PROTACs: Current Trends in Protein Degradation by Proteolysis-Targeting Chimeras
BioDrugs, 2022In the recent past, proteolysis-targeting chimera (PROTAC) technology has received enormous attention for its ability to overcome the limitations of protein inhibitors and its capability to target undruggable proteins. The PROTAC molecule consists of three components, a ubiquitin E3 ligase ligand, a linker, and a target protein ligand.
Jyotsana Madan +5 more
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Proteolysis Targeting Chimera (PROTAC) Design
2023In this chapter, carefully selected examples have been elaborated to illustrate how proteolysis targeting chimeras (PROTACs) can be elegantly developed based upon pre-existing active site-directed inhibitors for different types of enzymatic reactions involved in various life processes and therapeutic areas.
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Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs)
Drug Discovery Today, 2023Proteolysis targeting chimeras (PROTACs) have been extensively explored for targeted proteasomal degradation of disease-related proteins with enormous potential in the treatment of intractable diseases. However, PROTACs are poorly soluble and permeable bulky molecules facing several bioavailability challenges irrespective of the route of administration.
Aishwarya L, Saraswat +4 more
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Proteolysis-targeting chimera (PROTAC): A promising senolytic strategy
Ageing Research ReviewsSenescent cells (SCs) accumulate with aging and contribute to the development of age-related pathologies. These cells evade apoptosis through upregulation of senescent cell anti-apoptotic pathways (SCAPs), making their selective elimination, a strategy termed senolysis, a promising therapeutic avenue.
Gang Fan +6 more
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Discovery of a proteolysis targeting chimera (PROTAC) as a potent regulator of FOXP3
Bioorganic & Medicinal Chemistry LettersRegulatory T (Treg) cells play a central role in immune homeostasis. Forkhead box P3 (Foxp3), a hallmark molecule in Treg cells, is a vital transcription factor for their development and function. Studies have shown that degradation of the Foxp3 could provide therapeutic benefits in achieving effective anti-tumor immunity.
Bowen, Yang +9 more
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Proteolysis-Targeting Chimera (PROTAC): A Revolutionary Tool for Chemical Biology Research
Small MethodsAbstract Proteolysisâtargeting chimera (PROTAC) technology is a revolutionary tool for drug discovery that simultaneously recruits E3 ligase and the protein of interest to induce ubiquitination and subsequent proteasomal degradation. Since the inaugural PROTAC prototype emerged in 2001, this modality has garnered significant interest ...
Hongwei Hou, Li Jinghong
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Investigating the cell permeability of proteolysis-targeting chimeras (PROTACs)
Expert Opinion on Drug Discovery, 2023Hidetomo Yokoo +2 more
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Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs)
Mendeleev Communications, 2022Olga Bakulina +3 more
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Anti-apoptotic Proteolysis Targeted Chimeras (PROTACs) in Cancer Therapy
Medical Research ArchivesTargeted protein degradation is an emerging approach for novel drug discovery and basic research. Several degrader molecules have been developed including PROteolysis-TArgeting Chimeras (PROTACs), specific and nongenetic Inhibitor of APoptosis protein (IAP)-dependent Protein ERasers (SNIPERs), IAP antagonists, deubiquitylase inhibitors, hydrophobic ...
Muturi Njoka +2 more
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Selective CDK9 Degradation Using a Proteolysis-Targeting Chimera (PROTAC) Strategy
Future Medicinal Chemistry, 2021Jayapal Reddy Mallareddy +3 more
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