A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.

de Garavilla, Lawrence; Greco, Michael N; Sukumar, Narayanasami; Chen, Zhi-Wei; Pineda, Agustin O; Mathews, F Scott; Di Cera, Enrico; Giardino, Edward C; Wells, Grace I; Haertlein, Barbara J; Kauffman, Jack A; Corcoran, Thomas W; Derian, Claudia K; Eckardt, Annette J; Damiano, Bruce P; Andrade-Gordon, Patricia; Maryanoff, Bruce E

de Garavilla, Lawrence; Greco, Michael N; Sukumar, Narayanasami; Chen, Zhi-Wei; Pineda, Agustin O; Mathews, F Scott; Di Cera, Enrico; Giardino, Edward C; Wells, Grace I; Haertlein, Barbara J; Kauffman, Jack A; Corcoran, Thomas W; Derian, Claudia K; Eckardt, Annette J; Damiano, Bruce P; Andrade-Gordon, Patricia; Maryanoff, Bruce E.

Affiliation

de Garavilla L; Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, Spring House, Pennsylvania 19477-0776, USA.

J Biol Chem ; 280(18): 18001-7, 2005 May 06.

Article in En | MEDLINE | ID: mdl-15741158

Subject(s)

Anti-Inflammatory Agents, Non-Steroidal/pharmacology; Cathepsins/antagonists & inhibitors; Cathepsins/metabolism; Leukocytes/enzymology; Organophosphonates/pharmacology; Piperidines/pharmacology; Serine Endopeptidases/metabolism; Serine Proteinase Inhibitors/pharmacology; Acute Disease; Animals; Anti-Inflammatory Agents, Non-Steroidal/administration & dosage; Anti-Inflammatory Agents, Non-Steroidal/chemistry; Cathepsin G; Chymases; Crystallography, X-Ray; Humans; Leukocytes/drug effects; Male; Mast Cells/enzymology; Organophosphonates/administration & dosage; Organophosphonates/chemistry; Peritonitis/drug therapy; Peritonitis/enzymology; Piperidines/chemistry; Pulmonary Disease, Chronic Obstructive/drug therapy; Pulmonary Disease, Chronic Obstructive/enzymology; Rats; Rats, Sprague-Dawley; Serine Proteinase Inhibitors/administration & dosage; Serine Proteinase Inhibitors/chemistry

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Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Serine Endopeptidases / Cathepsins / Serine Proteinase Inhibitors / Anti-Inflammatory Agents, Non-Steroidal / Organophosphonates / Leukocytes Type of study: Prognostic_studies Limits: Animals / Humans / Male Language: En Journal: J Biol Chem Year: 2005 Type: Article Affiliation country: United States

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