Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases.

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作者： Franz,von Nussbaum ^[1] ; Volkhart M-J,Li ^[2] ; Swen,Allerheiligen ^[3] ; Sonja,Anlauf ^[3] ; Lars,Bärfacker ^[3] ; Martin,Bechem ^[4] ; Martina,Delbeck ^[4] ; Mary F,Fitzgerald ^[5] ; Michael,Gerisch ^[6] ; Heike,Gielen-Haertwig ^[3] ; Helmut,Haning ^[3] ; Dagmar,Karthaus ^[3] ; Dieter,Lang ^[6] ; Klemens,Lustig ^[6] ; Daniel,Meibom ^[3] ; Joachim,Mittendorf ^[3] ; Ulrich,Rosentreter ^[3] ; Martina,Schäfer ^[7] ; Stefan,Schäfer ^[4] ; Jens,Schamberger ^[3] ; Leila A,Telan ^[3] ; Adrian,Tersteegen ^[8]

作者单位： Medicinal Chemistry Berlin, Bayer HealthCare AG, 13353 Berlin (Germany). franz.nussbaum@bayer.com. ^[1] Lead Discovery Wuppertal, Bayer HealthCare AG, 42096 Wuppertal (Germany). volkhart.li@bayer.com. ^[2] Medicinal Chemistry Wuppertal, Bayer HealthCare AG, 42096 Wuppertal (Germany). ^[3] Department of Cardiology Research Wuppertal, Bayer HealthCare AG, 42096 Wuppertal (Germany). ^[4] COPD Research, Bayer Healthcare AG, Slough SL2 4LY, Berkshire (UK). ^[5] DMPK Wuppertal, Bayer HealthCare AG, 42096 Wuppertal (Germany). ^[6] Lead Discovery, Structural Biology Berlin, Bayer HealthCare AG, 13353 Berlin (Germany). ^[7] Lead Discovery Wuppertal, Bayer HealthCare AG, 42096 Wuppertal (Germany). ^[8]

关键词 biginelli reaction biological activity elastase inhibitors proteases pyrimidinones