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Bcl-2: research progress from target to launched drug
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Xiao-xian LI, Ren-shuai LIU, Hao FANG*
Acta Pharmaceutica Sinica | 2018, 53(4) : 509 - 517
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Acta Pharmaceutica Sinica | 2018, 53(4): 509-517
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Bcl-2: research progress from target to launched drug
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Xiao-xian LI, Ren-shuai LIU, Hao FANG*
Affiliations
  • Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China
Published: 2018-04-12 doi: 10.16438/j.0513-4870.2017-1210
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Apoptosis is an important self-stabilizing mechanism of multicellular organisms, which plays a vital role in the development of normal living organisms and the maintenance of tissue homeostasis. The abnormalities in apoptosis often lead to body lesions including tumors. Studies have shown that Bcl-2 protein with anti-apoptosis activity is an important target in the treatment of cancer. After nearly two decades of efforts, many small molecule Bcl-2 inhibitors have been discovered to induce cell apoptosis. The small-molecule Bcl-2 inhibitor, venetoclax, was developed based on fragment-based drug design strategy and approved by the FDA in 2016 for clinical application. This agent is the first approved small-molecule drug inhibiting Bcl-2 through protein-protein interaction to induce cell apoptosis. The achievement of venetoclax benefits from a combination of drug discovery technologies and represents a milestone in the history of drug discovery. In this review we will introduce the current progress in Bcl-2 inhibitors.

apoptosis  /  Bcl-2 inhibitor  /  protein-protein interaction
Xiao-xian LI, Ren-shuai LIU, Hao FANG. Bcl-2: research progress from target to launched drug[J]. Acta Pharmaceutica Sinica, 2018 , 53 (4) : 509 -517 . DOI: 10.16438/j.0513-4870.2017-1210
Year 2018 volume 53 Issue 4
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doi: 10.16438/j.0513-4870.2017-1210
  • Receive Date:2017-12-05
  • Online Date:2026-01-15
  • Published:2018-04-12
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  • Received:2017-12-05
  • Revised:2017-12-26
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    Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
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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