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Research progress of KRASG12C protein covalent inhibitors
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Tian-fu HAN, Chun-lei TANG, Wei-zheng FAN
Chinese Journal of New Drugs | 2023, 32(17) : 1732 - 1739
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Chinese Journal of New Drugs | 2023, 32(17): 1732-1739
Research progress of KRASG12C protein covalent inhibitors
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Tian-fu HAN, Chun-lei TANG, Wei-zheng FAN
Affiliations
  • School of Life Science And Health Engineering, Jiangnan University, Wuxi 214122, China
Published: 2023-09-15
Outline
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A small GTPase encoded by Kirsten rat sarcoma viral proto oncogene (RAS) is a key regulatory protein in multiple cellular signaling pathways. The mutation of glycine to cysteine (G12C) at position 12 often leads to abnormal activation of cellular pathways, which plays an important role in the occurrence and development of tumors. Small molecule covalent inhibitors targeting KRASG12C protein can directly inhibit the abnormal activation of cellular pathways caused by KRASG12C mutation. In this paper, the structure and function of KRAS protein, as well as the research and development progress, challenges and possible solutions of covalent inhibitors of its G12C mutant are reviewed. The development direction of (K) RAS inhibitors in the future is prospected in order to provide a useful reference for the research and development of such inhibitors.

KRASG12C protein  /  mutation  /  lung cancer  /  covalent inhibitor  /  clinical trial
Tian-fu HAN, Chun-lei TANG, Wei-zheng FAN. Research progress of KRASG12C protein covalent inhibitors[J]. Chinese Journal of New Drugs, 2023 , 32 (17) : 1732 -1739 .
Year 2023 volume 32 Issue 17
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  • Online Date:2026-03-05
  • Published:2023-09-15
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  • Accepted:2022-09-22
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    School of Life Science And Health Engineering, Jiangnan University, Wuxi 214122, 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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