title: Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2011-2015).
abstract: BACKGROUND
  Hypoxia-inducible factor (HIF)-1α regulates the expression of genes involved in angiogenesis, cellular energy metabolism, and cell survival during cancer development. The increased expression of HIF-1α in most solid tumors is associated with poor prognoses and therapeutic outcomes. Therefore, HIF has been recognized as an attractive target for cancer therapy, and many HIF inhibitors have been reported.
  
  
  METHODS
  This patent survey summarizes the information about patented HIF inhibitors over the last 5 years (2011-2015).
  
  
  CONCLUSIONS
  Although many of the HIF inhibitors reviewed in this patent survey possess inhibitory activity against cancer and HIF-related diseases, the compounds are still in the early stages of development, most likely due to the complexity of the HIF-1 pathway and their different mechanisms of action for HIF inhibition. Most cancer cells use the glycolytic pathway for energy production and HIF-1α participates deeply in the expression of several glycolytic enzymes. Therefore, a detailed study of HIF's function in cancer metabolisms may provide us an alternative strategy for further development of HIF inhibitors in cancer therapy.
authors.affiliation: a Biomedical Translational Research Center , Korea Research Institute of Bioscience and Biotechnology , Daejeon , Republic of Korea.
authors.forename: Hyun Seung
authors.initials: HS
authors.lastname: Ban
authors.affiliation: b Venture Science Laboratories , Daiichi Sankyo Co., Ltd ., Tokyo , Japan.
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Uto
authors.affiliation: c Biomedical Genomics Research Center , Korea Research Institute of Bioscience and Biotechnology , Daejeon , Republic of Korea.
authors.forename: Misun
authors.initials: M
authors.lastname: Won
authors.affiliation: d Chemical Resources Laboratory , Tokyo Institute of Technology , Yokohama , Japan.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Nakamura
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D015195:Drug Design; D005786:Gene Expression Regulation; D006801:Humans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit / Q000037:antagonists & inhibitors*; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000473:pathology; D010330:Patents as Topic
chemical_list: D000970:Antineoplastic Agents; D051795:Hypoxia-Inducible Factor 1, alpha Subunit
keywords: Carcinogenesis; HIF inhibitors; cancer; hypoxia; hypoxia-inducible factor (HIF)