Synthesis and activity evaluation of a new bestatin derivative LYP2 as an aminopeptidase N inhibitor.
As a ubiquitous enzyme overexpressed on the epithelium of the tumor, aminopeptidase N (APN) plays important roles in the angiogenesis and metastasis of the tumor. Bestatin as an effective inhibitor against APN is used in the ancillary treatment of various cancers. In this study, we modified the structure of a bestatin derivative LYP reported in our former study to provide a new bestatin derivative LYP2 with enhanced stability. We also tested the inhibitive activity of LYP2, which retained good efficacy in vitro and in vivo towards APN.
Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Ji’nan, Shandong, PR China.
Yepeng
Y
Luan
Qiang
Q
Wang
Ning
N
Liu
Jiajia
J
Mou
Xijuan
X
Jiao
Hao
H
Fang
Minyong
M
Li
Wenfang
W
Xu
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D018826:CD13 Antigens / Q000037:antagonists & inhibitors*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D020014:K562 Cells; D007930:Leucine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D061965:Matrix Metalloproteinase Inhibitors; D051379:Mice; D008958:Models, Molecular; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013552:Swine; D023041:Xenograft Model Antitumor Assays
D000577:Amides; D000903:Antibiotics, Antineoplastic; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D018826:CD13 Antigens; D007930:Leucine; C012211:ubenimex