Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation

STATs in cancer inflammation and immunity: a leading role for STAT3

Yu, H., Pardoll, D., & Jove, R. (2009) · Nature reviews. Cancer · doi:10.1038/nrc2734 · Cited by 4,383

STATs and Gene Regulation

Darnell, J. E. (1997) · Science · doi:10.1126/science.277.5332.1630 · Cited by 3,979

Revisiting STAT3 signalling in cancer: new and unexpected biological functions

Yu, H., Lee, H., Herrmann, A., Buettner, R., & Jove, R. (2014) · Nature Reviews Cancer · doi:10.1038/nrc3818 · Cited by 2,137

Induced protein degradation: an emerging drug discovery paradigm

Lai, A. C., & Crews, C. M. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.211 · Cited by 1,486

Indoleamine 2,3-dioxygenase and tumor-induced tolerance

Munn, D. H., & Mellor, A. L. (2007) · Journal of Clinical Investigation · doi:10.1172/jci31178 · Cited by 1,093

Stat3 Dimerization Regulated by Reversible Acetylation of a Single Lysine Residue

Yuan, Z.-L., Guan, Y.-J., Chatterjee, D., & Chin, Y. E. (2005) · Science · doi:10.1126/science.1105166 · Cited by 790

Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity

Siddiquee, K., Zhang, S., Guida, W. C., Blaskovich, M. A., Greedy, B. M., Lawrence, H. R., Yip, M. L. R., Jove, R., McLaughlin, M. M., Lawrence, N. J., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0609757104 · Cited by 741

Oncogenic kinase NPM/ALK induces through STAT3 expression of immunosuppressive protein CD274 (PD-L1, B7-H1)

Marzec, M., Zhang, Q., Goradia, A., Raghunath, P. N., Liu, X., Paessler, M. E., Wang, H. Y., Wysocka, M., Cheng, M. M., Ruggeri, B., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0810958105 · Cited by 731

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

Bai, L., Zhou, H., Xu, R., Zhao, Y., Chinnaswamy, K., McEachern, D., Chen, J., Yang, C.-Y., Liu, Z., Wang, M., et al. (2019) · Cancer Cell · doi:10.1016/j.ccell.2019.10.002 · Cited by 652

Discovery of Diaryl Piperidone-Sulfonamide as a Novel Dual-Target Inhibitor of STAT3/CAIX Inducing Ferroptosis in Triple-Negative Breast Cancer Cells

Chen, L., Chen, X.-M., Mao, Z.-C., Gou, Y., Ma, X., Wei, J.-H., Huang, R.-Z., & Zhang, Y. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00126 · Cited by 8

Mangiferin attenuates Ang II-induced abdominal aortic aneurysm by blocking Lys591-mediated nuclear translocation of STAT3

Cheng, S., Wang, Y., Tong, T., Liu, C., Qian, J., Zong, Q., Wang, D., Li, K., Wu, X., & Yang, J. (2025) · Phytomedicine · doi:10.1016/j.phymed.2025.157101 · Cited by 8

miR-330-5p Suppress Cell Growth and Invasion via Disrupting HSF4-mediated MACC1/STAT3 Pathway in Colorectal Cancer

Liu, J., Yue, K., Yang, J., Bi, C., Zhang, Y., & Zhang, W. (2024) · Frontiers in Bioscience-Landmark · doi:10.31083/j.fbl2902053 · Cited by 8

Toosendanin induces hepatotoxicity by restraining autophagy and lysosomal function through inhibiting STAT3/CTSC axis

Luo, L., Ni, J., Zhang, J., Lin, J., Chen, S., Shen, F., & Huang, Z. (2024) · Toxicology Letters · doi:10.1016/j.toxlet.2024.03.002 · Cited by 8

Design, synthesis and biological evaluation of novel naphthoquinothiazole derivatives as potent antitumor agents through inhibiting STAT3

Fan, D., Liu, P., Li, Z., He, X., Zhang, L., Jiang, W., Ang, W., & Yang, T. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107565 · Cited by 9

IL-1β-induced pericyte dysfunction with a secretory phenotype exacerbates retinal microenvironment inflammation via Hes1/STAT3 signaling pathway

Huang, C., Zhang, X., Wu, M., Chen, Y., Ge, X., Chen, W., Li, X., Liu, S., & Yang, S. (2024) · International Immunopharmacology · doi:10.1016/j.intimp.2024.113611 · Cited by 7

Cardiomyocyte‐Enriched USP20 Ameliorates Pathological Cardiac Hypertrophy by Targeting STAT3 Deubiquitination

Zhong, L., Dai, S., Yu, F., Shi, G., Gong, Q., Zhang, Y., Duan, J., Lou, Z., Tang, Z., Gong, F., et al. (2025) · Advanced Science · doi:10.1002/advs.202416478 · Cited by 7

Synthesis and pharmacological evaluation of polyamine-diarylidenyl piperidone derivatives as potent antitumor agents

Mao, Z.-C., Liu, S.-Q., Chen, X.-M., Wei, J.-H., Huang, R.-Z., & Zhang, Y. (2024) · Monatshefte für Chemie - Chemical Monthly · doi:10.1007/s00706-024-03220-5 · Cited by 7

Eugenol suppresses VEGF-dependent angiogenesis by JAK2/STAT3 pathway in non-small cell lung cancer

Su, Y., Wang, Y., Yu, Q., Wu, Z., Zhang, D., & Yan, C. (2024) · Guidelines and Standards of Chinese Medicine · doi:10.1097/gscm.0000000000000021 · Cited by 7

Albumin nanocapsules and nanocrystals for efficient intracellular drug release

Chali, S. P., Westmeier, J., Krebs, F. K., Jiang, S., Neesen, F., Uncuer, D., Schelhaas, M., Grabbe, S., Becker, C., Landfester, K., et al. (2024) · Nanoscale Horizons · doi:10.1039/d4nh00161c · Cited by 7

Recent Developments in Targeting Bromodomain and Extra Terminal Domain Proteins for Cancer Therapeutics

Cai, M., Dong, J., Li, H., & Qin, J. (2022) · Current Medicinal Chemistry · doi:10.2174/0929867329666220211091806 · Cited by 7

Prioritizing drug targets by perturbing biological network response functions

Perrone, M. C., Lerner, M. G., Dunworth, M., Ewald, A. J., & Bader, J. S. (2024) · PLoS Computational Biology · doi:10.1371/journal.pcbi.1012195 · Cited by 7

Design and synthetic approaches to thalidomide based small molecule degraders

Kumar, A., Kumar, G., Kalia, N., & Sahoo, P. R. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117700 · Cited by 6

Synthesis and structure-activity relationship studies of naphthoquinones as STAT3 inhibitors

Yamashita, M., Nakamori, Y., Tsukamoto, A., Furuno, N., & Iida, A. (2023) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2023.117331 · Cited by 6

Clickable polyethyleneimine incorporated into triblock copolymeric micelles as an efficient platform in the delivery of siRNA to NSCLC cells

Marquet, F., Hagen, H., Stanchieri, M., Serre‐Beinier, V., Grasso, G., Danani, A., Patrulea, V., & Borchard, G. (2023) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2023.123632 · Cited by 6

Advanced Insights into Competitive Endogenous RNAs (ceRNAs) Regulated Pathogenic Mechanisms in Metastatic Triple-Negative Breast Cancer (mTNBC)

Qattan, A. T., Al‐Tweigeri, T., Suleman, K., Alkhayal, W., & Tulbah, A. M. (2024) · Cancers · doi:10.3390/cancers16173057 · Cited by 5

Leptin, NK cells, and the weight of immunity: Insights into obesity

de Andrade, A. G., Vanderley, S. E. R., Marques, L. C. D. S., Almeida, F. S., Silva, L. H. A. C., & Keesen, T. S. L. (2025) · International Immunopharmacology · doi:10.1016/j.intimp.2024.113992 · Cited by 7

Synthesis of a celastrol derivative as a cancer stem cell inhibitor through regulation of the STAT3 pathway for treatment of ovarian cancer

Liu, M., Li, N., Wang, Z., Wang, S., Ren, S., & Li, X. (2024) · RSC Medicinal Chemistry · doi:10.1039/d4md00468j · Cited by 5

STATs, promising targets for the treatment of autoimmune and inflammatory diseases

He, X., Liu, P., Luo, Y., Fu, X.-Y., & Yang, T. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116783 · Cited by 5

Identification of STAT3 phosphorylation inhibitors using generative deep learning, virtual screening, molecular dynamics simulations, and biological evaluation for non-small cell lung cancer therapy

Cai, W., Jiang, B., Yin, Y., Ma, L., Li, T., & Chen, J. (2024) · Molecular Diversity · doi:10.1007/s11030-024-11067-5 · Cited by 5

Ginkgetin inhibits the proliferation and migration of lung cancer cells via FAK/STAT3/AKT pathway

Sun, L., Chen, W., Yuan, W., Huang, Q., Yang, H., Zhang, W., Tang, J., & Hu, P. (2025) · Molecular Biology Reports · doi:10.1007/s11033-025-10540-0 · Cited by 5

Discovery of Potential Natural STAT3 Inhibitors: An in silico Molecular Docking and Molecular Dynamics Study

Gul, S., Muhammad, S., Irfan, M. I., Belali, T. M., Chaudhry, A. R., & Khan, M. N. (2023) · Journal of Computational Biophysics and Chemistry · doi:10.1142/s2737416523500588 · Cited by 7

Deguelin Restores Paclitaxel Sensitivity in Paclitaxel-Resistant Ovarian Cancer Cells via Inhibition of the EGFR Signaling Pathway

Bae, S., Bae, S., Kim, H. S., Lim, Y. J., Kim, G., Park, I., So, K. A., Kim, T. J., & Lee, J. (2024) · Cancer Management and Research · doi:10.2147/cmar.s457221 · Cited by 5

Research progress of multi-target HDAC inhibitors blocking the BRD4-LIFR-JAK1-STAT3 signaling pathway in the treatment of cancer

Jia, S., Jia, Y., Liang, S., & Wu, L. (2024) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2024.117827 · Cited by 5

A New Renieramycin T Right-Half Analog as a Small Molecule Degrader of STAT3

Phookphan, P., Racha, S., Yokoya, M., Zin, Z., Hotta, D., Zou, H., & Pithi Chanvorachote, B. (2024) · Marine Drugs · doi:10.3390/md22080370 · Cited by 5

Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2

Ang, G. C. K., Gupta, A., Yap, S. X. L., Surana, U., & Taneja, R. (2022) · Cancers · doi:10.3390/cancers14122855 · Cited by 5

Synthesis of 1,2,4‐triazole and 1,3,4‐oxadiazole derivatives as inhibitors for STAT3 enzymes of breast cancer

Fawzy, S. M., Loksha, Y. M., El‐Sadek, M. E., Ibrahim, S. M., Beshay, B. Y., Shamaa, M. M., & Kothayer, H. (2023) · Archiv der Pharmazie · doi:10.1002/ardp.202300345 · Cited by 5

Discovery of a potent and selective PROTAC degrader for STAT3

Wang, K., Zheng, Y., Mao, W., Xu, J., & Wang, Y. (2025) · RSC Medicinal Chemistry · doi:10.1039/d5md00260e · Cited by 5

Emerging opportunities to treat drug-resistant breast cancer: Discovery of novel small-molecule inhibitors against different targets

Chen, R., Zhou, Z.-L., Meng, X., Lei, Y., Wang, D., & Wang, Y. (2025) · Frontiers in Pharmacology · doi:10.3389/fphar.2025.1578342 · Cited by 6

Selective Targeting of STAT6: Recent Advances and Future Perspectives

Liu, H., Ma, F., Wang, Z., Li, Z. A., Bian, J., Yuan, Z., & Wu, T. (2026) · Medicinal Research Reviews · doi:10.1002/med.70069 · Cited by 4

Synthesis and characterization of piperic acid conjugates with homochiral and heterochiral dipeptides containing phenylalanine and their application in skin cancer

Rahim, J. U., Faheem, M. M., Nawaz, S., Goswami, A., & Rai, R. (2023) · Peptides · doi:10.1016/j.peptides.2023.171113 · Cited by 4

Design, synthesis and evaluation of diarylidenyl piperidone-ligated platinum (IV) complexes as chemoimmunotherapeutic agents

Mao, Z.-C., Chen, L., Chen, X.-M., Lu, X., Mo, Z., Gou, Y., Wei, J.-H., Huang, R.-Z., & Zhang, Y. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117338 · Cited by 4

The key regulator circPDE3B promotes arsenic-induced bladder carcinogenesis by affecting STAT3 and NF-κB stability

Gao, Y., Xu, H., Zhao, Q., Cai, D., Zhou, X. R., Chen, X., Yuan, S., Li, D., Ning, T., Dong, X., et al. (2025) · Cell Biology and Toxicology · doi:10.1007/s10565-025-10038-2 · Cited by 4

The Significance of STAT3 in Colonic Diseases: A Comprehensive Study of Pathological Roles and Therapeutic Implications

Ahmed, A. T., Oghenemaro, E. F., Hjazi, A., Jain, V. D., Ahmad, I., Roopashree, R., Soothwal, P. K., Goswami, M., Zwamel, A. H., & Kdhim, K. (2025) · Cell Biochemistry and Biophysics · doi:10.1007/s12013-025-01816-0 · Cited by 4

(+)-Isocryptotanshinone derivatives and its simplified analogs as STAT3 signaling pathway inhibitors

Shi, X., Du, T. T., Zhang, Z., Liu, X., Yang, Y., Xue, N., Jiao, X., Chen, X., & Xie, P. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.106015 · Cited by 4

A Novel Ageladine A Derivative Acts as a STAT3 Inhibitor and Exhibits Potential Antitumor Effects

He, N., Li, L., Li, R., Zhang, S., Wu, L., Guan, X., Zhang, Q.-Y., Jiang, T., & Yang, J. B. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24108859 · Cited by 4

Bruceantinol targeting STAT3 exerts promising antitumor effects in in vitro and in vivo osteosarcoma models

Miao, J., Chen, S., Cao, H., Ding, Z., Li, Y., Wang, W., Nundlall, K., Deng, Y., & Li, J. (2024) · Molecular Carcinogenesis · doi:10.1002/mc.23714 · Cited by 4

Systematic drug screening and target analysis identify digitoxin as a potential therapy for uveal melanoma

Liu, H., Huang, C., Liu, Z., Li, Y., Zhu, Y., Gao, M., Chen, J., Zhang, H., Xiao, Z., & Zhao, W. (2024) · British Journal of Pharmacology · doi:10.1111/bph.17405 · Cited by 4

An artesunate-modified half-sandwich iridium( iii ) complex inhibits colon cancer cell proliferation and metastasis through the STAT3 pathway

Deng, D., Xu, N., Wang, M., Zhang, G., Su, Y. R., Fang, H., & Su, Z. G. (2024) · RSC Chemical Biology · doi:10.1039/d4cb00114a · Cited by 3

Qizhiweitong granule alleviates diarrhea-predominant irritable bowel syndrome via inhibition of the IL-6/Src/STAT3 feedback loop

Ma, Q., Jiang, Z., Zhang, Z., Su, T., Su, T., Liu, Z., & Zhang, R. (2025) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2025.120772 · Cited by 3

Target proteins profiling of irreversible kinase inhibitor pelitinib and discovery of degradation of PRDX4 by label free chemoproteomics

Li, J., Zheng, M., Xu, Y., Yang, X., & Kang, J. (2023) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2023.115398 · Cited by 3

Design, docking optimization, and evaluation of biotin-PEG4-1,8-naphthalimide as a potent and safe antitumor agent with dual targeting of ferroptosis and DNA

Wang, Q., Liang, S., Mao, Z.-C., Ma, X., Wei, J.-H., Huang, R.-Z., & Zhang, Y. (2024) · RSC Medicinal Chemistry · doi:10.1039/d4md00134f · Cited by 3

OTUD6B promotes cholangiocarcinoma growth by regulating STAT3 phosphorylation through deubiquitination of PTK2

Xing, G., Chen, H., Guo, Z., Cui, Y., Li, Y., & Shen, J. (2024) · Cell Biology International · doi:10.1002/cbin.12234 · Cited by 3

Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents

Duan, X., Wang, J., Huo, X., Shen, Z., & Ding, Y. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117283 · Cited by 3

STAT3 Inhibition Prevents Adaptive Resistance and Augments NK Cell Cytotoxicity to KRASG12C Inhibitors in Nonsmall Cell Lung Cancer

Pan, Z., Qian, Y., Wang, Y., Zhang, T.-S., Song, X., Ding, H., Li, R., Zhang, Y., Wang, Z., Wang, H., et al. (2025) · Cancer Science · doi:10.1111/cas.70017 · Cited by 3

Therapeutic Potential of Tricyclic Pyridazinone-Based Molecules: An Overview

Asproni, B., Pinna, G. A., Corona, P., Coinu, S., Piras, S., Carta, A., & Murineddu, G. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26083806 · Cited by 3

Discovery of novel β-carboline/melatonin hybrids as STAT3 inhibitors for the treatment of lung cancer via increasing DNA damage

Yang, X., Jia, S., Xia, C., & Yang, Y. (2025) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2025.118227 · Cited by 3

SAR Study and Molecular Mechanism Investigation of Novel Naphthoquinone-furan-2-cyanoacryloyl Hybrids with Antitumor Activity

Liu, P., Fan, D., Qiao, W., He, X., Zhang, L., Jiang, Y., & Yang, T. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14102104 · Cited by 3

Integration of signaling pathway and bromodomain and extra-terminal domain inhibition for the treatment of mutant Kirsten rat sarcoma viral oncogene homolog cancer

Hamilton, G., Stickler, S., & Rath, B. (2023) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2023.00178 · Cited by 3

Repurposing Sertraline for the Treatment of Colorectal Cancer by Blocking Autophagic Flux and Inhibiting Tumor Proliferation

He, L., Guo, X., Wang, W., Xu, W., Feng, X., Fu, Y., Tian, Y., He, Z., Luo, S., Bao, J., et al. (2024) · Advanced Therapeutics · doi:10.1002/adtp.202400199 · Cited by 3

An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer

Huang, M., Wang, W., Cao, L., Liu, J., Du, C., & Zhang, J. (2025) · RSC Medicinal Chemistry · doi:10.1039/d4md00926f · Cited by 2

Challenging the “Undruggable”─Targeting STAT3 but Identifying Potent TrkA-Targeted Inhibitors

Iliev, P., McCutcheon, C., Admas, T. H., Reithmeier, A., McDonald, M. C. L., Outryve, A. V., Hanke, D., Brown, J. I., Haraldsson, M., Toillon, R., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00214 · Cited by 2

Unveiling the Power of Dark State Photocages: An Efficient Pathway to Triplet State Under Near‐Infrared Light Irradiation

Hu, Q. L., Du, J., Abedi, S. A. A., Liu, X., Long, S., Sun, W. C., Fan, J., & Peng, X. (2025) · Angewandte Chemie · doi:10.1002/ange.202504670 · Cited by 2

A glycogen derived from sea urchin-Strongylocentyotus internedius shifts macrophages to the M1 phenotype and enhances the anti-pancreatic cancer activity of gemcitabine

Deng, Z., Yu, H., Wu, N., Wang, Q., Wang, J., Yue, Y., Geng, L., & Zhang, Q. (2025) · Frontiers in Pharmacology · doi:10.3389/fphar.2025.1600349 · Cited by 2

The JAK/STAT conundrum with mutational heterogeneity, immune defects, and the emergence of targeted therapies

Demirkaya, D. B., Colak, B. C., Sefer, A. P., & Barış, S. (2025) · Expert Review of Clinical Immunology · doi:10.1080/1744666x.2025.2543475 · Cited by 3

8-epi-Helenalin suppresses tumorigenesis and metastasis by modulating the STAT3/FAK signaling axis

Nie, F., Jiang, H., Cao, R., Rong, M., Bao, J., Wang, C., Xu, J., & Guo, Y. (2025) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2025.178111 · Cited by 2

Discovery of a novel napabucasin derivative B16 as a potent STAT3 inhibitor for the treatment of triple-negative breast cancer

Deng, X., Li, Y., Chen, L., Xie, Y., Liu, X., Ni, S., Sui, Z., Li, M., Zhu, X., Huang, X., et al. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118329 · Cited by 2

Beyond Passive Bystander: Glioblastoma-Educated Astrocyte Suppressing T Cell

Wang, Y.-Y., & Jin, W. (2025) · Frontiers in Bioscience-Landmark · doi:10.31083/fbl44810 · Cited by 3

Discovery of a novel diphenyl piperidinone-naphthoquinone STAT3 inhibitor as chemoimmunotherapeutic agent

Qin, Y.-G., Mao, Z.-C., Chen, L., Ma, X., Wei, J.-H., Huang, R.-Z., & Zhang, Y. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.109274 · Cited by 2

Limonin mitigates hepatic senescence and fibrosis in MASH mice by targeting STAT3 to inhibit Galectin-3/mTORC1 signaling

Lan, T., Wang, W., Zeng, X.-X., Mao, W.-L., Lu, T., & Wang, S. (2026) · Phytomedicine · doi:10.1016/j.phymed.2026.158244 · Cited by 2

3′‐Hydroxypterostilbene Potently Suppresses Tumor Growth via Inhibiting the Activation of the JAK2/STAT3 Pathway in Ovarian Clear Cell Carcinoma

Koh, Y., Huang, W., Nagabhushanam, K., Ho, C., & Pan, M. (2023) · Molecular Nutrition & Food Research · doi:10.1002/mnfr.202300108 · Cited by 2

In silico exploration of Elaeocarpus ganitrus extract phytochemicals on STAT3, to assess their anticancer potential

Mehnaj, Bhat, A. R., & Athar, F. (2024) · Medicinal Plant Biology · doi:10.48130/mpb-0024-0010 · Cited by 2

Identification of mitophagy and ferroptosis-related hub genes associated with intracerebral haemorrhage through bioinformatics analysis

Wang, Y., Wang, R., Zhu, J., & Chen, L. (2024) · Annals of Human Biology · doi:10.1080/03014460.2024.2334719 · Cited by 2

Alteration of lncRNA RHPN1-AS1 predicts clinical prognosis and regulates the progression of bladder cancer via modulating miR-485-5p

Zhou, J., Xu, J., Cheng, L., Li, S., Jiang, D.-Q., Zhang, J., & Sheng, Y. (2024) · The International Journal of Biological Markers · doi:10.1177/03936155241281076 · Cited by 2

Discovery of novel STAT3 inhibitors with anti-breast cancer activity: structure-based virtual screening, molecular dynamics and biological evaluation

Wang, J., Zhang, P., Yu, Y., Yi, Y., Jiang, Y., & Hu, S. (2025) · RSC Medicinal Chemistry · doi:10.1039/d5md00053j · Cited by 2

STAT3 as a biologically relevant target in H3K27M-mutant diffuse midline glioma

Anderson, J. B., Bouchal, S. M., Zhang, L., & Daniels, D. J. (2023) · Oncotarget · doi:10.18632/oncotarget.28516 · Cited by 2

Evaluation of STAT3 Inhibition by Cancer Chemopreventive Trichothecenes Derived from Metabolites of Trichothecium roseum

Yamashita, M., Nakanishi, A., Chang, C., Tsurushima, K., Nakamoto, K., & Iida, A. (2024) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c24-00300 · Cited by 1

In Silico Methods and Targeted Receptors Used in Cancer Studies

Bıçak, B., & Kecel‐Gunduz, S. (2024) · Interdisciplinary cancer research · doi:10.1007/16833_2024_421 · Cited by 1

Role of FHOD1 in tumor cells and tumor immune microenvironment

Yang, Y., Kang, Z., Cai, J., Jia, S., Fan, S., & Zhu, H. (2025) · Frontiers in Immunology · doi:10.3389/fimmu.2025.1514488 · Cited by 1

OZ-001 Suppresses the Growth of Triple-Negative Breast Cancer and Pancreatic Cancer by Targeting STAT3 Phosphorylation and the Calcium Signaling Pathway

Kim, J., Kim, H., Lee, S., Yu, Y.-J., Ullah, A., Kim, E. Y., Yoo, H., & Chae, H. (2025) · Biomolecules & Therapeutics · doi:10.4062/biomolther.2025.012 · Cited by 1

Recent progress of napabucasin as privileged scaffold in the discovery of anticancer agents

Yang, X., & Ma, G. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.118559 · Cited by 1

Out of Nucleus: Serine 727 Phosphorylation Orchestrates Non-Canonical STAT3 Functions—Relevance to Triple-Negative Breast Cancer

Viavattene, D., Marchetti, A. R., Schael, N., & Poli, V. (2026) · International Journal of Molecular Sciences · doi:10.3390/ijms27052242 · Cited by 2

The STAT3 paradox in aging: Molecular mechanisms and targeted therapeutic strategies

Yang, T., Huo, S., & Wei, S. L. (2026) · Ageing Research Reviews · doi:10.1016/j.arr.2026.103095 · Cited by 1

Discovery of novel napabucasins bearing sulfonylpiperazine scaffolds as potent STAT3 inhibitors for the treatment of prostate cancer

Zhang, C., Yang, L., Li, S., Ma, D., Qu, Y., & Wu, L. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.118774 · Cited by 1

Targeting STAT3 in Alzheimer's disease: Potential mechanisms and therapeutic implications

Chen, P., Wang, R., Zhou, T., Sun, Y. N., Kirchhoff, F., Miao, Z., & Zhuang, C. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.118785 · Cited by 1

Design, synthesis, and evaluation of novel C6-substituted purine-isoxazole derivatives and their Re(I) tricarbonyl complexes: antiproliferative activity and integrated in silico study

Benković, M. P., Sačer, L., Abhirami, R., Singh, S. K., Sedić, M., Persoons, L., Daelemans, D., Perić, B., Kirin, S. I., & Raić‐Malić, S. (2026) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2026.146076 · Cited by 1

Hyperoside accelerates myelin debris clearance by inhibiting signal transducer and activator of transcription 3 phosphorylation in peripheral nerve injury

Su, B., Wang, N., Xie, X., Huang, D., Yu, X., Jiang, Z., Wang, D., Gong, Y., Jia, R., Lu, L., et al. (2026) · Phytomedicine · doi:10.1016/j.phymed.2026.158214 · Cited by 1

DB-2B, a Novel and Selective STAT3 Inhibitor Inhibits Colorectal Cancer Progression In Vitro and In Vivo

Chen, Y., Li, D., Zhang, M., Qiu, Z., Zhang, H., Yu, W., Liang, Z. Y., & Lai, M. (2026) · Biomolecules · doi:10.3390/biom16050752 · Cited by 1

Discovery of SD-2301 as a Highly Potent and Selective PROTAC STAT3 Degrader Capable of Achieving Complete Tumor Regression with Single Administration

Acharyya, R. K., Bai, L., Zhou, H., Wu, D., Wang, M., Metwally, H., McEachern, D., Wang, M., Wen, B., Sun, D., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00743 · Cited by 1

New STAT3 inhibitor through biotransformation of celastrol by Streptomyces olivaceus CICC 23628

Feng, Y., Chen, P., Huang, C., Chen, H., Fan, R., Wang, L., Xu, S., Xu, W., Fan, Z., & Xu, W. (2022) · Arabian Journal of Chemistry · doi:10.1016/j.arabjc.2022.104456 · Cited by 1

FNIP1 suppresses colorectal cancer progression through inhibiting STAT3 phosphorylation and nuclear translocation

Zhang, G., Chen, X., Yu, C., Cui, L., Chen, N., Yi, G., Wang, S., Wei, H., Liang, Y., Ye, S., et al. (2024) · iScience · doi:10.1016/j.isci.2024.110730 · Cited by 1

Photoswitchable Stat3 inhibitors: design, synthesis and anticancer activity study on 2D and 3D breast cancer cell cultures

Bera, S., Bose, S., Paul, N., Bhunia, S., Das, A., & Samanta, S. (2025) · RSC Medicinal Chemistry · doi:10.1039/d5md00490j · Cited by 1

The Goldilocks Principle of JAKs and STATs: Gain-of function mutations, loss-of-function mutations, and their clinical consequencesPreprint

Ott, N., Faletti, L. E., Heeg, M., Andreani, V., & Grimbacher, B. (2022) · Research Square · doi:10.21203/rs.3.rs-1948968/v1 · Cited by 1

Total Synthesis of Phaeosphaerides with STAT3 Inhibitory Activity

Kobayashi, K., Kogen, H., & Tamura, O. (2022) · Journal of Synthetic Organic Chemistry Japan · doi:10.5059/yukigoseikyokaishi.80.755

Histological Study on the Possible Ameliorating Consequence of Blocking STAT-3 Pathway on Psoriasis Model in Adult Male Albino rat

Yousry, M. M., Farag, E. A., & Omar, A. I. (2023) · Egyptian Journal of Medical Research · doi:10.21608/ejmr.2023.214067.1397

Design, Synthesis, and Biological Evaluation of Benzo[B]Thiophene 1,1-Dioxide (BTP) DerivativesPreprint

Ding, L., Li, X., Yan, W., Liu, X., Deng, F., Chen, X., Zhang, Y., Jia, Q., & He, D. (2023) · SSRN Electronic Journal · doi:10.2139/ssrn.4565703

Cardiomyocyte-enriched USP20 ameliorates pathological cardiac hypertrophy by targeting STAT3-CARM1 axisPreprint

Yin, D., Zhong, L., Dai, S., Yu, F., Shi, G., Gong, Q., Zhang, Y., Duan, J., Lou, Z., Tang, Z., et al. (2024) · Research Square · doi:10.21203/rs.3.rs-5264946/v1

Anti-Inflammatory Regulatory Role of Signal Transducer and Activator of Transcription 3 Phosphorylation in Regulating Hypersensitivity Responses to Echinococcus granulosus Hydatid Cyst Fluid

Li, S., Zhou, J., Wang, C., Wang, J., Li, Y., Kulaixi, X., Cao, L., Bayina, B., & Ye, J. (2025) · Journal of Inflammation Research · doi:10.2147/jir.s509286

Molecular Evolution and Functional Characterization of Lethenteron reissneri STAT3

Wang, N., Zheng, X., Zheng, J., Fang, Y., Duan, X., & Li, Y. (2025) · Iranian Journal of Science · doi:10.1007/s40995-025-01820-2

The natural HLA-Peptidome of Sezary Syndrome: uncovering antigens for T cell-based immunotherapy

Nyambura, L. W., Textoris‐Taube, K., & Walden, P. (2025) · Journal of Medical Science · doi:10.20883/medical.e1335

Study of the Mutational Profile of the STAT3 Protein in Relation to Cancer Treatment

Zakaria, E., Rhalem, W., & Ziti, S. (2025) · Lecture notes in networks and systems · doi:10.1007/978-3-032-01967-7_25

The Modified Shuyu Pill Inhibits the Formation of Pre-Metastatic Niches in Triple-Negative Breast Cancer by Reducing the Number of Myeloid-Derived Suppressor Cells (MDSCs) via the JAK2/STAT3 Pathway

Huang, Y., Meng, Y., Lou, X., Feng, D., Ling, X., Jin, Y., Lin, X., & Su, X. (2025) · Breast Cancer Targets and Therapy · doi:10.2147/bctt.s549554

Pristimerin Suppresses STAT3 Signaling in Colorectal Cancer Cells by Targeting JAK2: In Silico and In Vitro Evidence

Yousef, B. A., Elhafiz, M., Ahmedani, E. I., Ismail, M., Bahafi, A. A., El‐Moselhy, M. A., & Saleh, M. A. (2025) · Oriental Journal Of Chemistry · doi:10.13005/ojc/410609

Development of a Series of Tanshinone Derivatives Through Scaffold Hopping for Treating Non-Small-Cell Lung Cancer (NSCLC)

Zhou, L.-X., Shu, Z.-Y., Li, H., Zhong, H., Xu, D.-N., Tang, L., Hu, C.-J., Luo, C., & Xiong, H. (2026) · Molecules · doi:10.3390/molecules31030446

Shenxiao decoction ameliorates podocyte injury in diabetic nephropathy via upregulating RUNX3 expression and inhibiting the JAK2/STAT3 signaling pathway

Liu, W., Peng, X., Gao, S., Song, Z., Li, J., Wu, L., Chang, H., Yang, J., Vikasari, S. N., Xu, Z., et al. (2026) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2026.121300 · Cited by 1

Recent advances in spasmolytic polypeptide expressing metaplasia research

Yang, R.-R., Yan, Y.-R., & Li, Y.-F. (2026) · World Journal of Gastrointestinal Oncology · doi:10.4251/wjgo.v18.i2.113995

Discovery of a potent STAT3 inhibitor WR-S-647 for the treatment of ADPKD

Kang, Z., Zhao, W., Jin, W., Sun, Y., Peng, Y., Wong, J., Guo, D. M., & Chen, Y. (2026) · Archives of Pharmacal Research · doi:10.1007/s12272-026-01594-0

Psoralen and Isopsoralen from Psoralea corylifolia Suppress NSCLC by Dual Mechanisms: STAT3 Inhibition and ROS Modulation

Bi, L., Chen, G., Liu, W., Cagabhion, A. T., Chang, Y.-W., Yao, Z., Feng, J., Liu, Y., Chen, S., & Chen, Y. (2026) · Pharmaceuticals · doi:10.3390/ph19020257

Discovery of SD-965 as a Potent, Selective, and Efficacious STAT3 PROTAC Degrader

Wu, D., Zhou, H., Bai, L., Acharyya, R. K., Metwally, H., McEachern, D., Wang, M., Tošović, J., Rej, R. K., Wang, M., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c03767

Exploration of Potential Core Targets for Acute Liver Injury Based on a Novel Network Pharmacology Strategy Integrating the Common Efficacy and Mechanisms of Active Monomers

Lyu, M., Li, J., Hu, R., Mm, M., Huang, Q., Fan, K., Wang, Y., Yang, J., Cai, B., Wu, Q., et al. (2026) · The FASEB Journal · doi:10.1096/fj.202504908r

Small molecular inhibitors and degraders targeting STAT3 for cancer therapy: An updated review (from 2022 to 2024)

Kang, Z., Shen, L., Li, Y., Song, J., Peng, Y., & Chen, Y. (2024) · Chinese Chemical Letters · doi:10.1016/j.cclet.2024.110447 · Cited by 42

Targeting the STAT3 pathway with STAT3 degraders

Wang, Z., Liao, X., He, H., Guo, X., & Chen, J. (2024) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2024.07.003 · Cited by 46

Discovery of STAT3 Inhibitors: Recent Advances and Future Perspectives

Song, J., Wang, J., Tian, S., & Li, H. (2022) · Current Medicinal Chemistry · doi:10.2174/0929867329666220819093117 · Cited by 54

Small Molecule Inhibitors of STAT3 for Cancer Therapy

Zhao, M. L., Jiang, B., & Gao, F. (2011) · Current Medicinal Chemistry · doi:10.2174/092986711796957284 · Cited by 82

Strategies and Approaches of Targeting STAT3 for Cancer Treatment

Furtek, S. L., Backos, D. S., Matheson, C. J., & Reigan, P. (2016) · ACS Chemical Biology · doi:10.1021/acschembio.5b00945 · Cited by 356