CD86 expression as a surrogate cellular biomarker for pharmacologic inhibition of the histone demethylase LSD1.
Affiliation
Cancer Research UK Leukaemia Biology Laboratory, Paterson Institute for Cancer Research, The University of Manchester, Manchester, M20 4BX, United Kingdom.Issue Date
2013-07-30
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There is a lack of rapid cell-based assays that read out enzymatic inhibition of the histone demethylase LSD1. Through transcriptome analysis of human acute myeloid leukemia THP1 cells treated with a tranylcypromine-derivative inhibitor of LSD1 active in the low nanomolar range, we identified the cell surface marker CD86 as a sensitive surrogate biomarker of LSD1 inhibition. Within 24 hours of enzyme inhibition there was substantial and dose-dependent up regulation of CD86 expression, as detected by quantitative PCR, flow cytometry and ELISA. Thus, use of CD86 expression may facilitate screening of compounds with putative LSD1 inhibitory activities in cellular assays.Citation
CD86 expression as a surrogate cellular biomarker for pharmacologic inhibition of the histone demethylase LSD1. 2013: Anal BiochemJournal
Analytical BiochemistryDOI
10.1016/j.ab.2013.07.032PubMed ID
23911524Type
ArticleLanguage
enISSN
1096-0309ae974a485f413a2113503eed53cd6c53
10.1016/j.ab.2013.07.032
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