title: Substituted purine and 7-deazapurine compounds as modulators of epigenetic enzymes: a patent evaluation (WO2012075381).
abstract: The patent presents 140 purine and 7-azapurine derivatives as potent inhibitors of DOT1L histone methyltransferase that might be useful in the treatment of leukemia with MLL rearrangements. It is becoming more and more evident that the deregulation of chromatin modifiers such as DOT1L plays a critical role in tumorigenesis. As yet, the number of pharmaceutical agents targeting chromatin modifiers is still limited. The market for such compounds has been estimated to be potentially as large as one third of all cancer patients. Overall, the prospective of a targeted product (i.e., a drug targeting a commonly affected chromatin modifier) is very promising, and exponentially growing investments into this market are anticipated.
authors: German Cancer Research Center (DKFZ), Division Epigenomics and Cancer Risk Factors, Heidelberg, Germany.
authors: Daniel B
authors: DB
authors: Lipka
authors: Dirk
authors: D
authors: Kuck
authors: Christian
authors: C
authors: Kliem
authors: Clarissa
authors: C
authors: Gerhauser
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D004335:Drug and Narcotic Control; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D044127:Epigenesis, Genetic / Q000187:drug effects*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D011495:Histone-Lysine N-Methyltransferase; D006801:Humans; D007938:Leukemia / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics / Q000473:pathology; D008780:Methyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015394:Molecular Structure; D058990:Molecular Targeted Therapy; D010330:Patents as Topic; D011687:Purines / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: C512929:7-deazapurine; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011687:Purines; C473477:DOT1L protein, human; D008780:Methyltransferases; D011495:Histone-Lysine N-Methyltransferase