ArticleChemistry (Weinheim an der Bergstrasse, Germany)2020
Stafia-1: a STAT5a-Selective Inhibitor Developed via Docking-Based Screening of in Silico O-Phosphorylated Fragments.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 20 citations in OpenAlex.
- Stafib-2-CR: an Improved Nanomolar and Selective Inhibitor of the Transcription Factor STAT5b Developed by Conformational Restriction of Stafib-2.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Fusion Molecules Between the STAT5b Inhibitor Stafib-2-CR and a Cereblon Ligand.ChemistryOpen · 2026Article
- Activity Analysis of the P2X Receptor Antagonist PPADS against Signal Transducer and Activator of Transcription Proteins.Chembiochem : a European journal of chemical biology · 2025Article
- Biaryl Phosphates and Phosphonates as Selective Inhibitors of the Transcription Factor STAT4.Angewandte Chemie (International ed. in English) · 2025Article
- Non-Canonical TERT Activity Initiates Osteogenesis in Calcific Aortic Valve Disease.Circulation research · 2025Article
- Identification of Active Phytochemicals to Inhibit Signal Transducer and Activator of Transcription 5A (STAT5A) Dimerization for Prostate Cancer Therapy: AnAnti-cancer agents in medicinal chemistry · 2025Article
- Co-expression of IL-15/IL-15Ra complex enhances NKG2D-CAR T cell-mediated anti-pancreatic cancer immunity by activating the JAK/STAT5 signaling pathway.Frontiers in immunology · 2025Article
- Article
- Review
- Stafiba: A STAT5-Selective Small-Molecule Inhibitor.Chembiochem : a European journal of chemical biology · 2023Article
- GM-CSF-activated STAT5A regulates macrophage functions and inflammation in atherosclerosis.Frontiers in immunology · 2023Article
- A High-Throughput Fluorescence Polarization-Based Assay for the SH2 Domain of STAT4.Methods and protocols · 2022Article
- Asymmetrically Substituted m-Terphenyl Phosphates Inhibit the Transcription Factor STAT5a.Chembiochem : a European journal of chemical biology · 2022Article
- The Selectivity of Fosfosal for STAT5b over STAT5a is Mediated by Arg566 in the Linker Domain.Chembiochem : a European journal of chemical biology · 2020Article
- Stafia-1: a STAT5a-Selective Inhibitor Developed via Docking-Based Screening of in Silico O-Phosphorylated Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Direct Targeting Options for STAT3 and STAT5 in Cancer.Cancers · 2019Review
- Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
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-phosphorylation before docking-based screening. From a database of 10 369 180 compounds, we identified 85 021 natural product-derived phenolic fragments, which were virtually O-phosphorylated and screened for in silico binding to the STAT3 SH2 domain. Nine screening hits were then synthesized, eight of which showed a degree of in vitro inhibition of STAT3. After analysis of its selectivity profile, the most potent inhibitor was then developed to Stafia-1, the first small molecule shown to preferentially inhibit the STAT family member STAT5a over the close homologue STAT5b. A phosphonate prodrug based on Stafia-1 inhibited STAT5a with selectivity over STAT5b in human leukemia cells, providing the first demonstration of selective in vitro and intracellular inhibition of STAT5a by a small-molecule inhibitor.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.