ArticleCancer letters2022
Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo.
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Article in Cancer letters, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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10citing papers in PubMed
1.9field-weighted citation impact, top 16% of its field
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Who cites it
10 citing papers in PubMed, 18 citations in OpenAlex.
- STAT3 signaling inhibitors for cancer treatment.Trends in pharmacological sciences · 2026Review
- Pharmacological combination of simvastatin and doxorubicin reduces tumor growth and lung metastasis in triple-negative breast cancer.Frontiers in cell and developmental biology · 2026Article
- Targeting MAD2L2-dependent translesion synthesis impairs DNA damage tolerance and enhances cellular response to cisplatin.Frontiers in cell and developmental biology · 2026Article
- miR-21-5p Alleviates Retinal Ischemia-Reperfusion Injury by Inhibiting M1 Polarization of Microglia via Suppression of STAT3 Signaling.Biomedicines · 2025Article
- STAT3 Signaling Pathway in Health and Disease.MedComm · 2025Review
- Stattic suppresses p‑STAT3 and induces cell death in T‑cell acute lymphoblastic leukemia.Molecular medicine reports · 2025Article
- Targeting Disulfidptosis with Potentially Bioactive Natural Products in Metabolic Cancer Therapy.Metabolites · 2024Review
- Article
- Potential therapeutic targets of the JAK2/STAT3 signaling pathway in triple-negative breast cancer.Frontiers in oncology · 2024Review
- The role of AFAP1-AS1 in mitotic catastrophe and metastasis of triple-negative breast cancer cells by activating the PLK1 signaling pathway.Oncology research · 2023Article
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Authors and funding
22 authors at 4 institutions in 1 country.
Peibin YueDepartment of Medicine, Division of Medical Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angenes, CA, 90048, USA; Cancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Yinsong ZhuDepartment of Medicine, Division of Medical Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angenes, CA, 90048, USA; Cancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Christine Brotherton-PleissCancer Biology Program, University of Hawaii Cancer Center, 701 Ilalo St, Honolulu, HI, 96813, USA; Department of Chemistry, University of Hawaii, Manoa, 2545 McCarthy Mall, Honolulu, HI, 96825, USA.
Wenzhen FuCancer Biology Program, University of Hawaii Cancer Center, 701 Ilalo St, Honolulu, HI, 96813, USA; Department of Chemistry, University of Hawaii, Manoa, 2545 McCarthy Mall, Honolulu, HI, 96825, USA.
Nagendra VermaDepartment of Medicine, Division of Medical Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angenes, CA, 90048, USA; Cancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Jasmine ChenCancer Biology Program, University of Hawaii Cancer Center, 701 Ilalo St, Honolulu, HI, 96813, USA.
Kayo NakamuraDepartment of Chemistry, University of Hawaii, Manoa, 2545 McCarthy Mall, Honolulu, HI, 96825, USA.
Weiliang ChenDepartment of Chemistry, University of Hawaii, Manoa, 2545 McCarthy Mall, Honolulu, HI, 96825, USA.
Yue ChenDepartment of Medicine, Division of Medical Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angenes, CA, 90048, USA; Cancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Felix Alonso-ValenteenCancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA; Department of Biomedical Sciences, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Simoun MikhaelCancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA; Department of Biomedical Sciences, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Lali Medina-KauweCancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA; Department of Biomedical Sciences, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Kathleen M KershawCancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA; Department of Radiation Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Maria CeleridadCell and Molecular Biology of Cancer Program, Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 N. Torrey Pines Rd, La Jolla, CA, 92037, USA.
Songqin PanW. M. Keck Proteomics Laboratory, University of California, Riverside, CA, 92521, USA.
Allison S LimpertCell and Molecular Biology of Cancer Program, Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 N. Torrey Pines Rd, La Jolla, CA, 92037, USA.
Douglas J ShefflerCell and Molecular Biology of Cancer Program, Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 N. Torrey Pines Rd, La Jolla, CA, 92037, USA.
Nicholas D P CosfordCell and Molecular Biology of Cancer Program, Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 N. Torrey Pines Rd, La Jolla, CA, 92037, USA.
Stephen L ShiaoCancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA; Department of Radiation Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
Marcus A TiusCancer Biology Program, University of Hawaii Cancer Center, 701 Ilalo St, Honolulu, HI, 96813, USA; Department of Chemistry, University of Hawaii, Manoa, 2545 McCarthy Mall, Honolulu, HI, 96825, USA.
Francisco Lopez-TapiaDepartment of Medicine, Division of Medical Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angenes, CA, 90048, USA; Cancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA.
James TurksonDepartment of Medicine, Division of Medical Oncology, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angenes, CA, 90048, USA; Cancer Biology Program, Cedars-Sinai Cancer, Cedars-Sinai Medical Center, 8700 Beverly Blvd, Los Angeles, CA, 90048, USA. Electronic address: james.tusrkson@cshs.org.
Cedars-Sinai Medical Center · USUniversity of Hawaiʻi at Mānoa · USSanford Burnham Prebys Medical Discovery Institute · USUniversity of California, Riverside · US
Funding
UCLA Clinical Translational Science InstituteUL1TR001881 · NCATS · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI ARLEEN F. BROWN, ARASH NAEIM · 2016 to 2026
$118.1MTumor Microenvironment and Cancer ImmunologyP30CA030199 · NCI · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · PI ELENA B PASQUALE · 1985 to 2026
$107.2MSTAT3, G6PD and TrxR as underlying mechanisms for antitumor responses tohirsutinolidesR01CA208851 · NCI · UNIVERSITY OF HAWAII AT MANOA · PI TURKSON, JAMES K · 2017 to 2021
$2.9MTargeting inhibitor-resistant breast tumors with HER3-homing nano-capsidsR01CA258204 · NCI · CEDARS-SINAI MEDICAL CENTER · PI LALI K MEDINA-KAUWE · 2022 to 2026
$1.9MNucleocapsid bioparticles eliciting multi-pronged attack on tumor metastasesR01CA270324 · NCI · CEDARS-SINAI MEDICAL CENTER · PI LALI K MEDINA-KAUWE · 2022 to 2026
$1.5MAn LTQ-Orbitrap Elite with ETD for the Keck Proteomics FacilityS10OD010669 · OD · UNIVERSITY OF CALIFORNIA RIVERSIDE · PI WANG, YINSHENG · 2013 to 2013
$600kNCATS NIH HHS UL1 TR001881NCI NIH HHS P30 CA030199NCI NIH HHS R01 CA208851NCI NIH HHS R01 CA258204NCI NIH HHS R01 CA270324NIH HHS S10 OD010669
Abstract
Signal transducer and activator of transcription (Stat)3 is a valid anticancer therapeutic target. We have discovered a highly potent chemotype that amplifies the Stat3-inhibitory activity of lead compounds to levels previously unseen. The azetidine-based compounds, including H172 (9f) and H182, irreversibly bind to Stat3 and selectively inhibit Stat3 activity (IC
Indexed as
AzetidinesTriple Negative Breast NeoplasmsAnimalsApoptosisCell Line, TumorHumansMicePhosphorylationSignal TransductionSTAT3 Transcription FactorazetidineAzetidinesSTAT3 protein, humanSTAT3 Transcription FactorAntitumor cell effectsCovalent modificationSignal transducer and activator of transcriptionSmall-molecule inhibitorsTumor growth inhibition
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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.