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Abstract
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 CGRP(1) receptor.
Original language | English |
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Pages (from-to) | 843-846 |
Number of pages | 4 |
Journal | Biochemical Society Transactions |
Volume | 32 |
DOIs | |
Publication status | Published - 1 Jan 2004 |
Keywords
- calcitonin receptor-like receptor
- RAMP3
- calcitonin gene-related peptide (CGRP)
- RAMP2
- receptor activity-modifying protein 1 (RAMP1)
- adrenomedullin
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Dive into the research topics of 'Heterodimers and Family B GPCRs, CGRP and adrenomedullin'. Together they form a unique fingerprint.Projects
- 1 Finished
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Structural Analysis of RAMPs and their Role in CGRP Binding
Wheatley, M.
Biotechnology & Biological Sciences Research Council
1/01/04 → 31/12/06
Project: Research Councils