Výsledky vyhledávání - "James K. Gierse"

Interactions of C4 Subtype Metabolic Activities and Transport in Maize Are Revealed through the Characterization of DCT2 Mutants

Autor: Fangfang Ma, Howard Berg, Thomas P. Brutnell, Mitsutaka Taniguchi, Sarit Weissmann, Doug K. Allen, James K. Gierse, Koki Furuyama, Ying Shao

Publikováno v: The Plant Cell. 28:466-484

C4 photosynthesis in grasses requires the coordinated movement of metabolites through two specialized leaf cell types, mesophyll (M) and bundle sheath (BS), to concentrate CO2 around Rubisco. Despite the importance of transporters in this process, fe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff102fd702e432ff296e6c607ee0842a
https://doi.org/10.1105/tpc.15.00497

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Structure-based parallel medicinal chemistry approach to improve metabolic stability of benzopyran COX-2 inhibitors

Autor: James K. Gierse, Jeffery S. Carter, Li Xing, Bruce C. Hamper, Liao Subo, Jay M. Wendling, Theresa R. Fletcher

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:993-996

Combination of the structure-based design and solid-phase parallel synthesis provided an integrated approach to rapidly develop the structure-activity relationship of benzopyran COX-2 inhibitors. Binding free energies predicted by free energy perturb

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3d81c3439d005cb61361c5519f07153
https://doi.org/10.1016/j.bmcl.2010.12.023

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Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor

Autor: Stephen J. Mnich, Olga V. Nemirovskiy, James K. Gierse, Gabriel Mbalaviele, Adele M. Pauley, Alexander F. Shaffer, William M. Moore, Sumathy Mathialagan, Ben S. Zweifel, Jeffrey S. Carter, Jaime L. Masferrer, Michael L. Vazquez, Jane L. Wang

Publikováno v: Biochemical Pharmacology. 79:1445-1454

Inflammation-induced microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal enzyme that synthesizes prostaglandin E(2) (PGE(2)) downstream of cyclooxygenase-2 (COX-2). The efficacy of nonsteroidal anti-inflammatory drugs and COX-2 inhibitors

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52f2b47310c2ae7d1f319e11e57535cc
https://doi.org/10.1016/j.bcp.2010.01.003

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Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template

Autor: Jeff Carter, David C. Limburg, Jane Wang, James K. Gierse, Gabriel Mbalaviele, Michael L. Vazquez

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:1604-1609

Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE(2) inhibition in a cell-based as

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f957469e458a5b931551f698b66e9466
https://doi.org/10.1016/j.bmcl.2010.01.060

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Development of a fluorescence-based enzyme assay of human 5-lipoxygenase

Autor: Rob Hills, Robin A. Weinberg, Thomas P. Kasten, Beverly A. Reitz, Jaime L. Masferrer, Robert A. Pufahl, James K. Gierse

Publikováno v: Analytical Biochemistry. 364:204-212

Leukotrienes are important mediators in a number of inflammatory diseases and therefore are a target of several therapeutic approaches. The first committed step in the synthesis of leukotrienes is the conversion of arachidonic acid to leukotriene A(4

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f12ee570c709786c1a173079c7efe50e
https://doi.org/10.1016/j.ab.2007.02.009

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Enzymologic and Pharmacologic Profile of Loxoprofen Sodium and Its Metabolites

Autor: Mark C. Walker, Ben S. Zweifel, Masao Sasamata, Aishi Kimoto, Masahiro Noguchi, Kazutoshi Nozaki, James K. Gierse

Publikováno v: Biological and Pharmaceutical Bulletin. 28:2075-2079

We investigated the mechanism of inhibition of loxoprofen sodium, a non-steroidal anti-inflammatory drug (NSAID), and its active metabolite (loxoprofen-SRS) on cyclooxygenase (COX). In in vitro assays, loxoprofen sodium appeared inactive against reco

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fb4c8ab41b552b02108b7f7dba9dccc
https://doi.org/10.1248/bpb.28.2075

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Synthesis of Potent Leukotriene A4 Hydrolase Inhibitors. Identification of 3-[Methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic Acid

Autor: Walter G. Smith, Suzanne H Kim, Doreen Villani-Price, Matthew W Mahoney, Nayereh S Ghoreishi-Haack, Helen Y. Chen, Thomas D. Penning, Stella Siu-Tzyy Yu, James W. Malecha, Leslie J Askonas, Chi-Dean Liang, Elizabeth I Harding, E.Yvonne Pyla, Maureen K Highkin, James K. Gierse, Julie M Miyashiro, Mark A Russell, James F Kachur, Chen Barbara B

Publikováno v: Journal of Medicinal Chemistry. 45:3482-3490

Leukotriene B(4) (LTB(4)) is a potent, proinflammatory mediator involved in the pathogenesis of a number of diseases including inflammatory bowel disease, psoriasis, rheumatoid arthritis, and asthma. The enzyme LTA(4) hydrolase represents an attracti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49aaaeb42023ad7fd78de02ecc724a97
https://doi.org/10.1021/jm0200916

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Quantification of peptide m/z distributions from 13C-labeled cultures with high-resolution mass spectrometry

Autor: Dominic E. Mandy, Doug K. Allen, James K. Gierse, Joshua E. Goldford, Christine H. Diepenbrock, Igor G. L. Libourel

Publikováno v: Analytical Chemistry

Isotopic labeling studies of primary metabolism frequently utilize GC/MS to quantify (13)C in protein-hydrolyzed amino acids. During processing some amino acids are degraded, which reduces the size of the measurement set. The advent of high-resolutio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5859ac91838ffcd0ea4ad31d5db0705
https://pubmed.ncbi.nlm.nih.gov/24387081

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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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Spatial Requirements for 15-(R)-Hydroxy-5Z,8Z,11Z,13E-eicosatetraenoic Acid Synthesis within the Cyclooxygenase Active Site of Murine COX-2

Autor: Lawrence J. Marnett, Douglas C. Goodwin, Brenda C. Crews, Scott W. Rowlinson, James K. Gierse, Claus Schneider

Publikováno v: Journal of Biological Chemistry. 275:6586-6591

The two isoforms of cyclooxygenase, COX-1 and COX-2, are acetylated by aspirin at Ser-530 and Ser-516, respectively, in the cyclooxygenase active site. Acetylated COX-2 is essentially a lipoxygenase, making 15-(R)-hydroxyeicosatetraenoic acid (15-HET

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a85644973b27443cb27d888d43aac077
https://doi.org/10.1074/jbc.275.9.6586

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