Výsledky vyhledávání - "Carol M. Koboldt"

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

Autor: Mark C. WALKER, Ravi G. KURUMBAIL, James R. KIEFER, Kirby T. MORELAND, Carol M. KOBOLDT, Peter C. ISAKSON, Karen SEIBERT, James K. GIERSE

Publikováno v: Biochemical Journal. 357:709-718

Cyclo-oxygenase (COX) enzymes are the targets for non-steroidal anti-inflammatory drugs (NSAIDs). These drugs demonstrate a variety of inhibitory mechanisms, which include simple competitive, as well as slow binding and irreversible inhibition. In ge

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6e9b9e573e979585f32e04be32523c50
https://doi.org/10.1042/bj3570709

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Characterization of the Recombinant IKK1/IKK2 Heterodimer

Autor: Troii Hall, Catherine S. Tripp, Bryan F. Kilpatrick, Beverly A. Reitz, Carol M. Koboldt, Cindy Sommers, Rodney G. Combs, Hymavathi Boddupalli, Jennifer L. Pierce, Q. Khai Huynh, Sharon A. Rouw, Robin A. Weinberg, Scott D. Hauser, Becky L. Hood, Judy A. Diaz-Collier

Publikováno v: Journal of Biological Chemistry. 275:25883-25891

Nuclear factor kappa B (NF-kappaB) is a ubiquitous, inducible transcription factor that regulates the initiation and progression of immune and inflammatory stress responses. NF-kappaB activation depends on phosphorylation and degradation of its inhib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b22aa869e2c4f4a40e73ba43cbda7da2
https://doi.org/10.1074/jbc.m000296200

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4,5-Diaryloxazole inhibitors of cyclooxygenase-2 (COX-2)

Autor: Jeffery S. Carter, John J. Talley, Karen Seibert, Stephen R. Bertenshaw, D. Joseph Rogier, Carol M. Koboldt, Graneto Matthew J, David L. Brown, Ben S. Zweifel, Jaime L. Masferrer, Bryan H. Norman

Publikováno v: Medicinal Research Reviews. 19:199-208

A series of methysulfonyl or sulfonamido substituted 4,5-diaryloxazole were prepared and evaluated for their ability to inhibit the inducible form of cyclooxygenase (COX-2) in vitro and in vivo. Several unique substitution patterns were identified th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::efe6962fa7e482f1968255b75b942a14
https://doi.org/10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co

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Kinetic basis for selective inhibition of cyclo-oxygenases

Autor: Carol M. Koboldt, Karen Seibert, Peter C. Isakson, James K. Gierse, Mark C. Walker

Publikováno v: Biochemical Journal. 339:607-614

Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit the formation of prostaglandins by cyclo-oxygenases (COX). The discovery of a second COX isoform (COX-2) associated with inflammation led to agents that selectively inhibit COX-2, e.g. celecoxib.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::585a6f6c18dcc7974bc8740804be4104
https://doi.org/10.1042/bj3390607

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Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors

Autor: Ben S. Zweifel, Paul W. Collins, Talley John J, Carol M. Koboldt, Jaime L. Masferrer, Jeffery S. Carter, Matthew J. Graneto, Karen Seibert, Thomas D. Penning, Steven Kramer

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:1171-1174

A series of sulfonamide-substituted 4,5-diarylthiazoles was prepared via three synthetic routes as selective COX-2 inhibitors. Recently in the synthesis of selective COX-2 inhibitors we have discovered that the sulfonamide moiety is a suitable replac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c086ea6a372b9f5bdc6acf943b35f74
https://doi.org/10.1016/s0960-894x(99)00157-2

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Pharmacological analysis of cyclooxygenase-1 in inflammation

Autor: Peter C. Isakson, Jaime L. Masferrer, Jerry Muhammad, John J. Talley, Ben S. Zweifel, Carol M. Koboldt, Alex Shaffer, Christopher J. Smith, Karen Seibert, Yan Zhang

Publikováno v: Proceedings of the National Academy of Sciences. 95:13313-13318

The enzymes cyclooxygenase-1 and cyclooxygenase-2 (COX-1 and COX-2) catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. These lipid mediators play important roles in inflammation and pain and in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f47be237b2576bc990e0e88ce51e347
https://doi.org/10.1073/pnas.95.22.13313

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3,4-diarylpyrazoles: Potent and selective inhibitors of cyclooxygenase-2

Autor: Len F. Lee, Steven W. Kramer, A. W. Veenhuizen, Carol M. Koboldt, Paul W. Collins, Yan Y. Zhang, Peter C. Isakson, Karen Seibert, Thomas D. Penning

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:2121-2124

A series of 3,4-diarylpyrazoles was synthesized and evaluated for their ability to selectively inhibit cyclooxygenase-2 (COX-2). A number of potent and selective inhibitors were identified and found to have oral anti-inflammatory activity in a rat ca

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::479d32fe6815640e8bcff985c1ac75d3
https://doi.org/10.1016/s0960-894x(97)00372-7

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1,2-Diarylimidazoles as Potent, Cyclooxygenase-2 Selective, and Orally Active Antiinflammatory Agents

Autor: Yu Yi, Jacquelen J. Casler, Peter C. Isakson, Jaime L. Masferrer, Ish K. Khanna, Francis J. Koszyk, Paul W. Collins, Karen Seibert, Richard M. Weier, Yan Zhang, A. W. Veenhuizen, Carol M. Koboldt, Xiangdong Xu, William E. Perkins, S. A. Gregory

Publikováno v: Journal of Medicinal Chemistry. 40:1634-1647

Series of 1,2-diarylimidazoles has been synthesized and found to contain highly potent and selective inhibitors of the human COX-2 enzyme. The paper describes a short synthesis of the target 1,2-diarylimidazoles starting with aryl nitriles. Different

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c93724e239a9064506c442ec529d65fd
https://doi.org/10.1021/jm9700225

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1,2-Diarylpyrroles as Potent and Selective Inhibitors of Cyclooxygenase-2

Autor: Richard M. Weier, Julie M. Miyashiro, Karen Seibert, Jerry L. Currie, Paul W. Collins, Ish K. Khanna, A. W. Veenhuizen, Carol M. Koboldt, Peter C. Isakson, Yu Yi

Publikováno v: Journal of Medicinal Chemistry. 40:1619-1633

Series of 1,2-diarylpyrroles has been synthesized and found to contain very potent and selective inhibitors of the human cyclooxygenase-2 (COX-2) enzyme. The paper describes short and practical syntheses of the target molecules utilizing the Paal-Kno

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ae2f38b3e790d46f5eb64f1d1bd7a11
https://doi.org/10.1021/jm970036a

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Diarylspiro[2.4]heptenes as Orally Active, Highly Selective Cyclooxygenase-2 Inhibitors: Synthesis and Structure−Activity Relationships

Autor: Gary D. Anderson, A. W. Veenhuizen, Carol M. Koboldt, Karen Seibert, Robert E. Manning, William E. Perkins, Yan Zhang, Horng-Chi Huang, J. N. Cogburn, D. J. Garland, Jinglin Li, Emily J. Reinhard, David B. Reitz, S. A. Gregory, Timothy S. Chamberlain, E. G. Burton, Peter C. Isakson

Publikováno v: Journal of Medicinal Chemistry. 39:253-266

A novel series of 5,6-diarylspiro[2.4]hept-5-enes was shown to provide highly potent and selective cyclooxygenase-2 (COX-2) inhibitors. A study of structure-activity relationships in this series suggests that 3,4-disubstituted phenyl analogs are gene

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c9ef2e75bc7cbe29bd4ca9744f026f5
https://doi.org/10.1021/jm950664x

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