The Design of synthetic inhibitors of thrombin
著者
書誌事項
The Design of synthetic inhibitors of thrombin
(Advances in experimental medicine and biology, v. 340)
Plenum Press, c1993
大学図書館所蔵 全12件
  青森
  岩手
  宮城
  秋田
  山形
  福島
  茨城
  栃木
  群馬
  埼玉
  千葉
  東京
  神奈川
  新潟
  富山
  石川
  福井
  山梨
  長野
  岐阜
  静岡
  愛知
  三重
  滋賀
  京都
  大阪
  兵庫
  奈良
  和歌山
  鳥取
  島根
  岡山
  広島
  山口
  徳島
  香川
  愛媛
  高知
  福岡
  佐賀
  長崎
  熊本
  大分
  宮崎
  鹿児島
  沖縄
  韓国
  中国
  タイ
  イギリス
  ドイツ
  スイス
  フランス
  ベルギー
  オランダ
  スウェーデン
  ノルウェー
  アメリカ
注記
"Proceedings of an International Symposium on the Design of Synthetic Inhibitors of Thrombin, held July 8-9, 1991, in London, United Kingdom"--T.p. verso
Includes bibliographical references and index
内容説明・目次
内容説明
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.
目次
The Rational Design of Thrombin-Directed Antithrombotics.- X-Ray Crystal Structures of Thrombin in Complex with D-Phe-Pro-Arg and with Small Benzamidine and Arginine-Based "Non-Peptidic" Inhibitors.- Inhibitor Binding to Thrombin: X-Ray Crystallographic Studies.- Molecular Basis for the Inhibition of Thrombin by Hirudin.- Biophysical Studies of Interactions of Hirudin Analogs with Bovine and Human Thrombin by ESR and Fluorescence Labelling Studies.- pH-Dependent Binding Constants for the Inhibition of Thrombin by Transition State Analogues.- The Comparison of an Interim Tertiary Predicted Model of Bovine Thrombin and the X-Ray Structure of Human Thrombin.- Design of Novel Types of Thrombin Inhibitors Based on Modified D-Phe-Pro-Arg sequences.- Chemistry and Biology of the Peptide Anticoagulant D-MePhe-Pro-Arg-H (GYKI-14766).- Peptide Boronic Acid Inhibitors of Thrombin.- In Vitro and In Vivo Properties of Synthetic Inhibitors of Thrombin: Recent Advances.- The Use of Isosteric Bonds in the Design of Thrombin Inhibitors.- Synthetic Thrombin Inhibitors as Anticoagulants Pharmacological Aspects.- New Peptide Boronic Acid Inhibitors of Thrombin.- Substrate-Related Phosphonopeptides as Thrombin Inhibitors.- The Synthesis and Anticoagulant Activity of Novel Peptidylfluoroalkanes.- Transition State Analogue Inhibitors of Thrombin: Synthesis Activity and Molecular Modelling.- Hirudin: The Famous Anticoagulant Agent.- Mechanisms for the Anticoagulant Effects of Synthetic Antithrombins.- Pre-Clinical and Clinical Studies on Hirulog: A Potent and Specific Direct Thrombin Inhibitor.- The Effect of Recombinant Hirudin on Arterial Thrombosis.
「Nielsen BookData」 より