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  • Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling

    While GPCRs can exist as monomers, some types, like class C GPCRs, are obligate dimers, either as homodimers The possibility of dimerization in class A and class B GPCRs, however, has been more controversial, despite Class B1 GPCRs are an important subclass of GPCRs that include 15 receptors involved in regulating body Recent studies suggest that class B1 GPCRs can form both homodimers and heterodimers, which may play Examples of class B1 GPCRs forming homodimers include the secretin receptor (SecR)[6] and GLP-1R [7],

  • Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembra

    G protein-coupled receptors (GPCRs) are among the most promising drug targets. Specifically controlling the activity of GPCR dimers with ligands is a good approach to clarify their This region corresponds to the sodium ion binding site in class A GPCRs that controls the basal state reveal the possibility of developing allosteric compounds able to specifically modulate the activity of GPCR

  • Lipid Modulation of a Class B GPCR: Elucidating the Modulatory Role of PI(4,5)P 2 Lipids

    A G-protein coupled receptors (GPCRs) through a conserved binding site, not present in class B GPCRs For class B GPCRs, previous molecular dynamics (MD) simulation studies have shown PI(4,5)P2 interacting Interestingly, we find that in contrast to class A GPCRs, PI(4,5)P2 appear to stabilize the inactive conformation of GCGR through a binding site conserved across class B GPCRs but absent in class A GPCRs This suggests differences in the regulatory function of PI(4,5)P2 between class A and class B GPCRs."

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