title: High-throughput screening to identify inhibitors of lysine demethylases.
abstract: Lysine demethylases (KDMs) are epigenetic regulators whose dysfunction is implicated in the pathology of many human diseases including various types of cancer, inflammation and X-linked intellectual disability. Particular demethylases have been identified as promising therapeutic targets, and tremendous efforts are being devoted toward developing suitable small-molecule inhibitors for clinical and research use. Several High-throughput screening strategies have been developed to screen for small-molecule inhibitors of KDMs, each with advantages and disadvantages in terms of time, cost, effort, reliability and sensitivity. In this Special Report, we review and evaluate the High-throughput screening methods utilized for discovery of novel small-molecule KDM inhibitors.
authors: Department of Pathology, Yale School of Medicine, New Haven, 310 Cedar St., BML348C, PO Box 208023, New Haven, CT 06520, USA.
authors: Molly
authors: M
authors: Gale
authors: Qin
authors: Q
authors: Yan
mesh_terms: D000906:Antibodies; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D057166:High-Throughput Screening Assays / Q000379:methods*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors*; D013058:Mass Spectrometry
chemical_list: D000906:Antibodies; D004791:Enzyme Inhibitors; D056466:Histone Demethylases
keywords: High-throughput screening; JmjC; KDM; LSD1; lysine demethylase; small-molecule inhibitor