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Investigational Janus kinase inhibitors

, MBBS MD & , MD PhD
Pages 687-699 | Published online: 23 Feb 2013

Keep up to date with the latest research on this topic with citation updates for this article.

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Hui Gao, Songqing Mei, Jing Zhao, Kangcheng Zheng & Siyan Liao. (2019) Study on the binding mode of a pyrrolotriazin derivative with JAK2 by docking and MD simulation. Molecular Simulation 45:3, pages 230-238.
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Vivian Chow, Ashley Weissman, Casey Lee O’Connell, Azim Mehrvar & Mojtaba Akhtari. (2016) Emerging treatment options for myelofibrosis: focus on pacritinib. OncoTargets and Therapy 9, pages 2655-2665.
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Matteo Santoni, Francesco Massari, Marzia Del Re, Chiara Ciccarese, Francesco Piva, Giovanni Principato, Rodolfo Montironi, Daniele Santini, Romano Danesi, Giampaolo Tortora & Stefano Cascinu. (2015) Investigational therapies targeting signal transducer and activator of transcription 3 for the treatment of cancer. Expert Opinion on Investigational Drugs 24:6, pages 809-824.
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T. Devos, P. Zachée, D. Bron, L. Noens, J. Van Droogenbroeck, P. Mineur, Y. Beguin, Z. Berneman, F. S. Benghiat, A. Kentos, C. Chatelain, H. Demuynck, J. Lemmens, K. Van Eygen, K. Theunissen, F. Trullemans, P. Pierre, W. Pluymers & L. Knoops. (2015) Myelofibrosis patients in Belgium: disease characteristics. Acta Clinica Belgica 70:2, pages 105-111.
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Constantine S Tam, Aziz Nazha & Srdan Verstovsek. (2013) Pharmacotherapy of polycythemia vera. Expert Opinion on Orphan Drugs 1:12, pages 977-985.
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Håkon Reikvam, Ina Nepstad & Jerome Tamburini. (2013) Predicting effects of kinase inhibitor in therapy for myeloid malignancies – the challenges in capturing disease heterogeneity. Expert Opinion on Investigational Drugs 22:11, pages 1365-1370.
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Tomi K Sawyer, Joe C Wu, Jonathon R Sawyer & Jessie M English. (2013) Protein kinase inhibitors: breakthrough medicines and the next generation. Expert Opinion on Investigational Drugs 22:6, pages 675-678.
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Articles from other publishers (35)

Vikas Sharma & Mohit Gupta. (2022) Designing of kinase hinge binders: A medicinal chemistry perspective. Chemical Biology & Drug Design 100:6, pages 968-980.
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Pei Shen, Yezhi Wang, Xiangxiang Jia, Pengfei Xu, Lian Qin, Xi Feng, Zhiyu Li & Zhixia Qiu. (2022) Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases. European Journal of Medicinal Chemistry 239, pages 114551.
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Zhiqing Xu & Ming Chu. (2022) Advances in Immunosuppressive Agents Based on Signal Pathway. Frontiers in Pharmacology 13.
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Jordi Bach, Paul Eastwood, Jacob González, Elena Gómez, Juan Antonio Alonso, Silvia Fonquerna, Estrella Lozoya, Adela Orellana, Mónica Maldonado, Elena Calaf, Joan Albertí, Juan Pérez, Ana Andrés, Neus Prats, Cristina Carreño, Elena Calama, Jorge De Alba, Marta Calbet, Montserrat Miralpeix & Isabel Ramis. (2019) Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases. Journal of Medicinal Chemistry 62:20, pages 9045-9060.
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Srdan Verstovsek, Ruben A. Mesa, Mohamed E. Salama, Li Li, Celine Pitou, Fabio P. Nunes, Gregory L. Price, Jennifer L. Giles, Deborah N. D’Souza, Richard A. Walgren & Josef T. Prchal. (2017) A phase 1 study of the Janus kinase 2 (JAK2)V617F inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemia. Leukemia Research 61, pages 89-95.
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Rita Assi, Srdan Verstovsek & Naval Daver. (2017) ‘JAK–ing’ up the treatment of primary myelofibrosis. Current Opinion in Hematology 24:2, pages 115-124.
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Gege Feng, Tianjiao Zhang, Jinqin Liu, Xiaotang Ma, Bing Li, Lin Yang, Yue Zhang, Zefeng Xu, Tiejun Qin, Jiaxi Zhou, Gang Huang, Lihong Shi & Zhijian Xiao. (2017) MLF 1 IP promotes normal erythroid proliferation and is involved in the pathogenesis of polycythemia vera . FEBS Letters 591:5, pages 760-773.
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Charles Malemud. (2017) Negative Regulators of JAK/STAT Signaling in Rheumatoid Arthritis and Osteoarthritis. International Journal of Molecular Sciences 18:3, pages 484.
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Tingfang Wang, Xiaofei Liu, Meixi Hao, Jianan Qiao, Caoyun Ju, Lingjing Xue & Can Zhang. (2016) Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors. Bioorganic & Medicinal Chemistry Letters 26:12, pages 2936-2941.
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Ban Seok Lee, Sang Hyub Lee, Jun Hyuk Son, Dong Kee Jang, Kwang Hyun Chung, Yoon Suk Lee, Woo Hyun Paik, Ji Kon Ryu & Yong-Tae Kim. (2016) Neutrophil–lymphocyte ratio predicts survival in patients with advanced cholangiocarcinoma on chemotherapy. Cancer Immunology, Immunotherapy 65:2, pages 141-150.
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Melissa M. Vasbinder, Marat Alimzhanov, Martin Augustin, Geraldine Bebernitz, Kirsten Bell, Claudio Chuaqui, Tracy Deegan, Andrew D. Ferguson, Kelly Goodwin, Dennis Huszar, Aarti Kawatkar, Sameer Kawatkar, Jon Read, Jie Shi, Stefan Steinbacher, Holger Steuber, Qibin Su, Dorin Toader, Haixia Wang, Richard Woessner, Allan Wu, Minwei Ye & Michael Zinda. (2016) Identification of azabenzimidazoles as potent JAK1 selective inhibitors. Bioorganic & Medicinal Chemistry Letters 26:1, pages 60-67.
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Naveen Pemmaraju & Ruben Mesa. (2015) Evidence for Janus kinase (JAK) inhibitors for the prevention of major morbid events in patients with myeloproliferative neoplasms (MPNs). Hematology 2015:1, pages 649-651.
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Naveen Pemmaraju & Ruben Mesa. (2015) Evidence for Janus kinase (JAK) inhibitors for the prevention of major morbid events in patients with myeloproliferative neoplasms (MPNs). Hematology 2015:1, pages 649-651.
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Qiang Jeremy Wen, Qiong Yang, Benjamin Goldenson, Sébastien Malinge, Terra Lasho, Rebekka K Schneider, Lawrence J Breyfogle, Rachael Schultz, Laure Gilles, Priya Koppikar, Omar Abdel-Wahab, Animesh Pardanani, Brady Stein, Sandeep Gurbuxani, Ann Mullally, Ross L Levine, Ayalew Tefferi & John D Crispino. (2015) Targeting megakaryocytic-induced fibrosis in myeloproliferative neoplasms by AURKA inhibition. Nature Medicine 21:12, pages 1473-1480.
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Mi Kyoung Kim, Heerim Shin, Kwang-su Park, Hyungmi Kim, Jiseon Park, Kangjeon Kim, Joonwoo Nam, Hyunah Choo & Youhoon Chong. (2015) Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors. Journal of Medicinal Chemistry 58:18, pages 7596-7602.
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Li Tan, Koshi Akahane, Randall McNally, Kathleen M. S. E. ReyskensScott B. Ficarro, Suhu Liu, Grit S. Herter-Sprie, Shohei Koyama, Michael J. PattisonKatherine Labella, Liv Johannessen, Esra A. Akbay, Kwok-Kin Wong, David A. Frank, Jarrod A. Marto, Thomas A. Look, J. Simon C. ArthurMichael J. Eck & Nathanael S. Gray. (2015) Development of Selective Covalent Janus Kinase 3 Inhibitors. Journal of Medicinal Chemistry 58:16, pages 6589-6606.
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Honghe Wan, Gretchen M. Schroeder, Amy C. Hart, Jennifer Inghrim, James Grebinski, John S. Tokarski, Matthew V. Lorenzi, Dan You, Theresa Mcdevitt, Becky Penhallow, Ragini Vuppugalla, Yueping Zhang, Xiaomei Gu, Ramaswamy Iyer, Louis J. Lombardo, George L. Trainor, Stefan Ruepp, Jonathan Lippy, Yuval Blat, John S. Sack, Javed A. Khan, Kevin Stefanski, Bogdan Sleczka, Arvind Mathur, Jung-Hui Sun, Michael K. Wong, Dauh-Rurng Wu, Peng Li, Anuradha Gupta, P. N. Arunachalam, Bala Pragalathan, Sankara Narayanan, Nanjundaswamy K.C., Prakasam Kuppusamy & Ashok V. Purandare. (2015) Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. ACS Medicinal Chemistry Letters 6:8, pages 850-855.
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Amy C. Hart, Gretchen M. Schroeder, Honghe Wan, James Grebinski, Jennifer Inghrim, James Kempson, Junqing Guo, William J. Pitts, John S. Tokarski, John S. Sack, Javed A. Khan, Jonathan Lippy, Matthew V. Lorenzi, Dan You, Theresa McDevitt, Ragini Vuppugalla, Yueping Zhang, Louis J. Lombardo, George L. Trainor & Ashok V. Purandare. (2015) Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5- d ]pyrrolo[2,3- b ]pyridine Inhibitors . ACS Medicinal Chemistry Letters 6:8, pages 845-849.
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Kurt Zimmermann, Xiaopeng Sang, Harold A. Mastalerz, Walter L. Johnson, Guifen Zhang, Qingjie Liu, Douglas Batt, Louis J. Lombardo, Dinesh Vyas, George L. Trainor, John S. Tokarski, Matthew V. Lorenzi, Dan You, Marco M. Gottardis, Jonathan Lippy, Javed Khan, John S. Sack & Ashok V. Purandare. (2015) 9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors. Bioorganic & Medicinal Chemistry Letters 25:14, pages 2809-2812.
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Maria Gabriella Brasca, Paola Gnocchi, Marcella Nesi, Nadia Amboldi, Nilla Avanzi, Jay Bertrand, Simona Bindi, Giulia Canevari, Daniele Casero, Marina Ciomei, Nicoletta Colombo, Sabrina Cribioli, Gabriele Fachin, Eduard R. Felder, Arturo Galvani, Antonella Isacchi, Ilaria Motto, Achille Panzeri & Daniele Donati. (2015) Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders. Bioorganic & Medicinal Chemistry 23:10, pages 2387-2407.
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Srdan Verstovsek, Ronald Hoffman, John Mascarenhas, Jean-Charles Soria, Ratislav Bahleda, Patricia McCoon, Weifeng Tang, Jorge Cortes, Hagop Kantarjian & Vincent Ribrag. (2015) A phase I, open-label, multi-center study of the JAK2 inhibitor AZD1480 in patients with myelofibrosis. Leukemia Research 39:2, pages 157-163.
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Madappa KundrandaToufic Kachaamy. (2014) Promising new therapies in advanced pancreatic adenocarcinomas. Future Oncology 10:16, pages 2629-2641.
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Yordanka Tirefort, Xuan-Cuong Pham, Yasmine Lucile Ibrahim, Thomas Pierre Lecompte, Thomas Matthes, Christa Prins, Begonia Cortes, Michael Bernimoulin, Yves Chalandon & Kaveh Samii. (2014) A rare case of primary cutaneous follicle centre lymphoma presenting as a giant tumour of the scalp and combined with JAK2V617F positive essential thrombocythaemia. Biomarker Research 2:1.
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Chakrabhavi Dhananjaya Mohan, Hanumantharayappa Bharathkumar, Krishna C. Bulusu, Vijay Pandey, Shobith Rangappa, Julian E. Fuchs, Muthu K. Shanmugam, Xiaoyun Dai, Feng Li, Amudha Deivasigamani, Kam M. Hui, Alan Prem Kumar, Peter E. Lobie, Andreas Bender, Salundi Basappa, Gautam Sethi & Kanchugarakoppal S. Rangappa. (2014) Development of a Novel Azaspirane That Targets the Janus Kinase-Signal Transducer and Activator of Transcription (STAT) Pathway in Hepatocellular Carcinoma in Vitro and in Vivo. Journal of Biological Chemistry 289:49, pages 34296-34307.
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Peter J. Houghton, Raushan T. Kurmasheva, Dmitry Lyalin, John M. Maris, E. Anders Kolb, Richard Gorlick, C. Patrick Reynolds, Min H. Kang, Stephen T. Keir, Jianrong Wu & Malcolm A. Smith. (2014) Initial solid tumor testing (Stage 1) of AZD1480, an inhibitor of Janus kinases 1 and 2 by the pediatric preclinical testing program. Pediatric Blood & Cancer 61:11, pages 1972-1979.
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Sara C. MeyerMatthew D. KellerBrittany A. Woods, Lindsay M. LaFave, Lennart BastianMaria KleppeNeha Bhagwat, Sachie MarubayashiRoss L. Levine. (2014) Genetic studies reveal an unexpected negative regulatory role for Jak2 in thrombopoiesis. Blood 124:14, pages 2280-2284.
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Connie I Diakos, Kellie A Charles, Donald C McMillan & Stephen J Clarke. (2014) Cancer-related inflammation and treatment effectiveness. The Lancet Oncology 15:11, pages e493-e503.
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Hanyang Lin, Min Chen, Katharina Rothe, Matthew V. Lorenzi, Adrian Woolfson & Xiaoyan Jiang. (2014) Selective JAK2/ABL dual inhibition therapy effectively eliminates TKI-insensitive CML stem/progenitor cells. Oncotarget 5:18, pages 8637-8650.
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Anna M Eiring & Michael W Deininger. (2014) Individualizing kinase-targeted cancer therapy: the paradigm of chronic myeloid leukemia. Genome Biology 15:9.
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Maria Gabriella Brasca, Marcella Nesi, Nilla Avanzi, Dario Ballinari, Tiziano Bandiera, Jay Bertrand, Simona Bindi, Giulia Canevari, Davide Carenzi, Daniele Casero, Lucio Ceriani, Marina Ciomei, Alessandra Cirla, Maristella Colombo, Sabrina Cribioli, Cinzia Cristiani, Franco Della Vedova, Gabriele Fachin, Marina Fasolini, Eduard R. Felder, Arturo Galvani, Antonella Isacchi, Danilo Mirizzi, Ilaria Motto, Achille Panzeri, Enrico Pesenti, Paola Vianello, Paola Gnocchi & Daniele Donati. (2014) Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors. Bioorganic & Medicinal Chemistry 22:17, pages 4998-5012.
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Srdan Verstovsek, Constantine S. Tam, Martha Wadleigh, Lubomir Sokol, Catherine C. Smith, Lynne A. Bui, Chunyan Song, Douglas O. Clary, Patrycja Olszynski, Jorge Cortes, Hagop Kantarjian & Neil P. Shah. (2014) Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor. Leukemia Research 38:3, pages 316-322.
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Y Nakaya, K Shide, H Naito, T Niwa, T Horio, J Miyake & K Shimoda. (2014) Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis. Blood Cancer Journal 4:1, pages e174-e174.
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Qibin Su, Stephanos Ioannidis, Claudio Chuaqui, Lynsie Almeida, Marat Alimzhanov, Geraldine Bebernitz, Kirsten Bell, Michael Block, Tina Howard, Shan Huang, Dennis Huszar, Jon A. Read, Caroline Rivard Costa, Jie Shi, Mei Su, Minwei Ye & Michael Zinda. (2013) Discovery of 1-Methyl-1 H -imidazole Derivatives as Potent Jak2 Inhibitors . Journal of Medicinal Chemistry 57:1, pages 144-158.
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Charles J Malemud. (2014) Protein kinase small molecule inhibitors for rheumatoid arthritis: Medicinal chemistry/clinical perspectives. World Journal of Orthopedics 5:4, pages 496.
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A. Mortlock, K. Foote, J. Kettle & B. Aquila. 2014. Reference Module in Chemistry, Molecular Sciences and Chemical Engineering. Reference Module in Chemistry, Molecular Sciences and Chemical Engineering.

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