Results 21 to 30 of about 11,335 (243)
PROTACs in gastrointestinal cancers
Molecular Therapy - Oncolytics, 2022 Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase ligand covalently linked to a protein of interest (POI) via a linker. PROTAC can induce ubiquitinated proteasomal degradation of proteins by hijacking the ubiquitin-proteasome ...
Yu Chen +19 more
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AI-Based Prediction of PROTAC- and Molecular Glue-Mediated Ternary Complexes: A Comparative Evaluation of AlphaFold 3 and Boltz-2. [PDF]
Arch Pharm (Weinheim)Superposition of the lowest RMSD predictions for the ternary complex of SMARCA2‐VHL. The AlphaFold 3 prediction is shown in cyan, the Boltz‐2 prediction in pink, and the reference X‐ray structure in green. ABSTRACT Proteolysis targeting chimeras (PROTACs) and molecular glues induce ligand‐mediated ternary complexes between an E3 ubiquitin ligase and a ...
Riepenhausen L +3 more
europepmc +2 more sources
PROTACs targeting epigenetic proteins
Acta Materia Medica, 2023 The field of epigenetics pertains to alterations in gene function that are inherited without changes in the DNA sequence, including histone modifications, post-translational modifications of amino acids, and covalent modifications of DNA bases. These alteration pathways modulate the transformation of genotypes into specific phenotypes.
Chao Zhang +5 more
openaire +3 more sources
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
PROTACs: A novel strategy for cancer drug discovery and development
MedComm, 2023 Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists of three components: a small molecule that binds to a target protein, an ...
Xin Han, Yi Sun
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
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
Journal of Hematology & Oncology, 2020 Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently ...
Xin Li, Yongcheng Song
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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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
PROTAC-Induced Proteolytic Targeting [PDF]
, 2012 Small-molecule modulators of protein activity are increasingly being utilized as tools to examine the functional roles of proteins. Operating at the post-translational level, these molecules provide enhanced temporal and spatial control and mitigate the potential for compensatory responses in comparison with classical genetic approaches.
Kimberly Cornish, Carmony, Kyung-Bo, Kim
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