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Advances in JAK2 inhibitors for treatment of myeloproliferative neoplasms
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Min HU, Gao-na SHI, Jian-gong SHI*, Tian-tai ZHANG*
Acta Pharmaceutica Sinica | 2019, 54(6) : 971 - 977
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Acta Pharmaceutica Sinica | 2019, 54(6): 971-977
• Reviews •
Advances in JAK2 inhibitors for treatment of myeloproliferative neoplasms
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Min HU, Gao-na SHI, Jian-gong SHI*, Tian-tai ZHANG*
Affiliations
  • Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2019-06-12 doi: 10.16438/j.0513-4870.2019-0133
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Myeloproliferative neoplasms (MPNs) result from clonal expansion of haematopoietic stem cells and are characterized by abnormal proliferation of myeloid lineage cells in the bone marrow. Sustained activation of JAK-STAT signaling pathway due to JAK2 phosphorylation is an important cause of MPNs, and mutation of JAK2 kinase can keep it in a state of continuous phosphorylation. The most typical mutation in JAK2 is a site mutation of V617F in the pseudokinase domain. The JAK2V617F-activating mutation is highly prevalent in MPNs, with frequencies estimated at approximately 95% in polycythaemia vera (PV) and 50% in primary myelofibrosis (PMF) and essential thrombocytosis (ET) patients. It is now clear that JAK2 is an important target for treatment of MPNs. Inhibiting aberrant activation of the JAK2-STAT signaling pathway has become a popular trend in research for effective treatment of MPNs. This review summarizes the research progress in developing JAK2 inhibitors for treatment of MPNs in recent years, including the new discoveries of the biological functions of JAK2, the relationship between JAK2 and MPN, and the status of development of JAK2 small molecule inhibitors.

JAK2  /  JAK2 inhibitor  /  myeloproliferative neoplasm  /  JAK-STAT signaling pathway
Min HU, Gao-na SHI, Jian-gong SHI, Tian-tai ZHANG. Advances in JAK2 inhibitors for treatment of myeloproliferative neoplasms[J]. Acta Pharmaceutica Sinica, 2019 , 54 (6) : 971 -977 . DOI: 10.16438/j.0513-4870.2019-0133
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doi: 10.16438/j.0513-4870.2019-0133
  • Receive Date：2019-02-22
  • Online Date：2026-01-26
  • Published：2019-06-12
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  • Received：2019-02-22
  • Revised：2019-03-11
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    Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
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Genus		 种数
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Percentage of total
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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