The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
RP-1776, a Novel Cyclic Peptide Produced by Streptomyces sp., Inhibits the Binding of PDGF to the Extracellular Domain of Its Receptor
SHINICHIRO TOKI, TSUTOMU AGATSUMA, KEIKO OCHIAI, YUTAKA SAITOH, KATSUHIKO ANDO, SATOSHI NAKANISHI, NATALIE A. LOKKER, NEILL A. GIESE, YUZURU MATSUDA
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2001 Volume 54 Issue 5 Pages 405-414

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Abstract

RP-1776, a novel cyclic peptide, was isolated from the culture broth of Streptomyces sp. KYI 1784. RP-1776 selectively inhibited the binding of PDGF BB to the extracellular domain of the PDGF β-receptor with an IC50 value of 11±6 μM. Detailed binding experiments suggested that RP-1776 directly interacts with PDGF BB. RP-1776 inhibited the phosphorylation of the PDGF β-receptor induced by PDGF BB. These results suggested that RP-1776 antagonizes the signaling of PDGF BB probably through the inhibition of PDGF BB binding to the PDGF β-receptor.

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The Journal of Antibiotics, Series A

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