title: LSD1 inhibitors: a patent review (2010-2015).
abstract: BACKGROUND
  Lysine demethylase 1 (LSD1) plays an important role in mediating the expression of genes involved in cancer and non-cancer diseases such as viral infections, cardiovascular and neurodegenerative disorders. It is involved in a number of processes from adipogenesis to cell adhesion to viral latency, regulating several cell pathways related with proliferation, development, and cell cycle control. Numerous chemical entities have been studied in recent years and some of them entered the clinical arena.
  
  
  METHODS
  This review summarizes recent efforts in the drug development of LSD1 inhibitors reported in the patent literature covering the 2010-2015 period, including their potential use as therapeutics in cancerous, neurological, inflammatory, cardiovascular, and viral diseases.
  
  
  CONCLUSIONS
  The development of novel potent and selective LSD1 inhibitors is ongoing, in order to improve their potency and selectivity against specific types of cancer or non-cancer diseases. More in-depth studies are required to assess the role of LSD1 inhibitors in the expression of LSD1 target genes, for a better assessment of the biochemistry underlying their efficacy, and to provide evidence for any possible side effects. Furthermore, an interesting therapeutic approach is the use of LSD1 inhibitors in conjunction with other epidrugs to combine their therapeutic potential, leading to innovative, personalized treatments.
authors.affiliation: a Dipartimento di Chimica e Tecnologie del Farmaco , Sapienza Università di Roma , Rome , Italy.|b Istituto Pasteur-Fondazione Cenci Bolognetti , Sapienza Università di Roma , Rome , Italy.
authors.forename: Giulia
authors.initials: G
authors.lastname: Stazi
authors.affiliation: a Dipartimento di Chimica e Tecnologie del Farmaco , Sapienza Università di Roma , Rome , Italy.
authors.forename: Clemens
authors.initials: C
authors.lastname: Zwergel
authors.affiliation: a Dipartimento di Chimica e Tecnologie del Farmaco , Sapienza Università di Roma , Rome , Italy.
authors.forename: Sergio
authors.initials: S
authors.lastname: Valente
authors.affiliation: a Dipartimento di Chimica e Tecnologie del Farmaco , Sapienza Università di Roma , Rome , Italy.|b Istituto Pasteur-Fondazione Cenci Bolognetti , Sapienza Università di Roma , Rome , Italy.
authors.forename: Antonello
authors.initials: A
authors.lastname: Mai
mesh_terms: D000818:Animals; D015195:Drug Design; D005786:Gene Expression Regulation / Q000187:drug effects*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010330:Patents as Topic; D057285:Precision Medicine
chemical_list: D056466:Histone Demethylases; C495195:KDM1A protein, human
keywords: Cancer; epigenetics; lysine specific demethylase 1; small molecule inhibitors; viral infections