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JAK2 inhibitors for the treatment of Philadelphia-negative myeloproliferative neoplasms: current status and future directions

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机构： [1]School of Basic Medical Sciences, Southwest Medical University, Luzhou 646000, China [2]Zigong Mental Health Center, Zigong Afliated Hospital of Southwest Medical University, Zigong 643000, China [3]Key Laboratory of Medical Electrophysiology, Ministry of Education & Medical Electrophysiological Key Laboratory of Sichuan Province, Institute of Cardiovascular Research, Southwest Medical University, Luzhou 646000, China [4]Sichuan Key Medical Laboratory of New Drug Discovery and Druggability Evaluation, Luzhou Key Laboratory of Activity Screening and Druggability Evaluation for Chinese Materia Medica, School of Pharmacy, Southwest Medical University, Luzhou 646000, China

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关键词： JAK2 inhibitors Philadelphia-negative myeloproliferative neoplasms Allosteric inhibitors Covalent inhibitors Drug combination

摘要：

The overactivation of Janus kinases 2 (JAK2) by gain-of-function mutations in the JAK2, Myeloproliferative leukemia virus oncogene, or Calreticulin genes are the most important factor in the development of Philadelphia-negative myeloproliferative neoplasms (MPNs). The discovery of the JAK2V617F mutation is a significant breakthrough in understanding the pathogenesis of MPNs, and inhibition of JAK2 abnormal activation has become one of the most effective strategies against MPNs. Currently, three JAK2 inhibitors for treating MPNs have been approved, and several are being evaluated in clinical trials. However, persistent challenges in terms of drug resistance and off-target effects remain unresolved. In this review, we introduce and classify the available JAK2 inhibitors in terms of their mechanisms and clinical considerations. Additionally, through an analysis of target points, binding modes, and structure-activity inhibitor relationships, we propose strategies such as combination therapy and allosteric inhibitors to overcome specific challenges. This review offers valuable insights into current trends and future directions for optimal management of MPNs using JAK2 inhibitors.© 2023. The Author(s), under exclusive licence to Springer Nature Switzerland AG.

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出版当年[2023]版：

大类 | 2 区化学

小类 | 3 区应用化学 3 区药物化学 3 区化学：综合

最新[2023]版：

大类 | 2 区化学

小类 | 3 区应用化学 3 区药物化学 3 区化学：综合

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第一作者机构： [1]School of Basic Medical Sciences, Southwest Medical University, Luzhou 646000, China

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通讯机构： [1]School of Basic Medical Sciences, Southwest Medical University, Luzhou 646000, China [2]Zigong Mental Health Center, Zigong Afliated Hospital of Southwest Medical University, Zigong 643000, China [3]Key Laboratory of Medical Electrophysiology, Ministry of Education & Medical Electrophysiological Key Laboratory of Sichuan Province, Institute of Cardiovascular Research, Southwest Medical University, Luzhou 646000, China [4]Sichuan Key Medical Laboratory of New Drug Discovery and Druggability Evaluation, Luzhou Key Laboratory of Activity Screening and Druggability Evaluation for Chinese Materia Medica, School of Pharmacy, Southwest Medical University, Luzhou 646000, China

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JAK2 inhibitors for the treatment of Philadelphia-negative myeloproliferative neoplasms: current status and future directions

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