Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening

Andrew J. Souers; Alex A. Virgilio; Stephan S. Schürer; Jonathan A. Ellman; Timothy P. Kogan; Henry E. West; Wendy Ankener; Peter Vanderslice

doi:10.1016/S0960-894X(98)00416-8

Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening

Andrew J. Souers, Alex A. Virgilio, Stephan S. Schürer, Jonathan A. Ellman, Timothy P. Kogan, Henry E. West, Wendy Ankener, Peter Vanderslice

Research output: Contribution to journal › Article › peer-review

54 Scopus citations

Abstract

A library of 2302 small molecule β-turn mimetics was screened for inhibition of the α4β1 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 μM, and 2, IC₅₀ = 8 μM) to be reported for this class of integrins.

Original language	English (US)
Pages (from-to)	2297-2302
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	8
Issue number	17
DOIs	https://doi.org/10.1016/S0960-894X(98)00416-8
State	Published - Sep 8 1998
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(98)00416-8

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Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening. / Souers, Andrew J.; Virgilio, Alex A.; Schürer, Stephan S.; Ellman, Jonathan A.; Kogan, Timothy P.; West, Henry E.; Ankener, Wendy; Vanderslice, Peter.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 8, No. 17, 08.09.1998, p. 2297-2302.

Research output: Contribution to journal › Article › peer-review

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title = "Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening",

abstract = "A library of 2302 small molecule β-turn mimetics was screened for inhibition of the α4β1 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 μM, and 2, IC50 = 8 μM) to be reported for this class of integrins.",

author = "Souers, {Andrew J.} and Virgilio, {Alex A.} and Sch{\"u}rer, {Stephan S.} and Ellman, {Jonathan A.} and Kogan, {Timothy P.} and West, {Henry E.} and Wendy Ankener and Peter Vanderslice",

note = "Funding Information: Acknowledgement. This work was generously supported by the National Institutes of Health (GM-53696). The W.M. Keck Foundation is also greatly acknowledged for partial support of a MALDI mass spectrometry instrument. This paper is dedicated to the memory of Dr. Timothy P. Kogan.",

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AU - Souers, Andrew J.

AU - Virgilio, Alex A.

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AU - Kogan, Timothy P.

AU - West, Henry E.

AU - Ankener, Wendy

AU - Vanderslice, Peter

N1 - Funding Information: Acknowledgement. This work was generously supported by the National Institutes of Health (GM-53696). The W.M. Keck Foundation is also greatly acknowledged for partial support of a MALDI mass spectrometry instrument. This paper is dedicated to the memory of Dr. Timothy P. Kogan.

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Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening

Abstract

ASJC Scopus subject areas

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