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Author(s):
Lechner, Severin; Malgapo, Martin; Grätz, Christian; Baron, Agnes; Rüther, Patrick Leopold; Nadal, Simon; Stumpf, Carmen; Loos, Christina; Ku, Xin; Prokofeva, Polina; Lautenbacher, Ludwig; Heimburg, Tino; Würf, Vivian; Meng, Chen; Sippl, Wolfgang; Wilhelm, Mathias; Kleigrewe, Karin; Pauling, Josch; Kramer, Karl; Pfaffl, Michael; Linder, Maurine; Kuster, Bernhard; Médard, Guillaume
Title:
Target deconvolution of HDAC pharmacopoeia highlights MBLAC2 as common off-target
Abstract:
HDAC drugs have entered the pharmacopoeia in the 2000s. However, some enigmatic phenotypes suggest off-target engagement. Here, we developed a chemical proteomics assay using three promiscuous chemotypes and quantitative mass spectrometry that we deployed to establish the target landscape of 53 drugs. The results highlight 14 direct targets, including 9 out of the 11 human zinc-dependent HDACs, question the reported selectivity of widely-used molecules, notably for HDAC6, and delineate how the c...    »
Publisher:
Research Square
Year:
2021
Language:
de
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