Results 51 to 60 of about 504,547 (295)
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
Recruitment of Cbl-b to B cell antigen receptor couples antigen recognition to Toll-like receptor 9 activation in late endosomes. [PDF]
PLoS ONE, 2014 Casitas B-lineage lymphoma-b (Cbl-b) is a ubiquitin ligase (E3) that modulates signaling by tagging molecules for degradation. It is a complex protein with multiple domains and binding partners that are not involved in ubiquitinating substrates.
Margaret Veselits +7 more
doaj +1 more source
Exploring the Target Scope of KEAP1 E3 Ligase-based PROTACs
Cell Chemical Biology, 2022 SUMMARY: Targeted protein degradation (TPD) uses small molecules to recruit E3 ubiquitin ligases into proximity of proteins of interest, inducing ubiquitination-dependent degradation.
Guang-Yan Du +18 more
semanticscholar +1 more source
, 2022 Proteolysis-targeting chimeras (PROTACs) are novel therapeutics for the treatment of human disease. They exploit the enormous potential of the E3 ligases, a class of proteins that mark a target protein for degradation via the ubiquitin-proteasome system.
Cross, Simon +9 more
core +1 more source
ChemBioChem, 2023 Proteolysis targeting chimeras (PROTACs) are a promising therapeutic strategy to selectively promote the degradation of protein targets by exploiting the ubiquitin‐proteasome system. Among the limited number of E3 ligase ligands discovered for the PROTAC
Chelsi M. Almodóvar-Rivera +7 more
semanticscholar +1 more source
Functional Diversity and Structural Disorder in the Human Ubiquitination Pathway [PDF]
, 2013 The ubiquitin-proteasome system plays a central role in cellular regulation and protein quality control (PQC). The system is built as a pyramid of increasing complexity, with two E1 (ubiquitin activating), few dozen E2 (ubiquitin conjugating) and several
Mainak Guharoy +15 more
core +1 more source
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay [PDF]
ACS Medicinal Chemistry Letters, 2020 Abstract Repurposing E3 ubiquitin ligases for targeted protein degradation via customized molecular glues or proteolysis-targeting chimeras (PROTACs) is an increasingly important therapeutic modality. Currently, a major limitation in the design of suitable molecular glues and PROTACs is our fragmentary understanding of E3 ligases and ...
Samuel Maiwald +3 more
openaire +3 more sources
Inhibition of PDGF-B induction and cell growth by syndecan-1 involves the ubiquitin and SUMO-1 ligase, Topors. [PDF]
PLoS ONE, 2012 Syndecans are receptors for soluble ligands, including heparin-binding growth factors, and matrix proteins. However, intracellular targets of syndecan-1 (Sdc-1)-mediated signaling are not fully understood. A yeast two-hybrid protein interaction screening
Kathleen R Braun +7 more
doaj +1 more source
bioRxiv, 2023 We have developed a novel chemical handle (PFI-E3H1) and a chemical probe (PFI-7) as ligands for the Gid4 subunit of the human E3 ligase CTLH degradation complex.
A. K. Yazdi +25 more
semanticscholar +1 more source
Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2
Nature Communications, 2023 Abstract 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 of phosphate and its mimetics.
Sarath Ramachandran +10 more
openaire +5 more sources