Results 21 to 30 of about 8,212 (230)
Novel approaches for the rational design of PROTAC linkers
Exploration of Targeted Anti-tumor Therapy, 2020 Proteolysis targeting chimeras (PROTACs) represent a promising class of hetero-bivalent molecules that facilitate ubiquitination of a target protein by simultaneously binding and bringing together both the E3 enzyme and the target.
Almaz Zagidullin +3 more
doaj +1 more source
Interdisciplinary Medicine, 2023 Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD) technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells.
Xuyang Zhao +3 more
doaj +1 more source
Frontiers in Pharmacology, 2022 Gastric cancer is a common malignant tumor that threatens human health, and its occurrence and development mechanism is a complex process involving multiple genes and multiple signals.
Haobin Li +14 more
doaj +1 more source
PROTAC-Design-Evaluator (PRODE): An Advanced Method for In-Silico PROTAC Design
ACS Omega, 2023 Abstract PROTAC (proteolysis-targeting chimeras) is a rapidly evolving technology to target undruggable targets. The mechanism by which this happens is when a bifunctional molecule binds to a target protein and also brings in proximity an E3 ubiquitin ligase to trigger ubiquitination and degradation of the target protein.
Ben Geoffrey A S +4 more
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BRD4-targeting PROTAC as a unique tool to study biomolecular condensates
Cell Discovery, 2023 Biomolecular condensates play key roles in various biological processes. However, specific condensation modulators are currently lacking. PROTAC is a new technology that can use small molecules to degrade target proteins specifically.
Yi Shi +8 more
doaj +1 more source
Targeting Protein Kinases Degradation by PROTACs
Frontiers in Chemistry, 2021 Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development.
Fei Yu +3 more
doaj +1 more source
PROTACs– a game-changing technology [PDF]
Expert Opinion on Drug Discovery, 2019 Introduction: Proteolysis - targeting chimeras (PROTACs) have emerged as a new modality with the potential to revolutionize drug discovery. PROTACs are heterobifunctional molecules comprising of a ligand targeting a protein of interest, a ligand targeting an E3 ligase and a connecting linker.
Konstantinidou, Markella +7 more
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Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope
Acta Pharmaceutica Sinica B, 2022 The proteolysis targeting chimeras (PROTACs) technology has been rapidly developed since its birth in 2001, attracting rapidly growing attention of scientific institutes and pharmaceutical companies. At present, a variety of small molecule PROTACs have entered the clinical trial.
Sinan Ma +10 more
openaire +3 more sources
Protacs for Treatment of Cancer [PDF]
Pediatric Research, 2010 Protein degradation is the cell's mechanism of eliminating misfolded or unwanted proteins. The pathway by which proteins are degraded occurs through the ubiquitin-proteasome system. Ubiquitin is a small 9-kD (kDa) protein that is attached to proteins. A minimum of four ubiquitins are required for proteins to be recognized by the degradation machinery ...
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PROTAC Technology: Opportunities and Challenges [PDF]
ACS Medicinal Chemistry Letters, 2020 PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions, large pharmaceutical enterprises (e.g., AstraZeneca, Bayer, Novartis, Amgen, Pfizer, GlaxoSmithKline, Merck, and Boehringer Ingelheim, etc.), and biotechnology companies.
Hongying Gao, Xiuyun Sun, Yu Rao
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