title: Discovery of a synthetic Aminopeptidase N inhibitor LB-4b as a potential anticancer agent.
abstract: APN inhibitors have been considered as potential anticancer agents for years. LB-4b is the first synthetic APN inhibitor to be evaluated for both of its anti-invasion and anti-angiogenesis effects. As a potent synthetic APN inhibitor (IC50=850 nM, versus bestatin of 8.1 μM), LB-4b was determined to have more significant block effects to cancer cell invasion and angiogenesis than bestatin. Besides, it is able to be easily synthesized with a high total yield, while the reported synthetic methods of bestatin are much more complex.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan, Shandong 250012, PR China.
authors.forename: Li
authors.initials: L
authors.lastname: Su
authors.forename: Yuping
authors.initials: Y
authors.lastname: Jia
authors.forename: Xuejian
authors.initials: X
authors.lastname: Wang
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.forename: Hao
authors.initials: H
authors.lastname: Fang
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001011:Aorta / Q000166:cytology / Q000187:drug effects; D001593:Benzyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D018919:Neovascularization, Physiologic; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats
chemical_list: D000970:Antineoplastic Agents; D001593:Benzyl Compounds; C584235:LB-4b compound; D011480:Protease Inhibitors; D018826:CD13 Antigens