Lead discovery for microsomal prostaglandin e synthase using a combination of high-throughput fluorescent-based assays and RapidFire mass spectrometry

Journal of Biomolecular Screening

Volumn 17, Issue 5, 2012, Pages 641-650

  Leveridge, Melanie V ^a   Bardera, Ana Isabel ^b   Lamarr, William ^c   Billinton, Andrew ^a   Bellenie, Ben ^a   Edge, Colin ^a   Francis, Peter ^a   Christodoulou, Erica ^a   Shillings, Anthony ^a   Hibbs, Martin ^a   Fosberry, Andrew ^a   Tanner, Rob ^a   Hardwicke, Philip ^a   Craggs, Peter ^a   Sinha, Yugesh ^a   Elegbe, Oluseyi ^a   Alvarez Ruiz, Emilio ^b   Martin Plaza, Jose Julio ^b   Barroso Poveda, Vanessa ^b   Baddeley, Stuart ^a   Chung, Chun Wa ^a   Hutchinson, Jonathan ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (Spain)

^c Agilent Technologies   (United States)

Author keywords

fluorescence; HTS; mPGES 1; RapidFire mass spectrometry

Indexed keywords

15 HYDROXYPROSTAGLANDIN DEHYDROGENASE; ARACHIDONIC ACID; CYCLOOXYGENASE 2; DIHYDROLIPOAMIDE DEHYDROGENASE; ENZYME INHIBITOR; PROSTAGLANDIN E SYNTHASE; PROSTAGLANDIN E SYNTHASE INHIBITOR; PROSTAGLANDIN E2; PROSTAGLANDIN H2; UNCLASSIFIED DRUG;

ANALYTIC METHOD; CONTROLLED STUDY; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME MECHANISM; ENZYME SUBSTRATE; FLUORESCENCE; HIGH THROUGHPUT SCREENING; HUMAN; IC 50; MASS SPECTROMETER; MASS SPECTROMETRY; MICROSOME; PAIN; PRIORITY JOURNAL; REPRODUCIBILITY; REVIEW; RHEUMATOID ARTHRITIS; VALIDITY;

CYCLOOXYGENASE 2; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; ENZYME INHIBITORS; FLUORESCENT DYES; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INHIBITORY CONCENTRATION 50; INTRAMOLECULAR OXIDOREDUCTASES; MASS SPECTROMETRY;

EID: 84861799753     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057111435700     Document Type: Review

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