The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
RP-1551s, a Family of Azaphilones Produced by Penicillium sp., Inhibit the Binding of PDGF to the Extracellular Domain of Its Receptor
SHINICHIRO TOKITAKEO TANAKAYOUICHI UOSAKIMAYUMI YOSHIDAYASUHIRO SUZUKIKATSUNORI KITAAKIRA MIHARAKATSUHIKO ANDONATALIE A. LOKKERNEILL A. GIESEYUZURU MATSUDA
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1999 Volume 52 Issue 3 Pages 235-244

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Abstract

Nine azaphilones designated RP-1551-1, -2, -3, -4, -5, -6, -7, -M1, and -M2 were isolated from the culture broth of Penicillium sp. SPC-21609 as inhibitors of PDGF binding to its receptor. RP-1551s inhibit the binding of PDGF AA to the extracellular domain of PDGF α-receptor with IC50 values ranging from 0.1 to 2μM without affecting PDGF BB binding to the extracellular domain of PDGF β-receptor. PDGF binding was not restored after the PDGF α-receptor extracellular domain was washed in an attempt to remove the RP-1551-1 bound to the receptor. This result suggests that RP-1551-1 may irreversibly interact with the PDGF α-receptor. Since many azaphilone compounds possess high reactivity with an aminol group, RP-1551-1 may prevent PDGF AA binding by reacting with amino groups on the α-receptor extracellular domain.

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© Japan Antibiotics Research Association
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