PMID: 2480016Jan 1, 1988Paper

Ligand activation causes a phosphorylation-dependent change in platelet-derived growth factor receptor conformation.

Transactions of the Association of American Physicians
M T KeatingL T Williams

Abstract

The effect of ligand binding on PDGF receptor conformation was examined using peptide antisera directed against specific receptor domains. Antiserum 83, which recognizes the receptor's carboxyl terminus, preferentially immunoprecipitated the ligand-activated form of the PDGF receptor from 35S-labeled BALB/c 3T3 cells. By contrast, two antisera directed against other receptor sequences precipitated unactivated and activated receptors equally well. Denatured receptors were recognized equally by all antisera, even 83. Thus, ligand activation caused a change in PDGF receptor conformation that enhanced accessibility of the receptor was induced by the three different forms of PDGF (AA and BB homodimers and AB heterodimer) and was reversed by suramin, a polyanionic compound that dissociates PDGF from the receptor. The inhibitory effect of suramin on receptor conformation was abolished by the phosphatase inhibitor sodium orthovanadate, suggesting that receptor phosphorylation mediated the conformational change. In a cell-free assay, the change in receptor conformation was induced by PDGF only in the presence of ATP and was inhibited by AMP-PNP, a nonhydrolyzable analog of ATP. The functional significance of receptor conformation was ex...Continue Reading

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