Abstract
Serine proteases are involved in the blood coagulation cascade- composed of intrinsic, extrinsic, and common pathways affecting coagulation responses. Among the three pathways of the blood coagulation cascade involving serine proteases, this review focuses on serine protease inhibitors of the understudied extrinsic pathway, which is responsible for bleeding and bleeding complications targeting the (activated factor VII-Tissue Factor) fVIIa-TF complex. In lieu of our search for fVIIa-soluble TF (fVIIa-sTF) inhibitors or scaffolds, we review the serine protease inhibitors present as synthetic and natural products, which are involved in the blood coagulation cascade, and compare them with the serine protease peptide inhibitors found in toxic Microcystis cyanobacteria. Some scaffolds for the extrinsic pathway as inhibitors from the toxic Microcystis cyanobacteria will be identified in the review.
Keywords: Cyanobacteria peptides, blood coagulation cascade, extrinsic pathway, FVIIa-sTF inhibitors, thrombin inhibitors; microcystis.
Letters in Drug Design & Discovery
Title:Evaluation of Serine Protease Inhibitors as Potent FVIIa-sTF Inhibitors in the Blood Coagulation Cascade
Volume: 13 Issue: 1
Author(s): Andrea Roxanne J. Anas and Ken-ichi Harada
Affiliation:
Keywords: Cyanobacteria peptides, blood coagulation cascade, extrinsic pathway, FVIIa-sTF inhibitors, thrombin inhibitors; microcystis.
Abstract: Serine proteases are involved in the blood coagulation cascade- composed of intrinsic, extrinsic, and common pathways affecting coagulation responses. Among the three pathways of the blood coagulation cascade involving serine proteases, this review focuses on serine protease inhibitors of the understudied extrinsic pathway, which is responsible for bleeding and bleeding complications targeting the (activated factor VII-Tissue Factor) fVIIa-TF complex. In lieu of our search for fVIIa-soluble TF (fVIIa-sTF) inhibitors or scaffolds, we review the serine protease inhibitors present as synthetic and natural products, which are involved in the blood coagulation cascade, and compare them with the serine protease peptide inhibitors found in toxic Microcystis cyanobacteria. Some scaffolds for the extrinsic pathway as inhibitors from the toxic Microcystis cyanobacteria will be identified in the review.
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Cite this article as:
Roxanne J. Anas Andrea and Harada Ken-ichi, Evaluation of Serine Protease Inhibitors as Potent FVIIa-sTF Inhibitors in the Blood Coagulation Cascade, Letters in Drug Design & Discovery 2016; 13 (1) . https://dx.doi.org/10.2174/1570180812666150608230214
DOI https://dx.doi.org/10.2174/1570180812666150608230214 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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