BINDING OF HEPARIN AND COMPOUND-Y TO ENDOTHELIAL-CELLS STIMULATES THE SYNTHESIS OF AN ANTITHROMBOTIC HEPARAN-SULFATE PROTEOGLYCAN
Pinhal, Maria Aparecida da Silva [UNIFESP]
Silva, I. F.
Lee, T. C.
Dietrich, Carl Peter [UNIFESP]
Nader, Helena Bonciani [UNIFESP]
Is part ofBrazilian Journal Of Medical And Biological Research
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The mechanism by which heparin and antithrombotic agents, including a cyclic octaphenolsulfonic acid (compound Y), stimulate the synthesis of an antithrombotic heparan sulfate by endothelial cells in culture was investigated. Compound Y increases the amount of heparan sulfate from the cell surface and secreted to the medium by endothelial cells by three-fold. Binding experiments have shown saturation of the endothelial cell receptors at a concentration of 0.16 mu M for heparin and 2.7 mu M for compound Y. The kinetic binding constants (Ks) for compound Y and heparin were 1,333 nM and 42 nM, respectively. It was also shown that both compounds bind to the same receptors. The Scatchard plots indicated that 1,319 nmoles compound Y and 35 nmoles heparin bound per microgram cell protein, indicating that 40-fold more molecules of compound Y bound to the receptors when compared to heparin. No significant internalization Of the compounds was observed.
CitationBrazilian Journal Of Medical And Biological Research. Sao Paulo: Assoc Bras Divulg Cientifica, v. 27, n. 9, p. 2191-2195, 1994.
KeywordsENDOTHELIAL HEPARAN SULFATE AND HEPARIN
ENDOTHELIAL HEPARAN SULFATE AND ANTITHROMBOTIC DRUGS
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