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

Histone deacetylase (HDAC) targeting drugs have entered the pharmacopoeia in the 2000s. However, some enigmatic phenotypes suggest off-target engagement. Here, we developed a quantitative chemical proteomics assay using immobilized HDAC inhibitors and mass spectrometry that we deployed to establish...

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Detalles Bibliográficos
Autores principales: Lechner, Severin, Malgapo, Martin Ian P., Grätz, Christian, Steimbach, Raphael R., Baron, Agnes, Rüther, Patrick, Nadal, Simon, Stumpf, Carmen, Loos, Christina, Ku, Xin, Prokofeva, Polina, Lautenbacher, Ludwig, Heimburg, Tino, Würf, Vivian, Meng, Chen, Wilhelm, Mathias, Sippl, Wolfgang, Kleigrewe, Karin, Pauling, Josch K., Kramer, Karl, Miller, Aubry K., Pfaffl, Michael W., Linder, Maurine E., Kuster, Bernhard, Médard, Guillaume
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9339481/
https://www.ncbi.nlm.nih.gov/pubmed/35484434
http://dx.doi.org/10.1038/s41589-022-01015-5