منابع مشابه
Fluorescent ligands to investigate GPCR binding properties and oligomerization.
Fluorescent ligands for GPCRs (G-protein-coupled receptors) have been synthesized for a long time but their use was usually restricted to receptor localization in the cell by fluorescent imaging microscopy. During the last two decades, the emergence of new fluorescence-based strategies and the concomitant development of fluorescent measurement apparatus have dramatically widened the use of fluo...
متن کاملExcitements and challenges in GPCR oligomerization: molecular insight from FRET.
G protein-coupled receptors (GPCRs) are the largest family of proteins involved in signal transduction across cell membranes, and they represent major drug targets in all clinical areas. Oligomerization of GPCRs and its implications in drug discovery constitute an exciting area in contemporary biology. In this Review, we have highlighted the application of fluorescence resonance energy transfer...
متن کاملBiochemical and biophysical demonstration of GPCR oligomerization in mammalian cells.
In contrast to other families of cell surface receptors, like tyrosine kinase receptors, for which dimerization is an integral part of the activation process, G-protein-coupled receptors (GPCRs) were thought, until recently, to function as monomeric units. However, a growing body of evidence indicates that GPCRs could exist and be active as oligomeric complexes. Because they are major pharmacol...
متن کاملPathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
G-protein coupled receptors (GPCRs) are cell surface proteins responsible for translating >80% of extracellular reception to intracellular signals. The extracellular information in the form of neurotransmitters, peptides, ions, odorants etc is converted to intracellular signals via a wide variety of effector molecules activating distinct downstream signaling pathways. All GPCRs share common str...
متن کاملBRET and Time-resolved FRET strategy to study GPCR oligomerization: from cell lines toward native tissues
The concept of oligomerization of G protein-coupled receptor (GPCR) opens new perspectives regarding physiological function regulation. The capacity of one GPCR to modify its binding and coupling properties by interacting with a second one can be at the origin of regulations unsuspected two decades ago. Although the concept is interesting, its validation at a physiological level is challenging ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Current Opinion in Cell Biology
سال: 2019
ISSN: 0955-0674
DOI: 10.1016/j.ceb.2018.10.007