title: [Progress in study of the structure, catalytic mechanism and inhibitors of aromatase].
abstract: Aromatase is a key enzyme responsible for in vivo estrogen biosynthesis. Inhibition of the activity of the aromatase has become an alterative way for treatment of breast cancer. In this review, the structure and catalytic mechanism of the aromatase is briefly introduced followed by thorough review of the progress in the study of the steroidal and non-steroidal aromatase inhibitors. This review is focused on the natural compounds that exhibit the aromatase inhibition, which include flavonoids, xanthones, coumarins, and sesquiterpenes. The structure-activity relationship of these compounds is also discussed.
authors.affiliation: School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Fu
authors.forename: Zhong-Hua
authors.initials: ZH
authors.lastname: Shen
authors.forename: Fei-Xiong
authors.initials: FX
authors.lastname: Cheng
authors.forename: Gui-Xia
authors.initials: GX
authors.lastname: Liu
authors.forename: Wei-Hua
authors.initials: WH
authors.lastname: Li
authors.forename: Yun
authors.initials: Y
authors.lastname: Tang
mesh_terms: D000735:Androstenedione / Q000031:analogs & derivatives; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D001141:Aromatase / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D047072:Aromatase Inhibitors / Q000737:chemistry / Q000145:classification / Q000494:pharmacology / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy; D002384:Catalysis; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology; D004967:Estrogens / Q000096:biosynthesis; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D000077289:Letrozole; D009570:Nitriles / Q000737:chemistry / Q000494:pharmacology; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology; D044004:Xanthones / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D003374:Coumarins; D004967:Estrogens; D005419:Flavonoids; D009570:Nitriles; D012717:Sesquiterpenes; D014230:Triazoles; D044004:Xanthones; D000735:Androstenedione; D000077289:Letrozole; D001141:Aromatase; C014594:formestane