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PJ‑001, a small‑molecule proteolysis‑targeting chimera, ameliorates atopic dermatitis‑like inflammation in mice by inhibiting the JAK2/STAT3 pathway and repairing the skin barrier. [PDF]
Exp Ther MedLin P, Chen Z, Lu Y, Shi H, Lin J.
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Reversible Assembly of Proteolysis Targeting Chimeras
ACS Chemical Biology, 2023PROteolysis TArgeting Chimeras (PROTACs) are of significant current interest for the development of probe molecules and drug leads. However, they suffer from certain limitations. PROTACs are rule-breaking molecules with sub-optimal cellular permeability, solubility, and other drug-like properties.
Weijun Gui +4 more
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The rise of covalent proteolysis targeting chimeras
Current Opinion in Chemical Biology, 2021Targeted protein degradation offers several advantages over direct inhibition of protein activity and is gaining increasing interest in chemical biology and drug discovery. Proteolysis targeting chimeras (PROTACs) in particular are enjoying widespread application.
Ronen Gabizon, Nir London
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Proteolysis-Targeting Chimera Molecules Targeting SHP2
Future Medicinal Chemistry, 2022SHP2 is a member of the non-receptor protein tyrosine phosphatases, encoded by PTPN11, and exhibits oncogenic activities. The close association between SHP2 and human cancer has made SHP2 a promising target for clinical therapy. Proteolysis-targeting chimera (PROTAC) technology utilizes the degradation mechanism of the ubiquitin proteasome system to ...
Dandan Yu +4 more
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Advancing Strategies for Proteolysis-Targeting Chimera Design
Journal of Medicinal Chemistry, 2023Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by degrading various disease-causing proteins, particularly those related to tumors. Therefore, the introduction of PROTACs has ushered in a new chapter of antitumor drug development, marked by significant advances over recent years.
Minglei Li +3 more
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Proteolysis-targeting Chimeras for Targeting Protein for Degradation
Future Medicinal Chemistry, 2019Proteolysis-targeting chimeras (PROTACs) are an emerging tool for therapeutic intervention by reducing or eliminating disease-causing proteins. PROTACs are bifunctional molecules that consist of a target protein ligand, a linker and an E3 ligase ligand, which mediate the polyubiquitination of the target protein, ultimately leading to the target protein
Jianguo, Qi, Gang, Zhang
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Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras
Current Pharmaceutical Design, 2023Abstract: The most frequent mutated oncogene KRAS in lung cancer is targeted by KRAS G12C-directed drugs, such as Sotorasib and Adagrasib. Still, other alleles frequently expressed in pancreatic and colon cancer may be attacked indirectly by hitting the guanine nucleotide exchange factor (GEF) SOS1 that loads and activates KRAS.
Gerhard, Hamilton +2 more
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PROTAC (PROteolysis TArgeting Chimera)
La Chimica e l'Industria, 2022PROTAC technology represents the spearhead of Targeted Protein Degradation, a new paradigm that in the past recent years has become increasingly used in pharmacology. Characterized by a profoundly different mechanism of action compared to classic approaches, it can be useful in tackling elusive molecular targets and hopefully help dealing with ...
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Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies
Cancer Letters, 2022PROteolysis TArgeting Chimeras (PROTACs) degrade target proteins via the ubiquitin-proteasome system, providing novel insights into drug development for hematologic malignancies. PROTACs outperform conventional therapeutics and currently available small molecule inhibitors in terms of efficacy, tissue-and cell-selectivity, and side effect profile. Most
Yangping Wu +3 more
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Triazol: A Privileged Scaffold for Proteolysis Targeting Chimeras
Future Medicinal Chemistry, 2019Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown ...
Li-Wen Xia +8 more
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