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Can I read Simultaneous Covalent Modification of K-Ras(G12D) and K-Ras(G12C) with Tunable Oxirane Electrophiles on EtoBox?
Simultaneous Covalent Modification of K-Ras(G12D) and K-Ras(G12C) with Tunable Oxirane Electrophiles by Zhongtang Yu; Xiaoqiang He; Ruiliu Wang; Xinxin Xu; Zhang Zhang; Ke Ding; Zhi-Min Zhang; Yi Tan; Zhengqiu Li is a Chemistry article available to read on EtoBox.
What is Simultaneous Covalent Modification of K-Ras(G12D) and K-Ras(G12C) with Tunable Oxirane Electrophiles about?
Owing to their remarkable pharmaceutical properties compared to those of noncovalent inhibitors, the development of targeted covalent inhibitors (TCIs) has emerged as a powerful method for cancer treatment. The K-Ras mutant, which is prevalent in multiple cancers, has been confirmed to be a crucial drug target in the treatment of various malignancies. However, although the K-Ras(G12D) mutation is present in up to 33% of K-Ras mutations, no covalent inhibitors targeting K-Ras(G12D) have been developed to date. The relatively weak nucleophilicity of the acquired aspartic acid (12D) residue in K-Ras may be the reason for this. Herein, we present the first compound capable of covalently engaging both K-Ras(G12D) and K-Ras(G12C) mutants. Proteome profiling revealed that this compound effectively conjugates with G12C and G12D residues, modulating the protein functions in situ. These findings offer a unique pathway for the development of novel dual covalent inhibitors.
Who reads Simultaneous Covalent Modification of K-Ras(G12D) and K-Ras(G12C) with Tunable Oxirane Electrophiles?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Zhongtang Yu; Xiaoqiang He; Ruiliu Wang; Xinxin Xu; Zhang Zhang; Ke Ding; Zhi-Min Zhang; Yi Tan; Zhengqiu Li
- Publisher
- American Chemical Society (ACS)
- Published
- 2023
- Language
- EN
- Field
- Chemistry (Physical Sciences)