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Recent advances in mechanisms of KRASG12C inhibitors anti-tumor resistance and relevant overcoming strategies
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Ke-xin LIU, Rui-lin WU, Tao YUAN, Kai-yue PU, Qiao-jun HE, Hong ZHU*, Bo YANG*
Acta Pharmaceutica Sinica | 2022, 57(2) : 271 - 276
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Acta Pharmaceutica Sinica | 2022, 57(2): 271-276
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Recent advances in mechanisms of KRASG12C inhibitors anti-tumor resistance and relevant overcoming strategies
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Ke-xin LIU, Rui-lin WU, Tao YUAN, Kai-yue PU, Qiao-jun HE, Hong ZHU*, Bo YANG*
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  • College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
Published: 2022-02-12 doi: 10.16438/j.0513-4870.2021-1093
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KRAS is one of the most frequently mutated human oncogenes. In spite of mounting efforts on the development of direct or indirect inhibition targeting KRAS, little has been achieved because of insurmountable difficulties, titling KRAS "undruggable". Recently, subtype-specific inhibitors have shown great hope. Some KRASG12C inhibitors have entered clinical trials, including adagrasib and sotorasib, and have shown preliminary clinical effectiveness. Experiences from the inhibitors targeting the downstream factors of RAS pathways show that the anticancer activity of these drugs will be limited due to the development of drug resistance. Preclinical studies of KRASG12C inhibitors have revealed that the application of these agents might be hampered by the drug resistance issue. The current review aims to describe the current status of KRASG12C inhibitors, and discuss the mechanisms underlying KRASG12Cinhibitor resistance, so as to provide the clues for the combat of drug resistance.

KRAS  /  G12C mutation  /  oncogene  /  targeted therapy  /  drug resistance
Ke-xin LIU, Rui-lin WU, Tao YUAN, Kai-yue PU, Qiao-jun HE, Hong ZHU, Bo YANG. Recent advances in mechanisms of KRASG12C inhibitors anti-tumor resistance and relevant overcoming strategies[J]. Acta Pharmaceutica Sinica, 2022 , 57 (2) : 271 -276 . DOI: 10.16438/j.0513-4870.2021-1093
Year 2022 volume 57 Issue 2
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doi: 10.16438/j.0513-4870.2021-1093
  • Receive Date:2021-07-25
  • Online Date:2025-12-22
  • Published:2022-02-12
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  • Received:2021-07-25
  • Revised:2021-08-25
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    College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, 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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