BINDING OF HEPARIN AND COMPOUND-Y TO ENDOTHELIAL-CELLS STIMULATES THE SYNTHESIS OF AN ANTITHROMBOTIC HEPARAN-SULFATE PROTEOGLYCAN

BINDING OF HEPARIN AND COMPOUND-Y TO ENDOTHELIAL-CELLS STIMULATES THE SYNTHESIS OF AN ANTITHROMBOTIC HEPARAN-SULFATE PROTEOGLYCAN

Author Pinhal, Maria Aparecida da Silva Autor UNIFESP Google Scholar
Silva, I. F. Google Scholar
Lee, T. C. Google Scholar
Dietrich, Carl Peter Autor UNIFESP Google Scholar
Nader, Helena Bonciani Autor UNIFESP Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
GENELABS INC
Abstract 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.
Keywords ENDOTHELIAL HEPARAN SULFATE AND HEPARIN
ENDOTHELIAL HEPARAN SULFATE AND ANTITHROMBOTIC DRUGS
ENDOTHELIAL CELLS
HEPARIN BINDING
Language English
Date 1994-09-01
Published in Brazilian Journal Of Medical And Biological Research. Sao Paulo: Assoc Bras Divulg Cientifica, v. 27, n. 9, p. 2191-2195, 1994.
ISSN 0100-879X (Sherpa/Romeo, impact factor)
Publisher Assoc Bras Divulg Cientifica
Extent 2191-2195
Access rights Closed access
Type Article
Web of Science ID WOS:A1994PG03900013
URI http://repositorio.unifesp.br/11600/43077

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