The Pseudo‐Natural Product Tafbromin Selectively Targets the TAF1 Bromodomain 2
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 of osteogenesis inhibitors. The most potent PQ, termed Tafbromin, impairs canonical Hh signaling and modulates osteoblast differentiation through binding to the bromodomain 2 of the 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.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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The Pseudo‐Natural Product Tafbromin Selectively Targets the TAF1 Bromodomain 2 ; day:04 ; month:07 ; year:2024 ; extent:13
Angewandte Chemie ; (04.07.2024) (gesamt 13)
- Creator
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Patil, Sohan
Cremosnik, Gregor
Dötsch, Lara
Flegel, Jana
Schulte, Britta
Maier, Kerstin C.
Žumer, Kristina
Cramer, Patrick
Janning, Petra
Sievers, Sonja
Ziegler, Slava
Waldmann, Herbert
- DOI
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10.1002/ange.202404645
- URN
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urn:nbn:de:101:1-2407081442060.672301600293
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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14.08.2025, 10:46 AM CEST
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Associated
- Patil, Sohan
- Cremosnik, Gregor
- Dötsch, Lara
- Flegel, Jana
- Schulte, Britta
- Maier, Kerstin C.
- Žumer, Kristina
- Cramer, Patrick
- Janning, Petra
- Sievers, Sonja
- Ziegler, Slava
- Waldmann, Herbert
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Pablo Picasso : the illustrated books ; catalogue raisonné
RNA polymerase I structure and transcription regulation
Genome-wide occupancy profiling of the RNA polymerase II transcription machinery in S. cerevisiae
RNA polymerase I complex structures elucidate mechanisms of transcription initiation and elongation
Transient transcriptome sequencing captures enhancer landscapes immediately after T-cell stimulation
Global analysis of mRNA metabolism by comparative dynamic transcriptome analysis
Structure and function of RNA Polymerase II-Bye1 complexes
Role of the RNA polymerase II C-terminal domain in transcription termination and function of Spt5 in 3' RNA-processing factor recruitment
Structure of the closed Pol II transcription initiation complex and implications for promoter opening
Integrative structural and functional studies of Mediator and RNA polymerase II transcription initiation assemblies
Context-specific methods for sequence homology searching and alignment
The Pseudo‐Natural Product Tafbromin Selectively Targets the TAF1 Bromodomain 2
Pablo Picasso : the illustrated books ; catalogue raisonné
RNA polymerase I structure and transcription regulation
Genome-wide occupancy profiling of the RNA polymerase II transcription machinery in S. cerevisiae
RNA polymerase I complex structures elucidate mechanisms of transcription initiation and elongation
Transient transcriptome sequencing captures enhancer landscapes immediately after T-cell stimulation
Global analysis of mRNA metabolism by comparative dynamic transcriptome analysis
Structure and function of RNA Polymerase II-Bye1 complexes
Role of the RNA polymerase II C-terminal domain in transcription termination and function of Spt5 in 3' RNA-processing factor recruitment
Structure of the closed Pol II transcription initiation complex and implications for promoter opening
Integrative structural and functional studies of Mediator and RNA polymerase II transcription initiation assemblies