Chemical modulation of transcription factors

B Wiedemann, J Weisner, D Rauh - Medchemcomm, 2018 - pubs.rsc.org
Transcription factors (TFs) constitute a diverse class of sequence-specific DNA-binding
proteins, which are key to the modulation of gene expression. TFs have been associated …

Stafia‐1: a STAT5a‐Selective Inhibitor Developed via Docking‐Based Screening of in Silico O‐Phosphorylated Fragments

K Natarajan, D Müller‐Klieser… - … –A European Journal, 2020 - Wiley Online Library
We present a new approach for the identification of inhibitors of phosphorylation‐dependent
protein–protein interaction domains, in which phenolic fragments are adapted by in silico O …

Stafiba: A STAT5‐Selective Small‐Molecule Inhibitor

KS Eckhardt, T Münzel, J Gräb, T Berg - Chembiochem, 2023 - Wiley Online Library
The transcription factors STAT5a and STAT5b are constitutively active in many human
tumors. Combined inhibition of both STAT5 proteins is a valuable approach with promising …

A small-molecule screen identifies the antitrypanosomal agent suramin and analogues NF023 and NF449 as inhibitors of STAT5a/b

A Berg, T Berg - Bioorganic & Medicinal Chemistry Letters, 2017 - Elsevier
The transcription factor STAT5a is a potential target for tumor therapy. We present a
fluorescence polarization-based, high-throughput screen of chemical libraries containing …

ATP inhibits the transcription factor STAT5b

A Berg, B Sperl, T Berg - ChemBioChem, 2019 - Wiley Online Library
Although naturally occurring low‐molecular‐weight compounds have many known roles
within the cell, these do not usually involve the direct inhibition of protein–protein …

Asymmetrically Substituted m‐Terphenyl Phosphates Inhibit the Transcription Factor STAT5a

D Müller‐Klieser, T Berg - ChemBioChem, 2022 - Wiley Online Library
We recently presented Stafia‐1 as the first chemical entity that inhibits the transcription factor
STAT5a with selectivity over the highly homologous STAT5b. Stafia‐1, which was identified …

The selectivity of fosfosal for STAT5b over STAT5a is mediated by Arg566 in the linker domain

J Gräb, T Berg - ChemBioChem, 2020 - Wiley Online Library
Fosfosal is the O‐phosphorylated derivative of salicylic acid, with documented clinical use
as a prodrug for the treatment of inflammatory diseases. We recently discovered that fosfosal …