Histone Acetyltransferase Assays in Drug and Chemical Probe Discovery
نویسندگان
چکیده
Histone acetyltransferases (HATs) are a class of epigenetic enzymes involved in critical cellular processes like nucleosome assembly, DNA damage repair, and transcriptional regulation. HATs are implicated in many human pathologies including cancers. This chapter describes essential experimental considerations for performing high-throughput screening assays, and offers practical strategies for assay optimization and validation. Illustrative walkthroughs for several HAT assay formats are provided. This content should be useful for those performing HTS assays, orthogonal assays, and counter-screens involving HATs in the context of drug discovery, chemical biology, and molecular pharmacology. 1 Division of Pre-Clinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, USA. 2 Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD, USA. 3 Quantitative Biology, Eli Lilly and Company, Indianapolis, IN, USA. 4 Department of Pathology, Brigham and Women’s Hospital, Boston, MA, USA; Email: [email protected]. Corresponding author. NLM Citation: Gadhia S, Shrimp JH, Meier JL, et al. Histone Acetyltransferase Assays in Drug and Chemical Probe Discovery. 2017 Jul 26. In: Sittampalam GS, Coussens NP, Brimacombe K, et al., editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-. All Assay Guidance Manual content, except where otherwise noted, is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 3.0 Unported license (CC BY-NC-SA 3.0), which permits copying, distribution, transmission, and adaptation of the work, provided the original work is properly cited and not used for commercial purposes. Any altered, transformed, or adapted form of the work may only be distributed under the same or similar license to this
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