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

Zhang, Xiaolei, Yue, Peibin, Fletcher, Steven, Zhao, Wei, Gunning, Patrick T., Turkson, James·2010·Biochemical Pharmacology

DOI 10.1016/j.bcp.2010.01.001

Cited by (199)

Items 101–199 of 199

Natural product preferentially targets redox and metabolic adaptations and aberrantly active STAT3 to inhibit breast tumor growth in vivo
Yinsong Zhu, Peibin Yue, Cody F. Dickinson, Justin K. Yang, Kyrstin Datanagan, Ning Zhai, Yi Zhang, Gabriella Miklóssy, Francisco Lopez‐Tapia, Marcus A. Tius et al. · 2022 · Cell Death and Disease
Antitumor activity of a novel oral signal transducer and activator of transcription 3 inhibitor YHO‐1701
Fukiko Nishisaka, Keisuke Taniguchi, Momomi Tsugane, Genya Hirata, Akimitsu Takagi, Naoyuki Asakawa, Akinobu Kurita, Hiroyuki Takahashi, Naohisa Ogo, Yoshiyuki Shishido et al. · 2020 · Cancer Science
Structure–Activity Studies of Phosphopeptidomimetic Prodrugs Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 3 (Stat3)
Pijus Kumar Mandal, Zhiyong Ren, Xiaomin Chen, Kumar K. Kaluarachchi, Warren S.‐L. Liao, John S. McMurray · 2012 · International Journal of Peptide Research and Therapeutics
Linker Variation and Structure–Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors
Francisco Lopez‐Tapia, Christine Brotherton‐Pleiss, Peibin Yue, Heide A. Murakami, Ana Carolina Costa Araujo, Bruna Reis dos Santos, Erin Ichinotsubo, Anna Rabkin, Raj Shah, Megan J. Lantz et al. · 2018 · ACS Medicinal Chemistry Letters
Discovery of new benzensulfonamide derivatives as tripedal STAT3 inhibitors
Jianpeng Guo, Wenying Yu, Guiping Cai, Wenda Zhang, Shanshan Li, Jiawen Zhu, Dongmei Song, Ling‐Yi Kong · 2018 · European Journal of Medicinal Chemistry
Trichothecin Inhibits Cancer-Related Features in Colorectal Cancer Development by Targeting STAT3
Xin Qi, Meng Li, Xiaomin Zhang, Xiu-fen Dai, Jian Tao Cui, Dehai Li, Qianqun Gu, Zhihua Lv, Jing Li · 2020 · Molecules
Could Signal Transducer and Activator of Transcription 3 be a Therapeutic Target in Obesity-Related Gastrointestinal Malignancy?
Katie E. O’Sullivan, John Vincent Reynolds, Ciara O’Hanlon Brown, Jacintha N O'Sullivan, Joanne Lysaght · 2013 · Journal of Gastrointestinal Cancer
Targeted therapy of obesity-associated colon cancer
Jiezhong Chen · 2012 · Translational gastrointestinal cancer
S3I-201 derivative incorporating naphthoquinone unit as effective STAT3 inhibitors: Design, synthesis and anti-gastric cancer evaluation
Haobin Li, Maohua Cai, Fei Cao, Dehua Yu, Jing Yang, Wen-Kai Yu, Chu Chu, Xiaoqing Guan, Jiang‐Jiang Qin, Jinyun Dong · 2022 · Bioorganic & Medicinal Chemistry
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Miriam Avadisian, Steven Fletcher, Baoxu Liu, Wei Ming Zhao, Peibin Yue, Daniel S. Badali, Wei Xu, Aaron David Schimmer, James Turkson, Claudiu C. Gradinaru et al. · 2011 · Angewandte Chemie International Edition
Design, synthesis and evaluation of XZH-5 analogues as STAT3 inhibitors
Philias Daka, Aiguo Liu, Chamini V. Karunaratne, Erika E. Csatary, Cameron Williams, Hui Xiao, Jiayuh Lin, Zhenghu Xu, Richard C. Page, Hong Wang · 2015 · Bioorganic & Medicinal Chemistry
Antagonism of STAT3 signalling by Ebola virus
Angela R. Harrison, Shawn Todd, Megan Dearnley, Cassandra T. David, Diane Green, Stephen M. Rawlinson, Gough G. Au, Glenn A. Marsh, Gregory W. Moseley · 2021 · PLoS Pathogens
Expression and prognostic value of HER-2/neu, STAT3 and SOCS3 in hepatocellular carcinoma
Li-Hua Jiang, Ying-Li Hao, Jingwei Zhu · 2018 · Clinics and Research in Hepatology and Gastroenterology
The Jak-STAT Signal Transduction Pathway in Melanoma
Courtney Nicholas, Gregory B. · 2011 · InTech eBooks
Dual-inhibitors of STAT5 and STAT3: studies from molecular docking and molecular dynamics simulations
Shengjuan Shao, Rilei Yu, Yanqing Yu, Yanni Li · 2014 · Journal of Molecular Modeling
Pharmacological targeting of the JAK–STAT pathway: new concepts and emerging indications
T. Haikarainen, Anniina T. Virtanen, Benjamin F. Cravatt, Olli Silvennoinen · 2026 · Nature Reviews Drug Discovery
A potent and selective inhibitor for the UBLCP1 proteasome phosphatase
Yantao He, Xing Guo, Zhi-Hong Yu, Li Wu, Andrea Michelle Gunawan, Yan Zhang, Jack E. Dixon, Zhong‐Yin Zhang · 2015 · Bioorganic & Medicinal Chemistry
The role and mechanism of JAK2/STAT3 signaling pathway regulated by m6A methyltransferase KIAA1429 in osteosarcoma
Jiaquan Luo, Xuhua Wang, Zhaoyuan Chen, Huaqiang Zhou, Yihui Xiao · 2023 · Journal of bone oncology
Uncovering influence links in molecular knowledge networks to streamline personalized medicine
Dmitriy Shin, Gerald Arthur, Mihail Popescu, Dmitry Korkin, Chi‐Ren Shyu · 2014 · Journal of Biomedical Informatics
Stattic sensitizes osteosarcoma cells to epidermal growth factor receptor inhibitors via blocking the interleukin 6-induced STAT3 pathway
Shenglin Wang, Yunqing Wang, Zhen Huang, Hongxiang Wei, Xinwen Wang, Rongkai Shen, Wenbin Lan, Guang‐Xian Zhong, Jianhua Lin · 2021 · Acta Biochimica et Biophysica Sinica
Emerging role of signal transducer and activator of transcription 3 (STAT3) in pituitary adenomas
Cyndy Liu, Tae Nakano-Tateno, Motoyasu Satou, Constance L. Chik, Toru Tateno · 2021 · Endocrine Journal
BP‑1‑102 exerts an antitumor effect on the AGS human gastric cancer cell line through modulating the STAT3 and MAPK signaling pathways
Xiaoxia Jiang, Jian Hua Tang, Mengjie Wu, Shitu Chen, Zhenzhen Xu, Haiyong Wang, Haohao Wang, Xiongfei Yu, Zhongqi Li, Lisong Teng · 2019 · Molecular Medicine Reports
The Tetramethylpyrazine Derivative Statmp-151: A Novel Small Molecule Stat3 Inhibitor With Promising Activity Against Breast Cancer
Fan Chen, Yijie Wang, Hui Huang, Wenzhen Li, Jialin Ma, Dongping Yao, Zi-Jun Tang, Taixiong Xue, Liyang Ha, Yan Ren et al. · 2021 · Frontiers in Pharmacology
STAT3 and Importins Are Novel Mediators of Early Molecular and Cellular Responses in Experimental Duodenal Ulceration
Tetyana Khomenko, Xiaoming Deng, Amrita Ahluwalia, Andrzej S. Tarnawski, Khushin N. Patel, Zsuzsanna Sandor, Sándor Szabó · 2014 · Digestive Diseases and Sciences
Discovery of Novel Polycyclic Polyprenylated Acylphloroglucinols from the Fruits of Garcinia xanthochymus as Antitumor Agents by Suppressing the STAT3 Signaling
Shan Jin, Wen Wang, Fei Gan, Wenli Xie, Jing Xu, Yu Chen, Zhinan Mei, Guangzhong Yang · 2021 · International Journal of Molecular Sciences
N-Acetyl cysteine prevents activities of STAT3 inhibitors, Stattic and BP-1-102 independently of its antioxidant properties
Yuki Uchihara, Tomoyuki Ohe, Tadahiko Mashino, Takayuki Kidokoro, Kenji Tago, Hiroomi Tamura, Megumi Funakoshi‐Tago · 2019 · Pharmacological Reports
An Isoxazoloquinone Derivative Inhibits Tumor Growth by Targeting STAT3 and Triggering Its Ubiquitin-Dependent Degradation
Yuanzhu Xie, Shuaiwen Zhu, Ling Chen, Hongdou Liu, Ting Peng, Zhengnan Ming, Zizheng Zou, Xiyuan Hu, Wensong Luo, Kunjian Peng et al. · 2023 · Cancers
Prognostic value of survivin expression in parotid gland cancer in consideration of different histological subtypes
Markus Stenner, Ariane Demgensky, Christoph Molls, Aline Hardt, Jan-Christoffer Lüers, Maria Grosheva, Christian Ulrich Huebbers, Jens Peter Klußmann · 2011 · European Journal of Cancer
4-Carbonyl-2,6-dibenzylidenecyclohexanone derivatives as small molecule inhibitors of STAT3 signaling pathway
Peng Ji, Congmin Yuan, Shuhua Ma, Junchao Fan, Wei Fu, Chunhua Qiao · 2016 · Bioorganic & Medicinal Chemistry
Targeting STAT3 Enzyme for Cancer Treatment
Sowmiya Arun, Praveen Kumar Patel, Kaviarasan Lakshmanan, Kalirajan Rajangopal, Gomathi Swaminathan, Gowramma Byran · 2024 · Mini-Reviews in Medicinal Chemistry
A 2-Benzylmalonate Derivative as STAT3 Inhibitor Suppresses Tumor Growth in Hepatocellular Carcinoma by Upregulating β-TrCP E3 Ubiquitin Ligase
Ting Peng, Orawan Wonganan, Zhonghui Zhang, Jialing Yu, Ruiying Xi, Yu Cao, Apichart Suksamrarn, Guolin Zhang, Fei Wang · 2021 · International Journal of Molecular Sciences
STAT Activation in Malignancies: Roles in Tumor Progression and in the Generation of Antineoplastic Effects of IFNs
Ben X. Wang, Leonidas C. Platanias, Eleanor N. Fish · 2013 · Journal of Interferon & Cytokine Research
Discovery of Novel STAT3 DNA Binding Domain Inhibitors
Bocheng Wu, Benny Payero, Sydney Taylor, Adegboyega K. Oyelere · 2021 · Future Medicinal Chemistry
Current and Future Intratumoral Targeted Treatment for Pancreatic Cancer
Paul Zarogoulidis, Paschalis Pavlioglou, Patrick J. M. Le Pivert, Nikolaos Machairiotis, Nikolaos Katsikogiannis, Ioanna Kougioumtzi, Konstantinos E. Tsimogiannis, Stylianos Kakolyris, Nikolaos A. Courcoutsakis, Theodora Tsiouda et al. · 2014 · Therapeutic Delivery
Targeting the Tumor Microenvironment by Immunotherapy: Part 2
Judith Leibovici, Orit Itzhaki, Monica Huszar, Judith Sinai · 2011 · Immunotherapy
Prevention of Tobacco Carcinogen-Induced Lung Tumor Development by a Novel STAT3 Decoy Inhibitor
Christian Njatcha, Mariya Farooqui, Abdulaziz A. Almotlak, Jill M. Siegfried · 2020 · Cancer Prevention Research
CAVS—Novel in silico selection strategy of specific STAT inhibitory compounds
Anna Czerwoniec, Małgorzata Szeląg, Kajetan Juszczak, Joanna Wesoły, Hans A.R. Bluyssen · 2015 · Journal of Computational Science
Total Saponins of Rubus Parvifolius L. Exhibited Anti-Leukemia Effect in vivo through STAT3 and eIF4E Signaling Pathways
Xiaofeng Xu, Rubin Cheng, Xuejin Zhang, Rui-lan Gao · 2018 · Chinese Journal of Integrative Medicine
Design, synthesis, and in vitro evaluation of BP-1-102 analogs with modified hydrophobic fragments for STAT3 inhibition
Patrik Olekšák, Miroslav Psotka, Markéta Vančurová, Olena Sapega, Jana Bieblová, Milan Reiniš, David Rysanek, Romana Mikyšková, Katarina Chalupova, David Maliňák et al. · 2021 · Journal of Enzyme Inhibition and Medicinal Chemistry
Novel carbazole attenuates vascular remodeling through STAT3/CIAPIN1 signaling in vascular smooth muscle cells
Joo‐Hui Han, Jong Beom Heo, Hyung-Won Lee, Min‐Ho Park, Jangmi Choi, Eun Joo Yun, Seongpyo Lee, Gyu‐Yong Song, Chang‐Seon Myung · 2025 · Acta Pharmaceutica Sinica B
Identification of STAT3 phosphorylation inhibitors using generative deep learning, virtual screening, molecular dynamics simulations, and biological evaluation for non-small cell lung cancer therapy
Weiji Cai, Beier Jiang, Yichen Yin, Lei Ma, Tao Li, Jing Chen · 2024 · Molecular Diversity
BP‑1‑102 exerts antitumor effects on T‑cell acute lymphoblastic leukemia cells by suppressing the JAK2/STAT3/c‑Myc signaling pathway
Can Ye, Xueqin Ruan, Yan Gang Zhao, Hongkai Zhu, Canfei Wang, Zhao Cheng, Hongling Peng · 2023 · Experimental and Therapeutic Medicine
Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3
Yue Chen, Ning Zhai, Yinsong Zhu, Peibin Yue, Nagendra Verma, Christine Brotherton‐Pleiss, Wenzhen Fu, Kayo Nakamura, Weiliang Chen, Joel K. Kawakami et al. · 2023 · Bioorganic & Medicinal Chemistry Letters
Electrochemical detection of the Fc-STAT3 phosphorylation and STAT3–Fc-STAT3 dimerization and inhibition
Sanela Martić, Meghan K. Rains, Sina Haftchenary, Vijay M. Shahani, Dziyana Kraskouskaya, Daniel P. Ball, Patrick Thomas Gunning, Heinz‐Bernhard Kraatz · 2013 · Molecular BioSystems
Effect of STAT3 inhibitor in chronic myeloid leukemia associated signaling pathway: a mathematical modeling, simulation and systems biology study
Himansu Kumar, Swapnil Tichkule, Utkarsh Raj, Saurabh Kumar Gupta, Swati Srivastava, Pritish Kumar Varadwaj · 2016 · 3 Biotech
Evaluation of the STAT3 inhibitor GLG‑302 for the prevention of estrogen receptor‑positive and ‑negative mammary cancers
Robert H. Shoemaker, Jennifer T. Fox, M. Margaret Juliana, Fariba L. Moeinpour, Clinton J. Grubbs · 2019 · Oncology Reports
The Emerging Role of Janus Kinase Inhibitors in the Treatment of Cancer
Dipanjan Karati, Kakasaheb Ramoo Mahadik, Piyush Trivedi, Dileep Kumar · 2022 · Current Cancer Drug Targets
Expression and Production of SH2 Domain Proteins
Bernard A. Liu, Mari Ogiue-Ikeda, Kazuya Machida · 2017 · Methods in molecular biology
Discovering novel derivatives of STAT3 and HDAC inhibitors with anti‐tumor activity
Yuchao Yang, Yamin Pu, Xiaoli Huang, Mengya Liao, Yiwen Zhang · 2024 · Chemical Biology & Drug Design
Bruceantinol targeting STAT3 exerts promising antitumor effects in in vitro and in vivo osteosarcoma models
Jinglei Miao, Shijie Chen, Hongqing Cao, Zhiyu Ding, Yuezhan Li, Weiguo Wang, Keshav Nundlall, Youwen Deng, Jinsong Li · 2024 · Molecular Carcinogenesis
Analysis of key genes and related transcription factors in liver fibrosis based on bioinformatic technology.
Xue Yong Yang, Qi-Ni Cheng, Jiangfeng Wu, Wen‐Bing Ai, Lan Ma · 2021 · PubMed Central
Small Molecule Induces Time‐Dependent Inhibition of Stat3 Dimerization and DNA‐Binding Activity and Regresses Human Breast Tumor Xenografts
Peibin Yue, Yue Chen, Monday Ogaba Ogese, Shan Sun, Xiaolei Zhang, Taiwo Esan, John K. Buolamwini, James Turkson · 2024 · ChemBioChem
Docosahexaenoic Acid Inhibits Cell Proliferation through a Suppression of c-Myc Protein in Pancreatic Ductal Adenocarcinoma Cells
Jia‐Ning Syu, Der‐Yen Lee, Hung‐Chang Hung, Chia-Ying Li, Hung‐Yu Lin, En‐Pei Isabel Chiang, Yiheng Chen, Shu‐Ming Huang, Feng‐Yao Tang · 2021 · Antioxidants
Artificially Induced Protein–Membrane Anchorage with Cholesterol‐Based Recognition Agents as a New Therapeutic Concept
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Historical Development of STAT3 Inhibitors and Early Results in Clinical Trials
Chao‐Lan Yu, Richard Jove, James Turkson · 2016 · Cancer drug discovery and develogment/Cancer drug discovery and development
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Wenda Zhang, Wenying Yu, Guiping Cai, Jiawen Zhu, Chao Zhang, Shanshan Li, Jianpeng Guo, Guo-Ping Yin, Chen Chen, Lingyi Kong · 2021 · Cell Death and Disease · Retracted
Computational Identification of FDA‐Approved Drugs as STAT3 Dimerization Inhibitors for Therapeutic Applications
Muhammad Yasir, Jinyoung Park, Jongseon Choe, Wanjoo Chun · 2026 · ChemistrySelect
STAT3 as a Major Contributor to Chemoresistance
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Targeting Signal Transducer and Activator of Transcripion (STAT) 3 with Small Molecules
Andrew E. Shouksmith, Patrick Thomas Gunning · 2018 · Royal Society of Chemistry eBooks
WITHDRAWN: Intrinsic molecular characteristics of inhibiting STAT3 activation and dimerization through targeting the phosphotyrosine binding site within the SH2 domain—A molecular dynamics study
Yubo Fan, Ren Kong, David John Tweardy, Stephen T. C. Wong · 2013 · Journal of Structural Biology
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Andrew M. Lewis, Daniel P. Ball, Rahul Rana, Ji Sung Park, David A. Rosa, Ping‐Shan Lai, Rodolfo F. Gómez‐Biagi, Patrick Thomas Gunning · 2015
Small Molecule Inhibitors of Stat3 Protein as Cancer Therapeutic Agents
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Study Of The Egfr, Src And Stat3 Pathway In Pancreatic Cancer
Soumya Jaganathan · 2010 · Journal of International Crisis and Risk Communication Research
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BindingDB Entry 50040568: Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
BindingDB · 2013 · UC San Diego
BindingDB Entry 50018256: Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation.
BindingDB · 2024 · UC San Diego
BindingDB Entry 50043420: Inhibiting aberrant signal transducer and activator of transcription protein activation with tetrapodal, small molecule Src homology 2 domain binders: promising agents against multiple myeloma.
BindingDB · 2014 · UC San Diego
BindingDB Entry 50021926: Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3.
BindingDB · 2025 · UC San Diego
BindingDB Entry 50046705: Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importina-2 Expression, and Induce Antitumor Effects against Human Glioma.
BindingDB · 2016 · UC San Diego
BindingDB Entry 50002965: Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors.
BindingDB · 2020 · UC San Diego
BindingDB Entry 50018446: 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?
BindingDB · 2024 · UC San Diego
BindingDB Entry 50033063: Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
BindingDB · 2011 · UC San Diego
BindingDB Entry 50049215: Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking.
BindingDB · 2019 · UC San Diego
BindingDB Entry 50039697: Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity.
BindingDB · 2013 · UC San Diego
BindingDB Entry 50008569: 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.
BindingDB · 2021 · UC San Diego
BindingDB Entry 50012355: Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors.
BindingDB · 2022 · UC San Diego
BindingDB Entry 50013362: Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy.
BindingDB · 2022 · UC San Diego
BindingDB Entry 50039359: Identification of Purine-Scaffold Small-Molecule Inhibitors of Stat3 Activation by QSAR Studies.
BindingDB · 2013 · UC San Diego
BindingDB Entry 50032974: Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
BindingDB · 2011 · UC San Diego
BindingDB Entry 50048013: 4-Carbonyl-2,6-dibenzylidenecyclohexanone derivatives as small molecule inhibitors of STAT3 signaling pathway.
BindingDB · 2018 · UC San Diego
BindingDB Entry 50019392: Research progress of STAT3-based dual inhibitors for cancer therapy.
BindingDB · 2024 · UC San Diego
BindingDB Entry 50015942: S3I-201 derivative incorporating naphthoquinone unit as effective STAT3 inhibitors: Design, synthesis and anti-gastric cancer evaluation.
BindingDB · 2023 · UC San Diego
BindingDB Entry 50046709: Novel aminotetrazole derivatives as selective STAT3 non-peptide inhibitors.
BindingDB · 2016 · UC San Diego
BindingDB Entry 50045874: A potent and selective inhibitor for the UBLCP1 proteasome phosphatase.
BindingDB · 2016 · UC San Diego
BindingDB Entry 50033894: Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain.
BindingDB · 2012 · UC San Diego
BindingDB Entry 50043264: Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
BindingDB · 2014 · UC San Diego
PTPRT/D MUTATION OR PROMOTER METHYLATION: IMPLICATIONS FOR STAT3 INHIBITION
Noah D. Peyser · 2015 · D-Scholarship@Pitt (University of Pittsburgh)
Uncovering morphoproteomic relationships using probabilistic graphical models and resource description framework knowledgebases
Dmitriy Shin · 2012