A three-step kinetic mechanism for selective inhibition of cyclo-oxygenase-2 by diarylheterocyclic inhibitors (Q28344403)

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R G Kurumbail

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J R Kiefer

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K T Moreland

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C M Koboldt

5

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P C Isakson

6

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K Seibert

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J K Gierse

Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis

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language of work or name

English

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publication date

1 August 2001

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published in

Biochemical Journal

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volume

357

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issue

Pt 3

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page(s)

709-18

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cites work

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Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor

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Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents

20 March 2017

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Synthesis and use of iodinated nonsteroidal antiinflammatory drug analogs as crystallographic probes of the prostaglandin H2 synthase cyclooxygenase active site

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The kinetic factors that determine the affinity and selectivity for slow binding inhibition of human prostaglandin H synthase 1 and 2 by indomethacin and flurbiprofen

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The X-ray crystal structure of the membrane protein prostaglandin H2 synthase-1

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Differential allosteric regulation of prostaglandin H synthase 1 and 2 by arachidonic acid

20 March 2017

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Acetylation of human prostaglandin endoperoxide synthase-2 (cyclooxygenase-2) by aspirin

20 March 2017

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Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase

7 April 2017

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Arachidonic acid oxygenation by COX-1 and COX-2. Mechanisms of catalysis and inhibition

29 September 2017

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Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles

29 September 2017

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The in vivo assessment of nimesulide cyclooxygenase-2 selectivity

29 September 2017

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Overview of nimesulide

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Pharmacological analysis of cyclooxygenase-1 in inflammation

29 September 2017

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Aspirin-like molecules that covalently inactivate cyclooxygenase-2.

29 September 2017

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Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).

29 September 2017

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Role of Val509 in time-dependent inhibition of human prostaglandin H synthase-2 cyclooxygenase activity by isoform-selective agents

29 September 2017

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Involvement of arginine 120, glutamate 524, and tyrosine 355 in the binding of arachidonate and 2-phenylpropionic acid inhibitors to the cyclooxygenase active site of ovine prostaglandin endoperoxide H synthase-1.

29 September 2017

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Mechanism of selective inhibition of the inducible isoform of prostaglandin G/H synthase

29 September 2017

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The behavior and significance of slow-binding enzyme inhibitors

29 September 2017

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Prostaglandin endoperoxide synthase: structure and catalysis

29 September 2017

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Structural requirements for time-dependent inhibition of prostaglandin biosynthesis by anti-inflammatory drugs

29 September 2017

1 reference

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Acetylation of prostaglandin synthase by aspirin

29 September 2017

1 reference

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Kinetic basis for selective inhibition of cyclo-oxygenases

29 September 2017

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Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms

2 June 2018

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Expression and selective inhibition of the constitutive and inducible forms of human cyclo-oxygenase

2 June 2018

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Anti-inflammatory and safety profile of DuP 697, a novel orally effective prostaglandin synthesis inhibitor

2 June 2018

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The dynamics of prostaglandin H synthases. Studies with prostaglandin h synthase 2 Y355F unmask mechanisms of time-dependent inhibition and allosteric activation

2 June 2018

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A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors.

27 November 2018

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Fluorescence quenching analysis of the association and dissociation of a diarylheterocycle to cyclooxygenase-1 and cyclooxygenase-2: dynamic basis of cyclooxygenase-2 selectivity

27 November 2018

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12 December 2020

Acetylation of prostaglandin endoperoxide synthetase with acetylsalicylic acid

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12 December 2020

Kinetics of factor Xa inhibition by tissue factor pathway inhibitor

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12 December 2020

NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro

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12 December 2020

Role of inducible cyclooxygenase (COX-2) in inflammation

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12 December 2020

Conversion of prostaglandin G/H synthase-1 into an enzyme sensitive to PGHS-2-selective inhibitors by a double His513 --> Arg and Ile523 --> val mutation

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12 December 2020

The advent of highly selective inhibitors of cyclooxygenase--a review

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12 December 2020

Hydroperoxide dependence and cooperative cyclooxygenase kinetics in prostaglandin H synthase-1 and -2

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12 December 2020