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International Union of Pharmacology. XXXII. The Mammalian Calcitonin Gene-Related Peptides, Adrenomedullin, Amylin, and Calcitonin Receptors
TLDR
A review of the calcitonin family of peptides aims to reconcile what is observed when the receptors are reconstituted in vitro with the properties they show in native cells and tissues.
Activation and allosteric modulation of a muscarinic acetylcholine receptor
TLDR
The structure of an agonist-bound, active state of the human M2 muscarinic acetylcholine receptor stabilized by a G-protein mimetic camelid antibody fragment isolated by conformational selection using yeast surface display reveals larger conformational changes in the extracellular region and orthosteric binding site than observed in the active states of the β2AR and rhodopsin.
Functional Selectivity and Classical Concepts of Quantitative Pharmacology
TLDR
Besides the heuristically interesting nature of functional selectivity, there is a clear impact on drug discovery, because this mechanism raises the possibility of selecting or designing novel ligands that differentially activate only a subset of functions of a single receptor, thereby optimizing therapeutic action.
Novel Receptor Partners and Function of Receptor Activity-modifying Proteins*
TLDR
These findings identify a new functional consequence of RAMP-receptor interaction, suggesting that RAMPs play a more general role in modulating cell signaling through other GPCRs than is currently appreciated.
G-Protein–Coupled Receptor Mas Is a Physiological Antagonist of the Angiotensin II Type 1 Receptor
TLDR
It is demonstrated that Mas can hetero-oligomerize with the AT1 receptor and by so doing inhibit the actions of angiotensin II, a novel demonstration that a G-protein–coupled receptor acts as a physiological antagonist of a previously characterized receptor.
Multiple amylin receptors arise from receptor activity-modifying protein interaction with the calcitonin receptor gene product.
TLDR
The data suggest that in the CT family of receptors, and potentially in other class II G protein-coupled receptors, the cellular phenotype is likely to be dynamic in regard to the level and combination of both the receptor and the RAMP proteins.
Emerging paradigms in GPCR allostery: implications for drug discovery
TLDR
New findings have the potential to alter how screening for allosteric drugs is performed and may increase the chances of success in the development ofallosteric modulators as clinical lead compounds.
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.
TLDR
How the concepts of collateral efficacy and permissive agonism-antagonism intersect the field of allosteric GPCR modulation is discussed, which could pave the way for not only receptor-selective but also signalling-pathway- selective therapies.
Allosteric modulation of G protein-coupled receptors: A pharmacological perspective
TLDR
The ever-expanding array of allosteric modulators arising from both academic and industrial research also highlights the need for the development of a uniform approach to nomenclature of such compounds.
GPCR modulation by RAMPs.
TLDR
This article aims to provide the reader with a comprehensive appraisal of RAMP literature and perhaps some insight into the impact that their discovery has had on those who study GPCRs.
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