- PII
- S0132342325010086-1
- DOI
- 10.31857/S0132342325010086
- Publication type
- Article
- Status
- Published
- Authors
- Volume/ Edition
- Volume 51 / Issue number 1
- Pages
- 82-93
- Abstract
- G protein-coupled receptors (GPCRs) are a family of heptahelical transmembrane proteins consisting of more than 800 representatives in the human genome that regulate most processes in the human body and are targets for up to a third of all modern drugs. Many GPCRs, despite their importance for pharmacology, are still considered orphan, i.e., their endogenous ligand is unknown. Orphan receptor GPR17, belonging to class A GPCR, is expressed mainly in the central nervous system, plays an important role in the formation of the myelin sheath of neurons and is a potential target for the development of new drugs against multiple sclerosis, Alzheimer's disease and ischemia. The aim of this work was to prepare GPR17 for structure-functional studies, starting with the heterologous expression and ending with obtaining a stable protein sample. Screening of various genetically engineered constructs was performed, a number of point mutations were analyzed, and a significant number of potential ligands of this receptor were tested. As a result of the work, the conditions for expression, isolation, and purification of GPR17 were optimized, which together made it possible to obtain a fairly stable and monomeric protein preparation suitable for further structural studies.
- Keywords
- GPCR GPR17 стабилизация белка
- Date of publication
- 09.11.2025
- Year of publication
- 2025
- Number of purchasers
- 0
- Views
- 46
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