Literature DB >> 21538731

Oral, direct thrombin and factor Xa inhibitors: the replacement for warfarin, leeches, and pig intestines?

Alexander Straub1, Susanne Roehrig, Alexander Hillisch.   

Abstract

To prevent thromboses after surgery, patients have until now had to inject themselves daily with heparin. For stroke prophylaxis in atrial fibrillation, patients take vitamin K antagonists of the coumarin type, which have a narrow therapeutic window and whose dosage must be regularly monitored. In order to improve the standard of therapy in thromboembolic diseases such as deep-vein thrombosis, pulmonary embolism, and stroke in atrial fibrillation, intensive research has been carried out over the last decade in the search for new, orally active thrombin and factor Xa inhibitors. A number of these compounds are already on the market or are in advanced clinical development; they could revolutionize the anticoagulant market.
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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Year:  2011        PMID: 21538731     DOI: 10.1002/anie.201004575

Source DB:  PubMed          Journal:  Angew Chem Int Ed Engl        ISSN: 1433-7851            Impact factor:   15.336


  10 in total

1.  Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.

Authors:  Rami A Al-Horani; Akul Y Mehta; Umesh R Desai
Journal:  Eur J Med Chem       Date:  2012-06-23       Impact factor: 6.514

2.  Rational design of potent, small, synthetic allosteric inhibitors of thrombin.

Authors:  Preetpal Singh Sidhu; Aiye Liang; Akul Y Mehta; May H Abdel Aziz; Qibing Zhou; Umesh R Desai
Journal:  J Med Chem       Date:  2011-07-18       Impact factor: 7.446

3.  Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.

Authors:  May H Abdel Aziz; Preetpal Singh Sidhu; Aiye Liang; Ji Yeong Kim; Philip D Mosier; Qibing Zhou; David H Farrell; Umesh R Desai
Journal:  J Med Chem       Date:  2012-07-25       Impact factor: 7.446

4.  Comparative Transcriptome Sequencing Analysis of Hirudo nipponia in Different Growth Periods.

Authors:  Xiaocong Ma; Xiuying Yan; Ren Ke; Huiquan Shan; Saif Ur Rehman; Tong Feng; Yalin Zheng; Chen Chuang; Weiguan Zhou; Qingyou Liu; Jinghui Zheng
Journal:  Front Physiol       Date:  2022-06-23       Impact factor: 4.755

Review 5.  Proteolysis in Reproduction: Lessons From Gene-Modified Organism Studies.

Authors:  Daiji Kiyozumi; Masahito Ikawa
Journal:  Front Endocrinol (Lausanne)       Date:  2022-05-04       Impact factor: 6.055

6.  Designing allosteric regulators of thrombin. Exosite 2 features multiple subsites that can be targeted by sulfated small molecules for inducing inhibition.

Authors:  Preetpal Singh Sidhu; May H Abdel Aziz; Aurijit Sarkar; Akul Y Mehta; Qibing Zhou; Umesh R Desai
Journal:  J Med Chem       Date:  2013-06-13       Impact factor: 7.446

7.  Dynamic affinity chromatography in the separation of sulfated lignins binding to thrombin.

Authors:  Aiye Liang; Jay N Thakkar; Michael Hindle; Umesh R Desai
Journal:  J Chromatogr B Analyt Technol Biomed Life Sci       Date:  2012-10-02       Impact factor: 3.205

8.  Protein-Templated Formation of an Inhibitor of the Blood Coagulation Factor Xa through a Background-Free Amidation Reaction.

Authors:  Mike Jaegle; Torsten Steinmetzer; Jörg Rademann
Journal:  Angew Chem Int Ed Engl       Date:  2017-02-15       Impact factor: 15.336

9.  Electrostatic recognition in substrate binding to serine proteases.

Authors:  Birgit J Waldner; Johannes Kraml; Ursula Kahler; Alexander Spinn; Michael Schauperl; Maren Podewitz; Julian E Fuchs; Gabriele Cruciani; Klaus R Liedl
Journal:  J Mol Recognit       Date:  2018-05-22       Impact factor: 2.137

Review 10.  New Approaches to the Role of Thrombin in Acute Coronary Syndromes: Quo Vadis Bivalirudin, a Direct Thrombin Inhibitor?

Authors:  María Asunción Esteve-Pastor; Diana Hernández-Romero; Mariano Valdés; Francisco Marín
Journal:  Molecules       Date:  2016-02-27       Impact factor: 4.411

  10 in total

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