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. Author manuscript; available in PMC: 2021 Apr 1.
Published in final edited form as: Trends Pharmacol Sci. 2020 Feb 27;41(4):249–265. doi: 10.1016/j.tips.2020.01.009

Table 1:

Currently identified RAMP-interacting GPCRs, methods of interaction, identification, and FDA approved drugsa

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]
a

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.

b

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.

c

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.