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The Design of Synthetic Inhibitors of Thrombin : Advances in Experimental Medicine and Biology - Goran Claeson

The Design of Synthetic Inhibitors of Thrombin

Advances in Experimental Medicine and Biology

By: Goran Claeson (Editor), Michael F. Scully (Editor), Vijay V. Kakkar (Editor), John Deadman (Editor)

Hardcover

Published: 31st January 1994
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In one generation, the numerous factors involved in blood coagulation have become real protein entities, isolated in pure form, expressed by recombinant DNA techniques, and subjected to structure elucidation by the modem methods of physical chemistry, viz. , X-ray diffraction, and NMR, ESR and fluorescence spectroscopy. The major milestone in this field was the breakthrough achieved by W. Bode, R. Huber and their colleagues in 1989 in of human a-thrombin, inhibited with D-Phe-Pro-Arg determining the crystal structure chioromethyl ketone. The availability of this structure will greatly facilitate the interpretation of experiments designed to gain an understanding of the interatomic interactions between this enzyme and fibrinogen and its other substrates. At the same time, it provides a rational basis for the design and synthesis of inhibitors of thrombin, the subject of this symposium. The symposium was organized in four sessions: (1) Structural features of the interaction of thrombin with substrates and inhibitors, (2) Synthetic inhibitors, (3) Hirudin and its analogues, and (4) Pharmacological and clinical considerations. This book contains summaries of most of the papers presented, and takes its rigbful place among two others that provide a comprehensive picture of our current knowledge about thrombin, viz. the 1977 volume entitled "Chemistry and Biology of Thrombin", edited by R. L. Lundblad, J. W. Fenton II, and K. G. Mann, and the 1992 volume entitled "Thrombin: Structure and Function", edited by L. J. Berliner.

The Rational Design of Thrombin-Directed Antithromboticsp. 1
X-Ray Crystal Structures of Thrombin in Complex with D-Phe-Pro-Arg and with Small Benzamidine and Arginine-Based "Non-Peptidic" Inhibitorsp. 15
Inhibitor Binding to Thrombin: X-Ray Crystallographic Studiesp. 27
Molecular Basis for the Inhibition of Thrombin by Hirudinp. 35
Biophysical Studies of Interactions of Hirudin Analogs with Bovine and Human Thrombin by ESR and Fluorescence Labelling Studiesp. 51
pH-Dependent Binding Constants for the Inhibition of Thrombin by Transition State Analoguesp. 67
The Comparison of an Interim Tertiary Predicted Model of Bovine Thrombin and the X-Ray Structure of Human Thrombinp. 79
Design of Novel Types of Thrombin Inhibitors Based on Modified D-Phe-Pro-Arg sequencesp. 83
Chemistry and Biology of the Peptide Anticoagulant D-MePhe-Pro-Arg-H (GYKI-14766)p. 91
Peptide Boronic Acid Inhibitors of Thrombinp. 109
In Vitro and In Vivo Properties of Synthetic Inhibitors of Thrombin: Recent Advancesp. 119
The Use of Isosteric Bonds in the Design of Thrombin Inhibitorsp. 131
Synthetic Thrombin Inhibitors as Anticoagulants Pharmacological Aspectsp. 143
New Peptide Boronic Acid Inhibitors of Thrombinp. 173
Substrate-Related Phosphonopeptides as Thrombin Inhibitorsp. 179
The Synthesis and Anticoagulant Activity of Novel Peptidylfluoroalkanesp. 185
Transition State Analogue Inhibitors of Thrombin: Synthesis Activity and Molecular Modellingp. 189
Hirudin: The Famous Anticoagulant Agentp. 191
Mechanisms for the Anticoagulant Effects of Synthetic Antithrombinsp. 213
Pre-Clinical and Clinical Studies on Hirulog: A Potent and Specific Direct Thrombin Inhibitorp. 227
The Effect of Recombinant Hirudin on Arterial Thrombosisp. 237
Indexp. 243
Table of Contents provided by Blackwell. All Rights Reserved.

ISBN: 9780306445934
ISBN-10: 030644593X
Series: Advances in Experimental Medicine and Biology
Audience: Professional
Format: Hardcover
Language: English
Number Of Pages: 246
Published: 31st January 1994
Publisher: Springer Science+Business Media
Country of Publication: US
Dimensions (cm): 25.4 x 17.8  x 1.91
Weight (kg): 1.57