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

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STATs and Gene Regulation

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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

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Indoleamine 2,3-dioxygenase and tumor-induced tolerance

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Stat3 Dimerization Regulated by Reversible Acetylation of a Single Lysine Residue

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

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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

Unphosphorylated STAT3 accumulates in response to IL-6 and activates transcription by binding to NFκB

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Targeted protein degradation by PROTACs

Neklesa, T. K., Winkler, J. D., & Crews, C. M. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.02.027 · Cited by 599

JAK/STAT3-Regulated Fatty Acid β-Oxidation Is Critical for Breast Cancer Stem Cell Self-Renewal and Chemoresistance

Wang, T., Fahrmann, J., Lee, H., Li, Y.-J., Tripathi, S. C., Yue, C., Zhang, C.-Y., Lifshitz, V., Song, J., Yuan, Y., et al. (2017) · Cell Metabolism · doi:10.1016/j.cmet.2017.11.001 · Cited by 580

A Review on Anti-Inflammatory Activity of Monoterpenes

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Terpenes: substances useful in human healthcare

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STAT3 as a potential therapeutic target in triple negative breast cancer: a systematic review

Qin, J., Li, Y., Zhang, J., & Zhang, W. (2019) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-019-1206-z · Cited by 424

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

Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts

Zhang, X., Yue, P., Page, B. D. G., Li, T., Zhao, W. M., Namanja, A. T., Paladino, D., Zhao, J., Chen, Y., Gunning, P. T., et al. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1121606109 · Cited by 348

The biology of Stat4 and Stat6

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First-in-Human Trial of a STAT3 Decoy Oligonucleotide in Head and Neck Tumors: Implications for Cancer Therapy

Sen, M., Thomas, S. M., Kim, S., Yeh, J. I., Ferris, R. L., Johnson, J. T., Duvvuri, U., Lee, J., Sahu, N., Joyce, S., et al. (2012) · Cancer Discovery · doi:10.1158/2159-8290.cd-12-0191 · Cited by 313

Activation of Stat3 Sequence-specific DNA Binding and Transcription by p300/CREB-binding Protein-mediated Acetylation

Wang, R., Cherukuri, P., & Luo, J. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m413930200 · Cited by 275

Medicinal chemistry strategies to discover P-glycoprotein inhibitors: An update

Dong, J., Qin, Z., Zhang, W., Cheng, G., Assaraf, Y. G., Ashby, C. R., Chen, Z., Cheng, X., & Qin, J. (2020) · Drug Resistance Updates · doi:10.1016/j.drup.2020.100681 · Cited by 263

Requirement for Ras/Rac1-Mediated p38 and c-Jun N-Terminal Kinase Signaling in Stat3 Transcriptional Activity Induced by the Src Oncoprotein

Turkson, J., Bowman, T. L., Adnane, J., Zhang, Y., Djeu, J. Y., Sekharam, M., Frank, D. A., Holzman, L. B., Wu, J., Sebti, S. M., et al. (1999) · Molecular and Cellular Biology · doi:10.1128/mcb.19.11.7519 · Cited by 259

Stat3 signaling in acute myeloid leukemia: ligand-dependent and -independent activation and induction of apoptosis by a novel small-molecule Stat3 inhibitor

Redell, M. S., Ruiz, M. J., Alonzo, T. A., Gerbing, R. B., & Tweardy, D. J. (2011) · Blood · doi:10.1182/blood-2010-04-280123 · Cited by 258

Implications of STAT3 and STAT5 signaling on gene regulation and chromatin remodeling in hematopoietic cancer

Wingelhofer, B., Neubauer, H. A., Valent, P., Han, X., Constantinescu, S. N., Gunning, P. T., Müller, M. M., & Moriggl, R. (2018) · Leukemia · doi:10.1038/s41375-018-0117-x · Cited by 253

Acetylated STAT3 is crucial for methylation of tumor-suppressor gene promoters and inhibition by resveratrol results in demethylation

Lee, H., Zhang, P., Herrmann, A., Yang, C., Xin, H., Wang, Z., Hoon, D. S. �., Forman, S. J., Jove, R., Riggs, A. D., et al. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1205132109 · Cited by 241

Activation of STAT3 is a marker of poor prognosis in human colorectal cancer

Kusaba, T., Nakayama, T., Yamazumi, K., Yakata, Y., Yoshizaki, A., Inoue, K., Nagayasu, T., & Sekine, I. (2006) · Oncology Reports · doi:10.3892/or.15.6.1445 · Cited by 238

Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

Zhou, H., Bai, L., Xu, R., Zhao, Y., Chen, J., McEachern, D., Chinnaswamy, K., Wen, B., Dai, L., Kumar, P., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01530 · Cited by 233

Molecular Targeting Therapy against EGFR Family in Breast Cancer: Progress and Future Potentials

Maennling, A. E., Tur, M. K., Niebert, M., Klockenbring, T., Zeppernick, F. A., Gattenlöhner, S., Meinhold-Heerlein, I. M., & Hussain, A. F. (2019) · Cancers · doi:10.3390/cancers11121826 · Cited by 226

Regulation of STAT signaling by acetylation

Zhuang, S. (2013) · Cellular Signalling · doi:10.1016/j.cellsig.2013.05.007 · Cited by 211

Small Molecule Inhibitors of Signal Transducer and Activator of Transcription 3 (Stat3) Protein

Debnath, B., Xu, S., & Neamati, N. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm300207s · Cited by 206

Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Röhrig, U. F., Majjigapu, S. R., Vogel, P., Zoete, V., & Michielin, O. A. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00326 · Cited by 206

STAT3 inhibition, a novel approach to enhancing targeted therapy in human cancers

Wang, X., Crowe, P. J., Goldstein, D., & Yang, J. (2012) · International Journal of Oncology · doi:10.3892/ijo.2012.1568 · Cited by 204

Small molecule-drug conjugates: A novel strategy for cancer-targeted treatment

Zhuang, C., Guan, X., Ma, H., Cong, H., Zhang, W., & Miao, Z. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.12.035 · Cited by 188

A novel small-molecule disrupts Stat3 SH2 domain–phosphotyrosine interactions and Stat3-dependent tumor processes

Zhang, X., Yue, P., Fletcher, S., Zhao, W., Gunning, P. T., & Turkson, J. (2010) · Biochemical Pharmacology · doi:10.1016/j.bcp.2010.01.001 · Cited by 179

Structural Biology of STAT3 and Its Implications for Anticancer Therapies Development

Sgrignani, J., Garofalo, M., Matkovic, M., Merulla, J., Catapano, C. V., & Cavalli, A. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19061591 · Cited by 168

STAT3 in cancer: A double edged sword

Avalle, L., Camporeale, A., Camperi, A., & Poli, V. (2017) · Cytokine · doi:10.1016/j.cyto.2017.03.018 · Cited by 160

Napabucasin: an update on the first-in-class cancer stemness inhibitor

Hubbard, J. M., & Grothey, A. (2017) · Drugs · doi:10.1007/s40265-017-0759-4 · Cited by 157

A novel small molecule inhibits STAT3 phosphorylation and DNA binding activity and exhibits potent growth suppressive activity in human cancer cells

Lin, L., Deangelis, S., Foust, E., Fuchs, J. R., Li, C., Li, P., Schwartz, E. B., Lesinski, G. B., Benson, D., Lü, J., et al. (2010) · Molecular Cancer · doi:10.1186/1476-4598-9-217 · Cited by 152

Identification of a New Series of STAT3 Inhibitors by Virtual Screening

Matsuno, K., Masuda, Y., Uehara, Y., Satō, H., Muroya, A., Takahashi, O., Yokotagawa, T., Furuya, T., Okawara, T., Otsuka, M., et al. (2010) · ACS Medicinal Chemistry Letters · doi:10.1021/ml1000273 · Cited by 149

Mitochondrial Stat3, the need for design thinking

Yang, R., & Rincon, M. (2016) · International Journal of Biological Sciences · doi:10.7150/ijbs.15153 · Cited by 147

Inhibition of the STAT3 signaling pathway contributes to apigenin-mediated anti-metastatic effect in melanoma

Cao, H., Chu, J., Kwan, H. Y., Su, T., Yu, H., Cheng, C.-Y., Fu, X., Guo, H., Li, T., Tse, A. K., et al. (2016) · Scientific Reports · doi:10.1038/srep21731 · Cited by 147

Two decades of research in discovery of anticancer drugs targeting STAT3, how close are we?

Beebe, J., Liu, J., & Zhang, J. (2018) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2018.06.006 · Cited by 144

Pyrimethamine inhibits adult polycystic kidney disease by modulating STAT signaling pathways

Takakura, A., Nelson, E. A., Haque, N., Humphreys, B. D., Zandi-Nejad, K., Frank, D. A., & Zhou, J. (2011) · Human Molecular Genetics · doi:10.1093/hmg/ddr338 · Cited by 143

Mechanisms of Unphosphorylated STAT3 Transcription Factor Binding to DNA

Timofeeva, O. A., Chasovskikh, S., Lonskaya, I., Tarasova, N. I., Khavrutskii, L., Tarasov, S. G., Zhang, X., Korostyshevskiy, V. R., Cheema, A. K., Zhang, L., et al. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.323899 · Cited by 139

Capillarisin inhibits constitutive and inducible STAT3 activation through induction of SHP-1 and SHP-2 tyrosine phosphatases

Lee, J. H., Chiang, S. Y., Nam, D., Chung, W., Lee, J., Na, Y.-S., Sethi, G., & Ahn, K. S. (2013) · Cancer Letters · doi:10.1016/j.canlet.2013.12.008 · Cited by 138

Negative Regulation of STAT3 Protein-mediated Cellular Respiration by SIRT1 Protein

Bernier, M., Paul, R. K., Martín‐Montalvo, A., Scheibye‐Knudsen, M., Song, S., He, H., Armour, S. M., Hubbard, B. P., Bohr, V. A., Wang, L., et al. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.200311 · Cited by 133

Use of a Single CAR T Cell and Several Bispecific Adapters Facilitates Eradication of Multiple Antigenically Different Solid Tumors

Lee, Y. G., Marks, I. S., Srinivasarao, M., Kanduluru, A. K., Mahalingam, S. M., Liu, X., Chu, H., & Low, P. S. (2018) · Cancer Research · doi:10.1158/0008-5472.can-18-1834 · Cited by 131

Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma

Haftchenary, S., Luchman, H. A., Jouk, A. O., Veloso, A. J., Page, B. D. G., Cheng, X. R., Dawson, S. S., Grinshtein, N., Shahani, V. M., Kerman, K., et al. (2013) · ACS Medicinal Chemistry Letters · doi:10.1021/ml4003138 · Cited by 126

A Small Molecule Compound Targeting STAT3 DNA-Binding Domain Inhibits Cancer Cell Proliferation, Migration, and Invasion

Huang, W., Dong, Z., Wang, F., Peng, H., Liu, J., & Zhang, J. (2014) · ACS Chemical Biology · doi:10.1021/cb500071v · Cited by 125

The Role of Signal Transducer and Activator of Transcription 3 (STAT3) and Its Targeted Inhibition in Hematological Malignancies

Arora, L., Kumar, A. P., Arfuso, F., Chng, W. J., & Sethi, G. (2018) · Cancers · doi:10.3390/cancers10090327 · Cited by 124

Discovery of O-Alkylamino-Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents

Chen, H., Yang, Z., Ding, C., Chu, L., Zhang, Y., Terry, K., Liu, H., Shen, Q., & Zhou, J. (2013) · ACS Medicinal Chemistry Letters · doi:10.1021/ml3003082 · Cited by 121

Novel Nitrogen-Enriched Oridonin Analogues with Thiazole-Fused A-Ring: Protecting Group-Free Synthesis, Enhanced Anticancer Profile, and Improved Aqueous Solubility

Ding, C., Zhang, Y., Chen, H., Yang, Z., Wild, C., Chu, L., Liu, H., Shen, Q., & Zhou, J. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm400367n · Cited by 115

Emerging molecular targets in melanoma invasion and metastasis

Orgaz, J. L., & Sanz‐Moreno, V. (2012) · Pigment Cell & Melanoma Research · doi:10.1111/pcmr.12041 · Cited by 113

Identifying and targeting cancer stem cells in the treatment of gastric cancer

Bekaii‐Saab, T., & El‐Rayes, B. F. (2017) · Cancer · doi:10.1002/cncr.30538 · Cited by 112

Small-molecule inhibitors targeting the DNA-binding domain of STAT3 suppress tumor growth, metastasis and STAT3 target gene expression in vivo

Huang, W., Dong, Z., Chen, Y., Wang, F., Wang, C. J., Peng, H., He, Y., Hangoc, G., Pollok, K. E., Sandusky, G. E., et al. (2015) · Oncogene · doi:10.1038/onc.2015.215 · Cited by 110

Gene expression–based discovery of atovaquone as a STAT3 inhibitor and anticancer agent

Xiang, M. H., Kim, H. T., Ho, V. T., Walker, S. R., Bar‐Natan, M., Anahtar, M., Liu, S., Toniolo, P. A., Kroll, Y., Jones, N., et al. (2016) · Blood · doi:10.1182/blood-2015-07-660506 · Cited by 110

A Novel Sequence in the Coiled-coil Domain of Stat3 Essential for Its Nuclear Translocation

Ma, J., Zhang, T., Novotny-Diermayr, V., Tan, A. L. C., & Cao, X. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m304196200 · Cited by 110

Effect of the STAT3 inhibitor STX-0119 on the proliferation of cancer stem-like cells derived from recurrent glioblastoma

Ashizawa, T., Miyata, H., Iizuka, A., Komiyama, M., Oshita, C., KUME, A., Nogami, M., Yagoto, M., Ito, I., Oishi, T., et al. (2013) · International Journal of Oncology · doi:10.3892/ijo.2013.1916 · Cited by 101

Small Molecule STAT5-SH2 Domain Inhibitors Exhibit Potent Antileukemia Activity

Page, B. D. G., Khoury, H., Laister, R. C., Fletcher, S., Vellozo, M., Manzoli, A., Yue, P., Turkson, J., Minden, M. D., & Gunning, P. T. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm200720n · Cited by 99

The natural polyphenol curcumin induces apoptosis by suppressing STAT3 signaling in esophageal squamous cell carcinoma

Liu, Y., Wang, X., Zeng, S., Zhang, X., Zhao, J., Zhang, X., Chen, X., Yang, W., Yang, Y., Dong, Z., et al. (2018) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-018-0959-0 · Cited by 99

Hitting the right spot: Mechanism of action of OPB‐31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3)

Brambilla, L., Genini, D., Laurini, E., Merulla, J., Perez, L. H., Fermeglia, M., Carbone, G. M., Pricl, S., & Catapano, C. V. (2015) · Molecular Oncology · doi:10.1016/j.molonc.2015.02.012 · Cited by 98

Galiellalactone Is a Direct Inhibitor of the Transcription Factor STAT3 in Prostate Cancer Cells

Don‐Doncow, N., Escobar, Z., Johansson, M., Kjellström, S., Garcia, V., Muñóz, E., Sterner, O., Bjartell, A. S., & Hellsten, R. (2014) · Journal of Biological Chemistry · doi:10.1074/jbc.m114.564252 · Cited by 97

Review of STAT3 (Signal Transducers and Activators of Transcription) in head and neck cancer

Mali, S. B. (2015) · Oral Oncology · doi:10.1016/j.oraloncology.2015.03.004 · Cited by 96

Revisiting signal transducer and activator of transcription 3 (STAT3) as an anticancer target and its inhibitor discovery: Where are we and where should we go?

Huang, Q., Zhong, Y., Dong, H., Zheng, Q., Shi, S., Zhu, K., Qu, X., Hu, W., Zhang, X., & Wang, Y. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111922 · Cited by 94

Histone deacetylase 6 regulates the immunosuppressive properties of cancer-associated fibroblasts in breast cancer through the STAT3–COX2-dependent pathway

Li, A., Chen, P., Leng, Y., & Kang, J. (2018) · Oncogene · doi:10.1038/s41388-018-0379-9 · Cited by 91

Osthole inhibits triple negative breast cancer cells by suppressing STAT3

Dai, X., Yin, C., Zhang, Y., Guo, G.-L., Zhao, C., Wang, O., Xiang, Y., Zhang, X., & Liang, G. (2018) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-018-0992-z · Cited by 89

The STAT3 Inhibitor Stattic Impairs Cardiomyocyte Mitochondrial Function Through Increased Reactive Oxygen Species Formation

Boengler, K., Ungefug, E., Heusch, G., & Schulz, R. (2013) · Current Pharmaceutical Design · doi:10.2174/138161281939131127115940 · Cited by 89

Curcumin interacts directly with the Cysteine 259 residue of STAT3 and induces apoptosis in H-Ras transformed human mammary epithelial cells

Hahn, Y., Kim, S., Choi, B., Cho, K.-C., Bandu, R., Kim, K. P., Kim, D., Kim, W.-K., Park, J. S., Han, B. W., et al. (2018) · Scientific Reports · doi:10.1038/s41598-018-23840-2 · Cited by 89

Anti-myeloma Effects of Icariin Are Mediated Through the Attenuation of JAK/STAT3-Dependent Signaling Cascade

Jung, Y. Y., Lee, J. H., Nam, D., Narula, A. S., Namjoshi, O. A., Blough, B. E., Um, J., Sethi, G., & Ahn, K. S. (2018) · Frontiers in Pharmacology · doi:10.3389/fphar.2018.00531 · Cited by 84

Targeting colon cancer with the novel STAT3 inhibitor bruceantinol

Wei, N., Li, J., Fang, C., Chang, J., Xirou, V., Syrigos, N. K., Marks, B. J., Chu, E., & Schmitz, J. C. (2018) · Oncogene · doi:10.1038/s41388-018-0547-y · Cited by 84

Shikonin suppresses IL-17-induced VEGF expression via blockage of JAK2/STAT3 pathway

Xu, Y., Xu, X., Gao, X., Chen, H., & Geng, L. (2014) · International Immunopharmacology · doi:10.1016/j.intimp.2014.01.027 · Cited by 83

Signal Transducer and Activator of Transcription 3 (STAT3): A Promising Target for Anticancer Therapy

Masciocchi, D., Gelain, A., Villa, S., Meneghetti, F., & Barlocco, D. (2011) · Future Medicinal Chemistry · doi:10.4155/fmc.11.22 · Cited by 80

Quinazoline Ligands Induce Cancer Cell Death through Selective STAT3 Inhibition and G-Quadruplex Stabilization

Jamroškovič, J., Doimo, M., Chand, K., Obi, I. R., Kumar, R., Brännström, K., Hedenström, M., Das, R. N., Akhunzianov, A., Deiana, M., et al. (2020) · Journal of the American Chemical Society · doi:10.1021/jacs.9b11232 · Cited by 80

Observation of unphosphorylated STAT3 core protein binding to target ds DNA by PEMSA and X‐ray crystallography

Nkansah, E., Shah, R., Collie, G. W., Parkinson, G. N., Palmer, J. M., Rahman, K. M., Bui, T. T. T., Drake, A. F., Husby, J., Neidle, S., et al. (2013) · FEBS Letters · doi:10.1016/j.febslet.2013.01.065 · Cited by 79

Silibinin is a direct inhibitor of STAT3

Verdura, S., Cuyàs, E., Llorach-Parés, L., Pérez-Sánchez, A., Micol, V., Nonell‐Canals, A., Joven, J., Valiente, M., Sánchez-Martínez, M., Bosch‐Barrera, J., et al. (2018) · Food and Chemical Toxicology · doi:10.1016/j.fct.2018.04.028 · Cited by 79

Inhibiting signal transducer and activator of transcription 3: rationality and rationale design of inhibitors

Mankan, A. K., & Greten, F. R. (2011) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.2011.601739 · Cited by 77

An anti-prostate cancer benzofuran-conjugated iridium(III) complex as a dual inhibitor of STAT3 and NF-κB

Kang, T., Wang, W., Zhong, H., Dong, Z., Huang, Q., Mok, S. W. F., Leung, C., Wong, V. K. W., & Ma, D. (2017) · Cancer Letters · doi:10.1016/j.canlet.2017.03.016 · Cited by 77

Discovery of fluorescent coumarin-benzo[b]thiophene 1, 1-dioxide conjugates as mitochondria-targeting antitumor STAT3 inhibitors

Cai, G., Yu, W., Song, D., Zhang, W., Guo, J., Zhu, J., Ren, Y., & Kong, L. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.04.024 · Cited by 76

Isoalantolactone induces apoptosis through ROS-mediated ER stress and inhibition of STAT3 in prostate cancer cells

Chen, W., Li, P., Liu, Y., Yu, Y., Ye, X., Zhang, F., & Huang, H. (2018) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-018-0987-9 · Cited by 76

Piceatannol inhibits migration and invasion of prostate cancer cells: possible mediation by decreased interleukin-6 signaling

Kwon, G. T., Jung, J. I., Song, H. R., Woo, E. Y., Jun, J., Kim, J., Her, S., & Park, J. H. Y. (2011) · The Journal of Nutritional Biochemistry · doi:10.1016/j.jnutbio.2010.11.019 · Cited by 75

STAT2 phosphorylation and signaling

Steen, H. C., & Gamero, A. M. (2013) · JAK-STAT · doi:10.4161/jkst.25790 · Cited by 73

Hydroxamic Acid and Benzoic Acid–Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes In Vitro and In Vivo

Yue, P., Lopez‐Tapia, F., Paladino, D., Li, Y., Chen, C., Namanja, A. T., Hilliard, T. S., Chen, Y., Tius, M. A., & Turkson, J. (2015) · Cancer Research · doi:10.1158/0008-5472.can-14-3558 · Cited by 72

Napabucasin and Related Heterocycle-Fused Naphthoquinones as STAT3 Inhibitors with Antiproliferative Activity against Cancer Cells

Löcken, H., Clamor, C., & Müller, K. (2018) · Journal of Natural Products · doi:10.1021/acs.jnatprod.8b00247 · Cited by 71

Suppressive Effects of Plumbagin on Invasion and Migration of Breast Cancer Cells via the Inhibition of STAT3 Signaling and Down-regulation of Inflammatory Cytokine Expressions

Yan, W., Tu, B., Liu, Y., Wang, T., Qiao, H., Zhai, Z., Li, H., & Tang, T. (2013) · Bone Research · doi:10.4248/br201304007 · Cited by 68

HO-3867, a curcumin analog, sensitizes cisplatin-resistant ovarian carcinoma, leading to therapeutic synergy through STAT3 inhibition

Selvendiran, K., Ahmed, S., Dayton, A., Kuppusamy, M. L., Rivera, B. K., Kálai, T., Hideg, K., & Kuppusamy, P. (2011) · Cancer Biology & Therapy · doi:10.4161/cbt.12.9.17713 · Cited by 68

Impact of the N-Terminal Domain of STAT3 in STAT3-Dependent Transcriptional Activity

Hu, T., Yeh, J., Pinello, L., Jacob, J., Chakravarthy, S., Yuan, G., Chopra, R., & Frank, D. A. (2015) · Molecular and Cellular Biology · doi:10.1128/mcb.00060-15 · Cited by 65

Immunotherapeutic Suppression of Indoleamine 2,3-Dioxygenase and Tumor Growth with Ethyl Pyruvate

Muller, A. J., DuHadaway, J. B., Jaller, D., Curtis, P. J., Metz, R. A., & Prendergast, G. C. (2010) · Cancer Research · doi:10.1158/0008-5472.can-09-3613 · Cited by 64

Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91

Hanafi, M., Chen, X., & Neamati, N. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01897 · Cited by 61

A STAT inhibitor patent review: progress since 2011

Lai, P., Rosa, D. A., Ali, A. M., Gómez‐Biagi, R. F., Ball, D. P., Shouksmith, A. E., & Gunning, P. T. (2015) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.2015.1086749 · Cited by 59

Mutations in the linker domain affect phospho-STAT3 function and suggest targets for interrupting STAT3 activity

Mertens, C., Haripal, B., Klinge, S., & Darnell, J. E. (2015) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1515876112 · Cited by 59

Alkylation of Cysteine 468 in Stat3 Defines a Novel Site for Therapeutic Development

Buettner, R., Corzano, R., Rashid, R., Lin, J., Senthil, M., Hedvat, M., Schroeder, A., Mao, A., Herrmann, A., Yim, J. H., et al. (2011) · ACS Chemical Biology · doi:10.1021/cb100253e · Cited by 58

Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation

Xi, M., Chen, Y., Yang, H., Xu, H., Du, K., Wu, C., Xu, Y., Deng, L., Luo, X., Yu, L., et al. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.04.036 · Cited by 57

STAT3 transcription factor as target for anti-cancer therapy

Mohassab, A. M., Hassan, H. A., Abdelhamid, D. S., & Abdel‐Aziz, M. (2020) · Pharmacological Reports · doi:10.1007/s43440-020-00156-5 · Cited by 57

Antagonism of the Stat3–Stat3 Protein Dimer with Salicylic Acid Based Small Molecules

Fletcher, S., Page, B. D. G., Zhang, X., Yue, P., Li, Z. H., Sharmeen, S., Singh, J., Zhao, W. M., Schimmer, A. D., Trudel, S., et al. (2011) · ChemMedChem · doi:10.1002/cmdc.201100194 · Cited by 52

Signal Transducer and Activator of Transcription Protein 3 (STAT3): An Update on its Direct Inhibitors as Promising Anticancer Agents

Gelain, A., Mori, M., Meneghetti, F., & Villa, S. (2018) · Current Medicinal Chemistry · doi:10.2174/0929867325666180719122729 · Cited by 49

Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking

Yu, W., Li, C., Zhang, W., Xia, Y., Li, S., Lin, J., Yu, K., Liu, M., Yang, L. F., Luo, J., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01489 · Cited by 48

Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3

Huang, R.-Z., Jing, X.-T., Huang, X., Pan, Y.-M., Fang, Y., Liang, G.-B., Liao, Z., Wang, H., Chen, Z., & Zhang, Y. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01386 · Cited by 48

JAB1 regulates unphosphorylated STAT3 DNA-binding activity through protein–protein interaction in human colon cancer cells

Nishimoto, A., Kugimiya, N., Hosoyama, T., Enoki, T., Li, T., & Hamano, K. (2013) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2013.07.105 · Cited by 47

Antagonizing STAT3 activation with benzo[b]thiophene 1, 1-dioxide based small molecules

Zhang, W., Ma, T., Li, S., Yang, Y., Guo, J., Yu, W., & Kong, L. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.09.068 · Cited by 46

A novel series of napabucasin derivatives as orally active inhibitors of signal transducer and activator of transcription 3 (STAT3)

Li, C., Chen, C., An, Q., Yang, T., Sang, Z., Yang, Y., Ju, Y., Tong, A., & Luo, Y. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.10.067 · Cited by 46

Small-molecule compounds targeting the STAT3 DNA-binding domain suppress survival of cisplatin-resistant human ovarian cancer cells by inducing apoptosis

Huang, W., Liu, Y., Wang, J., Yuan, X., Jin, H.-W., Zhang, L.-R., Zhang, J., Liu, Z.-M., & Cui, J.-R. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.08.037 · Cited by 45

UPLC/MS/MS method for quantification and cytotoxic activity of sesquiterpene lactones isolated from Saussurea lappa

Kumar, A., Kumar, S., Kumar, D., & Agnihotri, V. K. (2014) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2014.07.037 · Cited by 45

Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors

Brotherton‐Pleiss, C., Yue, P., Zhu, Y., Nakamura, K., Chen, W., Fu, W., Kubota, C. S., Chen, J., Alonso-Valenteen, F., Mikhael, S., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01705 · Cited by 43

Design, synthesis and activity of BBI608 derivatives targeting on stem cells

Zhou, Q., Peng, C., Du, F., Zhou, L., Shi, Y., Du, Y., Liu, D., Sun, W., Zhang, M., & Chen, G. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.03.054 · Cited by 43

Isoalantolactone induces apoptosis through reactive oxygen species-dependent upregulation of death receptor 5 in human esophageal cancer cells

Lu, Z., Zhang, G., Zhang, Y., Hua, P., Fang, M.-D., Wu, M., & Liu, T. (2018) · Toxicology and Applied Pharmacology · doi:10.1016/j.taap.2018.05.026 · Cited by 43

Synthesis and structure-activity relationship studies of α-naphthoflavone derivatives as CYP1B1 inhibitors

Dong, J., Wang, Z., Cui, J., Meng, Q., & Li, S. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111938 · Cited by 43

STAT3 Inhibitor ODZ10117 Suppresses Glioblastoma Malignancy and Prolongs Survival in a Glioblastoma Xenograft Model

Kim, B., Lee, H., Park, C. G., Jeong, A. J., Lee, S. H., Noh, K. H., Park, J. B., Lee, C.-G., Paek, S. H., Kim, H., et al. (2020) · Cells · doi:10.3390/cells9030722 · Cited by 42

Blockage of STAT3 Signaling Pathway by Morusin Induces Apoptosis and Inhibits Invasion in Human Pancreatic Tumor Cells

Kim, C., Kim, J. H., Oh, E. Y., Nam, D., Lee, S., Lee, J., Kim, S., Shim, B. S., & Ahn, K. S. (2015) · Pancreas · doi:10.1097/mpa.0000000000000496 · Cited by 41

An in vivo active 1,2,5-oxadiazole Pt(II) complex: A promising anticancer agent endowed with STAT3 inhibitory properties

Porta, F., Facchetti, G., Ferri, N., Gelain, A., Meneghetti, F., Villa, S., Barlocco, D., Masciocchi, D., Asai, A., Miyoshi, N., et al. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.03.017 · Cited by 41

Identification of new shikonin derivatives as STAT3 inhibitors

Qiu, H., Fu, J., Yang, M., Han, H., Wang, P., Zhang, Y., Lin, H., Tang, C., Qi, J., Yang, R., et al. (2017) · Biochemical Pharmacology · doi:10.1016/j.bcp.2017.10.009 · Cited by 40

Revisiting the development of small molecular inhibitors that directly target the signal transducer and activator of transcription 3 (STAT3) domains

Shih, P. (2019) · Life Sciences · doi:10.1016/j.lfs.2019.117241 · Cited by 40

Crispene E, a cis-clerodane diterpene inhibits STAT3 dimerization in breast cancer cells

Mantaj, J., Rahman, S. M. A., Bokshi, B., Hasan, C. M., Jackson, P. J., Parsons, R. B., & Rahman, K. M. (2015) · Organic & Biomolecular Chemistry · doi:10.1039/c5ob00052a · Cited by 39

Discovery of monocarbonyl curcumin-BTP hybrids as STAT3 inhibitors for drug-sensitive and drug-resistant breast cancer therapy

Zhang, W., Guo, J., Li, S., Ma, T., Xu, D., Han, C., Liu, F., Yu, W., & Kong, L. (2017) · Scientific Reports · doi:10.1038/srep46352 · Cited by 39

MMPP Attenuates Non-Small Cell Lung Cancer Growth by Inhibiting the STAT3 DNA-Binding Activity via Direct Binding to the STAT3 DNA-Binding Domain

Son, D. J., Zheng, J., Jung, Y. Y., Hwang, C. J., Lee, H. P., Woo, J. R., Baek, S. Y., Ham, Y. W., Kang, M. W., Shong, M., et al. (2017) · Theranostics · doi:10.7150/thno.18630 · Cited by 39

Novel aminotetrazole derivatives as selective STAT3 non-peptide inhibitors

Pallandre, J., Borg, C., Rognan, D., Boibessot, T., Luzet, V., Yesylevskyy, S. O., Ramseyer, C., & Pudlo, M. (2015) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2015.08.054 · Cited by 38

Inhibiting Aberrant Signal Transducer and Activator of Transcription Protein Activation with Tetrapodal, Small Molecule Src Homology 2 Domain Binders: Promising Agents against Multiple Myeloma

Page, B. D. G., Croucher, D. C., Li, Z., Haftchenary, S., Jimenez-Zepeda, V. H., Atkinson, J. M., Spagnuolo, P. A., Wong, Y. L., Colaguori, R., Lewis, A. M., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm3017255 · Cited by 38

Effect of the STAT3 inhibitor STX-0119 on the proliferation of a temozolomide-resistant glioblastoma cell line

Ashizawa, T., Akiyama, Y., Miyata, H., Iizuka, A., Komiyama, M., Kume, A., Omiya, M., Sugino, T., Asai, A., Hayashi, N., et al. (2014) · International Journal of Oncology · doi:10.3892/ijo.2014.2439 · Cited by 38

Rhodium(II) proximity-labeling identifies a novel target site on STAT3 for inhibitors with potent anti-leukemia activity

Minus, M. B., Liu, W., Vohidov, F., Kasembeli, M. M., Long, X., Krueger, M. J., Stevens, A., Kolosov, M. I., Tweardy, D. J., Sison, E. A. R., et al. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201506889 · Cited by 38

Preclinical Characterization of 3β-(N-Acetyl l -cysteine methyl ester)-2aβ,3-dihydrogaliellalactone (GPA512), a Prodrug of a Direct STAT3 Inhibitor for the Treatment of Prostate Cancer

Escobar, Z., Bjartell, A. S., Canesin, G., Axelsson, S. E., Sterner, O., Hellsten, R., & Johansson, M. H. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01814 · Cited by 37

GSTP1 negatively regulates Stat3 activation in epidermal growth factor signaling

Kou, X., Chen, N., Feng, Z., Luo, L., & Yin, Z. (2012) · Oncology Letters · doi:10.3892/ol.2012.1098 · Cited by 36

NO-releasing STAT3 inhibitors suppress BRAF-mutant melanoma growth

Kaoud, T. S., Mohassab, A. M., Hassan, H. A., Yan, C., Ravenstein, S. X. V., Abdelhamid, D. S., Dalby, K. N., & Abdel‐Aziz, M. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111885 · Cited by 36

Aspeterreurone A, a Cytotoxic Dihydrobenzofuran–Phenyl Acrylate Hybrid from the Deep-Sea-Derived Fungus Aspergillus terreus CC-S06-18

Wang, W., Yang, J., Liao, Y., Cheng, G., Chen, J., Mo, S., Li, Y., Cheng, X., Qin, J., & Shao, Z. (2020) · Journal of Natural Products · doi:10.1021/acs.jnatprod.0c00189 · Cited by 36

Identification of New Shikonin Derivatives as Antitumor Agents Targeting STAT3 SH2 Domain

Qiu, H., Zhu, X., Luo, Y., Lin, H., Tang, C., Qi, J., Pang, Y.-J., Yang, R., Lu, G., Wang, X., et al. (2017) · Scientific Reports · doi:10.1038/s41598-017-02671-7 · Cited by 35

2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors

Lamie, P. F., & Philoppes, J. N. (2020) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2020.1740922 · Cited by 34

Inhibition of STAT3 acetylation is associated with attenuated renal fibrosis in the obstructed kidney

Ni, J., Shen, Y., Wang, Z., Shao, D., Liu, J., Fu, L., Kong, Y.-L., Zhou, L., Xue, H., Huang, Y., et al. (2014) · Acta Pharmacologica Sinica · doi:10.1038/aps.2014.42 · Cited by 34

A thiazole-derived oridonin analogue exhibits antitumor activity by directly and allosterically inhibiting STAT3

Shen, X., Zhao, L., Chen, P., Gong, Y., Liu, D., Zhang, X., Dai, L., Sun, Q., Lou, J., Jin, Z., et al. (2019) · Journal of Biological Chemistry · doi:10.1074/jbc.ra119.009801 · Cited by 34

Discovery of heterocycle-containing α-naphthoflavone derivatives as water-soluble, highly potent and selective CYP1B1 inhibitors

Dong, J., Huang, G., Cui, Q., Meng, Q., Li, S., & Cui, J. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112895 · Cited by 34

Geranylnaringenin (CG902) inhibits constitutive and inducible STAT3 activation through the activation of SHP-2 tyrosine phosphatase

Jin, Y., Yoon, Y. J., Jeon, Y. J., Choi, J., Lee, Y.-J., Lee, J., Choi, S., Nash, O., Han, D. C., & Kwon, B. (2017) · Biochemical Pharmacology · doi:10.1016/j.bcp.2017.06.131 · Cited by 33

Allosteric inhibitors of the STAT3 signaling pathway

Qin, J., Shen, X., Zhang, J., & Jia, D. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112122 · Cited by 33

LL1, a novel and highly selective STAT3 inhibitor, displays anti‐colorectal cancer activities in vitro and in vivo

Liu, Z., Wang, H., Guan, L., Lai, C., Yu, W., & Lai, M. (2019) · British Journal of Pharmacology · doi:10.1111/bph.14863 · Cited by 32

A novel small molecule STAT3 inhibitor SLSI-1216 suppresses proliferation and tumor growth of triple-negative breast cancer cells through apoptotic induction

Park, S. K., Byun, W. S., Lee, S., Han, Y. T., Jeong, Y., Jang, K., Chung, S., Lee, J., Suh, Y., & Lee, S. K. (2020) · Biochemical Pharmacology · doi:10.1016/j.bcp.2020.114053 · Cited by 32

Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors

Gao, D., Jin, N., Fu, Y., Zhu, Y., Wang, Y., Wang, T., Chen, Y., Zhang, M., Xiao, Q., Huang, M., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113333 · Cited by 32

The anti-tumor activity of the STAT3 inhibitor STX-0119 occurs via promotion of tumor-infiltrating lymphocyte accumulation in temozolomide-resistant glioblastoma cell line

Akiyama, Y., Nonomura, C., Ashizawa, T., Iizuka, A., Kondou, R., Miyata, H., Sugino, T., Mitsuya, K., Hayashi, N., Nakasu, Y., et al. (2017) · Immunology Letters · doi:10.1016/j.imlet.2017.07.005 · Cited by 32

C188-9, a small-molecule STAT3 inhibitor, exerts an antitumor effect on head and neck squamous cell carcinoma

Di, J.-X., & Zhang, H. (2019) · Anti-Cancer Drugs · doi:10.1097/cad.0000000000000783 · Cited by 32

Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors

LaPorte, M. G., Wang, Z., Colombo, R., Garzan, A., Peshkov, V. A., Liang, M., Johnston, P. A., Schurdak, M. E., Sen, M., Camarco, D. P., et al. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.06.017 · Cited by 31

N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling

Lai, M.-J., Lee, H., Chuang, H., Chang, L., Tsai, A.-C., Chen, M.-C., Huang, H.-L., Wu, Y., Teng, C., Pan, S., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00659 · Cited by 30

Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importin α-2 Expression, and Induce Antitumor Effects against Human Glioma

Miklóssy, G., Youn, U. J., Yue, P., Zhang, M., Chen, C.-H., Hilliard, T. S., Paladino, D., Li, Y., Choi, J. C.-B., Sarkaria, J. N., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00686 · Cited by 29

Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy

Feng, K.-R., Wang, F., Shi, X., Tan, Y., Zhao, J., Zhang, J., Li, Q., Lin, G., Gao, D., & Tian, P. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112428 · Cited by 29

Development of Erasin: a chromone-based STAT3 inhibitor which induces apoptosis in Erlotinib-resistant lung cancer cells

Lis, C., Rubner, S., Roatsch, M., Berg, A., Gilcrest, T., Fu, D., Nguyen, E. D., Schmidt, A.-M., Krautscheid, H., Meiler, J., et al. (2017) · Scientific Reports · doi:10.1038/s41598-017-17600-x · Cited by 28

Crispenes F and G, cis-Clerodane Furanoditerpenoids from Tinospora crispa, Inhibit STAT3 Dimerization

Noman, M. A. A., Hossain, T., Ahsan, M., Jamshidi, S., Hasan, C. M., & Rahman, K. M. (2018) · Journal of Natural Products · doi:10.1021/acs.jnatprod.7b00377 · Cited by 27

Development of benzochalcone derivatives as selective CYP1B1 inhibitors and anticancer agents

Dong, J., Huang, G., Zhang, Q., Wang, Z., Cui, J., Wu, Y. F., Meng, Q., & Li, S. (2019) · MedChemComm · doi:10.1039/c9md00258h · Cited by 27

2′-Hydroxyflavanone inhibits the progression of pancreatic cancer cells and sensitizes the chemosensitivity of EGFR inhibitors via repressing STAT3 signaling

Yue, Y., Qian, W., Li, J., Wu, S., Zhang, M., Wu, Z., Ma, Q., & Wang, Z. (2019) · Cancer Letters · doi:10.1016/j.canlet.2019.11.041 · Cited by 26

LYW-6, a novel cryptotanshinone derived STAT3 targeting inhibitor, suppresses colorectal cancer growth and metastasis

Wang, H., Liu, Z., Guan, L., Li, J., Chen, S., Yu, W., & Lai, M. (2020) · Pharmacological Research · doi:10.1016/j.phrs.2020.104661 · Cited by 25

Design, synthesis and activity of novel 2,6-disubstituted purine derivatives, potential small molecule inhibitors of signal transducer and activator of transcription 3

Wang, X., He, Q., Wu, K., Guo, T., Du, X., Zhang, H., Fang, L., Zheng, N., Zhang, Q., & Ye, F. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.06.017 · Cited by 24

Development of a STAT3 reporter prostate cancer cell line for high throughput screening of STAT3 activators and inhibitors

Chau, M. N., & Banerjee, P. P. (2008) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2008.10.025 · Cited by 22

Identification of galiellalactone-based novel STAT3-selective inhibitors with cytotoxic activities against triple-negative breast cancer cell lines

Kim, H. S., Kim, T., Ko, H., Lee, J., Kim, Y. S., & Suh, Y. (2017) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2017.06.036 · Cited by 22

Small molecule STAT3 inhibitor, 6Br-6a suppresses breast cancer growth in vitro and in vivo

Liu, Z., Ge, X., Gu, Y., Huang, Y., Liu, H., Yu, M., & Liu, Y. (2019) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2019.109502 · Cited by 22

Unphosphorylated STAT3 regulates the antiproliferative, antiviral, and gene-inducing actions of type I interferons

Pfeffer, S. R., Fan, M., Du, Z., Yang, C. H., & Pfeffer, L. M. (2017) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2017.06.111 · Cited by 21

Development of Oxadiazole-Based ODZ10117 as a Small-Molecule Inhibitor of STAT3 for Targeted Cancer Therapy

Kim, B., Lee, H., Song, Y., Park, J.-S., Gadhe, C. G., Choi, J., Lee, C.-G., Pae, A. N., Kim, S., & Ye, S. (2019) · Journal of Clinical Medicine · doi:10.3390/jcm8111847 · Cited by 21

Selective Inhibition of STAT3 with Respect to STAT1: Insights from Molecular Dynamics and Ensemble Docking Simulations

Yesylevskyy, S. O., Ramseyer, C., Pudlo, M., Pallandre, J., & Borg, C. (2016) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.6b00198 · Cited by 20

Pharmacokinetic evaluation, molecular docking and in vitro biological evaluation of 1, 3, 4-oxadiazole derivatives as potent antioxidants and STAT3 inhibitors

Khanam, R., Hejazi, I. I., Shahabuddin, S., Bhat, A. R., & Athar, F. (2018) · Journal of Pharmaceutical Analysis · doi:10.1016/j.jpha.2018.12.002 · Cited by 20

Linker Variation and Structure–Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors

Lopez‐Tapia, F., Brotherton‐Pleiss, C., Yue, P., Murakami, H. A., Araujo, A. C. C., dos Santos, B. R., Ichinotsubo, E., Rabkin, A., Shah, R., Lantz, M. J., et al. (2018) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.7b00544 · Cited by 19

Discovery of new benzensulfonamide derivatives as tripedal STAT3 inhibitors

Guo, J., Yu, W., Cai, G., Zhang, W., Li, S., Zhu, J., Song, D., & Kong, L. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.03.053 · Cited by 19

Antitumor activity of a novel oral signal transducer and activator of transcription 3 inhibitor YHO‐1701

Nishisaka, F., Taniguchi, K., Tsugane, M., Hirata, G., Takagi, A., Asakawa, N., Kurita, A., Takahashi, H., Ogo, N., Shishido, Y., et al. (2020) · Cancer Science · doi:10.1111/cas.14369 · Cited by 19

N-Arylsulfonylsubstituted-1H indole derivatives as small molecule dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and tubulin

Zhou, Q., Zhu, J., Chen, J., Ji, P., & Qiao, C. (2017) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2017.11.023 · Cited by 19

Screening and biological evaluation of a novel STAT3 signaling pathway inhibitor against cancer

Huang, M., Chen, Z., Zhang, L., Huang, Z., Chen, Y., Xu, J., Zhang, J., & Shu, X. H. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.09.073 · Cited by 18

Discovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide

Wang, X., Wu, K., Fang, L., Yang, X., Zheng, N., Du, Z., Lu, Y., Xie, Z., Liu, Z., Zuo, Z., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113362 · Cited by 18

Inhibition of STAT3 by Anticancer Drug Bendamustine

Iwamoto, K., Uehara, Y., Inoue, Y., Taguchi, K., Muraoka, D., Ogo, N., Matsuno, K., & Asai, A. (2017) · PLoS ONE · doi:10.1371/journal.pone.0170709 · Cited by 17

Design, synthesis and biological evaluation of novel plumbagin derivatives as potent antitumor agents with STAT3 inhibition

Li, N., Ou, J., Bao, N., Cheng, C., Shi, Z., Chen, L., & Sun, J. (2020) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2020.104208 · Cited by 17

Shikonin inhibits IFN-γ-induced K17 over-expression of HaCaT cells by interfering with STAT3 signaling.

Liu, L., Wu, Y., Cao, K., Xu, Y.-Y., Gao, X. H., Chen, H. D., & Geng, L. (2015) · PubMed Central · Cited by 15

Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action

Kim, K., Kim, S., Han, Y. T., Hong, S.-J., An, H., Chang, D., Kim, T., Lim, B., Lee, J., Surh, Y., et al. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.07.063 · Cited by 15

Targeting STAT3 anti-apoptosis pathways with organic and hybrid organic–inorganic inhibitors

Minus, M. B., Wang, H., Munoz, J. O., Stevens, A. M., Mangubat-Medina, A. E., Krueger, M., Liu, W., Kasembeli, M. M., Cooper, J. C., Kolosov, M. I., et al. (2020) · Organic & Biomolecular Chemistry · doi:10.1039/c9ob02682g · Cited by 13

Discovery of a New STAT3 Inhibitor Acting on the Linker Domain

Koseki, T., Suehiro, N., Masuda, Y., Miyoshi, N., Muraoka, D., Ogo, N., & Asai, A. (2019) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.b18-00992 · Cited by 13

Efficacy of combination treatment using YHO-1701, an orally active STAT3 inhibitor, with molecular-targeted agents on cancer cell lines

Taniguchi, K., Konishi, H., Yoshinaga, A., Tsugane, M., Takahashi, H., Nishisaka, F., Shishido, Y., & Asai, A. (2021) · Scientific Reports · doi:10.1038/s41598-021-86021-8 · Cited by 12

Identification of novel STAT3 inhibitors bearing 2-acetyl-7-phenylamino benzofuran scaffold for antitumour study

Wang, F., Feng, K., Zhao, J., Zhang, J., Shi, X., Zhou, J. E., Gao, D., Lin, G., & Tian, P. (2020) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2020.115822 · Cited by 11

Small Molecule Inhibitor C188-9 Synergistically Enhances the Demethylated Activity of Low-Dose 5-Aza-2′-Deoxycytidine Against Pancreatic Cancer

Kong, R., Sun, G., Li, X., Wu, L., Li, L., Li, Y., Wang, F., Xuan, P., Yang, S., Sun, B., et al. (2020) · Frontiers in Oncology · doi:10.3389/fonc.2020.00612 · Cited by 11

4-Carbonyl-2,6-dibenzylidenecyclohexanone derivatives as small molecule inhibitors of STAT3 signaling pathway

Ji, P., Yuan, C., Ma, S., Fan, J., Fu, W., & Qiao, C. (2016) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2016.09.070 · Cited by 10

Synthesis and biological evaluation of novel isothiazoloquinoline quinone analogues

Chen, L., Xie, Y., Luo, Z.-Y., Liu, L., Zou, Z., Liu, H., Kong, F.-R., Hao, Y., Gao, J., Wang, L., et al. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127286 · Cited by 9

Abstract 387: Pyrimethamine inhibits STAT3 transcriptional activity via dihydrofolate reductase

Heppler, L. N., Walker, S. R., Attarha, S., Page, B. D. G., & Frank, D. A. (2019) · Cancer Research · doi:10.1158/1538-7445.am2019-387 · Cited by 1

Targeting cytokine and chemokine signaling pathways for cancer therapy

Yi, M., Li, T., Niu, M., Zhang, H., Wu, Y., Wu, K., & Dai, Z. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01868-3 · Cited by 528

Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy

Wang, Z., Zhang, Z.-C., Wu, Y., Pi, Y., Lou, S., Liu, T., Lou, G., & Yang, C. Q. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01647-6 · Cited by 251

Strategies to overcome cancer multidrug resistance (MDR) through targeting P-glycoprotein (ABCB1): An updated review

Dong, J., Li, Y., Hu, C., Cheng, X., & Qin, J. (2023) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2023.108488 · Cited by 193

Protein degradation technology: a strategic paradigm shift in drug discovery

Li, H., Dong, J., Cai, M., Xu, Z., Cheng, X., & Qin, J. (2021) · Journal of Hematology & Oncology · doi:10.1186/s13045-021-01146-7 · Cited by 96

Targeting Undruggable Transcription Factors with PROTACs: Advances and Perspectives

Li, Y., Song, J. H., Zhou, P., Zhou, J., & Xie, S. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00691 · Cited by 91

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