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The therapeutic potential of PROTACs
Expert Opinion on Therapeutic Patents, 2021PROTACs 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 +2 more
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Controlling PROTACs with Light
ChemMedChem, 2020AbstractProteolysis 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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Drugtamer-PROTAC Conjugation Strategy for Targeted PROTAC Delivery and Synergistic Antitumor Therapy
Advanced ScienceProteolysis‐targeting chimeras (PROTACs) have emerged as a promising strategy for targeted protein degradation and drug discovery. To overcome the inherent limitations of conventional PROTACs, an innovative drugtamer‐PROTAC conjugation approach is ...
Chunquan Sheng +2 more
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The PROTAC technology in drug development [PDF]
Cell Biochemistry and Function, 2019 Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein.
Yinyin Wang
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From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation
PharmaceuticalsPROTAC is a rapidly developing engineering technology for targeted protein degradation using the ubiquitin–proteasome system, which has promising applications for inflammatory diseases, neurodegenerative diseases, and malignant tumors. This paper gives a
Chunyan Tian, Aihua Sun, Siqi Wang
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Optimization of a Series of RIPK2 PROTACs
Journal of Medicinal Chemistry, 2021Receptor-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 +17 more
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PROTACs: past, present and future
Chemical Society Reviews, 2022This 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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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 +2 more
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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 +2 more
openaire +3 more sources
PROTACs in Treatment of Cancer: A Review
Mini-Reviews in Medicinal Chemistry, 2021Cancer 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 +4 more
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Chemistries of bifunctional PROTAC degraders
Chemical Society Reviews, 2022Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins.
Chaoguo Cao +4 more
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