Target deconvolution of HDAC pharmacopoeia highlights MBLAC2 as common off-target

Abstract excerpt

<title>Abstract</title> <p>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-dependen...

Topics

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• Histone Deacetylase Inhibitors Research
• HIV/AIDS drug development and treatment
• Peptidase Inhibition and Analysis
• Protein Degradation and Inhibitors
• Synthetic Organic Chemistry Methods

Identifiers and source

Literature Corpus work

fb2c08ac-d670-593b-aa81-b400bd19c50f

DOI

10.21203/rs.3.rs-646613/v1