Literature DB >> 16524727

Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.

Hongfeng Deng1, Thomas D Bannister, Lei Jin, Robert E Babine, Jesse Quinn, Pamela Nagafuji, Cassandra A Celatka, Jian Lin, Tsvetelina I Lazarova, Michael J Rynkiewicz, Frank Bibbins, Pramod Pandey, Joan Gorga, Harold V Meyers, Sherin S Abdel-Meguid, James E Strickler.   

Abstract

Using an alpha-ketothiazole arginine moiety as a key recognition element, a series of small peptidomimetic molecules was designed and synthesized, and their co-crystal structures with factor XIa were studied in an effort to develop smaller, less peptidic inhibitors as antithrombotic agents.

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Year:  2006        PMID： 16524727     DOI： 10.1016/j.bmcl.2006.02.052

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  15 in total

1.  A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits.

Authors:  Pancras C Wong; Earl J Crain; Carol A Watson; William A Schumacher
Journal:  J Thromb Thrombolysis       Date:  2011-08       Impact factor: 2.300

2.  Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.

Authors:  Zhenfu Han; Peter K W Harris; Darin E Jones; Ryan Chugani; Tommy Kim; Manjula Agarwal; Wei Shen; Scott A Wildman; James W Janetka
Journal:  ACS Med Chem Lett       Date:  2014-10-09       Impact factor: 4.345

3.  High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.

Authors:  Xavier Fradera; Bert Kazemier; Emma Carswell; Andrew Cooke; Arthur Oubrie; William Hamilton; Maureen Dempster; Stephan Krapp; Susanna Nagel; Anja Jestel
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2012-03-27

Review 4.  Future prospects for contact factors as therapeutic targets.

Authors:  David Gailani
Journal:  Hematology Am Soc Hematol Educ Program       Date:  2014-11-18

5.  The kunitz protease inhibitor domain of protease nexin-2 inhibits factor XIa and murine carotid artery and middle cerebral artery thrombosis.

Authors:  Wenman Wu; Hongbo Li; Duraiswamy Navaneetham; Zachary W Reichenbach; Ronald F Tuma; Peter N Walsh
Journal:  Blood       Date:  2012-06-06       Impact factor: 22.113

Review 6.  Recent advances in the discovery and development of factor XI/XIa inhibitors.

Authors:  Rami A Al-Horani; Daniel K Afosah
Journal:  Med Res Rev       Date:  2018-05-04       Impact factor: 12.944

7.  Discovery of allosteric modulators of factor XIa by targeting hydrophobic domains adjacent to its heparin-binding site.

Authors:  Rajesh Karuturi; Rami A Al-Horani; Shrenik C Mehta; David Gailani; Umesh R Desai
Journal:  J Med Chem       Date:  2013-03-18       Impact factor: 7.446

8.  Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa.

Authors:  Rami A Al-Horani; Pooja Ponnusamy; Akul Y Mehta; David Gailani; Umesh R Desai
Journal:  J Med Chem       Date:  2013-01-28       Impact factor: 7.446

9.  P1 and P2' site mutations convert protease nexin-2 from a factor XIa inhibitor to a plasmin inhibitor.

Authors:  Duraiswamy Navaneetham; Wenman Wu; Hongbo Li; Dipali Sinha; Ronald F Tuma; Peter N Walsh
Journal:  J Biochem       Date:  2012-11-20       Impact factor: 3.387

Review 10.  Factor XI as a target for antithrombotic therapy.

Authors:  Charles E Bane; David Gailani
Journal:  Drug Discov Today       Date:  2014-06-02       Impact factor: 7.851
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