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Original Article
Phase I Study of OPB-31121, an Oral STAT3 Inhibitor, in Patients with Advanced Solid Tumors
Do-Youn Oh, Se-Hoon Lee, Sae-Won Han, Mi-Jung Kim, Tae-Min Kim, Tae-You Kim, Dae Seog Heo, Miyuki Yuasa, Yasuo Yanagihara, Yung-Jue Bang
Cancer Res Treat. 2015;47(4):607-615.   Published online February 26, 2015
DOI: https://doi.org/10.4143/crt.2014.249
AbstractAbstract PDFPubReaderePub
Purpose
OPB-31121 is an oral STAT3 inhibitor with a good preclinical antitumor activity. This phase I dose-escalation study of OPB-31121 was conducted to determine maximum-tolerated dose (MTD), safety, pharmacokinetics, and preliminary antitumor efficacy in patients with advanced solid tumors. Materials and Methods Patients received OPB-31121 once daily for 28 days of each cycle followed by 2 weeks rest. A standard 3+3 design was used for dose-escalation. Safety and response were evaluated by the National Cancer Institute–Common Terminology Criteria for Adverse Events (NCICTCAE) ver. 3.0 and Response Evaluation Criteria in Solid Tumor (RECIST) ver. 1.0, respectively.
Results
Twenty-five patients were treated with OPB-31121 at five dose levels: 100 mg (n=4), 200 mg (n=3), 400 mg (n=3), 600 mg (n=7), and 800 mg (n=8). Seven patients discontinued treatment during cycle 1 for various reasons other than study drug-related adverse events. Among 18 patients who were evaluable for dose-limiting toxicity (DLT), three DLTs were observed: one DLT (grade 3 vomiting) at 600 mg and two DLTs (grade 3 vomiting, grade 3 diarrhea) at 800 mg. The MTD was determined as 800 mg/day. Common adverse events were gastrointestinal adverse event including nausea (84%), vomiting (80%), and diarrhea (72%). Pharmacokinetics did not demonstrate dose-proportionality of OPB-31121. Eight patients had stable disease and 10 patients had disease progression. Two patients (1 colon cancer, 1 rectal cancer) showed tumor shrinkage. One gastric cancer patient continued treatment up to cycle 13 before disease progression. Conclusion This study demonstrates feasibility of STAT3 inhibition in patients with advanced solid tumor. OPB-31121, at the MTD of 800 mg/day, was safe and relatively well tolerated, and has a preliminary antitumor activity.

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  • Expression of STAT3, IL27p28 and IL12p35 is deregulated and linked to autoimmune markers in chronic spontaneous urticaria
    Sahar Rastgoo, Mojgan Mohammadi, Marcus Maurer, Mahdi Atabaki, Jalil Tavakkol-Afshari, Maryam Khoshkhui
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  • Insights into IL-6/JAK/STAT3 signaling in the tumor microenvironment: Implications for cancer therapy
    Win Lwin Thuya, Yang Cao, Paul Chi-Lui Ho, Andrea Li-Ann Wong, Lingzhi Wang, Jianbiao Zhou, Christophe Nicot, Boon Cher Goh
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  • CTSL Promotes Autophagy in Laryngeal Cancer Through the IL6‐JAK‐STAT3 Signalling Pathway
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  • Hepatocellular carcinoma: signaling pathways and therapeutic advances
    Jiaojiao Zheng, Siying Wang, Lei Xia, Zhen Sun, Kui Ming Chan, René Bernards, Wenxin Qin, Jinhong Chen, Qiang Xia, Haojie Jin
    Signal Transduction and Targeted Therapy.2025;[Epub]     CrossRef
  • STAT3 Inhibition Prevents Adaptive Resistance and Augments NK Cell Cytotoxicity to KRASG12C Inhibitors in Nonsmall Cell Lung Cancer
    Zehao Pan, Yuxian Qian, Yajing Wang, Te Zhang, Xuming Song, Hanling Ding, Rutao Li, Yijian Zhang, Zi Wang, Hui Wang, Wenjie Xia, Lei Wei, Lin Xu, Gaochao Dong, Feng Jiang
    Cancer Science.2025;[Epub]     CrossRef
  • STAT signaling in the pathogenesis and therapy of acute myeloid leukemia and myelodysplastic syndromes
    Zoe King, Sudhamsh Reddy Desai, David A. Frank, Aditi Shastri
    Neoplasia.2025; 61: 101137.     CrossRef
  • Unraveling the complexity of STAT3 in cancer: molecular understanding and drug discovery
    Yamei Hu, Zigang Dong, Kangdong Liu
    Journal of Experimental & Clinical Cancer Research.2024;[Epub]     CrossRef
  • Hepatocellular Carcinoma: Old and Emerging Therapeutic Targets
    Greta Pessino, Claudia Scotti, Maristella Maggi
    Cancers.2024; 16(5): 901.     CrossRef
  • Impact of STAT-signaling pathway on cancer-associated fibroblasts in colorectal cancer and its role in immunosuppression
    Damián Sánchez-Ramírez, Mónica G Mendoza-Rodríguez, Omar R Alemán, Fernando A Candanedo-González, Miriam Rodríguez-Sosa, Juan José Montesinos-Montesinos, Mauricio Salcedo, Ismael Brito-Toledo, Felipe Vaca-Paniagua, Luis I Terrazas
    World Journal of Gastrointestinal Oncology.2024; 16(5): 1705.     CrossRef
  • Targeted Treatment against Cancer Stem Cells in Colorectal Cancer
    Julia Martínez-Pérez, Carlos Torrado, María A. Domínguez-Cejudo, Manuel Valladares-Ayerbes
    International Journal of Molecular Sciences.2024; 25(11): 6220.     CrossRef
  • Interleukin-6 serves as a critical factor in various cancer progression and therapy
    Asma’a H. Mohamed, Abdulrahman T. Ahmed, Waleed Al Abdulmonem, Dmitry Olegovich Bokov, Alaa Shafie, Hussein Riyadh Abdul Kareem Al-Hetty, Chou-Yi Hsu, Mohammed Alissa, Shahid Nazir, Mohammad Chand Jamali, Mustafa Mudhafar
    Medical Oncology.2024;[Epub]     CrossRef
  • Targeting cytokine and chemokine signaling pathways for cancer therapy
    Ming Yi, Tianye Li, Mengke Niu, Haoxiang Zhang, Yuze Wu, Kongming Wu, Zhijun Dai
    Signal Transduction and Targeted Therapy.2024;[Epub]     CrossRef
  • Recent advances in targeted drug delivery systems for multiple myeloma
    Ashruti Pant, Aayushi Laliwala, Sarah A. Holstein, Aaron M. Mohs
    Journal of Controlled Release.2024; 376: 215.     CrossRef
  • A strategic review of STAT3 signaling inhibition by phytochemicals for cancer prevention and treatment: Advances and insights
    Suryaa Manoharan, Ekambaram Perumal
    Fitoterapia.2024; 179: 106265.     CrossRef
  • The STAT family: Key transcription factors mediating crosstalk between cancer stem cells and tumor immune microenvironment
    Mengxuan Zhu, Suyao Li, Xin Cao, Khalid Rashid, Tianshu Liu
    Seminars in Cancer Biology.2023; 88: 18.     CrossRef
  • Dual inhibition of MYC and SLC39A10 by a novel natural product STAT3 inhibitor derived from Chaetomium globosum suppresses tumor growth and metastasis in gastric cancer
    Xiaoqing Guan, Jing Yang, Weiyi Wang, Bing Zhao, Shiyu Hu, Dehua Yu, Li Yuan, Yunfu Shi, Jingli Xu, Jinyun Dong, Jinxin Wang, Xiang-Dong Cheng, Jiang-Jiang Qin
    Pharmacological Research.2023; 189: 106703.     CrossRef
  • JAK/STAT pathway: Extracellular signals, diseases, immunity, and therapeutic regimens
    Qian Hu, Qihui Bian, Dingchao Rong, Leiyun Wang, Jianan Song, Hsuan-Shun Huang, Jun Zeng, Jie Mei, Peng-Yuan Wang
    Frontiers in Bioengineering and Biotechnology.2023;[Epub]     CrossRef
  • Brevilin A is a potent anti-metastatic CRC agent that targets the VEGF-IL6-STAT3 axis in the HSCs-CRC interplay
    Xueying Fan, Mingjing Meng, Baoting Li, Hui Chen, Jincheng Tan, Keyang Xu, Shilin Xiao, Hiu-Yee Kwan, Zhongqiu Liu, Tao Su
    Journal of Translational Medicine.2023;[Epub]     CrossRef
  • Application of Nano-Antibodies for Cancer Immunotherapy
    Sunanda Singh, Samara P. Singh, Ashutosh S. Parihar
    Current Tissue Microenvironment Reports.2023; 4(2): 17.     CrossRef
  • Exploring the dynamic interplay between cancer stem cells and the tumor microenvironment: implications for novel therapeutic strategies
    Yan-Ruide Li, Ying Fang, Zibai Lyu, Yichen Zhu, Lili Yang
    Journal of Translational Medicine.2023;[Epub]     CrossRef
  • C188-9, a specific inhibitor of STAT3 signaling, prevents thermal burn-induced skeletal muscle wasting in mice
    Yuko Ono, Masafumi Saito, Kazuho Sakamoto, Yuko Maejima, Shingen Misaka, Kenju Shimomura, Nobuto Nakanishi, Shigeaki Inoue, Joji Kotani
    Frontiers in Pharmacology.2022;[Epub]     CrossRef
  • Signaling Pathways and Targeted Therapies for Stem Cells in Prostate Cancer
    Madhuvanthi Giridharan, Vasu Rupani, Satarupa Banerjee
    ACS Pharmacology & Translational Science.2022; 5(4): 193.     CrossRef
  • Insights into the role of STAT3 in intrahepatic cholangiocarcinoma (Review)
    Ranzhiqiang Yang, Yinghui Song, Kashif Shakoor, Weimin Yi, Chuang Peng, Sulai Liu
    Molecular Medicine Reports.2022;[Epub]     CrossRef
  • Inhibition of STAT3-ferroptosis negative regulatory axis suppresses tumor growth and alleviates chemoresistance in gastric cancer
    Shumin Ouyang, Huaxuan Li, Linlin Lou, Qiuyao Huang, Zhenhua Zhang, Jianshan Mo, Min Li, Jiaye Lu, Kai Zhu, Yunjie Chu, Wen Ding, Jianzheng Zhu, Ziyou Lin, Lin Zhong, Junjian Wang, Peibin Yue, James Turkson, Peiqing Liu, Yuanxiang Wang, Xiaolei Zhang
    Redox Biology.2022; 52: 102317.     CrossRef
  • Digesting the Role of JAK-STAT and Cytokine Signaling in Oral and Gastric Cancers
    Yanhong Ni, Jun T. Low, John Silke, Lorraine A. O’Reilly
    Frontiers in Immunology.2022;[Epub]     CrossRef
  • A Broad-Based Characterization of a Cell-Penetrating, Single Domain Camelid Bi-Specific Antibody Monomer That Targets STAT3 and KRAS Dependent Cancers
    Sunanda Singh, Genoveva Murillo, Justin Richner, Samara P. Singh, Erica Berleth, Vijay Kumar, Rajendra Mehta, Vijay Ramiya, Ashutosh S. Parihar
    International Journal of Molecular Sciences.2022; 23(14): 7565.     CrossRef
  • Molecular mechanisms underlying the action of carcinogens in gastric cancer with a glimpse into targeted therapy
    Elham Patrad, Solmaz Khalighfard, Taghi Amiriani, Vahid Khori, Ali Mohammad Alizadeh
    Cellular Oncology.2022; 45(6): 1073.     CrossRef
  • STAT3 and Its Targeting Inhibitors in Oral Squamous Cell Carcinoma
    Mingjing Jiang, Bo Li
    Cells.2022; 11(19): 3131.     CrossRef
  • The Role of IL-6 in Cancer Cell Invasiveness and Metastasis—Overview and Therapeutic Opportunities
    Magdalena Rašková, Lukáš Lacina, Zdeněk Kejík, Anna Venhauerová, Markéta Skaličková, Michal Kolář, Milan Jakubek, Daniel Rosel, Karel Smetana, Jan Brábek
    Cells.2022; 11(22): 3698.     CrossRef
  • An update on investigational therapies that target STAT3 for the treatment of cancer
    Matteo Santoni, Francesca Miccini, Alessia Cimadamore, Francesco Piva, Francesco Massari, Liang Cheng, Antonio Lopez-Beltran, Rodolfo Montironi, Nicola Battelli
    Expert Opinion on Investigational Drugs.2021; 30(3): 245.     CrossRef
  • RETRACTED: GATA4 Regulates Inflammation-Driven Pancreatic Ductal Adenocarcinoma Progression
    Weiliang Jiang, Congying Chen, Li Huang, Jie Shen, Lijuan Yang
    Frontiers in Cell and Developmental Biology.2021;[Epub]     CrossRef
  • Phytochemicals Targeting JAK–STAT Pathways in Inflammatory Bowel Disease: Insights from Animal Models
    Sun Young Moon, Kwang Dong Kim, Jiyun Yoo, Jeong-Hyung Lee, Cheol Hwangbo
    Molecules.2021; 26(9): 2824.     CrossRef
  • Development and Validation of an IL6/JAK/STAT3-Related Gene Signature to Predict Overall Survival in Clear Cell Renal Cell Carcinoma
    Chuanchuan Zhan, Chao Xu, Jiajun Chen, Chong Shen, Jinkun Li, Zichu Wang, Xiangrong Ying, Zhengang Luo, Yu Ren, Gangfeng Wu, Haojie Zhang, Manfei Qian
    Frontiers in Cell and Developmental Biology.2021;[Epub]     CrossRef
  • Emerging role of signal transducer and activator of transcription 3 (STAT3) in pituitary adenomas
    Cyndy Liu, Tae Nakano-Tateno, Motoyasu Satou, Constance Chik, Toru Tateno
    Endocrine Journal.2021; 68(10): 1143.     CrossRef
  • The JAK/STAT signaling pathway: from bench to clinic
    Xiaoyi Hu, Jing li, Maorong Fu, Xia Zhao, Wei Wang
    Signal Transduction and Targeted Therapy.2021;[Epub]     CrossRef
  • Interleukin-6 and colorectal cancer development
    I.А. Hromakova, P.P. Sorochan, N.E. Prokhach, I.S. Hromakova
    Український радіологічний та онкологічний журнал.2021; 29(4): 89.     CrossRef
  • Ailanthone suppresses the activity of human colorectal cancer cells through the STAT3 signaling pathway
    Haixiang Ding, Xiuchong Yu, Zhilong Yan
    International Journal of Molecular Medicine.2021;[Epub]     CrossRef
  • Radiation induces an inflammatory response that results in STAT3-dependent changes in cellular plasticity and radioresistance of breast cancer stem-like cells
    Kimberly M. Arnold, Lynn M. Opdenaker, Nicole J. Flynn, Daniel Kwesi Appeah, Jennifer Sims-Mourtada
    International Journal of Radiation Biology.2020; 96(4): 434.     CrossRef
  • Quinazoline Ligands Induce Cancer Cell Death through Selective STAT3 Inhibition and G-Quadruplex Stabilization
    Jan Jamroskovic, Mara Doimo, Karam Chand, Ikenna Obi, Rajendra Kumar, Kristoffer Brännström, Mattias Hedenström, Rabindra Nath Das, Almaz Akhunzianov, Marco Deiana, Kazutoshi Kasho, Sebastian Sulis Sato, Parham L. Pourbozorgi, James E. Mason, Paolo Medini
    Journal of the American Chemical Society.2020; 142(6): 2876.     CrossRef
  • Phosphotyrosine isosteres: past, present and future
    Robert A. Cerulli, Joshua A. Kritzer
    Organic & Biomolecular Chemistry.2020; 18(4): 583.     CrossRef
  • Anticancer activity of dietary xanthone α-mangostin against hepatocellular carcinoma by inhibition of STAT3 signaling via stabilization of SHP1
    Hai Zhang, Yu-ping Tan, Lin Zhao, Lun Wang, Nai-jie Fu, Song-ping Zheng, Xiao-fei Shen
    Cell Death & Disease.2020;[Epub]     CrossRef
  • JAK/STAT signaling in hepatocellular carcinoma
    Justin Jit Hin Tang, Dexter Kai Hao Thng, Jhin Jieh Lim, Tan Boon Toh
    Hepatic Oncology.2020;[Epub]     CrossRef
  • JAK–STAT pathway targeting for the treatment of inflammatory bowel disease
    Azucena Salas, Cristian Hernandez-Rocha, Marjolijn Duijvestein, William Faubion, Dermot McGovern, Severine Vermeire, Stefania Vetrano, Niels Vande Casteele
    Nature Reviews Gastroenterology & Hepatology.2020; 17(6): 323.     CrossRef
  • Targeting STAT3 in cancer and autoimmune diseases
    Tohid Gharibi, Zohreh Babaloo, Arezoo Hosseini, Meghdad Abdollahpour-alitappeh, Vida Hashemi, Faroogh Marofi, Kazem Nejati, Behzad Baradaran
    European Journal of Pharmacology.2020; 878: 173107.     CrossRef
  • Betacellulin drives therapy resistance in glioblastoma
    Qiwen Fan, Zhenyi An, Robyn A Wong, Xujun Luo, Edbert D Lu, Albert Baldwin, Manasi K Mayekar, Franziska Haderk, Kevan M Shokat, Trever G Bivona, William A Weiss
    Neuro-Oncology.2020; 22(4): 457.     CrossRef
  • A novel small molecule STAT3 inhibitor SLSI-1216 suppresses proliferation and tumor growth of triple-negative breast cancer cells through apoptotic induction
    Soo Kyung Park, Woong Sub Byun, Seungbeom Lee, Young Taek Han, Yoo-Seong Jeong, Kyungkuk Jang, Suk-Jae Chung, Jeeyeon Lee, Young-Ger Suh, Sang Kook Lee
    Biochemical Pharmacology.2020; 178: 114053.     CrossRef
  • STAT3 Pathway in Gastric Cancer: Signaling, Therapeutic Targeting and Future Prospects
    Milad Ashrafizadeh, Ali Zarrabi, Sima Orouei, Vahideh Zarrin, Ebrahim Rahmani Moghadam, Amirhossein Zabolian, Shima Mohammadi, Kiavash Hushmandi, Yashar Gharehaghajlou, Pooyan Makvandi, Masoud Najafi, Reza Mohammadinejad
    Biology.2020; 9(6): 126.     CrossRef
  • Towards the Inhibition of Protein–Protein Interactions (PPIs) in STAT3: Insights into a New Class of Benzothiadiazole Derivatives
    Matteo Mori, Ettore Gilardoni, Luca Regazzoni, Alessandro Pedretti, Diego Colombo, Gary Parkinson, Akira Asai, Fiorella Meneghetti, Stefania Villa, Arianna Gelain
    Molecules.2020; 25(15): 3509.     CrossRef
  • STAT3, the Challenge for Chemotherapeutic and Radiotherapeutic Efficacy
    Ping-Lian Yang, Lu-Xin Liu, En-Min Li, Li-Yan Xu
    Cancers.2020; 12(9): 2459.     CrossRef
  • Progress in Understanding the IL-6/STAT3 Pathway in Colorectal Cancer


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  • Systemic Therapy for Hepatocellular Carcinoma: Advances and Hopes
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  • Decoration of Anti-CD38 on Nanoparticles Carrying a STAT3 Inhibitor Can Improve the Therapeutic Efficacy Against Myeloma
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    Cancer Research and Treatment.2019; 51(2): 510.     CrossRef
  • IL-6 signaling contributes to radioresistance of prostate cancer through key DNA repair-associated molecules ATM, ATR, and BRCA 1/2
    Xiaodong Chen, Feng Chen, Yu Ren, Guobin Weng, Lijun Xu, Xiang Xue, Peter C. Keng, Soo Ok Lee, Yuhchyau Chen
    Journal of Cancer Research and Clinical Oncology.2019; 145(6): 1471.     CrossRef
  • Proton pump inhibitor: The dual role in gastric cancer
    Moon Kyung Joo, Jong-Jae Park, Hoon Jai Chun
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  • Transcriptional Reprogramming and Novel Therapeutic Approaches for Targeting Prostate Cancer Stem Cells
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    Frontiers in Oncology.2019;[Epub]     CrossRef
  • STAT3 as a potential therapeutic target in triple negative breast cancer: a systematic review
    Jiang-Jiang Qin, Li Yan, Jia Zhang, Wei-Dong Zhang
    Journal of Experimental & Clinical Cancer Research.2019;[Epub]     CrossRef
  • JAK/STAT inhibition in macrophages promotes therapeutic resistance by inducing expression of protumorigenic factors
    Emily A. Irey, Chelsea M. Lassiter, Nicholas J. Brady, Pavlina Chuntova, Ying Wang, Todd P. Knutson, Christine Henzler, Thomas S. Chaffee, Rachel I. Vogel, Andrew C. Nelson, Michael A. Farrar, Kathryn L. Schwertfeger
    Proceedings of the National Academy of Sciences.2019; 116(25): 12442.     CrossRef
  • Elevated HOX gene expression in acute myeloid leukemia is associated with NPM1 mutations and poor survival
    Ádám Nagy, Ágnes Ősz, Jan Budczies, Szilvia Krizsán, Gergely Szombath, Judit Demeter, Csaba Bödör, Balázs Győrffy
    Journal of Advanced Research.2019; 20: 105.     CrossRef
  • Antitumor activity of novel pyrazole-based small molecular inhibitors of the STAT3 pathway in patient derived high grade glioma cells
    Liang Zhang, Timothy E. Peterson, Victor M. Lu, Ian F. Parney, David J. Daniels, Ilya Ulasov
    PLOS ONE.2019; 14(7): e0220569.     CrossRef
  • Inhibition of Stat3 Signaling Pathway by Natural Product Pectolinarigenin Attenuates Breast Cancer Metastasis
    Yali Li, Cailing Gan, Yange Zhang, Yan Yu, Chen Fan, Yuanle Deng, Qianyu Zhang, Xi Yu, Yiwen Zhang, Liqun Wang, Fang He, Yongmei Xie, Tinghong Ye, Wenya Yin
    Frontiers in Pharmacology.2019;[Epub]     CrossRef
  • Impact of combination therapy with anti-PD-1 blockade and a STAT3 inhibitor on the tumor-infiltrating lymphocyte status
    Tadashi Ashizawa, Akira Iizuka, Chie Maeda, Emiko Tanaka, Ryota Kondou, Haruo Miyata, Takashi Sugino, Takuya Kawata, Shoichi Deguchi, Koichi Mitsuya, Nakamasa Hayashi, Akira Asai, Mamoru Ito, Ken Yamaguchi, Yasuto Akiyama
    Immunology Letters.2019; 216: 43.     CrossRef
  • Signal Transducer and Activator of Transcription Protein 3 (STAT3): An Update on its Direct Inhibitors as Promising Anticancer Agents
    Arianna Gelain, Matteo Mori, Fiorella Meneghetti, Stefania Villa
    Current Medicinal Chemistry.2019; 26(27): 5165.     CrossRef
  • The effects of signal transducer and activator of transcription three mutations on human platelets
    Floor E. Aleva, Frank L. van de Veerdonk, Yang Li, Rahajeng N. Tunjungputri, Sami Simons, Philip G. De Groot, Mihai M. Netea, Yvonne F. Heijdra, Quirijn de Mast, André J.A.M. van der Ven
    Platelets.2018; 29(6): 602.     CrossRef
  • Mechanisms Linking Obesity and Thyroid Cancer Development and Progression in Mouse Models
    Won Gu Kim, Sheue-yann Cheng
    Hormones and Cancer.2018; 9(2): 108.     CrossRef
  • Targeting the IL-6/JAK/STAT3 signalling axis in cancer
    Daniel E. Johnson, Rachel A. O'Keefe, Jennifer R. Grandis
    Nature Reviews Clinical Oncology.2018; 15(4): 234.     CrossRef
  • Arsenic trioxide attenuates STAT-3 activity and epithelial-mesenchymal transition through induction of SHP-1 in gastric cancer cells
    Sung Ho Kim, Hyo Soon Yoo, Moon Kyung Joo, Taehyun Kim, Jong-Jae Park, Beom Jae Lee, Hoon Jai Chun, Sang Woo Lee, Young-Tae Bak
    BMC Cancer.2018;[Epub]     CrossRef
  • Linker Variation and Structure–Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors
    Francisco Lopez-Tapia, Christine Brotherton-Pleiss, Peibin Yue, Heide Murakami, Ana Carolina Costa Araujo, Bruna Reis dos Santos, Erin Ichinotsubo, Anna Rabkin, Raj Shah, Megan Lantz, Suzie Chen, Marcus A. Tius, James Turkson
    ACS Medicinal Chemistry Letters.2018; 9(3): 250.     CrossRef
  • Decoy-Based, Targeted Inhibition of STAT3: A New Step forward for B Cell Lymphoma Immunotherapy
    Mario M. Soldevilla, Fernando Pastor
    Molecular Therapy.2018; 26(3): 675.     CrossRef
  • Two decades of research in discovery of anticancer drugs targeting STAT3, how close are we?
    Jenny D. Beebe, Jing-Yuan Liu, Jian-Ting Zhang
    Pharmacology & Therapeutics.2018; 191: 74.     CrossRef
  • Translational and clinical advances in JAK-STAT biology: The present and future of jakinibs
    Massimo Gadina, Catrina Johnson, Daniella Schwartz, Michael Bonelli, Sarfaraz Hasni, Yuka Kanno, Paul Changelian, Arian Laurence, John J O’Shea
    Journal of Leukocyte Biology.2018; 104(3): 499.     CrossRef
  • Targeting JAK-STAT signal transduction in IBD
    Christoffer Soendergaard, Fredrik Holmberg Bergenheim, Jakob Tveiten Bjerrum, Ole Haagen Nielsen
    Pharmacology & Therapeutics.2018; 192: 100.     CrossRef
  • “Do We Know Jack” About JAK? A Closer Look at JAK/STAT Signaling Pathway
    Emira Bousoik, Hamidreza Montazeri Aliabadi
    Frontiers in Oncology.2018;[Epub]     CrossRef
  • Plasticity of Type I Interferon-Mediated Responses in Cancer Therapy: From Anti-tumor Immunity to Resistance
    Megha Budhwani, Roberta Mazzieri, Riccardo Dolcetti
    Frontiers in Oncology.2018;[Epub]     CrossRef
  • STAT3 in Breast Cancer Onset and Progression: A Matter of Time and Context
    Ilenia Segatto, Gustavo Baldassarre, Barbara Belletti
    International Journal of Molecular Sciences.2018; 19(9): 2818.     CrossRef
  • Suppression of STAT3 signaling promotes cellular reprogramming into insulin-producing cells induced by defined transcription factors
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    EBioMedicine.2018; 36: 358.     CrossRef
  • Aptamer-iRNAs as Therapeutics for Cancer Treatment
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  • A First-in-Human Phase I Study of OPB-111077, a Small-Molecule STAT3 and Oxidative Phosphorylation Inhibitor, in Patients with Advanced Cancers
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    The Oncologist.2018; 23(6): 658.     CrossRef
  • Impact of STAT3 phosphorylation in glioblastoma stem cells radiosensitization and patient outcome
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    Oncotarget.2018; 9(3): 3968.     CrossRef
  • Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking
    Wenying Yu, Chenglong Li, Wenda Zhang, Yuanzheng Xia, Shanshan Li, Jia-yuh Lin, Keqin Yu, Mu Liu, Lei Yang, Jianguang Luo, Yijun Chen, Hongbin Sun, Lingyi Kong
    Journal of Medicinal Chemistry.2017; 60(7): 2718.     CrossRef
  • Exploiting the Ref-1-APE1 node in cancer signaling and other diseases: from bench to clinic
    Fenil Shah, Derek Logsdon, Richard A. Messmann, Jill C. Fehrenbacher, Melissa L. Fishel, Mark R. Kelley
    npj Precision Oncology.2017;[Epub]     CrossRef
  • Mitochondrial dysfunction induced by a SH2 domain-targeting STAT3 inhibitor leads to metabolic synthetic lethality in cancer cells
    Davide Genini, Lara Brambilla, Erik Laurini, Jessica Merulla, Gianluca Civenni, Shusil Pandit, Rocco D'Antuono, Laurent Perez, David E. Levy, Sabrina Pricl, Giuseppina M. Carbone, Carlo V. Catapano
    Proceedings of the National Academy of Sciences.2017;[Epub]     CrossRef
  • Identification of novel small molecules that inhibit STAT3-dependent transcription and function
    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, Aamir Ahmad
    PLOS ONE.2017; 12(6): e0178844.     CrossRef
  • Antineoplastic effects of CPPTL via the ROS/JNK pathway in acute myeloid leukemia
    Hui-Er Gao, Yue Sun, Ya-Hui Ding, Jing Long, Xiao-Lei Liu, Ming Yang, Qing Ji, Ying-Hui Li, Yue Chen, Quan Zhang, Ying-Dai Gao
    Oncotarget.2017; 8(24): 38990.     CrossRef
  • Stattic and metformin inhibit brain tumor initiating cells by reducing STAT3-phosphorylation
    Verena Leidgens, Judith Proske, Lisa Rauer, Sylvia Moeckel, Kathrin Renner, Ulrich Bogdahn, Markus J. Riemenschneider, Martin Proescholdt, Arabel Vollmann-Zwerenz, Peter Hau, Corinna Seliger
    Oncotarget.2017; 8(5): 8250.     CrossRef
  • Identification of antipsychotic drug fluspirilene as a potential anti-glioma stem cell drug
    Yu Dong, Takuya Furuta, Hemragul Sabit, Tomohiro Kitabayashi, Shabierjiang Jiapaer, Masahiko Kobayashi, Yasushi Ino, Tomoki Todo, Lei Teng, Atsushi Hirao, Shi-Guang Zhao, Mitsutoshi Nakada
    Oncotarget.2017; 8(67): 111728.     CrossRef
  • Feedback Activation of STAT3 as a Cancer Drug-Resistance Mechanism
    Chengguang Zhao, Huameng Li, Huey-Jen Lin, Shulin Yang, Jiayuh Lin, Guang Liang
    Trends in Pharmacological Sciences.2016; 37(1): 47.     CrossRef
  • Targeting transcription factor STAT3 for cancer prevention and therapy
    Edna Zhi Pei Chai, Muthu K. Shanmugam, Frank Arfuso, Arunasalam Dharmarajan, Chao Wang, Alan Prem Kumar, Ramar Perumal Samy, Lina H.K. Lim, Lingzhi Wang, Boon Cher Goh, Kwang Seok Ahn, Kam Man Hui, Gautam Sethi
    Pharmacology & Therapeutics.2016; 162: 86.     CrossRef
  • Molecular Bases for Combinatorial Treatment Strategies in Patients with KRAS Mutant Lung Adenocarcinoma and Squamous Cell Lung Carcinoma
    Chiara Lazzari, Alberto Verlicchi, Anastasios Gkountakos, Sara Pilotto, Mariacarmela Santarpia, Imane Chaib, Jose Luis Ramirez Serrano, Santiago Viteri, Daniela Morales-Espinosa, Claudio Dazzi, Filippo de Marinis, Peng Cao, Niki Karachaliou, Rafael Rosell
    Pulmonary Therapy.2016; 2(1): 1.     CrossRef
  • 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
    Zilma Escobar, Anders Bjartell, Giacomo Canesin, Susan Evans-Axelsson, Olov Sterner, Rebecka Hellsten, Martin H Johansson
    Journal of Medicinal Chemistry.2016; 59(10): 4551.     CrossRef
  • A Positive TGF-β/c-KIT Feedback Loop Drives Tumor Progression in Advanced Primary Liver Cancer
    Andres Rojas, Pingyu Zhang, Ying Wang, Wai Chin Foo, Nina M. Muñoz, Lianchun Xiao, Jing Wang, Gregory J. Gores, Mien-Chie Hung, Boris Blechacz
    Neoplasia.2016; 18(6): 371.     CrossRef
  • Novel STAT 3 inhibitors for treating gastric cancer
    Catherine Cafferkey, Ian Chau
    Expert Opinion on Investigational Drugs.2016; 25(9): 1023.     CrossRef
  • ‘Acute myeloid leukemia: a comprehensive review and 2016 update’
    I De Kouchkovsky, M Abdul-Hay
    Blood Cancer Journal.2016; 6(7): e441.     CrossRef
  • Recent updates of precision therapy for gastric cancer: Towards optimal tailored management
    Moon Kyung Joo, Jong-Jae Park, Hoon Jai Chun
    World Journal of Gastroenterology.2016; 22(19): 4638.     CrossRef
  • Targeted inhibition of STATs and IRFs as a potential treatment strategy in cardiovascular disease
    Malgorzata Szelag, Anna Piaszyk-Borychowska, Martyna Plens-Galaska, Joanna Wesoly, Hans A.R. Bluyssen
    Oncotarget.2016; 7(30): 48788.     CrossRef
  • Cell-cell and cell-matrix adhesion in survival and metastasis: Stat3 versus Akt
    Maximilian Niit, Victoria Hoskin, Esther Carefoot, Mulu Geletu, Rozanne Arulanandam, Bruce Elliott, Leda Raptis
    Biomolecular Concepts.2015; 6(5-6): 383.     CrossRef
  • Phase 1 and pharmacological trial of OPB‐31121, a signal transducer and activator of transcription‐3 inhibitor, in patients with advanced hepatocellular carcinoma
    Takuji Okusaka, Hideki Ueno, Masafumi Ikeda, Shuichi Mitsunaga, Masato Ozaka, Hiroshi Ishii, Osamu Yokosuka, Yoshihiko Ooka, Ryo Yoshimoto, Yasuo Yanagihara, Kiwamu Okita
    Hepatology Research.2015; 45(13): 1283.     CrossRef
  • STAT3 Inhibition Enhances the Therapeutic Efficacy of Immunogenic Chemotherapy by Stimulating Type 1 Interferon Production by Cancer Cells
    Heng Yang, Takahiro Yamazaki, Federico Pietrocola, Heng Zhou, Laurence Zitvogel, Yuting Ma, Guido Kroemer
    Cancer Research.2015; 75(18): 3812.     CrossRef
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