Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes

Journal of the American Chemical Society

Volumn 134, Issue 25, 2012, Pages 10345-10348

  Adibekian, Alexander ^a,c   Martin, Brent R ^a,d   Chang, Jae Won ^a   Hsu, Ku Lung ^a   Tsuboi, Katsunori ^a   Bachovchin, Daniel A ^a   Speers, Anna E ^a   Brown, Steven J ^b   Spicer, Timothy ^b   Fernandez Vega, Virneliz ^b   Ferguson, Jill ^b   Hodder, Peter S ^b   Rosen, Hugh ^a   Cravatt, Benjamin F ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

^b SCRIPPS RESEARCH INSTITUTE   (United States)

^c UNIVERSITY OF GENEVA   (Switzerland)

^d UNIVERSITY OF MICHIGAN   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVITY-BASED PROBE; ACTIVITY-BASED PROTEIN PROFILING; ANIMAL MODEL; ENZYME FUNCTIONS; IN-VIVO; SERINE HYDROLASES; SMALL MOLECULES; SMALL-MOLECULE INHIBITORS; TARGET ENGAGEMENTS;

AMIDES; AMINO ACIDS; MOLECULES; PROBES;

ENZYME INHIBITION;

2 FUROYL PIPERAZINE AMIDE; LYASE INHIBITOR; N(P METHOXYPHENYL)PIPERAZINE AMIDE; SERINE DEHYDRATASE; SERINE HYDROLASE LYSOPHOSPHOLIPASE 1; SERINE HYDROLASE LYSOPHOSPHOLIPASE 2; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; COMPETITIVE ACTIVITY BASED PROTEIN PROFILING; DRUG BINDING; ENZYME ACTIVITY; ENZYME BINDING; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VIVO STUDY; MOLECULAR PROBE; MOUSE; NONHUMAN; PROTEIN ANALYSIS;

AMIDES; ANIMALS; BINDING, COMPETITIVE; CELLS, CULTURED; DRUG DELIVERY SYSTEMS; ENZYME INHIBITORS; MICE; MOLECULAR STRUCTURE; PIPERIDINES; PROTEIN BINDING; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84863443024     PISSN: 00027863     EISSN: 15205126     Source Type: Journal    
DOI: 10.1021/ja303400u     Document Type: Article

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