RAMPs (receptor activity-modifying proteins) are single-pass transmembrane proteins that associate with certain family-B GPCRs (G-protein-coupled receptors). Specifically for the CT (calcitonin) receptor-like receptor and the CT receptor, this results in profound changes in ligand binding and receptor pharmacology, allowing the generation of six distinct receptors with preferences for CGRP (CT gene-related peptide), adrenomedullin, amylin and CT. There are three RAMPs: RAMP1–RAMP3. The N-terminus appears to be the main determinant of receptor pharmacology, whereas the transmembrane domain contributes to association of the RAMP with the GPCR. The N-terminus of all members of the RAMP family probably contains two disulphide bonds; a potential third disulphide is found in RAMP1 and RAMP3. The N-terminus appears to be in close proximity to the ligand and plays a key role in its binding, either directly or indirectly. BIBN4096BS, a CGRP antagonist, targets RAMP1 and this gives the compound very high selectivity for the human CGRP1 receptor.
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November 2004
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Conference Article|
October 26 2004
Heterodimers and family-B GPCRs: RAMPs, CGRP and adrenomedullin
A.C. Conner;
A.C. Conner
*School of Life and Health Sciences, Aston University, Birmingham B4 7ET, U.K.
†School of Biosciences, University of Birmingham, Birmingham B15 2TT, U.K.
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J. Simms;
J. Simms
*School of Life and Health Sciences, Aston University, Birmingham B4 7ET, U.K.
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D.L. Hay;
D.L. Hay
‡School of Biological Sciences, University of Auckland, Symonds Street, Auckland, New Zealand
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K. Mahmoud;
K. Mahmoud
*School of Life and Health Sciences, Aston University, Birmingham B4 7ET, U.K.
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S.G. Howitt;
S.G. Howitt
*School of Life and Health Sciences, Aston University, Birmingham B4 7ET, U.K.
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M. Wheatley;
M. Wheatley
†School of Biosciences, University of Birmingham, Birmingham B15 2TT, U.K.
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D.R. Poyner
D.R. Poyner
1
*School of Life and Health Sciences, Aston University, Birmingham B4 7ET, U.K.
1To whom correspondence should be addressed (email D.R.Poyner@aston.ac.uk).
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Publisher: Portland Press Ltd
Received:
June 15 2004
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2004 The Biochemical Society
2004
Biochem Soc Trans (2004) 32 (5): 843–846.
Article history
Received:
June 15 2004
Citation
A.C. Conner, J. Simms, D.L. Hay, K. Mahmoud, S.G. Howitt, M. Wheatley, D.R. Poyner; Heterodimers and family-B GPCRs: RAMPs, CGRP and adrenomedullin. Biochem Soc Trans 1 November 2004; 32 (5): 843–846. doi: https://doi.org/10.1042/BST0320843
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