Heterodimers and Family B GPCRs, CGRP and adrenomedullin

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Heterodimers and Family B GPCRs, CGRP and adrenomedullin. / Conner, Alex; Simms, JH; Hay, DL; Mahmoud, K; Wheatley, Mark; Poyner, DR.

In: Biochemical Society Transactions, Vol. 32, 01.01.2004, p. 843-846.

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Conner, Alex ; Simms, JH ; Hay, DL ; Mahmoud, K ; Wheatley, Mark ; Poyner, DR. / Heterodimers and Family B GPCRs, CGRP and adrenomedullin. In: Biochemical Society Transactions. 2004 ; Vol. 32. pp. 843-846.

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@article{e22b4a67b53b42769e19a0b0249055a0,
title = "Heterodimers and Family B GPCRs, CGRP and adrenomedullin",
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.",
keywords = "calcitonin receptor-like receptor, RAMP3, calcitonin gene-related peptide (CGRP), RAMP2, receptor activity-modifying protein 1 (RAMP1), adrenomedullin",
author = "Alex Conner and JH Simms and DL Hay and K Mahmoud and Mark Wheatley and DR Poyner",
year = "2004",
month = "1",
day = "1",
doi = "10.1042/BST0320843",
language = "English",
volume = "32",
pages = "843--846",
journal = "Biochemical Society Transactions",
issn = "1470-8752",
publisher = "Portland Press",

}

RIS

TY - JOUR

T1 - Heterodimers and Family B GPCRs, CGRP and adrenomedullin

AU - Conner, Alex

AU - Simms, JH

AU - Hay, DL

AU - Mahmoud, K

AU - Wheatley, Mark

AU - Poyner, DR

PY - 2004/1/1

Y1 - 2004/1/1

N2 - 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.

AB - 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.

KW - calcitonin receptor-like receptor

KW - RAMP3

KW - calcitonin gene-related peptide (CGRP)

KW - RAMP2

KW - receptor activity-modifying protein 1 (RAMP1)

KW - adrenomedullin

UR - http://www.scopus.com/inward/record.url?scp=8744300052&partnerID=8YFLogxK

U2 - 10.1042/BST0320843

DO - 10.1042/BST0320843

M3 - Article

C2 - 15494030

VL - 32

SP - 843

EP - 846

JO - Biochemical Society Transactions

JF - Biochemical Society Transactions

SN - 1470-8752

ER -