Table 1:
Official IUPHAR Receptor Name |
Class | RAMP | Cell Line | Identification Method |
FDA Approved Drugsb |
Clinical Indication |
Ref. |
---|---|---|---|---|---|---|---|
Chemerin receptor 1 | A | RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/Ac | --- | [29] |
CCR1 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CCR2 | A | RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CCR3 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CCR4 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | mogamuli zumab | Cutaneous T-cell Lymphoma (Mycosis Fungoides, Sézary Syndrome) | [29] |
plerixafor | non-Hodgkin lymphoma, multiple myeloma | ||||||
CCR5 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | maraviroc | HIV/AIDS | [29] |
ibalizuma b | HIV/AIDS | ||||||
CCR6 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CCR7 | A | RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
CCR8 | A | RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CCR9 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CCR10 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
CXCR1 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CXCR2 | A | RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
CXCR3 | A | RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | [28] | ||||
CXCR4 | A | RAMP1, RAMP3 | HEK293T, COS-7 | BRET assay | plerixafor | non-Hodgkin lymphoma, multiple myeloma | [29] |
CXCR5 | A | RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
CXCR6 | A | RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
CX3CR1 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
XCR1 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
ACKR1 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
ACKR2 | A | RAMP1, RAMP3 | HEK293T, COS-7 | BRET assay, FACS | N/A | --- | [29] |
ACKR3 | A | RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS, PLA, Confocal microscopy | plerixafor | non-Hodgkin lymphoma, multiple myeloma | [29] |
RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | [28] | ||||
ACKR4 | A | RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay | N/A | --- | [29] |
ACKR5 | A | RAMP3 | COS-7 | FACS | N/A | --- | [29] |
GPR4 | A | RAMP1, RAMP2, RAMP3 | HEK293T, HEK293 FreeStyle | SBA immunoassay, PLA | N/A | --- | [28] |
GPR182 | A | RAMP1, RAMP2, RAMP3 | HEK293T, HEK293 FreeStyle | SBA immunoassay, PLA | N/A | --- | [28] |
GPER/GPR30 | A | RAMP3 | HEK293T | BRET assay, Co-IP, Confocal microscopy | estradiol (estrogen receptor agonist; naturally occurring) | Oral contraceptives, treatment of menopausal and perimenopausal symptoms, and hypoestrogenism | [27] |
CT receptor | B | RAMP1, RAMP2, RAMP3 | COS-7, CHO-P | Radioligand binding, Crosslinking analysis, Confocal microscopy | pramlintide | Type I & Type II Diabetes | [23] |
RAMP1, RAMP2, RAMP3 | HEK293T, HEK293 FreeStyle | SBA immunoassay | [28] | ||||
Calcitonin receptor like receptor | B | RAMP1, RAMP2, RAMP3 | Xenopus oocytes, HEK293T | Radioligand binding, FACS, Crosslinking analysis | eptinezumab, fremanez umab, glacanezumab, erenumab | Chronic Migraine | [4] |
RAMP1, RAMP2, RAMP3 | HEK293T, COS-7 | BRET assay, FACS, PLA, Confocal microscopy | [25, 29] | ||||
RAMP1, RAMP2, RAMP3 | HEK293T, HEK293 FreeStyle | SBA immunoassay, PLA | [28] | ||||
CRF1 receptor | B | RAMP2 | HEK293S, CHO-K1 | ELISA | N/A | --- | [8] |
RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | N/A | --- | [28] | ||
CRF2 receptor | B | RAMP3 | HEK293 FreeStyle | SBA immunoassay | N/A | --- | [28] |
GHRH receptor | B | RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | sermorelin | Growth hormone deficiency or growth failure, prevention of HIV-induced weight loss | [28] |
GIP receptor | B | RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | N/A | --- | [28] |
GLP-1 receptor | B | RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | exenatide, sorafenib, lixisenatide, mecaserm in rinfabate, dulaglutide, albiglutide, conivaptan, lenalidomide | Type II Diabetes | [28, 89] |
GLP-2 receptor | B | RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | teduglutide | Short Bowel Syndrome | [28] |
Glucagon receptor | B | RAMP2 | HEK293, COS-7 | Confocal microscopy, radioligand binding | glucagon recombinant, glucagon hydrochloride, oxyphenb utazone, chlordiaze poxide | Type II Diabetes | [7, 8, 25] |
RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | N/A | --- | [28] | ||
Secretin receptor | B | RAMP3 | COS-7, CHO-K1 | Bimolecular fluorescence complementation, BRET assay | secretin synthetic porcine, ezetimibe, pegfilgrastim | Treat High Blood Cholesterol, Lipid Abnormalities | [26] |
RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | [28] | ||||
PTH1 receptor | B | RAMP2 | HEK293, COS-7 | Confocal microscopy | teriparatide, abaloparatide | Osteoporosis | [25, 89] |
RAMP1, RAMP2, RAMP3 | HEK293T, HEK293 FreeStyle | SBA Immunoassay, PLA | [28, 89] | ||||
PTH2 receptor | B | RAMP3 | HEK293, COS-7 | Confocal microscopy | teriparatide, recombin ant parathyroid hormone | Osteoporosis | [25, 89] |
RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA Immunoassay | [28, 89] | ||||
PAC1 receptor | B | RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA Immunoassay | N/A | --- | [28] |
VPAC1 receptor | B | RAMP1, RAMP2, RAMP3 | HEK293, COS-7 | Confocal microscopy | N/A | --- | [25] |
RAMP2, RAMP3 | HEK293 FreeStyle | SBA Immunoassay | [28] | ||||
VPAC2 receptor | B | RAMP1, RAMP2, RAMP3 | HEK293S, CHO-K1 | ELISA | N/A | --- | [8] |
RAMP2, RAMP3 | HEK293 FreeStyle | SBA Immunoassay | [28] | ||||
CaS receptor | C | RAMP1, RAMP3 | COS-7, HEK293 | Confocal microscopy, Co-IP | etelcalcetide | Secondary Hyperparathyroidism | [13] |
ADGRF 5 | Adhesion Family | RAMP1, RAMP2, RAMP3 | HEK293 FreeStyle | SBA immunoassay | N/A | --- | [28] |
IUPHAR: The International Union of Basic and Clinical Pharmacology, RAMP: Receptor activity-modifying protein, BRET: Bioluminescence Resonance Energy Transfer, FACS: Fluorescenceactivated cell sorting, SBA: Suspension bead array, PLA: Proximity ligation assay, Co-IP: Coimmunoprecipitation.
To determine whether each RAMP-interacting GPCR listed in the table had an associated FDA approved drug, each GPCR was cross referenced against the public resource DrugBank [90], a database which combines drug data with drug target information, and a recent review profiling trends in GPCR drug discovery through 2017.
N/A acronym in the Drug column stands for None Approved and is meant to denote that for the given GPCR there are no currently approved therapies directed at this GPCR in DrugBank.