RP-1551s, a family of azaphilones produced by Penicillium sp., inhibit the binding of PDGF to the extracellular domain of its receptor.
J Antibiot (Tokyo)
; 52(3): 235-44, 1999 Mar.
Article
em En
| MEDLINE
| ID: mdl-10348038
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 alpha-receptor with IC50 values ranging from 0.1 to 2 microM without affecting PDGF BB binding to the extracellular domain of PDGF beta-receptor. PDGF binding was not restored after the PDGF alpha-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 alpha-receptor. Since many azaphilone compounds possess high reactivity with an amino group, RP-1551-1 may prevent PDGF AA binding by reacting with amino groups on the alpha-receptor extracellular domain.
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Base de dados:
MEDLINE
Assunto principal:
Penicillium
/
Benzopiranos
/
Fator de Crescimento Derivado de Plaquetas
/
Receptores do Fator de Crescimento Derivado de Plaquetas
/
Antibacterianos
Limite:
Humans
Idioma:
En
Ano de publicação:
1999
Tipo de documento:
Article