期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 7, 期 3, 页码 283-288出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00448
关键词
GPCR; S1P1; S1P3; biased signaling
Clinical validation of SIP receptor modulation therapy was achieved with the approval of fingolimod (Gilenya, 1) as the first oral therapy for relapsing remitting multiple sclerosis. However, 1 causes a dose-dependent reduction in the heart rate (bradycardia), which occurs within hours after first dose. We disclose the identification of clinical compound BMS-986104 (3d), a novel S1P(1) receptor modulator, which demonstrates ligand-biased signaling and differentiates from 1 in terms of cardiovascular and pulmonary safety based on preclinical pharmacology while showing equivalent efficacy in a T-cell transfer colitis model.
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