title: [Progress in small-molecule inhibitors of Bcl-2 family proteins].
abstract: Apoptosis is an essential factor in keeping homeostasis of the organism. Apoptosis is regulated by a series of cytokines. Bcl-2 family proteins are key regulators of apoptosis. The Bcl-2 family includes both anti- and pro-apoptotic proteins with opposing biological functions. Their interaction regulates the transmission of the apoptosis signal. High expression of anti-apoptotic members such as Bcl-2 and Bcl-xL are commonly found in human cancers. In recent years, following the disclosing of the crystal structures of Bcl-2 family proteins, researchers have paid attention to the development of the small molecule inhibitors of Bcl-2 family proteins. This article reviews the progress in this field from the view of drug design.
authors.affiliation: School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Tang
authors.forename: Da-yong
authors.initials: DY
authors.lastname: Zhang
authors.forename: Xiao-ming
authors.initials: XM
authors.lastname: Wu
mesh_terms: D000968:Antimycin A / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001578:Benzopyrans / Q000737:chemistry / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D015195:Drug Design; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology; D006072:Gossypol / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009570:Nitriles / Q000737:chemistry / Q000494:pharmacology; D009596:Nitrophenols / Q000737:chemistry / Q000494:pharmacology; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology; D045162:Thiazolidinediones; D051020:bcl-X Protein / Q000037:antagonists & inhibitors* / Q000494:pharmacology
chemical_list: C503945:5-(4-bromobenzylidene)-alpha-isopropyl-4-oxo-2-thioxo-3-thazolidineacetic acid; C501332:ABT-737; D000970:Antineoplastic Agents; D001578:Benzopyrans; D001713:Biphenyl Compounds; D004365:Drugs, Chinese Herbal; D009570:Nitriles; D009596:Nitrophenols; D010879:Piperazines; D019253:Proto-Oncogene Proteins c-bcl-2; D013449:Sulfonamides; D013844:Thiazoles; D045162:Thiazolidinediones; D051020:bcl-X Protein; C456800:ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate; D000968:Antimycin A; D006072:Gossypol