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Discovery of reactive peptide inhibitors of human papillomavirus oncoprotein E6

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CHEMICAL SCIENCE
卷 14, 期 44, 页码 -

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ROYAL SOC CHEMISTRY
DOI: 10.1039/d3sc02782a

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In this study, a covalent peptide inhibitor called reactide was designed to inhibit HPV-mediated degradation of p53 by targeting cysteine 58 in HPV16 E6. This reactide provides a starting point for the development of covalent peptidomimetic inhibitors against HPV-driven cancers.
Human papillomavirus (HPV) infections account for nearly all cervical cancer cases, which is the fourth most common cancer in women worldwide. High-risk variants, including HPV16, drive tumorigenesis in part by promoting the degradation of the tumor suppressor p53. This degradation is mediated by the HPV early protein 6 (E6), which recruits the E3 ubiquitin ligase E6AP and redirects its activity towards ubiquitinating p53. Targeting the protein interaction interface between HPV E6 and E6AP is a promising modality to mitigate HPV-mediated degradation of p53. In this study, we designed a covalent peptide inhibitor, termed reactide, that mimics the E6AP LXXLL binding motif by selectively targeting cysteine 58 in HPV16 E6 with quantitative conversion. This reactide provides a starting point in the development of covalent peptidomimetic inhibitors for intervention against HPV-driven cancers.

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