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3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3

Autor: Shevan Silva, Jack U. Flanagan, Daniel M. Heinrich, Ewald Schroeder, S.S. Samlal, P.J. Owen, Andrew P. Turnbull, Laurent Rigoreau, Tony Raynham, Emma J Hamilton, Darby G. Brooke, Christelle Soudy, Graham J. Atwell, William A. Denny, Elisabeth Trivier, Stephen M. F. Jamieson

Publikováno v: Journal of medicinal chemistry. 55(17)

A high-throughput screen identified 3-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic acid as a novel, highly potent (low nM), and isoform-selective (1500-fold) inhibitor of aldo-keto reductase AKR1C3: a target of interest in both breast and prostat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ba525a302b9dac275fadecf10b71aff
https://pubmed.ncbi.nlm.nih.gov/22877157

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Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets

Autor: Siobhan M. Hughes, Patricia Haus, Vanessa Petrucci, Thomas Leiser, Matthew J. Fuchter, S.S. Samlal, Andrew J. P. White, Robert J.K. Wood, Stephen Neidle, Fabrice Turlais, Matthias G. J. Baud, Ai Ching Wong, Lakjaya Buluwela, Franz-Josef Meyer-Almes, Mekala Gunaratnam

Publikováno v: Journal of medicinal chemistry. 55(4)

Psammaplin A (11c) is a marine metabolite previously reported to be a potent inhibitor of two classes of epigenetic enzymes: histone deacetylases and DNA methyltransferases. The design and synthesis of a focused library based on the psammaplin A core

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::746e44178705daaa043dcd345e13d517
https://pubmed.ncbi.nlm.nih.gov/22280363

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Abstract B166: Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets

Autor: Siobhan M. Hughes, Thomas Leiser, Mekala Gunaratnam, S.S. Samlal, Franz-Josef Meyer-Almes, Fabrice Turlais, Ai Ching Wong, Robert J.K. Wood, Stephen Neidle, Matthias G. J. Baud, Lakjaya Buluwela, Matthew J. Fuchter

Publikováno v: Molecular Cancer Therapeutics. 10:B166-B166

Naturally isolated products continue to play a significant role in anticancer drug discovery. In line with our interest in small molecule compounds which effect epigenetic gene regulation, we are interested in the structural and biological properties

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e19b546df9e0869de1d670de99e2b238
https://doi.org/10.1158/1535-7163.targ-11-b166

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