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Issues in the development of thrombin receptor antagonists.
Thromb Haemost. 1995 Jul; 74(1):499-505.TH

Abstract

The identification of the human thrombin receptor has prompted considerable interest in the development of receptor antagonists that can inhibit the effects of thrombin on cells without affecting fibrin formation. Increasing information about the biology of the receptor highlights some of the potential pitfalls in the development and application of such agents. However, it also provides additional insights into the potential mechanisms by which an antagonist might work beyond the original approach of developing competitive inhibitors of the tethered ligand domain. Thrombin receptors have proved to be present on a variety of cells other than platelets, including other vascular cells and cells within the central nervous system. Although most of the recent emphasis in thinking about the need for anti-thrombin receptor agents has focused on their use as anti-platelet agents, it is worth considering that the best clinical uses of such drugs may ultimately prove to have little to do with platelets.

Authors+Show Affiliations

Department of Medicine, University of Pennsylvania, Philadelphia 19104, USA.

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.
Review

Language

eng

PubMed ID

8578513

Citation

Brass, L F.. "Issues in the Development of Thrombin Receptor Antagonists." Thrombosis and Haemostasis, vol. 74, no. 1, 1995, pp. 499-505.
Brass LF. Issues in the development of thrombin receptor antagonists. Thromb Haemost. 1995;74(1):499-505.
Brass, L. F. (1995). Issues in the development of thrombin receptor antagonists. Thrombosis and Haemostasis, 74(1), 499-505.
Brass LF. Issues in the Development of Thrombin Receptor Antagonists. Thromb Haemost. 1995;74(1):499-505. PubMed PMID: 8578513.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Issues in the development of thrombin receptor antagonists. A1 - Brass,L F, PY - 1995/7/1/pubmed PY - 1995/7/1/medline PY - 1995/7/1/entrez SP - 499 EP - 505 JF - Thrombosis and haemostasis JO - Thromb Haemost VL - 74 IS - 1 N2 - The identification of the human thrombin receptor has prompted considerable interest in the development of receptor antagonists that can inhibit the effects of thrombin on cells without affecting fibrin formation. Increasing information about the biology of the receptor highlights some of the potential pitfalls in the development and application of such agents. However, it also provides additional insights into the potential mechanisms by which an antagonist might work beyond the original approach of developing competitive inhibitors of the tethered ligand domain. Thrombin receptors have proved to be present on a variety of cells other than platelets, including other vascular cells and cells within the central nervous system. Although most of the recent emphasis in thinking about the need for anti-thrombin receptor agents has focused on their use as anti-platelet agents, it is worth considering that the best clinical uses of such drugs may ultimately prove to have little to do with platelets. SN - 0340-6245 UR - https://www.unboundmedicine.com/medline/citation/8578513/Issues_in_the_development_of_thrombin_receptor_antagonists_ L2 - https://www.lens.org/lens/search/patent/list?q=citation_id:8578513 DB - PRIME DP - Unbound Medicine ER -