Discovery and characterization of potent macrocycle inhibitors of ubiquitin-specific protease-7.

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Tác giả: Emel Adaligil, Francesca Anson, Erin C Dueber, Brennan Farrell, Seth F Harris, Jeffrey K Holden, Rafael Miranda, Lionel Rougé, Shannon T Smith, Connie A Tenorio, Mark Ultsch

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: United States : Structure (London, England : 1993) , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 486460

The ubiquitin-specific protease (USP) family of deubiquitinases (DUBs) are regulators of Ub signaling that share a common catalytic-domain fold. The dynamic nature of this domain is important for controlling the function of USPs, with inter- and intramolecular interactions often influencing the structure and enzymatic activity of these DUBs. This conformational flexibility, in combination with the high sequence conservation of the USP active site, has made it challenging to readily identify potent and selective inhibitors for individual USPs. Here, we demonstrate how a naive, macrocycle-mRNA display selection rapidly yielded high-affinity binders to USP7 that specifically inhibit the DUB with nanomolar half-maximal inhibitory concentration (IC
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