Zobrazeno 1 - 10 of 24 pro vyhledávání: '"William R. Mann"'
2
Secondary Amides of (R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionic Acid as Inhibitors of Pyruvate Dehydrogenase Kinase
Autor: Gary M. Coppola, Xilin Liu, Robert C. Anderson, Douglas C. Knorr, William S. Fillers, James L. Stanton, Jiaping Gao, Tomaselli Hc, Christine C. Vinluan, Thomas Daniel Aicher, Carol J. Dragland, Suraj S. Shetty, Wieslawa Maniara, A. Islam, Emma L. Kaplan, William R. Mann, Leonard J. Brand, Donald Mark Sperbeck, R. E. Walter, Dominick DelGrande, R. J. Lozito
Publikováno v: Journal of Medicinal Chemistry. 43:236-249
N‘-Methyl-N-(4-tert-butyl-1,2,5,6-tetrahydropyridine)thiourea, SDZ048-619 (1), is a modest inhibitor (IC50 = 180 μM) of pyruvate dehydrogenase kinase (PDHK). In an optimization of the N-methylcarbothioamide moiety of 1, it was discovered that amid
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5a21921472d2095e7c5eea09d6d92805
https://doi.org/10.1021/jm990358+
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3
Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK)
Autor: Emma L. Kaplan, Jiaping Gao, Leonard J. Brand, Robert E. Damon, Judit Koletar, Christine C. Vinluan, Suraj S. Shetty, Thomas Daniel Aicher, William R. Mann
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:2223-2228
Several oximes of triterpenes with a 17-beta hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity. The oxime 12 and dehydroabietyl amine 2 exhibit a blood glucose lowering effect in the diabetic ob/ob mouse
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7845fb3e46576be1780877fa834d49f
https://doi.org/10.1016/s0960-894x(99)00380-7
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5
Heterologously expressed inner lipoyl domain of dihydrolipoyl acetyltransferase inhibits ATP-dependent inactivation of pyruvate dehydrogenase complex
Autor: Bing Yan, Sid Topiol, Thomas Daniel Aicher, Carol J. Dragland, Vijayayakumar Sundararajan, John C. Jackson, William R. Mann, John E. Blume, Philip A. Bell, Paul Ramage, Christine C. Vinluan, John S. Gounarides, N. R. Nirmala
Publikováno v: Biochemical Journal. 334:703-711
The activity of the pyruvate dehydrogenase multienzyme complex (PDC), which catalyses the oxidation of pyruvate to acetyl-CoA within the mitochondrion, is diminished in animal models of diabetes. Studies with purified PDC components have suggested th
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::405c028ae9929d1cb5f403e9247ed185
https://doi.org/10.1042/bj3340703
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6
Effects of substrate binding and pH on the secondary structure of carnitine acetyltransferase
Autor: Philip A. Bell, William R. Mann, Bing Yan
Publikováno v: Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology. 1253:175-180
Carnitine acetyltransferase (CAT) exists as a monomer in solution as demonstrated by dynamic light scattering measurements. Under these conditions, interactions between CAT and its substrates, L-carnitine and acetyl-CoA, were studied by circular dich
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8cec075c8dcbbd738d0d06aa6833364
https://doi.org/10.1016/0167-4838(95)00159-2
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7
Kinetic, Circular Dichroism and Fluorescence Studies on Heterologously Expressed Carnitine Palmitoyltransferase II
Autor: Carol J. Dragland, William R. Mann, Philip A. Bell, Bing Yan
Publikováno v: Journal of Enzyme Inhibition. 9:303-308
Km estimates for carnitine and palmitoyl-CoA of heterologously expressed rat liver carnitine palmitoyl-transferase-II (rCPT-II) were 950 +/- 27 microM and 34 +/- 6 microM, respectively. Vmax for the enzyme was 1.8 mumol/min/mg purified protein. Consi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fcd8d2e35893554780839c6cc36fb6b2
https://doi.org/10.3109/14756369509036559
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8
ChemInform Abstract: Triterpene and Diterpene Inhibitors of Pyruvate Dehydrogenase Kinase (PDK)
Autor: Emma L. Kaplan, William R. Mann, Suraj S. Shetty, Christine C. Vinluan, Judit Koletar, Robert E. Damon, Jiaping Gao, Leonard J. Brand, Thomas Daniel Aicher
Publikováno v: ChemInform. 30
Several oximes of triterpenes with a 17-β hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity. The oxime 12 and dehydroabietyl amine 2 exhibit a blood glucose lowering effect in the diabetic ob/ob mouse a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bffb978b3fe8103e27196390eda837ac
https://doi.org/10.1002/chin.199945217
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10
Diverse mechanisms of inhibition of pyruvate dehydrogenase kinase by structurally distinct inhibitors
Autor: Carol J. Dragland, William R. Mann, Philip A. Bell, T.R Vedananda, Thomas Daniel Aicher, Christine C. Vinluan
Publikováno v: Biochimica et biophysica acta. 1480(1-2)
The mechanism of action of structurally distinct pyruvate dehydrogenase kinase (PDK) inhibitors was examined in assays with experimental contexts ranging from an intact pyruvate dehydrogenase complex (PDC) with and without supplemental ATP or ADP to
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::409b5e166d22171d1c1e527822433cb6
https://pubmed.ncbi.nlm.nih.gov/11004568
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