ArticleJournal of medicinal chemistry2017
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
38 citing papers in PubMed, 69 citations in OpenAlex.
- Heat shock transcription factors in development and disease.Disease models & mechanisms · 2026Review
- Human DEAH-box helicase 8 regulates HSF1-mediated stress response and cancer-associated pre-mRNA splicing in tumour cells.NAR cancer · 2026Article
- Targeting the Spliceosomal Protein USP39 Through Allosteric Ligands and PROTAC-Induced Degradation.Angewandte Chemie (International ed. in English) · 2026Article
- Pirin does not bind to p65 or regulate NFκB-dependent gene expression but does modulate cellular quercetin levels.Molecular pharmacology · 2025Article
- Role of HSF1 in cell division, tumorigenesis and therapy: a literature review.Cell division · 2025Review
- Applications of Bridgehead Heterocycles in Drug Design and Medicinal Chemistry.Topics in current chemistry (Cham) · 2025Review
- NXP800 Activates the Unfolded Protein Response, Altering AR and E2F Function to Impact Castration-Resistant Prostate Cancer Growth.Clinical cancer research : an official journal of the American Association for Cancer Research · 2025Article
- HSF1 Activation Mechanisms, Disease Roles, and Small Molecule Therapeutics.International journal of biological sciences · 2025Review
- Pirin does not bind to p65 or regulate NFκB-dependent gene expression but does modulate cellular quercetin levels.bioRxiv : the preprint server for biology · 2024Article
- The Role of Heat Shock Factor 1 in Preserving Proteomic Integrity During Copper-Induced Cellular Toxicity.International journal of molecular sciences · 2024Article
- Iron-(Fe3+)-Dependent Reactivation of Telomerase Drives Colorectal Cancers.Cancer discovery · 2024Article
- Prognosis value of heat-shock proteins in esophageal and esophagogastric cancer: A systematic review and meta-analysis.World journal of gastrointestinal oncology · 2024Article
- HSF1 at the crossroads of chemoresistance: from current insights to future horizons in cell death mechanisms.Frontiers in cell and developmental biology · 2024Review
- The small-molecule drug homoharringtonine targets HSF1 to suppress pancreatic cancer progression.American journal of cancer research · 2024Article
- Heat Shock Factor 1 Inhibition: A Novel Anti-Cancer Strategy with Promise for Precision Oncology.Cancers · 2023Review
- HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies.Journal of medicinal chemistry · 2023Article
- Targeting HSF1 for cancer treatment: mechanisms and inhibitor development.Theranostics · 2023Review
- The era of high-quality chemical probes.RSC medicinal chemistry · 2022Article
- Prevention of bleomycin-induced lung fibrosis via inhibition of the MRTF/SRF transcription pathway.Pharmacology research & perspectives · 2022Article
- Pirin, an Nrf2-Regulated Protein, Is Overexpressed in Human Colorectal Tumors.Antioxidants (Basel, Switzerland) · 2022Article
Corrections and comments
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Authors and funding
26 authors at 1 institution in 1 country.
Funding
Abstract
Phenotypic screens, which focus on measuring and quantifying discrete cellular changes rather than affinity for individual recombinant proteins, have recently attracted renewed interest as an efficient strategy for drug discovery. In this article, we describe the discovery of a new chemical probe, bisamide (CCT251236), identified using an unbiased phenotypic screen to detect inhibitors of the HSF1 stress pathway. The chemical probe is orally bioavailable and displays efficacy in a human ovarian carcinoma xenograft model. By developing cell-based SAR and using chemical proteomics, we identified pirin as a high affinity molecular target, which was confirmed by SPR and crystallography.
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Registered trials
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.