Results 11 to 20 of about 419,478 (257)
Protein-protein interaction prediction for targeted protein degradation [PDF]
International Journal of Molecular Sciences, 2022 AbstractProtein-protein interactions (PPIs) play a fundamental role in various biological functions; thus, detecting PPI sites is essential for understanding diseases and developing new drugs. PPI prediction is of particular relevance for the development of drugs employing targeted protein degradation, as their efficacy relies on the formation of a ...
Oliver Orasch +5 more
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Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2
Nature Communications, 2023 The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties
Sarath Ramachandran +10 more
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Targeting proteins for degradation [PDF]
Nature Chemical Biology, 2009 Protein degradation plays a central role in many cellular functions. Misfolded and damaged proteins are removed from the cell to avoid toxicity. The concentrations of regulatory proteins are adjusted by degradation at the appropriate time. Both foreign and native proteins are digested into small peptides as part of the adaptive immune response.
Erin K, Schrader +2 more
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A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
Nature Communications, 2022 Protein degraders are an emerging drug modality; however, their properties lie beyond typical drug-like space. Here the authors report optimisation via structure-based exit vector and linker design towards the VHL-recruiting PROTAC ACBI2, an orally ...
Christiane Kofink +29 more
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mBio, 2022 The human pathogen Pseudomonas aeruginosa (Pa) is one of the most frequent and severe causes of nosocomial infection. This organism is also a major cause of airway infections in people with cystic fibrosis (CF). Pa is known to have a remarkable metabolic
Stephen K. Dolan +7 more
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Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future
Molecules, 2022 The PROteolysis TArgeting Chimeras (PROTACs) is an innovative technique for the selective degradation of target proteins via the ubiquitin–proteasome system.
Rui Li +5 more
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A TRIM21-based method for targeted protein degradation [PDF]
Acta Biochimica et Biophysica SinicaHu Weikang +6 more
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Modular Assembled Targeting Chimera Enables Multimodal Targeted Protein Degradation [PDF]
JACS AuWentao Zhu +5 more
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Chemical-Mediated Targeted Protein Degradation in Neurodegenerative Diseases
Life, 2021 Neurodegenerative diseases, including Alzheimer’s disease, Huntington’s disease, and Parkinson’s disease, are a class of diseases that lead to dysfunction of cognition and mobility.
Soonsil Hyun, Dongyun Shin
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