Bestatin analogue from Streptomyces neyagawaensis SL-387.
A bestatin analogue, (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valine (AHPA-Val), from the culture filtrate of Streptomyces neyagawaensis SL-387 was obtained in a chemically defined medium containing DL-3-amino-3-phenylpropionic acid. AHPA-Val was 6 times (IC50 = 1.2 micrograms/ml) as strong as bestatin (IC50 = 7.0 micrograms/ml) against porcine kidney microsomal aminopeptidase N, and 4 times (5.6 micrograms/ml) as strong as bestatin (IC50 = 20.7 micrograms/ml) against aminopeptidase N of human metastatic fibrosarcoma HT1080. To the best of our knowledge, this is the first report on the microbial production of AHPA-Val.
Chung
M C
MC
Enzyme Inhibitor Research Unit, Korea Research Institute of Bioscience and Biotechnology, KIST, Taejon, Korea.
Lee
H J
HJ
Chun
H K
HK
Lee
C H
CH
Kim
S I
SI
Kho
Y H
YH
D000596:Amino Acids / Q000737:chemistry; D000626:Aminopeptidases / Q000037:antagonists & inhibitors*; D018826:CD13 Antigens; D006801:Humans; D007930:Leucine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D009842:Oligopeptides / Q000737:chemistry / Q000378:metabolism; D010455:Peptides / Q000737:chemistry / Q000378:metabolism; D011480:Protease Inhibitors / Q000378:metabolism*; D013302:Streptomyces / Q000378:metabolism*; D014633:Valine / Q000737:chemistry
D000596:Amino Acids; C098403:MR 387A; D009842:Oligopeptides; D010455:Peptides; D011480:Protease Inhibitors; D000626:Aminopeptidases; D018826:CD13 Antigens; D007930:Leucine; D014633:Valine; C012211:ubenimex; C097277:apstatin