ArticleJournal of medicinal chemistry2011
Design and synthesis of novel small-molecule inhibitors of the hypoxia inducible factor pathway.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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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
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Who cites it
23 citing papers in PubMed, 48 citations in OpenAlex.
- HIF-1α inhibition by MO-2097, a novel chiral-free benzofuran targeting hnRNPA2B1.Journal of advanced research · 2024Article
- Hypoxia-induced signaling in the cardiovascular system: pathogenesis and therapeutic targets.Signal transduction and targeted therapy · 2023Review
- Drug Discovery Targeting Post-Translational Modifications in Response to DNA Damages Induced by Space Radiation.International journal of molecular sciences · 2023Review
- Glioblastoma: Current Status, Emerging Targets, and Recent Advances.Journal of medicinal chemistry · 2022Review
- Action Sites and Clinical Application of HIF-1α Inhibitors.Molecules (Basel, Switzerland) · 2022Review
- Hypoxia-dependent drivers of melanoma progression.Journal of experimental & clinical cancer research : CR · 2021Review
- A Bioreductive Prodrug of Cucurbitacin B Significantly Inhibits Tumor Growth in the 4T1 Xenograft Mice Model.ACS medicinal chemistry letters · 2019Article
- Arylsulfonamide 64B Inhibits Hypoxia/HIF-Induced Expression of c-Met and CXCR4 and Reduces Primary Tumor Growth and Metastasis of Uveal Melanoma.Clinical cancer research : an official journal of the American Association for Cancer Research · 2019Article
- Chemical modulation of transcription factors.MedChemComm · 2018Review
- Design and synthesis of benzopyran-based inhibitors of the hypoxia-inducible factor-1 pathway with improved water solubility.Journal of enzyme inhibition and medicinal chemistry · 2017Article
- A novel small-molecule arylsulfonamide causes energetic stress and suppresses breast and lung tumor growth and metastasis.Oncotarget · 2017Article
- Purifying Properly Folded Cysteine-rich, Zinc Finger Containing Recombinant Proteins for Structural Drug Targeting Studies: the CH1 Domain of p300 as a Case Example.Bio-protocol · 2017Article
- Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions.Chemical science · 2017Article
- Examining the structure-activity relationship of benzopyran-based inhibitors of the hypoxia inducible factor-1 pathway.Bioorganic & medicinal chemistry letters · 2017Article
- Targeting Protein-Protein Interactions in the HIF System.ChemMedChem · 2016Review
- Biology of advanced uveal melanoma and next steps for clinical therapeutics.Pigment cell & melanoma research · 2015Review
- Small-molecule proteomimetic inhibitors of the HIF-1α-p300 protein-protein interaction.Chembiochem : a European journal of chemical biology · 2014Article
- Hypoxia inducible factor pathway inhibitors as anticancer therapeutics.Future medicinal chemistry · 2013Review
- Arylsulfonamide KCN1 inhibits in vivo glioma growth and interferes with HIF signaling by disrupting HIF-1α interaction with cofactors p300/CBP.Clinical cancer research : an official journal of the American Association for Cancer Research · 2012Article
- Identification of Cys255 in HIF-1α as a novel site for development of covalent inhibitors of HIF-1α/ARNT PasB domain protein-protein interaction.Protein science : a publication of the Protein Society · 2012Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Hypoxia, a reduction in partial oxygen pressure, is a salient property of solid tumors. Hypoxia drives malignant progression and metastasis in tumors and participates in tumor resistance to radio- and chemotherapies. Hypoxia activates the hypoxia-inducible factor (HIF) family of transcription factors, which induce target genes that regulate adaptive biological processes such as anaerobic metabolism, cell motility, and angiogenesis. Clinical evidence has demonstrated that expression of HIF-1 is strongly associated with poor patient prognosis and activation of HIF-1 contributes to malignant behavior and therapeutic resistance. Consequently, HIF-1 has become an important therapeutic target for inhibition by small molecules. Herein, we describe the design and synthesis of small molecules that inhibit the HIF-1 signaling pathway. Many of these compounds exhibit inhibitory activity in the nanomolar range. Separate mechanistic studies indicate that these inhibitors do not alter HIF-1 levels but interfere with the ability of HIF-1α/HIF-1β to interact with cofactors p300/CBP to form an active transcriptional complex.
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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.