The Discovery of MORF-627, a Highly Selective Conformationally-Biased Zwitterionic Integrin αvβ6 Inhibitor for Fibrosis

Inhibition of integrin αvβ6 is a promising approach to the treatment of fibrotic disease such as idiopathic pulmonary fibrosis. Screening a small library combining head groups that stabilize the bent-closed conformation of integrin αIIbβ3 with αv integrin binding motifs resulted in the identificatio...

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التفاصيل البيبلوغرافية
المؤلف الرئيسي:	Bryce A. Harrison (1693699) (author)
مؤلفون آخرون:	James E. Dowling (1427728) (author), Matthew G. Bursavich (2272390) (author), Dawn M. Troast (2197303) (author), Katherine M. Chong (2545600) (author), Kristopher N. Hahn (19943210) (author), Cheng Zhong (573294) (author), Kristen M. Mulvihill (19943213) (author), Hanh Nguyen (793337) (author), Meghan F. Monroy (19943216) (author), Qi Qiao (623629) (author), Brian Sosa (19943219) (author), Siavash Mostafavi (9097289) (author), Inese Smukste (3033858) (author), Dooyoung Lee (2119468) (author), Laura Cappellucci (19943222) (author), Elizabeth H. Konopka (19943225) (author), Patrycja Nowakowski (19943228) (author), Lukasz Stawski (642534) (author), Mayra Senices (19943231) (author), Minh Hai Nguyen (9760791) (author), Parmita S. Kapoor (19943234) (author), Lia Luus (2705935) (author), Andrew Sullivan (8539326) (author), Andrea Bortolato (1276053) (author), Mats Svensson (1822822) (author), Eugene R. Hickey (589183) (author), Kyle D. Konze (1944235) (author), Tyler Day (1773151) (author), Byungchan Kim (1649704) (author), Ana Negri (60531) (author), Aleksey I. Gerasyuto (2175804) (author), Terence I. Moy (2362378) (author), Min Lu (238723) (author), Adrian S. Ray (120707) (author), Liangsu Wang (708928) (author), Dan Cui (553543) (author), Fu-Yang Lin (2084632) (author), Blaise Lippa (1484164) (author), Bruce N. Rogers (1621825) (author)
منشور في:	2024
الموضوعات:	Biophysics Biochemistry Medicine Cell Biology Pharmacology Biotechnology Hematology Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified useful tool compound highly selective inhibitor highly selective conformationally good oral pk fep +) calculations compound showed toxicity idiopathic pulmonary fibrosis development candidate morf fibrosis inhibition promising approach life resulted integrin αiibβ3 increase potency hit compounds fibrotic disease crystal structures compounds bound closed conformation
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The Discovery of MORF-627, a Highly Selective Conformationally-Biased Zwitterionic Integrin αvβ6 Inhibitor for Fibrosis

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