𝔖 Bobbio Scriptorium
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Initiation of blood coagulation: the tissue factor/factor VIIa complex

✍ Scribed by Daniel Kirchhofer; Yale Nemerson

Book ID
104361969
Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
637 KB
Volume
7
Category
Article
ISSN
0958-1669

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✦ Synopsis

Tissue factor (TF), a transmembrane glycoprotein, functions as an essential activator of the serine protease factor Vlla. This enzymatic complex is considered to be the principal initiator of in vivo coagulation. Recent studies emphasize the role of the TF/Vlla complex in a number of pathophysiological processes, such as Gram-negative sepsis, coronary artery disease and neointimal hyperplasia after angioplasty. Monocytes/macrophages are important contributors to some of these diseases and there have been new insights into the biology of TF regulation in monocytes. In the light of its structural similarity to cytokine receptors, there has been frequent speculation that TF has a role in intracellular signaling, a suggestion that is supported by some recent studies that propose a true receptor function for TE

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✍ Patrick Roussel; Mark Bradley; Peter Kane; Christine Bailey; Ruth Arnold; Andrew πŸ“‚ Article πŸ“… 1999 πŸ› Elsevier Science 🌐 French βš– 754 KB

Following a high throughput screen (HTS) for the inhibition of the tissue factor/factor Vlla complex and the identification of a number of original hits a lead optimisation programme was initiated to improve their potency. This necessitated the development of an amidine based linker which allowed th