Search Results

Concentration-response analysis: Become a CRC super-user Module 2 - Quantifying agonist pharmacology and biased

bound to these interaction partners available today do not reveal a clear conformational basis for signaling bias, which would have enabled the rational design of biased GRCR ligands. different types of partners rather than the structures of the final complexes might underlie transducer bias

or β-arrestin signaling pathways, are leading to the development of drugs with superior efficacy and Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling Our previous work demonstrated that GPR3-mediated β-arrestin signaling modulates amyloid-β (Aβ) generation consequences of selective elimination of GPR3-mediated β-arrestin signaling in vivo. We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease

Currently, attention was mainly paid to biased signaling modulators targeting G protein-coupled receptors The biased signaling modulation of non-GPCR receptors has yet to be exploited. receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent signaling Small molecules biasedly modulating the TLR4 signaling axis not only provide probes to fine-tune receptor conformation and signaling but also provide an opportunity to identify promising drug candidates.

In the Rajagopal Lab, Julia studies the mechanisms of 'biased signaling' at GPCRs, with a specific focus GRKs) can translocate to endosomes, and that the subcellular localization of the GRKs affects a GPCR's biased signaling profile.

receptors, in particular, the ligand identification, physiological functions and molecular mechanism of biased signaling of GPCRs. For arrestin mediated biased signaling, we have proposed the “flute model” and “poly proline region docking

since January 2021 and has contributed to multiple projects exploring the underlying mechanisms of biased signaling at chemokine receptor 3 (CXCR3). These previous endeavors involved exploring the effect of subcellular location on the signaling profile in the differential signaling outputs of biased agonists, and demonstrating the ligand specificity behind She is currently working on her senior thesis which involves identifying the non-canonical signaling