricercatori si aspettano di avere diverse centinaia di sequenze complete entro la fine dell'anno. Tali tentativi hanno portato alla creazione di grandi “pagliai”. 27 28/06/2016 Loeb L A Mutator Phenotype May Be Required for Multistage Carcinogenesis Cancer Res (1991) 51:3075–3079, Loeb LA Human cancers express mutator phenotypes: origin, consequences and targeting Nature Reviews Cancer 11, 450-457 (June 2011) | doi:10.1038/nrc3063 D’autres théories (par exemple celle du mutator phénotype) démontrent plutôt qu'un tissu dans le processus de transformation néoplasique a une tendance à accumuler des mutations (qui ne sont pas la cause de cancer, mais la conséquence de l'instabilité génétique acquise) Cell 144, 27–40, January 7, 2011 8505C, a thyroid cancer cell line, shows 77 rearrangements involving chromosome 9p. TK10, a hyperdiploid line, carries six copies of chromosome 5. Même les catastrophes génomiques récemment signalés dans des différentes formes de cancer sont difficiles à concilier avec la théorie de l'accumulation lente de mutations stochastiques (SMT) .. et dans ce cas aussi, le parallélisme avec ce qui se passe dans le domaine de l'évolution semble éclairante 28 28/06/2016 29 28/06/2016 Giampaolo Collecchia, Arezzo 2014 30 28/06/2016 Cancer Not Just Bad Luck Here we provide evidence that intrinsic risk factors contribute only modestly (less than ~10-30% of lifetime risk) to cancer development… we conclude that cancer risk is heavily influenced by extrinsic factors. Cancer Epidemiology Historical Perspective 1700s: tobacco and cancer Reports of cancer risks associated with tobacco in the 18th century included snuff taking and nasal cancer, reported by Hill in 1761, and pipe smoking and lip cancer by von Soemmering in 1795. Faina Linkov, PhD; Research Assistant Professor of Medicine and Epidemiology; University of Pittsburgh Cancer Institute 31 28/06/2016 Cancer Epidemiology Historical Perspective 1775 British surgeon, Percival Pott reported probably the first description of occupational carcinogenesis in the form of scrotum cancer among chimney sweeps. The actual association between this occupational hazard and scrotum cancer was increased incidence of squamous cell carcinoma due to exposure to soot. Faina Linkov, PhD; Research Assistant Professor of Medicine and Epidemiology; University of Pittsburgh Cancer Institute Tight corsets and cancer 1842 Rigoni-Stern, Italian physician, observed that married women in the city were getting cervical cancer, but nuns in nearby convents weren’t. He also observed that nuns had higher rates of breast cancer, and suggested that the nuns’ corsets were too tight. Faina Linkov, PhD; Research Assistant Professor of Medicine and Epidemiology; University of Pittsburgh Cancer Institute 32 28/06/2016 Nurture Exposure to asbestos is linked to lung cancer, and exposure to benzidine (a chemical found in some dyes) is linked to bladder cancer Exposure to carcinogens from tobacco use is linked to several types of cancer: cancers of the lung, bladder, mouth, lip, throat, voice box, and esophagus Nurture FOOD CHAINS ?!? About 20 ingredients in pesticides have been found to cause cancer in animals. Studies of people with high exposure to pesticides - farmers, crop duster pilots, pesticide manufacturers - have shown higher rates of blood and lymphatic system cancers, melanoma and cancers of the lip, stomach, brain, lung, and prostate. 33 28/06/2016 Nurture FOOD CHAINS !! ! ! ! ! Dioxins are byproducts of paper bleaching, smelting, and waste incineration They are widespread in the environment because they break down very slowly. They also accumulate in fat cells. Most of our exposure to dioxins comes from eating dairy products, fish, and meat. Nurture We commonly use more than 100,000 chemicals and this doesn't take into account mixtures or combinations of chemicals. Plus, some chemicals are altered by the atmosphere, water, incineration. 34 28/06/2016 Nurture Effetti cancerogeni delle sostanze emesse da un inceneritore secondo la IARC (Annali Istituto Superiore Sanità 2004) agente Grado di evidenza IARC Effetto cancerogeno Arsenico 1 Pelle, polmoni, fegato, vescica, rene, colon Berillio 1 Polmone Cadmio 1 Polmone, prostata Cromo 1 Polmone Nickel 1 Polmone Mercurio 2b Polmone, pancreas, colon, prostata, encefalo, rene Piombo 2a Polmone, vescica, rene, gastroenterica Benzene 1 Leucemia Idrocarburi policiclici 2b Fegato, polmone, leucemia Cloroformio 2b Vescica, rene, encefalo, linfoma Clorofenoli 2b Sarcomi tessuti molli, linfomi Hodgkin e non Hodgkin Tricloroetilene 2a Fegato, linfomi non Hodgkin TCDD 1 Linfomi, sarcomi non Hodgkin 35 28/06/2016 Carcinogenic mechanisms of arsenic compounds http://www.mdpi.com/2072-6694/2/2/376/htm The Role of Oxidative Stress in Carcinogenesis Induced by Metals Cancers 2010, 2(2), 376-396 Inorganic arsenic compounds and methylated metabolites display similar genotoxic properties. Generation of oxidative stress is regarded as central mechanism in As-mediated carcinogenesis. A mitochondria-dependent mechanism and a H2O2/hydroxy radical pathway are discussed. In addition, arsenic affects DNA methylation and DNA repair enzymes Carcinogenic mechanisms of chromium compounds. The Role of Oxidative Stress in Carcinogenesis Induced by Metals Cancers 2010, 2(2), 376-396 Chromium (VI) compounds are internalized in cells via anionic channels. Cr(VI) is then reduced and accumulates as trivalent ion. Formation of Cr(III)-DNA adducts is regarded as predominant carcinogenic mechanism. In parallel, chromium ions can engage in Fenton-like reactions, generating hydroxy radicals 36 28/06/2016 Carcinogenic mechanisms of nickel. Nickel ions can induce oxidative stress, which provides a primary genotoxic stimulus required for carcinogenesis (red lines). In addition, Ni(II) triggers multiple mechanisms that amplify the moderate effects of oxidative stress (+). An interplay of enhanced proliferation and up-regulation of p53 could constitute a strong selective pressure, favouring mutations, which may inactivate tumor suppressor genes Cadmium and oxidative stress. Cadmium does not belong to redox-active metals. Several mechanisms for generation of ROS have been proposed though. Chronic Cd(II) exposure can also induce expression of metallothionin (MT) and triggers adaption mechanisms towards oxidative stress, thus limiting the role of ROS in carcinogenesis. Alternate carcinogenic mechanisms of cadmium, such as inhibition of DNA repair, are not shown here 37 28/06/2016 Direttiva 2004/107/CE • Direttiva 2004/107/CE del parlamento europeo e del Consiglio del 15 dicembre 2004 concernente l’arsenico il cadmio, il mercurio, il nickel e gli idrocarburi policiclici aromatici nell’aria ambiente ! “ Dai dati scientifici disponibili risulta che l’arsenico, il cadmio, il nickel e alcuni IPA (Idrocarburi Policiclici Aromatici) sono agenti genotossici e cancerogeni per l’uomo e che non esiste una soglia identificabile al di sotto della quale queste sostanze non comportino un rischio per la salute umana La Modulazione (Epi)genetica in tossicologia 1 Studi recenti hanno dimostrato che alcuni Interferenti Endocrini (IE) sono in grado di modulare l'espressione genica e che tale effetto è trasferibile alle generazioni successive xenobiotics Jirtle RL and Skinner MK (2007) "Environmental epigenomics and disease susceptibility". Nat Rev Genet, 8(4):253-262. 38 28/06/2016 1 1 2 3 Nuclear Receptor Nuclear Receptor DNA Response Element Once thought to play a largely passive, structural role, it is now clear that chromatin plays a pivotal role in the regulation of gene expression, chromosome replication, cell cycle progression, and the maintenance of genome integrity by marshalling access to the DNA template. One of the principle ways in which a eukaryotic cell responds to changes in its environment is by altering gene expression to change the complement of expressed proteins and, thereby, maintain homeostasis. Consequently, practically all toxic events will result in changes in gene expression. The Nuclear Receptors, of which there are more than 48 in mammals, are a family of ligand-activated transcription factors. A growing number of xenobiotics have been shown to function by directly altering the activity of Nuclear Receptors. For example, peroxisome proliferators, dioxins, and estrogenic chemicals act via the Peroxisome Proliferator Activated Receptor α (PPAR α), Aryl hydrocarbon receptor (AhR), and Estrogen Receptors (ER), respectively 39 28/06/2016 Many toxicants cause rapid alterations in gene expression by activating protein kinase signaling cascades. Histone Acetyltransferases; Histone Methyltransferases Histone Deacetylases. Histone Lysine Acetylation P H3-K9 Nuclear Receptor DNA Response Element H3-S10 ATP-dependent Nucleosome Remodeling Complex These modifications are believed to be essential for the full transcriptional response to stress-inducing chemicals The resulting rapid, defensive alterations in gene activity require the transmission of a signal directly to the histones present in the chromatin of stress response genes: within minutes of exposure the phosphorylation of serine 10 of histone H3 and the acetylation of lysines 9 and/or 14 take place This makes DNA sequences at the transcriptional start site accessible to RNA polymerase II and the general transcription machinery and facilitates the initiation of gene transcription (or DNA repair). Nuclear Receptor General Transcription Factors and DNA Repair In an analogous manner to the chromatin decompaction that accompanies recruitment of RNA polymerase II during gene activation, DNA excision repair is associated with increased histone acetylation and localized chromatin remodeling 40 28/06/2016 Histone modifications as early markers of DNA damage P H2A.X – S 139 P P Phosphorylated H2A.X is thought to function by recruiting additional proteins that may enhance the accuracy or efficiency of DNA repair. P Phosphorylation of serine 139 within the specialized variant Histone H2A.X. P The sensing of double-strand DNA breaks (e.g., produced by ionizing radiation or DNA-binding drugs) is accompanied by the activation of protein kinases that rapidly phosphorylate the specialized Histone Variant H2A.X and also transduce signals to additional signaling and DNA repair proteins. P H2A.X functions as a tumor suppressor gene protecting cells from the deleterious effects of DNA damage P Phosphorylation of Serine 139 of histone H2A.X also occurs during apoptosis The toxic metal nickel can inhibit HAT enzymes and the inhibition of histone acetylation by nickel compounds in vivo has been associated with the silencing of gene expression (concomitant alterations in histone acetylation and gene expression appear to be important for nickel-induced cellular transformation) Another carcinogenic metal, chromium, has recently been shown to perturb HAT and HDAC enzymes occupancy on PAH–inducible genes, resulting in the inhibition of their transcription… Chromium is known to form DNA protein cross-links, and these might be responsible for blocking the normal function of chromatin-modifying enzymes during aryl hydrocarbon receptor AhR–mediated gene activation Una condizione di instabilità genomica (ipometilazione diffusa, iper-metilazione delle sequenze promoter di geni onco-soppressori, specifiche combinazioni del “codice istonico”) è di frequente riscontro nelle lesioni (pre)-neoplastiche e neoplastiche (e potrebbe essere, interpretata, come reattiva/adattativa) 41 28/06/2016 1 Controlling active and inactive states of embryonic and somatic cells 2 Gene- and tissue-specific epigenetic patterns A Hormones B Mismatch Repair Enzymes Trascription Factors Correct organization of chromatin 3 5 X chromosome inactivation Genomic imprinting 6 4 “Silencing “ mobile sequences E’ possibile a questo punto ipotizzare che anche il cancro, al pari di tante altre malattie cronico-degenerative e/o infiammatorie, tutte in grande aumento nel mondo intero, sia una malattia essenzialmente (primariamente) epigenetica a insorgenza precoce (periodo embrio-fetale) da alterata programmazione di organi e tessuti dovuta a esposizione precoce agli agenti inquinanti ? Cheryl Lyn Walker UT MD Anderson Cancer Center 42 28/06/2016 Notes on the epigenetic (transplacental and transgenerational) origins of childhood cancer ERNESTO BURGIO ECERI - European Cancer and Environment Research Institute ISDE Scientific Committee 1 2 3 43 28/06/2016 CHEMICAL FALL OUT 1 ENDOCRINE DISRUPTORS dioxin-like moleculles The gift our mothers never wanted to give us 2 HEAVY METALS 3 ULTRAFINE PARTICLES attualmente molti studi in varie parti del mondo stanno valutando il carico corporeo chimico .. soprattutto nelle donne, bambini, embrioni / feti, fornendo risultati drammatici… http://www.ewg.org/reports/generations/ 44 28/06/2016 Metalli pesanti, diossine e altre sostanze cancerogene immesse in ecosfera, e veicolate nei tessuti degli organismi viventi, possono bio-accumularsi in ossa e grassi e bio magnificarsi nelle catene alimentari . Dai tessuti dove si accumulano (a volte per decenni), il loro rilascio è generalmente lento e continuo Biomagnificazione What is the Global Chemical Burden.. Industrial chemicals in mothers and daughters: the pollution we share and inherit E’ così che nel sangue e nei tessuti di tutti gli uomini e le donne che vivono in ambienti urbani e/o industriali e persino nel sangue cordonale e placentare e nei tessuti fetali sono presenti questi stessi inquinanti in quantità di anno in anno, di decennio in decennio maggiori 45 28/06/2016 Monitoring Body-Burdens 700 different synthetic chemicals or heavy metals found in human blood, POPs Giuseppe Giordano “Diossina di Seveso”: sino a 10 anni negli adipociti ! Tanto più che metalli, diossine e altri inquinati lipofili accumulati nei tessuti materni possono passare, anche a distanza di anni dal loro assorbimento, nel sangue e raggiungere il feto Is it true that metals, dioxins and other lipophilic pollutants, accumulated in maternal tissue, may pass, even many years after their absorption, into the blood and reach the fetus? 46 28/06/2016 XXI e siècle: transformation spectaculaire de l'environnement et du microenvironnement utérine DOHAD 47 28/06/2016 Bisogna in effetti distinguere varie possibilità: 1) l'esposizione fetale ad agenti fisici (raggi X), chimici o biologici (virus) (trasmissione trans-placentare) che possono direttamente danneggiare l'embrione/feto 2) la trasmissione potenzialmente trans-generazionale di danni genetici o epigenetici insorti nei gameti 3) l’esposizione post-natale precoce Trasmissione transgenerazionale 2 3 1 (epi)mutations in gametes Transgenerational Carcinogenesis TEL-AML1 in cord blood: 1% or 0.01%? Competing models of TEL-AML1+ leukemogenesis. 48 28/06/2016 (5) Pro-leukemic translocations in foetuses .. the first unambiguous evidence for a prenatal origin of leukaemia was derived from studies in identical twins with leukaemia. A case of identical (monozygotic) infant twins with leukaemia was recorded in 1882, and, since that time, more than 70 pairs have been published albeit in variable detail ... 1 2 Chromosomal translocations and preleukaemic clones arise at a substantially higher frequency (~100 X) before birth than the cumulative incidence or risk of disease, reflecting the requirement for complementary and secondary genetic events that occur postnatally. A consequence of the latter is a very variable and occasionally protracted postnatal latency of disease (1—15 years). 3 The concordance rate of leukaemia varies according to subtype and age. For infants with ALL, the rate is exceedingly high (> 50%), for “COMMON” child-ALL, is ~10%. Adult leukaemia (ALL/ AML), in contrast, has a very low rate of concordance (< 1%). ~1% of newborns had TEL-AML1 positive B lineage clones… which represents 100 times the incidence of TEL-AML1 positive ALL (~1 in 12,000). ! MLL rearranged leukemias are associated with poor prognosis and very brief latency for MLL-AF4+ infant B ALL. This raises the question of how this disease can evolve so quickly, Even if leukaemia fusion gene formation is spontaneous, the risk of this occurring may be modified by other factors, including folate !! availability. There is dietary and genetic evidence that folate has an impact on the risk of infant and childhood leukaemia .. 49 28/06/2016 Translocations typical of myeloid leukaemia, probably due to maternal exposure to some toxic compound, were shown to be present at birth in children who developed the disease years later (while not sufficient per se to cause the disease, they might increase the risk for leukaemia by inducing genomic instability) Tomatis L. Identification of carcinogenic agents and primary prevention of cancer. Ann N Y Acad Sci. 2006 Sep;1076:1-14 Translocation involving band 11q23 in AML may occur as a result of a deletion or trans-locations with a number of other chromosomes and is usually associatedwith M4 or M5 and a poor prognosis IN ALL AND AML, THE ALL1 (ALSO NAMED MLL) GENE CAN FUSE WITH 1 OF MORE THAN 50 GENES. ALL1 IS PART OF A MULTIPROTEIN COMPLEX. MOST OF THE PROTEINS IN THE COMPLEX ARE COMPONENTS OF TRANSCRIPTION COMPLEXES; OTHERS ARE INVOLVED IN HISTONE METHYLATION AND RNA PROCESSING. THE ENTIRE COMPLEX REMODELS, ACETYLATES, DEACETYLATES, AND METHYLATES NUCLEOSOMES AND HISTONES. THE FUSION OF ALL1 WITH 1 OF these 50 PROTEINS RESULTS IN THE FORMATION OF THE CHIMERIC PROTEINS THAT UNDERLIE ALL AND AML. ALL1 (MLL) FUSION PROTEINS DEREGULATE HOMEOBOX GENES (WHICH ENCODE TRANSCRIPTIONS FACTORS)..and microRNAs GENES SUCH AS MIR191. The first and most striking property of MLL fusion proteins is their incredible diversity. MLL has been found in 73 different translocations and 54 partner genes have been cloned (http://atlasgeneticsoncology.org/Genes/MLL.html). Nakamura T, Mori T, Tada S, et al. ALL-1 is a histone methyltransferase that assembles a supercomplex of proteins involved in transcriptional regulation Cell 2002;10:1119-1128. AF9 Location 9p22 MLL Location 11q23 histone methyltransferase Several lines of evidence point to a mishap in non-homologous end joining of double strand breaks as the most likely reason for 11q23 translocations. 50 28/06/2016 Our study has supported the hypothesis that in utero exposure to chemicals causes MLL* infant leukemia and has generated specific hypotheses that require further testing. Exposure to dipyrone is widespread, particularly in Central and South America where it is available as an inexpensive, nonprescription drug. Mosquitocidals are similarly in general use in these same settings. Propoxur (Baygon°) is also widely used against cockroaches, fleas, and similar pests. Therefore, it is important that the associations observed in this study are reevaluated in an extended casecontrol study Exposure to NHL-associated carcinogens, such as dioxin or pesticides, may cause expansion of t(14;18)-positive clones. 51 28/06/2016 Figure 2. t(14;18)+ cells in HI are actively transcribing BCL2 from the translocated allele We can find exactly the same (reactive) translocation (++ expression of the antiapoptotic gene BCL-2) in many subjects chronically exposed to pesticides .. Agopian et al. Journal of Experimental Medicine 2009:206:1473-1483 52 28/06/2016 IN THE CANCEROUS B CELLS, THE PORTION OF CHROMOSOME 18 CONTAINING THE BCL-2 LOCUS HAS UNDERGONE A RECIPROCAL TRANSLOCATION WITH THE PORTION OF CHROMOSOME 14 CONTAINING THE ANTIBODY HEAVY CHAIN LOCUS. THIS T(14;18) TRANSLOCATION PLACES THE BCL-2 GENE CLOSE TO THE HEAVY CHAIN GENE ENHANCER. H Chain-enhancer is very active in B cells... 53 28/06/2016 …. les mêmes mutations génétiques et chromosomiques, d’ailleurs toujours assez complexes (aneuploïdie, translocations, mutations des oncogènes et des gènes suppresseurs) se trouvent non seulement dans les cellules du clone néoplasique primaire (dans ce cas, les lymphocytes), mais dans plusieurs tissus intéressés … 54 28/06/2016 Ces données suggèrent que, même dans les lymphomes, les cellules endothéliales (telles que les cellules du stroma dans les tumeurs solides) sont liées au cancer … + + + THE FIRST EVIDENCE THAT CANCER ARISES FROM SOMATIC GENETIC ALTERATIONS CAME FROM STUDIES OF BURKITT'S LYMPHOMA, IN WHICH ONE OF THREE DIFFERENT TRANSLOCATIONS JUXTAPOSES AN ONCOGENE, MYC, ON CHROMOSOME 8q24 TO ONE OF THE LOCI FOR IMMUNOGLOBULIN GENES. CHROMOSOMES 14q, 22q, AND 2q — THE TRANSLOCATION PARTNERS — EACH CARRIES ENHANCER ELEMENTS IN THE IMMUNOGLOBULIN LOCI, THEREBY ACTIVATING THE JUXTAPOSED C-MYC ONCOGENE Are the antibody gene loci quite“dangerous places” for proto-oncogenes to take up residence ? Croce CM. Oncogenes and Cancer. N Engl J Med 2008;358:502-11. 55 28/06/2016 22q11.2 The c-abl oncogene from the distal tip of chromosome 9q34 has been translocated into the bcr (breakpoint cluster region) locus on chromosome 22q11.2. This t(9;22) translocation generates a chimeric BCR-ABL gene that expresses a chimeric bcr-abl mRNA and fusion protein. The Bcr-Abl fusion protein stimulates unregulated growth and has been shown to be involved in the pathogenesis of chronic myeloid leukemia (CML) and a subset of acute lymphoblastic leukemia (ALL) … in Bielorussia l’incidenza aumentò di 30 volte nel ’95 e nelle zone più vicine a Chernobyl di 100 volte… inoltre, per dosi molto alte il rischio di CA diminuiva, mentre aumentava il rischio di ipotiroidismo, per distruzione di tessuto tiroideo… nella quasi totalità dei casi era implicato uno specifico oncogène (c-RET), coinvolto in traslocazioni interpretabili come reattivo-adattative … 56 28/06/2016 Towards an epigenetic model in carcinogenesis • .. there is now ample evidence that some specific epigenetic alterations, (primarily the hypomethylation of DNA, with activation of oncogenes and increased mobility of mobile sequences) ** are the result of protracted genomic stress (eg chronic inflammation and persistent oxidative stress) • and generally anticipate, to some extent preparing it, genetic modification and an overall genomic instability • Should these data change our way of representing cancer ? ** + an hypermethylation of tumor suppressor genes promoters 57 28/06/2016 The ‘‘methylation paradox’’ of cancer cells. In fact cancer cells present a gain of methylated streches at regions that are usually unmethylated (hypermethylation) concomitantly with loss of methylation at genomic loci that are normally methylated (global hypomethylation), R Villa, F De Santis, A Gutierrez, S Minucci, PG Pelicci, L Di Croce Epigenetic gene silencing in acute promyelocytic leukemia Biochem Pharmacol (2004) 68: 1247-54 Retrosequences activation Ce qui se passe, au début, ce n’est que des modifications épigénétiques produites par un stress prolongé du tissu et du génôme : une hypométhylation de séquence d’ADN et une hypeméthylation spécifique des promoteurs des gènes suppresseurs... 1 2 3 2 58 28/06/2016 In the present study, we demonstrate how one single type of DNA alteration, aberrant methylation of gene promoters, can point to pathways disrupted in every type of cancer and can provide markers for sensitive detection of virtually all tumor types. We have now analyzed a series of promoter hypermethylation changes in 12 genes.. each rigorously characterized for association with abnormal gene silencing in cancer… Our results provide an unusual view of the pervasiveness of DNA alterations, in this case an epigenetic change, in human cancer and a powerful set of markers to outline the disruption of critical pathways in tumorigenesis NOTE ! Bien que de nombreuses tumeurs partagent une même modification pour un gène donné, des profils uniques existent pour chaque type de tumeurs. Conclusions Our data demonstrate, using a candidate gene approach, that promoter hypermethylation of 12 genes involving important cellular pathways in tumorigenesis is a feature of each of 15 major human tumor types studied. Moreover, although many tumors share this change for a given gene, unique profiles do exist for the tumor types. 59 28/06/2016 ONE OR MORE OF THE GENES STUDIED IS HYPERMETHYLATED IN EVERY TUMOR TYPE. HOWEVER, THE PROFILE OF PROMOTER HYPERMETHYLATION FOR THE GENES DIFFERS FOR EACH CANCER TYPE, PROVIDING A TUMORTYPE AND GENE-SPECIFIC PROFILE. SOME GENES, SUCH AS THE CELL CYCLE INHIBITOR P16INK4A, ARE HYPERMETHYLATED ACROSS MANY TUMOR TYPES INCLUDING COLORECTAL, LUNG, AND BREAST CARCINOMAS Other changes, such as for the DNA repair gene MGMT and DAPK, also have a wide distribution REMARK • Those who adhere to the paradigm of stochastic mutations • and more generally to a linear and genecentric model of DNA • have obviously some difficulty to accept all this… 60 28/06/2016 The dynamic (epi)-genome 9 • En fait, seulement dans un modèle de génome conçu comme un réseau moléculaire unitaire et complexe (en même temps, dynamique et responsif) il est possible de suggérer que • toutes les modifications : épigénétiques (hypométhylation globale de l'ADN, hyper-méthylation des séquences promotrices de gènes suppresseurs de tumeurs, modifications des réseaux des ncRNAs), génétiques (instabilité génomique et mobilisation des séquences transposables ..), et même chromosomiques (translocations ) qui déterminent la progression d'un cancer • doivent être considérées comme des étapes dans un processus (déformé) d'évolution –adaptation –défense tissulaire Esteller M. Cancer epigenomics: DNA methylomes and histone-modification maps Nat Rev Genet (2007);8(4):286-98; Karpinets TV, Foy BD. Tumorigenesis: the adaptation of mammalian cells to sustained stress environment by epigenetic alterations and succeeding matched mutations. Carcinogenesis. (2005); 26(8):1323-34; Hauptmann S., Schmitt W.D. Transposable elements - Is there a link between evolution and cancer? Medical Hypotheses (2006), 66 (3):580-591; Is the carcinogenic process the ontogenic development gone awry ? Is the main cause of cancer a block in cell differentiation programs (just the “hallmark”, inexplicably neglected by major theorists of SMT) ? The Embryonic Rest Theory and the field theories of cancer Some Virckow’s followers (1870 ca) formulated the theory that adult tissues contain dormant embryonic remnants that could be activated to become cancer Perhaps the most intriguing aspect of the theory concerned the hypothesized trigger of the process: ..a change in the environment, a “disequilibrium” in the surrounding tissue, that would induce these embryonic remnants to resume cell proliferation and to produce masses of cells resembling fetal tissues (field theory) 61 28/06/2016 The Embryonic Rest Theory and the field theories of cancer From Cellular Pathology: Development of cancer from connective tissue in the carcinoma of the breast Virchow, Rudolf. Cellular Pathology as Based Upon Physiological and Pathological Histology. London, 1860 Virchow and other well known pathologists, on observing cancer tissue under the microscope, noted the similarity between embryonic tissue and cancer, and suggested that tumors arise from embryo-like cells [105]. On this basis, some Virckow’s followers [106-107] formulated the theory that adult tissues contain dormant embryonic remnants that could be activated to become cancer. Perhaps the most intriguing aspect of the theory concerned the hypothesized trigger of the process: it would be a change in the environment, a “disequilibrium” in the surrounding tissue, that would induce these embryonic remnants to resume cell proliferation and to produce masses of cells that resembled fetal tissues (field theory). The great lesson of teratocarcinoma and the stem cell theory of cancer • the transplantation of pluripotent or embryonic stem cells into adult mammals, frequently leads to the growth of teratocarcinomas • the microenvironment was central to this paradigm-breaking findings: the origin of the teratoma was a “dissonance”.. • intriguingly, putting the teratocarcinoma cells into an early mammal embryo at the blastocyst stage.. they can generate normal tissues in viable mosaic individuals .. • normal offspring could result from a… cancer cell • normal germinal stem cells who became cancerous, showed the potential to revert to normal cells if placed in embryo 62 28/06/2016 63 28/06/2016 PML-RAR α as well as other leukemia-associated fusion proteins induce changes in the chromatin structure. Specifically, aberrant recruitment of different chromatin modifying enzymes to specific promoters induces DNA hypermethylation and heterochromatin formation leading to transcriptional silencing of that genes 64 28/06/2016 vertical arrows pointing to the position in the PML exonic sequences of the breakpoints. The horizontal arrows point to the location of the oligonucleotide primer pairs used for nested PCR amplification Schematic representation of the step-wise silencing of PML-RARα target genes * 1 5 2 4 3 1 The oncoprotein PML-RARα recognizes a well-defined DNA sequence * 2 3 5 .. recruits repressor enzymes, such as HDACs and DNMTs leading to hypo-acetylation of histone tails, DNA methylation, and transcriptional silencing… Methylated CpGs are potential docking sites for MBD proteins, which can in turn recruit further repressor enzymes. 4 The progression wave.. might ‘‘close’’ the chromatin structure and could even influence neighboring genes. 65 28/06/2016 In conclusione • Il cancro può esser visto come un “incidente genetico” da mutazioni stocastiche del DNA a carico di geni fondamentali (oncogeni, oncosoppressori) in cellule somatiche di vari tessuti (SMT) • o come patologia di tessuto/organo dovuta a modifiche epigenetiche e/o genetiche indotte nelle cellule staminali da una esposizione protratta ad agenti inquinanti destabilizzanti 131 66 28/06/2016 3 1 4 2 67 28/06/2016 Il “paradosso epigenetico “ delle cellule neoplastiche In ogni caso è importante sottolineare che alcune modifiche epigenetiche – la ipometilazione della sequenza del DNA con attivazione delle sequenze mobili e la ipermetilazione delle sequenze promoter dei geni oncosoppressori – sono in genere precoci e sembrano poter dare avvio avvio al processo neoplastico R Villa, F De Santis, A Gutierrez, S Minucci, PG Pelicci, L Di Croce Epigenetic gene silencing in acute promyelocytic leukemia Biochem Pharmacol (2004) 68: 1247-54 Retrosequences activation .. mentre è verosimile che la gran parte delle migliaia di mutazioni somatiche che si accumulano nel DNA delle cellule neoplastiche siano la conseguenza dell'instabilità genomica progressiva più che non la "causa" del cancro 68 28/06/2016 69 28/06/2016 A new scientific truth does not triumph by convincing its opponents and making them see the light, but rather because its opponents eventually die, and a new generation grows up that is familiar with it. Max Planck (1858 - 1947) 70