Amylin receptors: molecular composition and pharmacology

2004 ◽  
Vol 32 (5) ◽  
pp. 865-867 ◽  
Author(s):  
D.L. Hay ◽  
G. Christopoulos ◽  
A. Christopoulos ◽  
P.M. Sexton
Keyword(s):  
Molecular Composition ◽  
Receptor Activity ◽  
Calcitonin Receptor ◽  
High Affinity

Several receptors which bind the hormone AMY (amylin) with high affinity have now been identified. The minimum binding unit is composed of the CT (calcitonin) receptor at its core, plus a RAMP (receptor activity modifying protein). The receptors have been named AMY1(a), AMY2(a) and AMY3(a) in accordance with the association of the CT receptor (CT(a)) with RAMP1, RAMP2 and RAMP3 respectively. The challenge is now to determine the localization and pharmacological nature of each of these receptors. Recent attempts to achieve these aims will be briefly discussed.

scholarly journals Immunohistochemical Localization of Calcitonin Receptor–Like Receptor and Receptor Activity–Modifying Proteins in the Human Cerebral Vasculature

2002 ◽  
Vol 22 (5) ◽  
pp. 620-629 ◽  
Author(s):  
Kevin R. Oliver ◽  
Anna Wainwright ◽  
Lars Edvinsson ◽  
John D. Pickard ◽  
Raymond G. Hill
Keyword(s):  
Calcitonin Gene Related Peptide ◽  
Immunohistochemical Localization ◽  
Receptor Activity ◽  
Cell Surface Expression ◽  
Cerebral Vasculature ◽  
Calcitonin Receptor ◽  
Trigeminovascular System ◽  
High Affinity ◽  
Related Peptide ◽  
Calcitonin Gene

Calcitonin gene-related peptide and adrenomedullin belong to a structurally related neuropeptide family and are potent vasodilators expressed in the trigeminovascular system. The molecular identity of receptors for these proteins has only recently been elucidated. Central to functional binding of these neuropeptides is the G-protein–coupled receptor, the calcitonin receptor–like receptor (CRLR), whose cell surface expression and pharmacology is determined by coexpression of a receptor activity-modifying protein (RAMP). CRLR combined with RAMP1 binds calcitonin gene-related peptide with high affinity, whereas CRLR coexpression with RAMP2 or −3 confers high-affinity binding of adrenomedullin. The authors investigated the expression of these receptor components in human cerebral vasculature to further characterize neuropeptide receptor content and the potential functions of these receptors. Localization has been carried out using specific antisera raised against immunogenic peptide sequences that were subsequently applied using modern immunohistochemical techniques and confocal microscopy. The results are the first to show the presence of these receptor component proteins in human middle meningeal, middle cerebral, pial, and superficial temporal vessels, and confirm that both calcitonin gene-related peptide and adrenomedullin receptors may arise from the coassembly of RAMPs with CRLR in these vessel types. These novel data advance the understanding of the molecular function of the trigeminovascular system, its potential role in vascular headache disorders such as migraine, and may lead to possible ways in which future synthetic ligands may be applied to manage these disorders.

scholarly journals Agonist-promoted Internalization of a Ternary Complex between Calcitonin Receptor-like Receptor, Receptor Activity-modifying Protein 1 (RAMP1), and β-Arrestin

2001 ◽  
Vol 276 (45) ◽  
pp. 42182-42190 ◽  
Author(s):  
Sandrine Hilairet ◽  
Charlène Bélanger ◽  
Johanne Bertrand ◽  
André Laperrière ◽  
Steven M. Foord ◽  
...  
Keyword(s):  
Ternary Complex ◽  
Receptor Activity ◽  
Calcitonin Receptor

Receptor Activity Modifying Proteins Have Limited Effects on the Class B G Protein-Coupled Receptor Calcitonin Receptor-Like Receptor Stalk

Biochemistry ◽  
2018 ◽  
Vol 57 (8) ◽  
pp. 1410-1422 ◽  
Author(s):  
Michael L. Garelja ◽  
Christina A. Walker ◽  
Andrew Siow ◽  
Sung H. Yang ◽  
Paul W.R. Harris ◽  
...  
Keyword(s):  
G Protein ◽  
Receptor Activity ◽  
Calcitonin Receptor ◽  
G Protein Coupled Receptor ◽  
Class B ◽  
Receptor Activity Modifying Proteins ◽  
G Protein Coupled

scholarly journals Post-endocytic Sorting of Calcitonin Receptor-like Receptor and Receptor Activity-modifying Protein 1

2007 ◽  
Vol 282 (16) ◽  
pp. 12260-12271 ◽  
Author(s):  
Graeme S. Cottrell ◽  
Benjamin Padilla ◽  
Stella Pikios ◽  
Dirk Roosterman ◽  
Martin Steinhoff ◽  
...  
Keyword(s):  
Receptor Activity ◽  
Calcitonin Receptor ◽  
Endocytic Sorting

Multiple Amylin Receptors Arise from Receptor Activity-Modifying Protein Interaction with the Calcitonin Receptor Gene Product

1999 ◽  
Vol 56 (1) ◽  
pp. 235-242 ◽  
Author(s):  
George Christopoulos ◽  
Katie J. Perry ◽  
Maria Morfis ◽  
Nanda Tilakaratne ◽  
Yongyi Gao ◽  
...  
Keyword(s):  
Gene Product ◽  
Protein Interaction ◽  
Receptor Gene ◽  
Receptor Activity ◽  
Calcitonin Receptor ◽  
Calcitonin Receptor Gene
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