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

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

Bioorg Med Chem Lett ; 8(17): 2297-302, 1998 Sep 08.

Article in English | MEDLINE | ID: mdl-9873531

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.

Subject(s)

Amino Acids/chemical synthesis , Carboxylic Acids/chemical synthesis , Databases as Topic , Integrins/antagonists & inhibitors , Integrins/genetics , Receptors, Lymphocyte Homing/antagonists & inhibitors , Receptors, Lymphocyte Homing/genetics , Alternative Splicing , Amino Acids/chemistry , Amino Acids/pharmacology , Binding Sites , Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , Drug Design , Integrin alpha4beta1 , Integrins/chemistry , Ligands , Molecular Conformation , Molecular Structure , Receptors, Lymphocyte Homing/chemistry , Receptors, Very Late Antigen/antagonists & inhibitors , Receptors, Very Late Antigen/chemistry , Receptors, Very Late Antigen/genetics , Reproducibility of Results , Stereoisomerism , Structure-Activity Relationship

ABSTRACT

Subject(s)

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