Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis (991 views)
Biol Chem Biological Chemistry (ISSN: 1431-6730, 1437-4315), 1998 Sep; 379(8-9): 987-1006.
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Paper type: Journal Article,
Impact factor: 2.636, 5-year impact factor: 3
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-0031664267&partnerID=40&md5=dcffad708f17b813f83ceaa152d152b4
Keywords: Antithrombotics, Hirunorms, Thrombin Synthetic Inhibitors, X-Ray Crystal Structure, Anticoagulant Agent, Hirudin, Serine Proteinase, Serine Proteinase Inhibitor, Thrombin Inhibitor, Chemical Structure, Comparative Study, Hemostasis, Human, Priority Journal, Review, Structure Activity Relation, Thrombosis, Amino Acid Chloromethyl Ketones, Animals, Antithrombins, Binding Sites, Molecular Mimicry, Protein Binding, Protein Conformation,
Affiliations:
Ctro. Interuniversitario di R. P. B., Ctro. Stud. Biocristallografia-CNR, University of Napoli Federico II, via Mezzocannone 4, 80134 Napoli, Italy
Dipartimento di Biochimica Mediche, University of Napoli Federico II, via Pansini 5, 80129 Napoli, Italy
References:
Not available.
Biol Chem Biological Chemistry (ISSN: 1431-6730, 1437-4315), 1998 Sep; 379(8-9): 987-1006.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 2.636, 5-year impact factor: 3
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-0031664267&partnerID=40&md5=dcffad708f17b813f83ceaa152d152b4
Keywords: Antithrombotics, Hirunorms, Thrombin Synthetic Inhibitors, X-Ray Crystal Structure, Anticoagulant Agent, Hirudin, Serine Proteinase, Serine Proteinase Inhibitor, Thrombin Inhibitor, Chemical Structure, Comparative Study, Hemostasis, Human, Priority Journal, Review, Structure Activity Relation, Thrombosis, Amino Acid Chloromethyl Ketones, Animals, Antithrombins, Binding Sites, Molecular Mimicry, Protein Binding, Protein Conformation,
Affiliations:
Ctro. Interuniversitario di R. P. B., Ctro. Stud. Biocristallografia-CNR, University of Napoli Federico II, via Mezzocannone 4, 80134 Napoli, Italy
Dipartimento di Biochimica Mediche, University of Napoli Federico II, via Pansini 5, 80129 Napoli, Italy
References:
Not available.
Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis
The central role of the serine protease thrombin in hemostasis and thrombosis brought many scientists to develop highly potent and selective thrombin inhibitors. Thrombin-inhibitor complexes have extensively been studied in order to understand structure-function relationships, and to design new inhibitors that can be used with broader efficacy over existing antithrombotic agents. In this paper, we summarize in a comparative manner the state of the art on reversible thrombin inhibitors and we discuss some structural aspects of thrombin-inhibitor interaction, which account for the different affinity and potency of these molecules. We also report here our approach to develop a new class of synthetic, multisite-directed thrombin inhibitors, named hirunorms, designed to mimic the distinctive binding mode of hirudin, We emphasize here that, despite the high specificity of thrombin action, the interaction of inhibitors in its active site may occur with quite different mechanisms.
The central role of the serine protease thrombin in hemostasis and thrombosis brought many scientists to develop highly potent and selective thrombin inhibitors. Thrombin-inhibitor complexes have extensively been studied in order to understand structure-function relationships, and to design new inhibitors that can be used with broader efficacy over existing antithrombotic agents. In this paper, we summarize in a comparative manner the state of the art on reversible thrombin inhibitors and we discuss some structural aspects of thrombin-inhibitor interaction, which account for the different affinity and potency of these molecules. We also report here our approach to develop a new class of synthetic, multisite-directed thrombin inhibitors, named hirunorms, designed to mimic the distinctive binding mode of hirudin, We emphasize here that, despite the high specificity of thrombin action, the interaction of inhibitors in its active site may occur with quite different mechanisms.
Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis
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Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis
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Impact Factor: 4.44
View Export to BibTeX Export to EndNote
Pavone V, Lombardi A, Saviano M, Di Blasio B, Nastri F, Fattorusso R, Zaccaro L, Maglio O, Yamada T, Omote Y
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Impact Factor: 2.425
View Export to BibTeX Export to EndNote
18 Records (18 excluding Abstracts).
Total impact factor: 68.085 (68.085 excluding Abstracts).
Total 5 year impact factor: 63.533 (63.533 excluding Abstracts).
Total impact factor: 68.085 (68.085 excluding Abstracts).
Total 5 year impact factor: 63.533 (63.533 excluding Abstracts).
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