title: BET inhibitors in cancer therapeutics: a patent review.
abstract: BACKGROUND
  Inhibition of Bromodomain and Extra Terminal (BET) proteins is an emerging approach for developing advanced cancer therapeutics. In 2015, at least thirty patents have been published for developing cancer chemotherapeutics by targeting BET. Currently there are seven small molecule BET inhibitors in various stages of clinical trials for the development of anti-cancer drugs.
  
  
  METHODS
  Important patents focusing on development of BET inhibitors as potential cancer therapeutics published in 2015 have been covered. The reports are presented together with a review of the related structural chemical space. This review mainly focuses on the therapeutic applications, chemical class and structural modifications along with the molecules currently in clinical trials.
  
  
  CONCLUSIONS
  BET sub-family proteins are one of the emerging targets to develop anti-cancer agents. Although many research groups have demonstrated the rationality of BET inhibition to combat cancer, a detailed molecular study needs to be performed to investigate the affected biological pathways. Selectivity among BET proteins should be kept in mind while developing BET inhibitors. In-silico molecular modelling studies can also provide valuable information for designing selective BET inhibitors towards anti-cancer drug discovery and development.
authors.affiliation: a Medicinal Chemistry and Pharmacology Division , CSIR - Indian Institute of Chemical Technology , Hyderabad , India.
authors.forename: Anirban
authors.initials: A
authors.lastname: Ghoshal
authors.affiliation: a Medicinal Chemistry and Pharmacology Division , CSIR - Indian Institute of Chemical Technology , Hyderabad , India.|b Chemical Science Division, Academy of Scientific & Innovative Research (AcSIR) , New Delhi , India.
authors.forename: D
authors.initials: D
authors.lastname: Yugandhar
authors.affiliation: a Medicinal Chemistry and Pharmacology Division , CSIR - Indian Institute of Chemical Technology , Hyderabad , India.|b Chemical Science Division, Academy of Scientific & Innovative Research (AcSIR) , New Delhi , India.
authors.forename: Ajay Kumar
authors.initials: AK
authors.lastname: Srivastava
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D003198:Computer Simulation; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods; D006801:Humans; D008958:Models, Molecular; D058990:Molecular Targeted Therapy; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors*; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors; D010330:Patents as Topic
chemical_list: D000970:Antineoplastic Agents; D009363:Neoplasm Proteins; D009687:Nuclear Proteins
keywords: BET; Bromodomain; Bromodomain and Extra Terminal Proteins; anti-cancer