Literature DB >> 22575869

Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.

Bénédicte Delouvrié1, Katherine Al-Kadhimi, Jean-Claude Arnould, Simon T Barry, Darren A E Cross, Myriam Didelot, Paul R Gavine, Hervé Germain, Craig S Harris, Adina M Hughes, David A Jude, Jane Kendrew, Christine Lambert-van der Brempt, Jean-Jacques Lohmann, Morgan Ménard, Andrew A Mortlock, Martin Pass, Claire Rooney, Michel Vautier, Jennifer L Vincent, Nicolas Warin.   

Abstract

Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22575869     DOI: 10.1016/j.bmcl.2012.04.063

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


  4 in total

1.  Dual antagonists of α5β1/αvβ1 integrin for airway hyperresponsiveness.

Authors:  Aparna Sundaram; Chun Chen; Nilgun Isik Reed; Sean Liu; Seul Ki Yeon; Joel McIntosh; You-Zhi Tang; Hyunjun Yang; Marc Adler; Richard Beresis; Ian B Seiple; Dean Sheppard; William F DeGrado; Hyunil Jo
Journal:  Bioorg Med Chem Lett       Date:  2020-09-29       Impact factor: 2.823

2.  Synthesis and evaluation of the aldolase antibody-derived chemical-antibodies targeting α5β1 integrin.

Authors:  Rajib K Goswami; Yuan Liu; Cheng Liu; Richard A Lerner; Subhash C Sinha
Journal:  Mol Pharm       Date:  2012-11-14       Impact factor: 4.939

Review 3.  The functions and applications of RGD in tumor therapy and tissue engineering.

Authors:  Fen Wang; Yuanyuan Li; Yingqiang Shen; Anming Wang; Shuling Wang; Tian Xie
Journal:  Int J Mol Sci       Date:  2013-06-27       Impact factor: 5.923

4.  Integrin α5β1, the Fibronectin Receptor, as a Pertinent Therapeutic Target in Solid Tumors.

Authors:  Florence Schaffner; Anne Marie Ray; Monique Dontenwill
Journal:  Cancers (Basel)       Date:  2013-01-15       Impact factor: 6.639

  4 in total

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