Comprehensive mechanistic view of the hydrolysis of oxadiazole-based inhibitors by Histone Deacetylase 6 (HDAC6) [PDF]
, 2023 Histone deacetylase (HDAC) inhibitors used in the clinic typically contain a hydroxamate zinc-binding group (ZBG). However, more recent work has shown that the use of alternative ZBGs, and, in particular, the heterocyclic oxadiazoles, can confer higher ...
Andris, Erik +14 more
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Cellular analysis of the action of epigenetics drugs and probes [PDF]
, 2017 Small molecule drugs and probes are important tools in drug discovery, pharmacology, and cell biology. This is of course also true for epigenetic inhibitors.
A. Ganesan +12 more
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Crystal structure of a TbIII–CuII glycinehydroxamate 15-metallacrown-5 sulfate complex
Acta Crystallographica Section E: Crystallographic Communications, 2021 The core of the title complex, bis[hexaaquahemiaquapentakis(μ3-glycinehydroxamato)sulfatopentacopper(II)terbium(III)] sulfate hexahydrate, [TbCu5(SO4)(GlyHA)5(H2O)6.5]2(SO4)·6H2O (1), which belongs to the 15-metallacrown-5 family, consists of five ...
Anna V. Pavlishchuk +3 more
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Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors [PDF]
, 2008 The antimalarial activity and pharmacology of a series of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors (HDACIs) was evaluated.
Dow, Geoffrey S. +11 more
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First crystal structures of 1-deoxy-D-xylulose 5-phosphate synthase (DXPS) from Mycobacterium tuberculosis indicate a distinct mechanism of intermediate stabilization [PDF]
, 2022 The development of drug resistance by Mycobacterium tuberculosis and other pathogenic bacteria emphasizes the need for new antibiotics. Unlike animals, most bacteria synthesize isoprenoid precursors through the MEP pathway. 1-Deoxy-D-xylulose 5-phosphate
Alhayek, Alaa +10 more
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Iraqi Journal of Pharmaceutical Sciences, 2023 Histone acetylation is a highly interesting epigenetic target for drug therapy. Histone deacetylase enzymes (HDACs) are overexpressed in several diseases, including cancers. Most of the clinically used HDAC inhibitors involve hydroxamate group as a zinc-
Ali Mohammed Saeed +1 more
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Archives of Pharmaceutical Sciences Ain Shams University, 2018 Despite the increased success rates of histone deacetylases inhibitors (HDACi) as potent anticancer agents, many metabolic obstacles face the hydroxamic acid-based HDAC inhibitors, which inspired us to develop non-hydroxamate HDAC inhibitors.
Heba M. Hesham +2 more
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Constitutive Stringent Response Restores Viability of Bacillus subtilis Lacking Structural Maintenance of Chromosome Protein. [PDF]
PLoS ONE, 2015 Bacillus subtilis mutants lacking the SMC-ScpAB complex are severely impaired for chromosome condensation and partitioning, DNA repair, and cells are not viable under standard laboratory conditions.
Camille Benoist +3 more
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Probes for Non-invasive Matrix Metalloproteinase-targeted Imaging with PET and SPECT [PDF]
, 2013 Dysregulation of matrix metalloproteinase (MMP) activity can lead to a wide range of disease states such as atherosclerosis, inflammation or cancer. The ability to image MMP activity non-invasively in vivo, by radiolabelled synthetic inhibitors, would ...
Bischoff, Rainer +6 more
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Acta Pharmaceutica Sinica B, 2011 Ligand- and structure-based virtual screening methods were employed to identify novel non-hydroxamate histone deacetylase (HDAC) inhibitors. Based on the newly identified hit compound 17a, three series of compounds were synthesized and evaluated for both
Hui Lu +3 more
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