Piperastatin B: a new selective serine carboxypeptidase inhibitor from Streptomyces lavendofoliae MJ908-WF13.
Piperastatin B, a new inhibitor of serine carboxypeptidase was purified from a culture broth of Streptomyces lavendofoliae MJ908-WF13 as a minor component by monitoring its inhibitory activity against carboxypeptidase Y (CP-Y). Its structure was determined to be N-formyl-Val-Thr-Leu-Val-Pip-Leu-Pip (pip: piperazic acid, hexahydropyridadine-3-carboxylic acid). Piperastatin B is a highly specific competitive inhibitor of CP-Y (Ki = 55 nM) with little effect on related enzymes and resembles the major component, piperastatin A, in these respects.
Murakami
S
S
Institute of Microbial Chemistry, Tokyo, Japan.
Harada
S
S
Takahashi
Y
Y
Naganawa
H
H
Takeuchi
T
T
Aoyagi
T
T
D000596:Amino Acids / Q000032:analysis / Q000737:chemistry; D002268:Carboxypeptidases / Q000037:antagonists & inhibitors*; D043402:Cathepsin A; D006867:Hydrolases / Q000037:antagonists & inhibitors; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D011724:Pyridazines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D013053:Spectrophotometry; D013302:Streptomyces / Q000737:chemistry*; D015003:Yeasts / Q000201:enzymology
D000596:Amino Acids; D009842:Oligopeptides; D011724:Pyridazines; D015842:Serine Proteinase Inhibitors; C103102:piperastatin A; C107156:piperastatin B; D006867:Hydrolases; D002268:Carboxypeptidases; D043402:Cathepsin A