Mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles: Long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency

Biochemistry

Volumn 50, Issue 32, 2011, Pages 6867-6878

  Tian, Gaochao ^a,c   Paschetto, Kathy A ^a   Gharahdaghi, Farzin ^a   Gordon, Euan ^b   Wilkins, Dee E ^a,d   Luo, Xincai ^a   Scott, Clay W ^a  

^a ASTRAZENECA   (United Kingdom)

^b ASTRAZENECA R AND D   (Sweden)

^c GLAXOSMITHKLINE   (United States)

^d MEDIMMUNE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTI-INFLAMMATORY DRUGS; BENZOTHIAZOLES; CLEAVAGE PRODUCTS; ENZYME-INHIBITOR COMPLEX; FATTY ACID AMIDE HYDROLASE; HIGH POTENCY; IRREVERSIBLE INHIBITIONS; KINETIC BARRIER; MASS SPECTROMETRIC ANALYSIS; MOLECULAR DOCKING; PARENT COMPOUNDS; REACTION MIXTURE; RESIDENCE TIME; SELECTIVE INHIBITORS; STRUCTURAL FEATURE; TIME DEPENDENCE; TIME DEPENDENT; TRANSITION STATE;

AMIDES; DIALYSIS; ENZYME ACTIVITY; HYDROGEN BONDS; HYDROLASES; SULFUR COMPOUNDS;

FATTY ACIDS;

BENZOTHIAZOLE DERIVATIVE; FATTY ACID AMIDASE INHIBITOR; SULFONAMIDE;

ANIMAL CELL; ARTICLE; CATALYSIS; CONTROLLED STUDY; DIALYSIS; DRUG POTENCY; ENZYME ACTIVITY; ENZYME INHIBITION; HYDROGEN BOND; IC 50; MASS SPECTROMETRY; MEAN RESIDENCE TIME; MOLECULAR DOCKING; NONHUMAN; PRIORITY JOURNAL; PROTEIN CLEAVAGE; STOICHIOMETRY; THERMODYNAMICS;

AMIDOHYDROLASES; ANIMALS; BENZOTHIAZOLES; CHO CELLS; CRICETINAE; CRICETULUS; ENZYME INHIBITORS; HUMANS; KINETICS; RECOMBINANT PROTEINS; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; SULFONAMIDES; THERMODYNAMICS;

EID: 80051509102     PISSN: 00062960     EISSN: 15204995     Source Type: Journal    
DOI: 10.1021/bi200552p     Document Type: Article

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