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Stickland, B.A.* ; Greulich, F.* ; Uhlenhaut, N.H.

The specificity of CTBP dehydrogenase inhibitors MTOB and 4-Cl-HIPP.

MicroPubl. Biol. 2025, DOI: 10.17912/micropub.biology.001415 (2025)
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C-terminal binding proteins (CTBPs) are conserved transcriptional repressors important in cancer and inflammation. Uniquely amongst transcriptional co-regulators, CTBPs possess a functional dehydrogenase domain. Since multiple malignancies display elevated CTBP levels, CTBP inhibitors targeting this dehydrogenase domain have been developed. While the importance of CTBPs dehydrogenase function for transcriptional regulation remains unclear, several studies have relied on CTBP inhibitors. In vitro experiments have confirmed binding of these compounds to CTBP's active site, however evidence for specificity is lacking. To address this, we treated wildtype and Ctbp1 , 2 double knockout J774.1 cells with MTOB or 4-Cl-HIPP and performed RNA-seq. We observed that both inhibitors elicit distinct transcriptional changes indicating non-overlapping modes of action. Moreover, the majority of changes induced by either inhibitor are observed in Ctbp1/2 double knockout cells suggesting off-target effects. We hypothesize that those CTBP dehydrogenase inhibitors lack specificity to CTBPs and emphasise careful revaluation of findings inferred from studies using those inhibitors.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Wissenschaftlicher Artikel
Sprache englisch
Veröffentlichungsjahr 2025
HGF-Berichtsjahr 2025
ISSN (print) / ISBN 2578-9430
e-ISSN 2578-9430
Zeitschrift microPublication biology
Quellenangaben Band: 2025 Heft: , Seiten: , Artikelnummer: , Supplement: ,
Verlagsort Pasadena, CA
Begutachtungsstatus Peer reviewed
Institut(e) Institute of Diabetes and Endocrinology (IDE)
POF Topic(s) 30202 - Environmental Health
PSP-Element(e) G-501900-259
DOI 10.17912/micropub.biology.001415
PubMed ID 39967797
Erfassungsdatum 2025-04-14
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