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A STAT inhibitor patent review: progress since 2011

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Haseeb Nisar, Bilal Wajid, Faria Anwar, Ashfaq Ahmad, Anum Javaid, Syed Awais Attique, Wardah Nisar, Amir Saeed, Samiah Shahid & Saima Sadaf. (2023) Bioinformatics and systems biology analysis revealed PMID26394986-Compound-10 as potential repurposable drug against covid-19. Journal of Biomolecular Structure and Dynamics 0:0, pages 1-14.
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Feng Wang, Xin-Yu Cao, Guo-Qiang Lin, Ping Tian & Dingding Gao. (2022) Novel inhibitors of the STAT3 signaling pathway: an updated patent review (2014-present). Expert Opinion on Therapeutic Patents 32:6, pages 667-688.
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Elena Gabriele, Dario Brambilla, Chiara Ricci, Luca Regazzoni, Kyoko Taguchi, Nicola Ferri, Akira Asai & Anna Sparatore. (2017) New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors. Journal of Enzyme Inhibition and Medicinal Chemistry 32:1, pages 1012-1028.
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Jianping Shao, Qingyan Meng & Yongyuan Li. (2016) Theaflavins suppress tumor growth and metastasis via the blockage of the STAT3 pathway in hepatocellular carcinoma. OncoTargets and Therapy 9, pages 4265-4275.
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Articles from other publishers (40)

Mohammadreza Torabi, Setayesh Yasami-Khiabani, Soroush Sardari, Majid Golkar, Horacio Pérez-Sánchez & Fahimeh Ghasemi. (2023) Identification of new potential candidates to inhibit EGF via machine learning algorithm. European Journal of Pharmacology, pages 176176.
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Najla Altwaijry, Rehab Sabour, Mona H. Ibrahim, Omkulthom Al kamaly, Omeima Abdullah & Marwa F. Harras. (2023) Design, synthesis, and anti-hepatocellular carcinoma of thiopyrimidine/chalcone hybrids as dual STAT3/STAT5 inhibitors. RSC Medicinal Chemistry 14:10, pages 1981-1991.
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Xiaojuan Yang, Lu Xu, Li Yang & Shaohong Xu. (2023) Research progress of STAT3-based dual inhibitors for cancer therapy. Bioorganic & Medicinal Chemistry 91, pages 117382.
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Mitsuaki Yamashita, Yuto Nakamori, Arisa Tsukamoto, Nagisa Furuno & Akira Iida. (2023) Synthesis and structure-activity relationship studies of naphthoquinones as STAT3 inhibitors. Bioorganic & Medicinal Chemistry 90, pages 117331.
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Siddhi Parab & Gaurav Doshi. (2022) An update on emerging immunological targets and their inhibitors in the treatment of psoriasis. International Immunopharmacology 113, pages 109341.
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Libing Hong, Yongqi Lin, Xiongyi Yang, Tong Wu, Yuxi Zhang, Zhuohang Xie, Jieli Yu, Hejia Zhao, Guoguo Yi & Min Fu. (2022) A Narrative Review of STAT Proteins in Diabetic Retinopathy: From Mechanisms to Therapeutic Prospects. Ophthalmology and Therapy 11:6, pages 2005-2026.
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Haobin Li, Lingling Wang, Fei Cao, Dehua Yu, Jing Yang, Xuefei Yu, Jinyun Dong, Jiang-Jiang Qin & Xiaoqing Guan. (2022) Design, synthesis, and biological characterization of a potent STAT3 degrader for the treatment of gastric cancer. Frontiers in Pharmacology 13.
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Kenichi Kobayashi, Hiroshi Kogen & Osamu Tamura. (2022) Total Synthesis of Phaeosphaerides with STAT3 Inhibitory ActivitySTAT3阻害活性を有するPhaeosphaeride類の全合成. Journal of Synthetic Organic Chemistry, Japan 80:8, pages 755-765.
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Yinan Wang, Chuanhe Yang, Michelle M. Sims, Joshua R. Sacher, Mithun Raje, Hemantkumar Deokar, Peibin Yue, James Turkson, John K. Buolamwini & Lawrence M. Pfeffer. (2022) SS-4 is a highly selective small molecule inhibitor of STAT3 tyrosine phosphorylation that potently inhibits GBM tumorigenesis in vitro and in vivo. Cancer Letters 533, pages 215614.
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Bilal Rah, Rafiq A Rather, Gh Rasool Bhat, Abdul Basit Baba, Ifra Mushtaq, Muzamil Farooq, Tahira Yousuf, Sadaf B Dar, Sabra Parveen, Rukhsana Hassan, Fozia Mohammad, Iqbal Qassim, Abida Bhat, Shazia Ali, Mahrukh Hamid Zargar & Dil Afroze. (2022) JAK/STAT Signaling: Molecular Targets, Therapeutic Opportunities, and Limitations of Targeted Inhibitions in Solid Malignancies. Frontiers in Pharmacology 13.
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Zhihai Ke & Ying-Yeung Yeung. 2022. Comprehensive Heterocyclic Chemistry IV. Comprehensive Heterocyclic Chemistry IV 412 449 .
Jinyun Dong, Xiang-Dong Cheng, Wei-Dong Zhang & Jiang-Jiang Qin. (2021) Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation. Journal of Medicinal Chemistry 64:13, pages 8884-8915.
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Hongkui Yang & Wenjun Xu. (2021) STAT3 promotes peritoneal metastasis of gastric cancer by enhancing mesothelial-mesenchymal transition. Biological Chemistry 402:6, pages 739-748.
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Sun Young Moon, Kwang Dong Kim, Jiyun Yoo, Jeong-Hyung Lee & Cheol Hwangbo. (2021) Phytochemicals Targeting JAK–STAT Pathways in Inflammatory Bowel Disease: Insights from Animal Models. Molecules 26:9, pages 2824.
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Hui Xu, Lei Liu, Weilin Li, Duowu Zou, Jun Yu, Lifu Wang & Chi Chun Wong. (2020) Transcription factors in colorectal cancer: molecular mechanism and therapeutic implications. Oncogene 40:9, pages 1555-1569.
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Huang Chen, Aiwu Bian, Lian-fang Yang, Xuan Yin, Jie Wang, Chaowen Ti, Ying Miao, Shihong Peng, Shifen Xu, Mingyao Liu, Wen-Wei Qiu & Zhengfang Yi. (2021) Targeting STAT3 by a small molecule suppresses pancreatic cancer progression. Oncogene 40:8, pages 1440-1457.
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Lara Brambilla, Tanaya Lahiri, Michael Cammer & David E. Levy. (2020) STAT3 Inhibitor OPB-51602 Is Cytotoxic to Tumor Cells Through Inhibition of Complex I and ROS Induction. iScience 23:12, pages 101822.
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Samar Imbaby, Naoyuki Matsuda, Kengo Tomita, Kohshi Hattori, Sailesh Palikhe, Hiroki Yokoo & Yuichi Hattori. (2020) Beneficial effect of STAT3 decoy oligodeoxynucleotide transfection on organ injury and mortality in mice with cecal ligation and puncture-induced sepsis. Scientific Reports 10:1.
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Sander Busker, Brent Page & Elias S.J. Arnér. (2020) To inhibit TrxR1 is to inactivate STAT3–Inhibition of TrxR1 enzymatic function by STAT3 small molecule inhibitors. Redox Biology 36, pages 101646.
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Sanaz Attarha, Anja Reithmeier, Sander Busker, Matthieu Desroses & Brent D. G. Page. (2020) Validating Signal Transducer and Activator of Transcription (STAT) Protein–Inhibitor Interactions Using Biochemical and Cellular Thermal Shift Assays. ACS Chemical Biology 15:7, pages 1842-1851.
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S. Busker, W. QianM. HaraldssonB. EspinosaL. JohanssonS. Attarha, I. KolosenkoJ. LiuM. Dagnell, D. GrandérE. S. J. Arnér, K. Pokrovskaja Tamm & B. D. G. Page. (2020) Irreversible TrxR1 inhibitors block STAT3 activity and induce cancer cell death. Science Advances 6:12.
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Young‑Lan Park, Seung‑Hun Kim, Sun‑Young Park, Min‑Woo Jung, Sang‑Yoon Ha, Jung‑Ho Choi, Dae‑Seong Myung, Sung‑Bum Cho, Wan‑Sik Lee, Hyun‑Soo Kim & Young‑Eun Joo. (2019) Forkhead‑box�A1 regulates tumor cell growth and predicts prognosis in colorectal cancer. International Journal of Oncology.
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Natalija Simonović, Agnieszka Witalisz-Siepracka, Katrin Meissl, Caroline Lassnig, Ursula Reichart, Thomas Kolbe, Matthias Farlik, Christoph Bock, Veronika Sexl, Mathias Müller & Birgit Strobl. (2019) NK Cells Require Cell-Extrinsic and -Intrinsic TYK2 for Full Functionality in Tumor Surveillance and Antibacterial Immunity. The Journal of Immunology 202:6, pages 1724-1734.
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Xiaoxia Jiang, Jian Tang, Mengjie Wu, Shitu Chen, Zhenzhen Xu, Haiyong Wang, Haohao Wang, Xiongfei Yu, Zhongqi Li & Lisong Teng. (2019) BP‑1‑102 exerts an antitumor effect on the AGS human gastric cancer cell line through modulating the STAT3 and MAPK signaling pathways. Molecular Medicine Reports.
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Matthieu Desroses, Sander Busker, Juan Astorga-Wells, Sanaz Attarha, Iryna Kolosenko, Roman A. Zubarev, Thomas Helleday, Dan Grandér & Brent D.G. Page. (2018) STAT3 differential scanning fluorimetry and differential scanning light scattering assays: Addressing a missing link in the characterization of STAT3 inhibitor interactions. Journal of Pharmaceutical and Biomedical Analysis 160, pages 80-88.
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Guoqing Duan, Shiqiang Song & Shuaishuai Niu. (2018) Long non-coding RNA HOTAIR promotes LPS-induced inflammatory injury by down-regulation of microRNA-124 in murine chondrogenic ATDC5 cells. Life Sciences.
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Sara Verdura, Elisabet Cuyàs, Laura Llorach-Parés, Almudena Pérez-Sánchez, Vicente Micol, Alfons Nonell-Canals, Jorge Joven, Manuel Valiente, Melchor Sánchez-Martínez, Joaquim Bosch-Barrera & Javier A. Menendez. (2018) Silibinin is a direct inhibitor of STAT3. Food and Chemical Toxicology 116, pages 161-172.
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Jacopo Sgrignani, Maura Garofalo, Milos Matkovic, Jessica Merulla, Carlo V. Catapano & Andrea Cavalli. (2018) Structural Biology of STAT3 and Its Implications for Anticancer Therapies Development. International Journal of Molecular Sciences 19:6, pages 1591.
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William Vainchenker, Emilie Leroy, Laure Gilles, Caroline Marty, Isabelle Plo & Stefan N. Constantinescu. (2018) JAK inhibitors for the treatment of myeloproliferative neoplasms and other disorders. F1000Research 7, pages 82.
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Han-Yue Qiu, Jiang-Yan Fu, Min-Kai Yang, Hong-Wei Han, Peng-Fei Wang, Ya-Han Zhang, Hong-Yan Lin, Cheng-Yi Tang, Jin-Liang Qi, Rong-Wu Yang, Xiao-Ming Wang, Hai-Liang Zhu & Yong-Hua Yang. (2017) Identification of new shikonin derivatives as STAT3 inhibitors. Biochemical Pharmacology 146, pages 74-86.
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Elvin D. de Araujo, Pimyupa Manaswiyoungkul, Johan Israelian, Jisung Park, Karen Yuen, Shiva Farhangi, Angelika Berger-Becvar, Lubna Abu-Jazar & Patrick T. Gunning. (2017) High-throughput thermofluor-based assays for inhibitor screening of STAT SH2 domains. Journal of Pharmaceutical and Biomedical Analysis 143, pages 159-167.
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Jonathan Metts, Heath L. Bradley, Zhengqi Wang, Neil P. Shah, Reuben Kapur, Jack L. Arbiser & Kevin D. Bunting. (2017) Imipramine blue sensitively and selectively targets FLT3-ITD positive acute myeloid leukemia cells. Scientific Reports 7:1.
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Iryna Kolosenko, Yasmin Yu, Sander Busker, Matheus Dyczynski, Jianping Liu, Martin Haraldsson, Caroline Palm Apergi, Thomas Helleday, Katja Pokrovskaja Tamm, Brent D. G. Page & Dan Grander. (2017) Identification of novel small molecules that inhibit STAT3-dependent transcription and function. PLOS ONE 12:6, pages e0178844.
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Han-Yue Qiu, Xiang Zhu, Yue-Lin Luo, Hong-Yan Lin, Cheng-Yi Tang, Jin-Liang Qi, Yan-Jun Pang, Rong-Wu Yang, Gui-Hua Lu, Xiao-Ming Wang & Yong-Hua Yang. (2017) Identification of New Shikonin Derivatives as Antitumor Agents Targeting STAT3 SH2 Domain. Scientific Reports 7:1.
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Shubhasree Banerjee, Ann Biehl, Massimo Gadina, Sarfaraz Hasni & Daniella M. Schwartz. (2017) JAK–STAT Signaling as a Target for Inflammatory and Autoimmune Diseases: Current and Future Prospects. Drugs 77:5, pages 521-546.
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Mariah G. Alorro, Thomas P. Pierce, Moritz F. Eissmann, Christine Dijkstra, Ross A. Dickins, Matthias Ernst, Michael Buchert & Frederic Masson. (2017) Generation of an inducible mouse model to reversibly silence Stat3. genesis 55:4, pages e23023.
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Meihua Liang, Fei Zhan, Juan Zhao, Qi Li, Jiazi Wuyang, Guannan Mu, Dianjun Li, Yanqiao Zhang & Xiaoyi Huang. (2016) CPA-7 influences immune profile and elicits anti-prostate cancer effects by inhibiting activated STAT3. BMC Cancer 16:1.
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Li-Juan Liu, Wanhe Wang, Tian-Shu Kang, Jia-Xin Liang, Chenfu Liu, Daniel W. J. Kwong, Vincent Kam Wai Wong, Dik-Lung Ma & Chung-Hang Leung. (2016) Antagonizing STAT5B dimerization with an osmium complex. Scientific Reports 6:1.
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Jing LiJose Pindado RodriguezFengfeng NiuMengchen PuJinan WangLi-Wei HungQiang ShaoYanping ZhuWei DingYanqing LiuYurong DaZhi YaoJie YangYongfang ZhaoGong-Hong WeiGenhong ChengZhi-Jie Liu & Songying Ouyang. (2016) Structural basis for DNA recognition by STAT6. Proceedings of the National Academy of Sciences 113:46, pages 13015-13020.
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Ahmed M. Ali, Rodolfo F. Gómez-Biagi, David A. Rosa, Ping-Shan Lai, William L. Heaton, Ji Sung Park, Anna M. Eiring, Nadeem A. Vellore, Elvin D. de Araujo, Dan P. Ball, Andrew E. Shouksmith, Ami B. Patel, Michael W. Deininger, Thomas O'Hare & Patrick T. Gunning. (2016) Disarming an Electrophilic Warhead: Retaining Potency in Tyrosine Kinase Inhibitor (TKI)-Resistant CML Lines While Circumventing Pharmacokinetic Liabilities. ChemMedChem 11:8, pages 850-861.
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