en
Doctoral thesis
English

Use of chemokines and chemokine analogs to study intracellular C-terminal phosphorylation and arrestin recruitment to CCR5

ContributorsMartins, Elsa
Defense date2020-01-17
Abstract

CCR5 is a chemokine receptor belonging to the superfamily of GPCRs, which are involved in various physiological/pathological processes. Upon agonist activation GPCRs trigger the activation of G proteins, followed by receptor intracellular phosphorylation and recruitment of arrestins. Arrestins are cytosolic proteins responsible for blocking G protein-mediated signalling, orchestrating receptor desensitization/post-endocytic intracellular trafficking and activating G protein-independent signalling. The capacity of certain ligands to preferentially elicit the G protein over the arrestin pathway, or vice versa, is designated ligand bias and is of great importance for drug discovery. A better understanding of (i) how arrestin recruitment to GPCRs is regulated, (ii) the potential role of phosphorylation patterns in that process as well as (iii) the phenomenon of ligand bias is required in the GPCR field, using new receptor models and well-characterized ligands. Here a panel of CCR5 chemokine analogs discovered and optimized by our group was used to investigate these phenomena.

eng
Keywords
  • GPCR
  • CCR5
  • Arrestin
  • Chemokine receptor
  • Chemokine analogs
Citation (ISO format)
MARTINS, Elsa. Use of chemokines and chemokine analogs to study intracellular C-terminal phosphorylation and arrestin recruitment to CCR5. 2020. doi: 10.13097/archive-ouverte/unige:139677
Main files (1)
Thesis
accessLevelRestricted
Identifiers
267views
16downloads

Technical informations

Creation06/30/2020 10:12:00 AM
First validation06/30/2020 10:12:00 AM
Update time03/12/2024 4:18:49 PM
Status update03/12/2024 4:18:49 PM
Last indexation03/12/2024 4:18:50 PM
All rights reserved by Archive ouverte UNIGE and the University of GenevaunigeBlack