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Titlebook: HDAC/HAT Function Assessment and Inhibitor Development; Methods and Protocol Oliver H. Krämer Book 2023Latest edition The Editor(s) (if app

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Investigating Physiopathological Roles for Sirtuins in a Mouse Model metabolism, DNA repair, epigenetics, gene expression, cell proliferation, differentiation, and survival. Using genetically modified model organisms, sirtuins are proved to be one of the most conserved aging-regulatory and longevity-promoting genes/pathways among species. Of the seven sirtuins, SIRT
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Development of Pyrazine-Anilinobenzamides as Histone Deacetylase HDAC1–3 Selective Inhibitors and Bithe synthesis of a novel series of class-I selective HDAC inhibitors containing anilinobenzamide moieties as ZBG connected with a central (piperazin-1-yl)pyrazine moiety. Compounds were tested in vitro against class-I HDAC1, 2, and 3 isoforms. Some highly potent HDAC inhibitors were obtained and wer
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Evaluation of Small-Molecule HDAC Inhibitors Through In Vitro and In Cellulo Approachesl-molecule inhibitors that target one or more members of the HDAC protein family. Emerging HDAC inhibitors that show promise in drug discovery programs must be assessed across a range of . assays to establish an inhibitor profile for potency and cellular selectivity towards target HDAC(s) as well as
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Synthesis, Biochemical, and Cellular Evaluation of HDAC6 Targeting Proteolysis Targeting Chimeras functions and in the diseased state. Proteolysis-targeting chimeras (PROTACs) are bifunctional molecules that hijack the cell’s ubiquitin-proteasome system (UPS). One of the promising targets for this approach is histone deacetylase 6 (HDAC6), which is highly expressed in several types of cancers a
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Synthesis and Characterization of Reversible Covalent HDAC4 Inhibitorsreasing the residence time and prolonging the inhibitory effect on the target protein under nonequilibrium conditions. Herein, we describe the synthetic access to cyanoacrylate-based HDAC4 inhibitors and the procedures for the characterization of the transient nature of the covalent bond between cya
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