Author:
Raynaud Pauline,Jugnarain Vinesh,Vaugrente Océane,Vallet Amandine,Boulo Thomas,Gauthier Camille,Inoue Asuka,Sibille Nathalie,Gauthier Christophe,Jean-Alphonse Frédéric,Reiter Eric,Crépieux Pascale,Bruneau Gilles
Abstract
AbstractIntracellular variable fragments from heavy-chain antibody from camelids (intra-VHH) have been successfully used as chaperones to solve the 3D structure of active G protein-coupled receptors bound to their transducers. However, their effect on signalling has been poorly explored, although they may provide a better understanding on the relationships between receptor conformation and activity. Here, we isolated and characterized iPRC1, the first intra-VHH recognizing a member of the large glycoprotein hormone receptors family, the follicle-stimulating hormone receptor (FSHR). This intra-VHH recognizes the FSHR 3rdintracellular loop and decreases cAMP production in response to FSH, without altering Gαs recruitment. Hence, iPRC1 behaves as an allosteric modulator and provides a new tool to complete structure/activity studies performed so far on this receptor.
Publisher
Cold Spring Harbor Laboratory
Cited by
1 articles.
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