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The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate

Jan 01, 2012 • By P Gergely1, B Nuesslein-Hildesheim1, D Guerini1, V Brinkmann1, M Traebert1, C Bruns1, S Pan2, NS Gray2, K Hinterding1, NG Cooke1, A Groenewegen1, A Vitaliti1, T Sing3, O Luttringer3, J Yang1, A Gardin1, N Wang1, WJ Crumb Jr4, M Saltzman5, M Rosenberg5 and E Wallström3

Background And Purpose BAF312 is a next-generation sphingosine 1-phosphate (S1P) receptor modulator, selective for S1P1 and S1P5 receptors. S1P1 receptors are essential for lymphocyte egress from lymph nodes and a drug target in immune-mediated diseases. Here, we have characterized the…

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Three-Dimensional Quantitative Structure-Activity Relationship for Inhibition of Human Ether-a-Go-Go-Related Gene Potassium Channel

Jun 08, 2002 • By SEAN EKINS, WILLIAM J. CRUMB, R. DUSTAN SARAZAN, JAMES H. WIKEL, and STEVEN A. WRIGHTON

Abstract The protein product of the human ether-a-go-go gene (hERG) is a potassium channel that when inhibited by some drugs may lead to cardiac arrhythmia. Previously, a three-dimensional quantitative structure-activity relationship (3D-QSAR) pharmacophore model was constructed using Catalyst with…

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