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Nature Chemical Biology (4)
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Showing 1–6 of 6 results

Advanced filters: Author: Frederic G. Jean-Alphonse Clear advanced filters

Endosomal GPCR signaling turned off by negative feedback actions of PKA and v-ATPase

A GPCR, the parathyroid hormone receptor, can elicit a sustained signal from internal membranes after internalization. The signal was found to be terminated by a feedback mechanism where PKA activates the proton pump v-ATPase, which acidifies endosomes.

Alexandre Gidon
Mohammad M Al-Bataineh
Jean-Pierre Vilardaga
Research27 Jul 2014
Nature Chemical Biology

Volume: 10, P: 707-709
PTH hypersecretion triggered by a GABA_B1 and Ca²⁺-sensing receptor heterocomplex in hyperparathyroidism

Parathyroid glands regulate calcium homeostasis by secreting parathyroid hormone. Chang et al. demonstrate that in parathyroid glands GABA receptor GABAB1R makes a heterocomplex with the calcium-sensing receptor and regulates the secretion of parathyroid hormone.

Wenhan Chang
Chia-Ling Tu
Jean-Pierre Vilardaga
Research09 Mar 2020
Nature Metabolism

Volume: 2, P: 243-255
Allosteric interactions in the parathyroid hormone GPCR–arrestin complex formation

Characterization of the interaction between PTH and its G-protein-coupled receptor, PTHR, shows conformational changes coupled to residues interacting with His9, which helps position the PTH N terminus at the PTHR transmembrane domain to facilitate β-arrestin coupling.

Lisa J. Clark
James Krieger
Jean-Pierre Vilardaga
Research06 Jul 2020
Nature Chemical Biology

Volume: 16, P: 1096-1104
β₂-adrenergic receptor control of endosomal PTH receptor signaling via Gβγ

The synergistic effect of the GPCR β₂AR on signaling through another GPCR, PTHR, is explained by the release of Gβγ from the heterotrimeric Gα_iβγ protein, activating adenylate cyclase AC2 and subsequent prolonged cAMP signaling in internal compartments

Frédéric G Jean-Alphonse
Vanessa L Wehbi
Jean-Pierre Vilardaga
Research26 Dec 2016
Nature Chemical Biology

Volume: 13, P: 259-261
Targeting the activated allosteric conformation of the endothelin receptor B in melanoma with an antibody-drug conjugate: mechanisms and therapeutic efficacy

Amaury Herbet
Marie Hautière
Didier Boquet
ResearchOpen Access20 Jan 2025
BJC Reports

Volume: 3, P: 1-11
Endosomal generation of cAMP in GPCR signaling

Besides signaling from the plasma membrane, evidence for noncanonical signaling by GPCRs from internal compartments has recently emerged and is highlighted in this Perspective. For the well-studied PTHR, agonists stabilize a distinct receptor conformation within endosomes, leading to sustained signaling.

Jean-Pierre Vilardaga
Frederic G Jean-Alphonse
Thomas J Gardella
Reviews18 Aug 2014
Nature Chemical Biology

Volume: 10, P: 700-706