Synthesis and SAR of N-Benzoyl-l-Biphenylalanine Derivatives: Discovery of TR-14035, A Dual α 4 β 7/α 4 β 1 Integrin Antagonist

…, KS Gudmundsson, R Martin, J Liang, S Nomura…

文献索引：Sircar, Ila; Gudmundsson, Kristjan S.; Martin, Richard; Liang, Jimmy; Nomura, Sumihiro; Jayakumar, Honnappa; Teegarden, Bradley R.; Nowlin, Dawn M.; Cardarelli, Pina M.; Mah, Jason R.; Connell, Samuel; Griffith, Ronald C.; Lazarides, Elias Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 6 p. 2051 - 2066

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被引用次数: 58

摘要

α4β1 and α4β7 integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The effectiveness of anti-integrin antibodies to attenuate a number of inflammatory/immune conditions provides a strong rationale to target integrins for drug development. Important advances have been made in identifying potent and selective candidates, peptides and peptidomimetics, for further development. Herein, ...