Abstract：
:An increasing number of genetic diseases are found to result from mutations that lead to retention of the affected proteins in the endoplasmic reticulum, where they are recognized as misfolded by the quality control system. Several of these conformational diseases involve mutations in G-protein-coupled receptors. Recent studies demonstrated that pharmacologically selective compounds, termed pharmacological chaperones, can stabilize the misfolded receptors, facilitating their export from the endoplasmic reticulum to the plasma membrane, where they can be active. Such functional rescue suggests that pharmacological chaperones could represent novel therapeutic agents for the treatment of conformational diseases. Although only a few examples are currently available, the observation that pharmacological chaperones can also favour the folding of wild-type G-protein-coupled receptors indicates that these compounds could have wide applications.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Bernier V,Bichet DG,Bouvier Mdoi
10.1016/j.coph.2004.08.001keywords:
subject
Has Abstractpub_date
2004-10-01 00:00:00pages
528-33issue
5eissn
1471-4892issn
1471-4973pii
S1471-4892(04)00131-6journal_volume
4pub_type
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