Literature DB >> 9873531

Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening.

A J Souers1, A A Virgilio, S S Schürer, J A Ellman, T P Kogan, H E West, W Ankener, P Vanderslice.   

Abstract

A library of 2302 small molecule beta-turn mimetics was screened for inhibition of the alpha 4 beta 1 integrin-CS1 splice variant binding interaction. Preliminary data revealed several active ligands, and validation with purified material culminated in the identification of some of the first small molecule ligands (1, IC50 = 5 microM, and 2, IC50 = 8 microM) to be reported for this class of integrins.

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Year:  1998        PMID: 9873531     DOI: 10.1016/s0960-894x(98)00416-8

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


  7 in total

1.  Combinatorial approaches to inhibitors of VLA-4: piperazine-peptoid-bisarylureas.

Authors:  I Lewis; B Rohde; M Mengus; M Weetall; S Maida; R Hugo; P Lake
Journal:  Mol Divers       Date:  2000       Impact factor: 2.943

2.  A small molecule inhibitor of alpha4 integrin-dependent cell migration.

Authors:  Jongkook Lee; Jiyong Hong; Tae-Gyu Nam; Eric C Peters; Anthony P Orth; Bernhard H Geierstanger; Lawrence E Goldfinger; Mark H Ginsberg; Charles Y Cho; Peter G Schultz
Journal:  Bioorg Med Chem       Date:  2008-02-26       Impact factor: 3.641

3.  A road less traveled by: exploring a decade of Ellman chemistry.

Authors:  Anang A Shelat; R Kiplin Guy
Journal:  Bioorg Med Chem       Date:  2008-03-04       Impact factor: 3.641

4.  Anti-inflammatory activity of c(ILDV-NH(CH2)5CO), a novel, selective, cyclic peptide inhibitor of VLA-4-mediated cell adhesion.

Authors:  D Haworth; A Rees; P J Alcock; L J Wood; A S Dutta; J J Gormley; H B Jones; A Jamieson; C F Reilly
Journal:  Br J Pharmacol       Date:  1999-04       Impact factor: 8.739

5.  The design and application of target-focused compound libraries.

Authors:  C John Harris; Richard D Hill; David W Sheppard; Martin J Slater; Pieter F W Stouten
Journal:  Comb Chem High Throughput Screen       Date:  2011-07       Impact factor: 1.339

Review 6.  Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes.

Authors:  Marta Pelay-Gimeno; Adrian Glas; Oliver Koch; Tom N Grossmann
Journal:  Angew Chem Int Ed Engl       Date:  2015-06-26       Impact factor: 15.336

Review 7.  Constrained peptides as miniature protein structures.

Authors:  Hang Yin
Journal:  ISRN Biochem       Date:  2012-09-26
  7 in total

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