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Journal Article

Tafbromin selectively targets the TAF1 bromodomain

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Maier,  Kerstin C.
Department of Molecular Biology, Max Planck Institute for Multidisciplinary Sciences, Max Planck Society;

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Žumer,  Kristina
Department of Molecular Biology, Max Planck Institute for Multidisciplinary Sciences, Max Planck Society;

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Cramer,  Patrick       
Department of Molecular Biology, Max Planck Institute for Multidisciplinary Sciences, Max Planck Society;

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Citation

Patil, S., Cremosnik, G., Dötsch, L., Flegel, J., Schulte, B., Maier, K. C., et al. (2024). Tafbromin selectively targets the TAF1 bromodomain. Angewandte Chemie International Edition. doi:10.1002/anie.202404645.


Cite as: https://hdl.handle.net/21.11116/0000-000F-5BFF-D
Abstract
Phenotypic assays detect small molecule bioactivity at functionally relevant cellular sites, and inherently cover a variety of targets and mechanisms of action. They can uncover new small molecule-target pairs and may give rise to novel biological insights. By means of an osteoblast differentiation assay which employs a Hedgehog (Hh) signaling agonist as stimulus and which monitors an endogenous marker for osteoblasts, we identified a pyrrolo[3,4-g]quinoline (PQ) pseudo-natural product (PNP) class as osteogenesis inhibitors. The most potent PQ, termed Tafbromin, impairs canonical Hh signaling and modulates osteoblast differentiation through binding to the bromodomain 2 of TATA-box binding protein-associated factor 1 (TAF1). Tafbromin is the most selective TAF1 bromodomain 2 ligand and promises to be an invaluable tool for the study of biological processes mediated by TAF1(2) bromodomains.