Výsledky vyhledávání - "Lawrence Ivan Kruse"

Synthesis of Novel Thiol-Containing Citric Acid Analogs. Kinetic Evaluation of These and Other Potential Active-Site-Directed and Mechanism-Based Inhibitors of ATP Citrate Lyase

Autor: Timothy N. C. Wells, Drake S. Eggleston, Tracey Wilkes, Pieter H. E. Groot, Lawrence Ivan Kruse, Andy Gribble, Roland E. Dolle, Barbara A. Saxty

Publikováno v: Journal of Medicinal Chemistry. 38:537-543

ATP citrate lyase is an enzyme involved in mammalian lipogenesis and cholesterogenesis. Inhibitors of the enzyme represent a potentially novel class of hypolipidemic agents. Citric acid analogues 5-16 bearing electrophilic and latent electrophilic su

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8e95ad83123e7a1aa1341cc38c340cc
https://doi.org/10.1021/jm00003a016

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ATP-citrate-lyase as a target for hypolipidemic intervention. Sulfoximine and 3-hydroxy-.beta.-lactam containing analogs of citric acid as potential tight-binding inhibitors

Autor: Lawrence Ivan Kruse, Drake Eggelston, Timothy N. C. Wells, David McNair, Pieter H. E. Groot, Roland E. Dolle, Mark J. Hughes, Barbara A. Saxty

Publikováno v: Journal of Medicinal Chemistry. 35:4875-4884

Citric acid analogues (+/-)-12a,b and (+/-)-17a,b, where one of the primary carboxylates has been replaced by a sulfoximinoyl and a 3-(3-hydroxy-beta-lactamyl) moiety, respectively, have been synthesized and evaluated as inhibitors of ATP-citrate lya

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bd5a27e3884e783ee004185eefc5e2b
https://doi.org/10.1021/jm00104a014

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Enantiospecific synthesis of (-)-tabtoxinine .beta.-lactam

Autor: Lawrence Ivan Kruse, Dolle Roland E, Chun Sing Li, Riccardo Novelli, Drake S. Eggleston

Publikováno v: The Journal of Organic Chemistry. 57:128-132

Key features of the synthetic route include preparation of a new γ-cation amino acid synthon and its use as an electrophile,the one pot conversion of methyl sulfide to the Cbz-protected amine via stereoselective sulfilimine rearrangement and chemose

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f7ac8c647acdf8b524343f5c52fb8c04
https://doi.org/10.1021/jo00027a024

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Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans .DELTA.24-sterol methyltransferase

Autor: Jerry L. Adams, Schmidt Stanley J, Lawrence Ivan Kruse, Carrie L. Frey, Roland E. Dolle, Mark A. Ator, Janice M. Barone

Publikováno v: Journal of Medicinal Chemistry. 35:100-106

A series of side chain modified analogues of cholesterol and lanosterol (1-10) have been synthesized and evaluated as inhibitors of the Candida albicans delta 24-sterol methyltransferase. Two sterol substrate analogues 1 and 2 which contained a 24-th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02db83aa7134f4b3ecaf8181ac11eb64
https://doi.org/10.1021/jm00079a012

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Bovine dopamine .beta.-hydroxylase, primary structure determined by cDNA cloning and amino acid sequencing

Autor: Walter E. DeWolf, Christopher Southan, Naiyin Wang, Timothy N. C. Wells, Robin J. Leatherbarrow, Lawrence Ivan Kruse

Publikováno v: Biochemistry. 29:6466-6474

A cDNA clone encoding bovine dopamine beta-hydroxylase (DBH) has been isolated from bovine adrenal glands. The clone hybridizes to two oligonucleotide probes, one based on a previously reported active site peptide [DeWolf, W. E., Jr., et al. (1988) B

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8330589e00c33da4b5fd76837ad9556f
https://doi.org/10.1021/bi00479a019

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Synthesis and evaluation of (+) and (-)-2,2-difluorocitrate as inhibitors of rat-liver ATP-citrate lyase and porcine-heart aconitase

Autor: David G. Reid, Patrick Camilleri, Riccardo Novelli, Barbara A. Saxty, Lawrence Ivan Kruse, Dolle Roland E, Timothy N. C. Wells

Publikováno v: European journal of biochemistry. 202(3)

The enantiomers (+) and (-)-2,2-difluorocitrate have been synthesized. Both are good inhibitors of ATP-citrate lyase, showing competitive inhibition against citrate, with Kis = 0.7 microM for (+)-2,2-difluorocitrate and 3.2 microM for (-)-2,2-difluor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c382908398f2c26b6631e467e4ececac
https://pubmed.ncbi.nlm.nih.gov/1765100

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Inactivation of dopamine .beta.-hydroxylase by .beta.-ethynyltyramine: kinetic characterization and covalent modification of an active site peptide

Autor: Christopher Southan, David R. Saunders, Lawrence Ivan Kruse, Walter E. DeWolf, Pamela Anne Chambers

Publikováno v: Biochemistry. 28:3833-3842

beta-Ethynyltyramine has been shown to be a potent, mechanism-based inhibitor of dopamine beta-hydroxylase (DBH). This is evidenced by pseudo-first-order, time-dependent inactivation of enzyme, a dependence of inactivation on the presence of ascorbat

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https://doi.org/10.1021/bi00435a032

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