Receptor activity-modifying protein
Receptor activity-modifying proteins (RAMPs) are a class of protein that interact with and modulate the activities of several Class B G Protein-Coupled Receptors including the receptors for secretin, calcitonin (CT), glucagon, and vasoactive intestinal peptide (VIP).[1] There are three distinct types of RAMPs, designated RAMP1, RAMP2, and RAMP3, each encoded by a separate gene.[2]
Function
Currently, the function of RAMPs is divided into classes of activities. When associated with the Calcitonin receptor (CTR) or Calcitonin receptor-like (CALCRL) (below), RAMPs can change the selectivity of the receptor for a specific hormone. In the cases of the other receptors mentioned, however, there is no evidence that they can do this, but instead function to regulate trafficking of receptors from the ER / golgi to the membrane. These functions appear to be ones where there is redundancy, as neither RAMP1 nor RAMP3 knockout mice (KO) have grossly abnormal phenotypes. The likelihood is that the phenotype of RAMP2 KO mice is more connected with the abolition of most adrenomedullin (AM) signalling than effects on trafficking of other receptors, as those mice are almost identical to AM KO mice.
Types
Association of RAMPs with either the CT or CALCRL proteins forms 6 different receptors from the calcitonin receptor family:[3][4][5]
References
- ↑ Sexton PM, Morfis M, Tilakaratne N, Hay DL, Udawela M, Christopoulos G, Christopoulos A (2006). "Complexing receptor pharmacology: modulation of family B G protein-coupled receptor function by RAMPs". Ann N Y Acad Sci. 1070: 90–104. PMID 16888151. doi:10.1196/annals.1317.076.
- ↑ Young A (2005). "Amylin: Physiology and Pharmacology; Chapter 3: Receptor pharmacology". Advances in Pharmacology. Advances in Pharmacology. 52: 47–65. ISBN 978-0-12-032954-0. PMID 16492540. doi:10.1016/S1054-3589(05)52003-9.
- ↑
- ↑ McLatchie LM, Fraser NJ, Main MJ, Wise A, Brown J, Thompson N, Solari R, Lee MG, Foord SM (May 1998). "RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor". Nature. 393 (6683): 333–9. PMID 9620797. doi:10.1038/30666.
- ↑ Foord SM, Marshall FH (May 1999). "RAMPs: accessory proteins for seven transmembrane domain receptors". Trends Pharmacol. Sci. 20 (5): 184–7. PMID 10354609. doi:10.1016/S0165-6147(99)01347-4.
- ↑ Kamitani S, Asakawa M, Shimekake Y, Kuwasako K, Nakahara K, Sakata T (April 1999). "The RAMP2/CRLR complex is a functional adrenomedullin receptor in human endothelial and vascular smooth muscle cells". FEBS Lett. 448 (1): 111–4. PMID 10217420. doi:10.1016/S0014-5793(99)00358-0.
External links
|
---|
Adiponectin | AdipoR1 |
- Antagonists: Peptide: ADP-400
|
---|
AdipoR2 |
- Antagonists: Peptide: ADP-400
|
---|
|
---|
Angiotensin | |
---|
Bradykinin | |
---|
CGRP | |
---|
Cholecystokinin | CCKA | |
---|
CCKB | |
---|
Unsorted |
- Antagonists: Nastorazepide
|
---|
|
---|
CRH | |
---|
Cytokine | See here instead. |
---|
Endothelin | |
---|
Galanin | GAL1 |
- Antagonists: C7
- Dithiepine-1,1,4,4-tetroxide
- Galantide (M15)
- M32
- M35
- M40
- SCH-202596
|
---|
GAL2 |
- Antagonists: C7
- Galantide (M15)
- M32
- M35
- M40
- M871
|
---|
GAL3 | |
---|
|
---|
Ghrelin/GHS | |
---|
GH | |
---|
GHRH | |
---|
GLP | |
---|
Glucagon |
- Antagonists: Adomeglivant
- L-168,049
- LGD-6972
|
---|
GnRH | |
---|
Gonadotropin | |
---|
Growth factor | See here instead. |
---|
Insulin |
- Antagonists: BMS-754807
- S661
- S961
- Antibodies: Xentuzumab (against IGF-1 and IGF-2)
|
---|
Kisspeptin |
- Antagonists: Kisspeptin-234
|
---|
Leptin | |
---|
MCH | |
---|
Melanocortin | |
---|
Neuropeptide FF |
- Agonists: Neuropeptide AF
- Neuropeptide FF
- Neuropeptide SF (RFRP-1)
- Neuropeptide VF (RFRP-3)
|
---|
Neuropeptide S | |
---|
Neuropeptide Y | |
---|
Neurotensin | |
---|
Opioid | See here instead. |
---|
Orexin | |
---|
Oxytocin | |
---|
Prolactin |
- Antagonists: Δ1–9-G129R-hPRL
- Δ1–14-G129R-hPRL
- G120K-hGH
- G129R-hPRL
|
---|
PTH | |
---|
Relaxin | |
---|
Somatostatin | |
---|
Tachykinin | |
---|
TRH | |
---|
TSH | |
---|
Vasopressin | |
---|
VIP/PACAP | VIPR1 |
- Agonists: Peptide: Bay 55-9837
- LBT-3393
- PACAP
- VIP
|
---|
VIPR2 | |
---|
PAC1 |
- Agonists: PACAP
- PACAP (1-27)
- PACAP (1-38)
- Antagonists: PACAP (6-38)
|
---|
Unsorted | |
---|
|
---|
Others |
- Endogenous: Adrenomedullin
- Apelin
- Asprosin
- Bombesin
- Calcitonin
- Carnosine
- CART
- CLIP
- DSIP
- Enteroglucagon
- Formyl peptide
- GALP
- GIP
- GRP
- Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin)
- Kininogens
- Motilin
- Natriuretic peptides (ANP, BNP, CNP, urodilatin)
- Nesfatin-1
- Neuromedin B
- Neuromedin N
- Neuromedin S
- Neuromedin U
- Obestatin
- Osteocalcin
- Resistin
- Secretin
- Thymopoietin
- Thymosins
- Thymulin
- Urotensin-II
- VGF
|
---|
- See also
- Receptor/signaling modulators
|
|
---|
Angiopoietin |
- Kinase inhibitors: Altiratinib
- CE-245677
- Rebastinib
|
---|
CNTF | |
---|
EGF (ErbB) | |
---|
FGF | FGFR1 | |
---|
FGFR2 |
- Agonists: Ersofermin
- FGF (1, 2 (bFGF), 3, 4, 5, 6, 7 (KGF), 8, 9, 10 (KGF2), 17, 18, 22)
- Palifermin
- Repifermin
- Sprifermin
- Trafermin
- Antibodies: Aprutumab
- Aprutumab ixadotin
|
---|
FGFR3 | |
---|
FGFR4 | |
---|
Unsorted | |
---|
|
---|
HGF (c-Met) | |
---|
IGF | IGF-1 |
- Kinase inhibitors: BMS-754807
- Linsitinib
- NVP-ADW742
- NVP-AEW541
- OSl-906
|
---|
IGF-2 |
- Antibodies: Dusigitumab
- Xentuzumab (against IGF-1 and IGF-2)
|
---|
Others |
- Cleavage products/derivatives with unknown target: Glypromate (GPE, (1-3)IGF-1)
- Trofinetide
|
---|
|
---|
LNGF (p75NTR) |
- Aptamers: Against NGF: RBM-004
- Decoy receptors: LEVI-04 (p75NTR-Fc)
|
---|
PDGF | |
---|
RET (GFL) | |
---|
SCF (c-Kit) | |
---|
TGFβ | |
---|
Trk | TrkA |
- Negative allosteric modulators: VM-902A
- Aptamers: Against NGF: RBM-004
- Decoy receptors: ReN-1820 (TrkAd5)
|
---|
TrkB |
- Agonists: 3,7-DHF
- 3,7,8,2'-THF
- 4'-DMA-7,8-DHF
- 7,3'-DHF
- 7,8-DHF
- 7,8,2'-THF
- 7,8,3'-THF
- Amitriptyline
- BDNF
- BNN-20
- Deoxygedunin
- Diosmetin
- GZ-389988
- HIOC
- LM22A-4
- N-Acetylserotonin
- NT-3
- NT-4
- Norwogonin (5,7,8-THF)
- R7
- TDP6
|
---|
TrkC | |
---|
|
---|
VEGF | |
---|
Others |
- Additional growth factors: Adrenomedullin
- Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
- Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
- Erythropoietin (see here instead)
- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
- Hepatoma-derived growth factor (HDGF)
- Interleukins/T-cell growth factors (see here instead)
- Leukemia inhibitory factor (LIF)
- Macrophage-stimulating protein (MSP; HLP, HGFLP)
- Midkine (NEGF2)
- Migration-stimulating factor (MSF; PRG4)
- Oncomodulin
- Pituitary adenylate cyclase-activating peptide (PACAP)
- Pleiotrophin
- Renalase
- Thrombopoietin (see here instead)
- Wnt signaling proteins
- Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
|
---|
- See also
- Receptor/signaling modulators
- Signaling peptide/protein receptor modulators
- Cytokine receptor modulators
|