ArticleJournal of medicinal chemistry2018
Exploration of Benzothiazole Rhodacyanines as Allosteric Inhibitors of Protein-Protein Interactions with Heat Shock Protein 70 (Hsp70).
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Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
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59citing papers in PubMed
4.9field-weighted citation impact, top 4% of its field
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Who cites it
59 citing papers in PubMed, 115 citations in OpenAlex.
- FBXL21 regulates diurnal proteostasis in skeletal muscle by targeting DNAJB6 and client proteins.EMBO reports · 2026Article
- The GENEVA platform models tumor mosaicism to reveal variations of responses to KRAS inhibitors and identify improved drug combinations.Nature cancer · 2026Article
- Hsp70: A Multifunctional Chaperone in Maintaining Proteostasis and Its Implications in Human Disease.Cells · 2025Review
- High-throughput screening identifies a novel small-molecule modulator of Hsp70 that selectively enhances ubiquitination and degradation of misfolded neuronal NO synthase.Molecular pharmacology · 2025Article
- Co-chaperones fine-tune the function of heat shock protein 70 (Hsp70), whether to fold, hold, or degrade substrates in ensuring cellular protein homeostasis.Journal of biosciences · 2025Review
- A bird's eye view of mitochondrial unfolded protein response in cancer: mechanisms, progression and further applications.Cell death & disease · 2024Review
- Heat shock proteins as hallmarks of cancer: insights from molecular mechanisms to therapeutic strategies.Journal of hematology & oncology · 2024Review
- Proteostasis perturbation of N-Myc leveraging HSP70 mediated protein turnover improves treatment of neuroendocrine prostate cancer.Nature communications · 2024Article
- Small molecule inhibitor targeting the Hsp70-Bim protein-protein interaction in estrogen receptor-positive breast cancer overcomes tamoxifen resistance.Breast cancer research : BCR · 2024Article
- Heat Shock Proteins and Breast Cancer.International journal of molecular sciences · 2024Review
- Autocrine regulation of tumor cell repopulation by Hsp70-HMGB1 alarmin complex.Journal of experimental & clinical cancer research : CR · 2023Article
- An Unbiased Screen Identified the Hsp70-BAG3 Complex as a Regulator of Myosin-Binding Protein C3.JACC. Basic to translational science · 2023Article
- Article
- HSP70 Family in Cancer: Signaling Mechanisms and Therapeutic Advances.Biomolecules · 2023Review
- Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models.Pharmacological research · 2023Article
- Synthetic Small Molecule Modulators of Hsp70 and Hsp40 Chaperones as Promising Anticancer Agents.International journal of molecular sciences · 2023Review
- N-myc-Mediated Translation Control Is a Therapeutic Vulnerability in Medulloblastoma.Cancer research · 2023Article
- Editorial: The role of mortalin in biology and disease.Frontiers in cell and developmental biology · 2023Article
- Maximizing CRISPRi efficacy and accessibility with dual-sgRNA libraries and optimal effectors.eLife · 2022Article
- GRP78 Activity Moderation as a Therapeutic Treatment against Obesity.International journal of environmental research and public health · 2022Review
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 1 country.
Hao ShaoDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.
Xiaokai LiDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.
Michael A MosesUrologic Oncology Branch, Center for Cancer Research , National Cancer Institute , Bethesda , Maryland 20892 , United States.
Luke A GilbertDepartment of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute , University of California at San Francisco , San Francisco , California 94158 , United States.ORCID 0000-0001-5854-0825
Chakrapani KalyanaramanDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.
Zapporah T YoungDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.
Margarita ChernovaDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.
Sara N JourneyDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.
Jonathan S WeissmanDepartment of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute , University of California at San Francisco , San Francisco , California 94158 , United States.
Byron HannHelen Diller Family Comprehensive Cancer Centre and Preclinical Therapeutics Core , University of California at San Francisco , San Francisco , California 94158 , United States.
Matthew P JacobsonDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.ORCID 0000-0001-6262-655X
Len NeckersUrologic Oncology Branch, Center for Cancer Research , National Cancer Institute , Bethesda , Maryland 20892 , United States.
Jason E GestwickiDepartment of Pharmaceutical Chemistry , University of California at San Francisco , Sandler Center, 675 Nelson Rising Lane , San Francisco , California 94158 , United States.ORCID 0000-0002-6125-3154
University of California, San Francisco · USHoward Hughes Medical Institute · USNational Cancer Institute · USUCSF Helen Diller Family Comprehensive Cancer Center · US
Funding
Project 4: Secondary Cancers Among NF1 Cancer SurvivorsU54CA196519 · NCI · INDIANA UNIVERSITY INDIANAPOLIS · PI David W Clapp, KEVIN M. SHANNON · 2015 to 2026
$26.9MRole of fumarate hydratase loss in development of HLRCC hereditary kidney cancerZIABC010683 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI NECKERS, LEONARD · 2009 to 2024
$8.6MMolecular Chaperones and Small MoleculesR01NS059690 · NINDS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Jason E Gestwicki · 2008 to 2026
$7.9MA functional genomics approach to determine the mechanism of cellular response to new anti-cancer R00CA204602 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI GILBERT, LUKE · 2017 to 2019
$747kNCI NIH HHS R00 CA204602NCI NIH HHS U54 CA196519NINDS NIH HHS R01 NS059690
Abstract
Cancer cells rely on the chaperone heat shock protein 70 (Hsp70) for survival and proliferation. Recently, benzothiazole rhodacyanines have been shown to bind an allosteric site on Hsp70, interrupting its binding to nucleotide-exchange factors (NEFs) and promoting cell death in breast cancer cell lines. However, proof-of-concept molecules, such as JG-98, have relatively modest potency (EC
Indexed as
Drug DesignAllosteric RegulationAnimalsBenzothiazolesCell Line, TumorFemaleHSP70 Heat-Shock ProteinsHumansMCF-7 CellsMiceMolecular Docking SimulationProtein BindingProtein ConformationPyridinium CompoundsStructure-Activity RelationshipThiazolesBenzothiazolesHSP70 Heat-Shock ProteinsPyridinium CompoundsrhodacyanineThiazoles
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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.