Kinetic and structural characterization of caspase-3 and caspase-8 inhibition by a novel class of irreversible inhibitors

Biochimica et Biophysica Acta - Proteins and Proteomics

Volumn 1804, Issue 9, 2010, Pages 1817-1831

  Wang, Zhigang ^a   Watt, William ^a,c   Brooks, Nathan A ^a,g   Harris, Melissa S ^b   Urban, Jan ^c   Boatman, Douglas ^d   McMillan, Michael ^e   Kahn, Michael ^e,f   Heinrikson, Robert L ^c   Finzel, Barry C ^a,h   Wittwer, Arthur J ^b   Blinn, James ^b   Kamtekar, Satwik ^b,i   Tomasselli, Alfredo G ^b,c  

^a PFIZER INC   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

^c University of Southern California ^*  (United States)

^d ARENA PHARMACEUTICALS   (United States)

^e UNIVERSITY OF SOUTHERN CALIFORNIA   (United States)

^f UNIVERSITY OF SOUTHERN CALIFORNIA   (United States)

^g ELI LILLY AND COMPANY   (United States)

^h UNIVERSITY OF MINNESOTA   (United States)

ⁱ PACIFIC BIOSCIENCES   (United States)

Author keywords

Caspase 3; Caspase 8; Crystal structure; Irreversible inhibition; Peptidomimetic inhibitors; Urazole

Indexed keywords

BENZYLOXYCARBONYLVALYLALANYLASPARTYL FLUOROMETHYL KETONE; CASPASE 3; CASPASE 3 INHIBITOR; CASPASE 8; CASPASE 8 INHIBITOR; PEPTIDOMIMETIC AGENT; CASPASE INHIBITOR; CYSTEINE PROTEINASE INHIBITOR;

ARTICLE; BINDING COMPETITION; BINDING SITE; COMPETITIVE INHIBITION; CRYSTAL STRUCTURE; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME KINETICS; ENZYME MECHANISM; ENZYME STRUCTURE; ENZYME SUBSTRATE; MOLECULAR INTERACTION; PRIORITY JOURNAL; STEADY STATE; STRUCTURE ANALYSIS; CHEMICAL STRUCTURE; CHEMISTRY; CRYSTALLIZATION; HUMAN; KINETICS; PROTEIN CONFORMATION; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

CASPASE 3; CASPASE 8; CASPASE INHIBITORS; CRYSTALLIZATION; CRYSTALLOGRAPHY, X-RAY; CYSTEINE PROTEINASE INHIBITORS; HUMANS; KINETICS; MOLECULAR STRUCTURE; PROTEIN CONFORMATION;

EID: 77955095875     PISSN: 15709639     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bbapap.2010.05.007     Document Type: Article

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