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Structure-guided engineering of an aptamer-PROTAC for targeted degradation of vaccinia-related kinase 1. [PDF]

Chem Sci
Yun Y, Gao Y, Shi Y, Zhang J.
europepmc   +1 more source

Development of Trivalent PROTACs Based on BRD4-targeting PROTACs

Development of Trivalent PROTACs Based on BRD4-targeting PROTACs
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The application of PROTAC in HDAC

European Journal of Medicinal Chemistry, 2023
Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great opportunities for scientific research and industrial applications. Histone deacetylase (HDAC)-PROTAC has been widely developed since the first report of its ability to induce the degradation of SIRT2 in 2017.
Shaoting Chen, Yuxiang Zheng, Benji Liang, Yudong Yin, Jian Yao, Quande Wang, Yanghan Liu, Nouri Neamati   +7 more
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The therapeutic potential of PROTACs

Expert Opinion on Therapeutic Patents, 2021
PROTACs represent a novel class of heterobifunctional molecules that simultaneously bind to a target protein and to an E3 ligase complex, resulting in the transfer of ubiquitin and initiating a process ultimately causing the proteasomal degradation of the target protein.
Andrew B, Benowitz, Katherine L, Jones, John D, Harling   +2 more
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Controlling PROTACs with Light

ChemMedChem, 2020
AbstractProteolysis targeting chimeras, PROTACs, are emerging as a powerful strategy for exerting exogenous control over protein levels, allowing small molecules to exploit the ubiquitin–proteasome pathway for targeted protein degradation. This highlight focuses on the fusion of photochemistry with these bifunctional compounds, which has provided a ...
Shreya Verma, Debasish Manna
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Optimization of a Series of RIPK2 PROTACs

Journal of Medicinal Chemistry, 2021
Receptor-interacting serine/threonine protein kinase 2 (RIPK2) is an important kinase of the innate immune system. Herein, we describe the optimization of a series of RIPK2 PROTACs which recruit members of the inhibitor of apoptosis (IAP) family of E3 ligases.
Afjal H. Miah, Ian E. D. Smith, Mark Rackham, Alina Mares, Aditya R. Thawani, Rakesh Nagilla, Pamela A. Haile, Bartholomew J. Votta, Laurie J. Gordon, Gillian Watt, Jane Denyer, Don T. Fisher, Phoebe Dace, Paul Giffen, Andrea Goncalves, Ian Churcher, Paul Scott-Stevens, John D. Harling   +17 more
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PROTACs: past, present and future

Chemical Society Reviews, 2022
This review highlights important milestones in the evolution of PROTACs, briefly discusses recent lessons about targeted protein degradation, and conjectures on the efforts still needed to expand the toolbox for PROTAC discovery.
Ke Li, Craig M. Crews
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PROTAC-ing tuberculosis

Nature Chemical Biology
Targeted protein degradation has emerged as a promising approach in drug discovery, harnessing a cell's intrinsic machinery to eliminate disease-related proteins. Now, a study paves the way to translating this technology into potential anti-mycobacterial therapies, by exploiting the bacterial protein-degradation complex.
Preti, Delia, Albanese, Valentina, Marconi, Peggy Carla Raffaella   +2 more
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PROTACs in Treatment of Cancer: A Review

Mini-Reviews in Medicinal Chemistry, 2021
Cancer treatment has become a major challenge amidst the resistance and relapse caused by the various treatments available. The PROteolysis TAargeting Chimera (PROTAC) technology involves the degradation of target protein against the inhibition by small drug molecules. The PROTACs with high potency and activity have been frequently reported; however,
Poonam Arora, Manjinder Singh, Varinder Singh, Shiveena Bhatia, Sandeep Arora   +4 more
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