PEPTIDE TAGS FOR LIGAND INDUCED DEGRADATION OF FUSION PROTEINSDescribed herein are compositions and methods for modulating protein abundance in a target-specific manner via degron tags.JAN MaxEBERT Benjamin L.FISCHER EricNOWAK Radoslaw
Heterobifunctional small-molecule degraders that induce protein degradation through ligase-mediated ubiquitination have shown considerable promise as a new pharmacological modality. However, we currently lack a detailed understanding of the molecular bas
F. (1983) Ligand-induced rapid redistribution of lysosomes is temporally distinct from endosome translocation. Nature 304: pp. 738-40Herman, B. and Albertini, D.F., Ligand-induced rapid redistribution of lysosomes is temporally distinct from endosome translocation. Nature, 304 (1983) 738-740....
Coexpression of p75 NTR attenuated ubiquitination of TrkA and TrkB and delayed nerve growth factor-induced TrkA receptor internalization and receptor degradation. These results indicate that p75 NTR may prolong cell-surface Trk-dependent signalling events by negatively regulating receptor ubiquitination. ...
The real time dynamics of vanilloid-induced cytotoxicity and the specific deletion of nociceptive neurons expressing the wild-type vanilloid receptor (VR1) were investigated. VR1 was C-terminally tagged with either the 27-kDa enhanced green fluorescent protein (eGFP) or a 12-amino acid ε-epitope...
3.2. Ligand-induced changes in tryptophan fluorescence To investigate the effect on the Trp fluorescence spectrum of ligands binding to the A2AR encapsulated in a SMALP, two ligands possessing different pharmacological properties (efficacy) were employed; i) ZM241385, an A2AR-selective inverse agonis...
Our results demonstrate that E4T and TGF伪 provoke decreased Cbl recruitment, EGFR ubiquitination and EGFR degradation compared with EGF. Furthermore, bafilomycin treatment blocks EGFR but not c-Cbl degradation. In contrast, lactacystin treatment blocks EGF-induced c-Cbl degradation but does not ...
Thus, the two leptin receptor isoforms, ObRa and ObRb, mediate leptin internalization by a coated pit-dependent mechanism, leptin degradation by a lysosomal pathway, and ligand-induced receptor downregulation. The differential capacity of the two receptor isoforms may relate to the different roles of...
The ligand-induced processing takes place in endosomes and involves the rapid degradation of the extracellular EphB2. EphrinB ligand stimulates ubiquitination of EphB2 receptor. Calcium influx- and N-methyl-d-aspartic acid-induced processing of EphB2 is inhibited by GM6001 and ADAM10 inhibitors but...
The dppf-induced polyhedral opening attendant in the formation of Ru6(μ6-C)(CO)15(μ-dppf) suggests that other diphosphine ligands have the potential to function similarly, which could in turn expose reactive ruthenium sites within an intact molecular cluster capable of participation in unusual ...