Timothy J. Harris Jr. and Darci J. Trader
RSC Med. Chem., 2025,16, 1067-1082
From themed collection:
Induced-Proximity Pharmacology
Abstract
Degrons are regions of a protein that are required to initiate their degradation by cellular machinery.
Yanyun Hong, Xiang Liu, Yinglong Li, Mengting Yu, Caolin Wang, Cunpeng Nie and Shan Xu
Chem. Commun., 2026, Advance Article
Abstract
This schematic illustrates the multidimensional optimization strategies for BRD4-targeting PROTACs, encompassing the rational design of the ternary complex, diverse controllable activation systems, and targeted delivery approaches.
Aliakbar Khalili Yazdi, Sumera Perveen, Cheng Dong, Xiaosheng Song, Aiping Dong, Magdalena M. Szewczyk, Matthew F. Calabrese, Agustin Casimiro-Garcia, Subramanyam Chakrapani, Matthew S. Dowling, Emel Ficici, Jisun Lee, Justin I. Montgomery, Thomas N. O'Connell, Grzegorz J. Skrzypek, Tuan P. Tran, Matthew D. Troutman, Feng Wang, Jennifer A. Young, Jinrong Min, Dalia Barsyte-Lovejoy, Peter J. Brown, Vijayaratnam Santhakumar, Cheryl H. Arrowsmith, Masoud Vedadi and Dafydd R. Owen
RSC Med. Chem., 2024,15, 1066-1071
From themed collection:
Highlights from Industry
Abstract
A chemical probe (PFI-7) for the Gid4 subunit of the human E3 ligase CTLH degradation complex.
Thomas P. Corner, Ryan Z. R. Teo, Yue Wu, Eidarus Salah, Yu Nakashima, Giorgia Fiorini, Anthony Tumber, Amelia Brasnett, James P. Holt-Martyn, William D. Figg, Xiaojin Zhang, Lennart Brewitz and Christopher J. Schofield
Chem. Sci., 2023,14, 12098-12120
Abstract
Optimised N-hydroxythiazoles are efficient and selective inhibitors of the 2-oxoglutrate dependent oxygenase factor inhibiting HIF, which has a key role in the human hypoxic response; the inhibitors decrease lipid accumualtion in adipocytes.
Jiseong Kim, Insuk Byun, Do Young Kim, Hyunhi Joh, Hak Joong Kim and Min Jae Lee
Chem. Soc. Rev., 2024,53, 3253-3272
Abstract
This review delineates emerging technologies for targeted protein degradation that directly involve lysosomes or proteasomes. It explores their unique features, advantages, and limitations, offering perspectives on future therapeutic applications.