| Autor: |
Li, Zhonghan, Huang, Yi, Hung, Ta I, Sun, Jianan, Aispuro, Desiree, Chen, Boxi, Guevara, Nathan, Ji, Fei, Cong, Xu, Zhu, Lingchao, Wang, Siwen, Guo, Zhili, Chang, Chia-en, Xue, Min |
| Zdroj: |
Journal of the American Chemical Society; January 2024, Vol. 146 Issue: 2 p1356-1363, 8p |
| Abstrakt: |
Here, we present the second generation of our bicyclic peptide library (NTB), featuring a stereodiversified structure and a simplified construction strategy. We utilized a tandem ring-opening metathesis and ring-closing metathesis reaction (ROM-RCM) to cyclize the linear peptide library in a single step, representing the first reported instance of this reaction being applied to the preparation of macrocyclic peptides. Moreover, the resulting bicyclic peptide can be easily linearized for MS/MS sequencing with a one-step deallylation process. We employed this library to screen against the E363-R378epitope of MYC and identified several MYC-targeting bicyclic peptides. Subsequent in vitro cell studies demonstrated that one candidate, NT-B2R, effectively suppressed MYC transcription activities and cell proliferation. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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