CXCR5

Mammalian protein found in Homo sapiens

CXCR5

Identifiers

Aliases

CXCR5, BLR1, CD185, MDR15, C-X-C motif chemokine receptor 5, C-X-C chemokine receptor type 5

External IDs

OMIM: 601613 MGI: 103567 HomoloGene: 1298 GeneCards: CXCR5

Gene location (Human)

Chr.	Chromosome 11 (human)^[1]

Band	11q23.3	Start	118,883,892 bp^[1]
Band	11q23.3	End	118,897,787 bp^[1]

Gene location (Mouse)

Chr.	Chromosome 9 (mouse)^[2]

Band	9 A5.2\|9 24.84 cM	Start	44,423,084 bp^[2]
Band	9 A5.2\|9 24.84 cM	End	44,473,174 bp^[2]

RNA expression pattern

Bgee

Human

Mouse (ortholog)

Top expressed in

spleen

lymph node

appendix

blood

ascending aorta

left coronary artery

stromal cell of endometrium

skin of abdomen

canal of the cervix

ganglionic eminence

Top expressed in

spleen

spermatid

blood

subcutaneous adipose tissue

spermatocyte

left lung

thymus

right lung lobe

white adipose tissue

meninges

More reference expression data

BioGPS


More reference expression data

Gene ontology
Molecular function	C-X-C chemokine receptor activity G protein-coupled receptor activity protein binding signal transducer activity C-C chemokine receptor activity chemokine binding C-C chemokine binding
Cellular component	integral component of membrane plasma membrane integral component of plasma membrane membrane external side of plasma membrane
Biological process	positive regulation of cytokinesis chemokine-mediated signaling pathway chemotaxis B cell activation G protein-coupled receptor signaling pathway lymph node development immune response signal transduction leukocyte chemotaxis positive regulation of cytosolic calcium ion concentration calcium-mediated signaling cell chemotaxis
Sources:Amigo / QuickGO

Orthologs

Species

Human

Mouse

Entrez


643


12145

Ensembl


ENSG00000160683


ENSMUSG00000047880

UniProt


P32302


Q04683

RefSeq (mRNA)


NM_032966 NM_001716


NM_007551

RefSeq (protein)


NP_001707 NP_116743


NP_031577

Location (UCSC)

Chr 11: 118.88 – 118.9 Mb

Chr 9: 44.42 – 44.47 Mb

PubMed search

^[3]

^[4]

Wikidata

View/Edit Human

View/Edit Mouse

C-X-C chemokine receptor type 5 (CXC-R5) also known as CD185 (cluster of differentiation 185) or Burkitt lymphoma receptor 1 (BLR1) is a G protein-coupled seven transmembrane receptor for chemokine CXCL13 (also known as BLC) and belongs to the CXC chemokine receptor family. It enables T cells to migrate to lymph node and the B cell zones. In humans, the CXC-R5 protein is encoded by the CXCR5 gene.^[5]

Tissue distribution and function

The BLR1 / CXCR5 gene is specifically expressed in Burkitt's lymphoma and lymphatic tissues, such as follicles in lymph nodes as well as in spleen. The gene plays an essential role in B cell migration.^[6] Through CXCL13 secretions B cells are able to locate the lymph node.^[6]

Additionally, some recent studies have suggested that CXCL13, through CXCR5, is capable of recruiting hematopoietic precursor cells (CD3⁻ CD4⁺) which would cause the development of lymph nodes and Peyer's Patches.^[7]^[8]

Other studies highlight the role of CXCR5 in T cells, as they are unable to access B cell follicles without CXCR5 expression.^[9]^[10] This is a key step in the production of high affinity antibodies as B cells and T cells need to interact in order to activate the Ig class switch.^[9]

CXCR5 has been shown to be expressed on both CD4^[11] and CD8^[12] T cells, though it is often regarded as the defining marker for T Follicular Helper (Tfh) cells.^[13]

Role in cancer development

Recently, it was shown that CXCR5 overexpression in breast cancer patients highly correlates with lymph node metastases,^[14] and elevated CXCR5 expression may contribute to abnormal cell survival and migration in breast tumors that lack functional p53 protein.^[15] Minor allele of SNP rs630923, located in the area of CXCR5 gene promoter and associated with the risk of multiple sclerosis, is responsible for appearance of MEF2C-binding site resulted in reduced CXCR5 gene promoter activity in B-cells during activation, that could lead to decreased autoimmune response ^[16]

While chemokines and chemokine receptors have been thought to be involved in cancer development and maintenance, recently CXCR5 has come under investigation for its role in metastatic progression of prostate cancer. A recent study has indicated that prostate cancer tissue as well as cell lines express higher non-basal levels of CXCR5.^[17] Furthermore, the study found a correlation between the level of CXCR5 and Gleason score. CXCR5 location was additionally considered and higher Gleason scores correlated with nuclear CXCR5 while cytoplasmic and membrane CXCR5 correlated with benign and early prostate cancers.^[17]

References

^ ^a ^b ^c GRCh38: Ensembl release 89: ENSG00000160683 - Ensembl, May 2017
^ ^a ^b ^c GRCm38: Ensembl release 89: ENSMUSG00000047880 - Ensembl, May 2017
^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ Dobner T, Wolf I, Emrich T, Lipp M (November 1992). "Differentiation-specific expression of a novel G protein-coupled receptor from Burkitt's lymphoma". European Journal of Immunology. 22 (11): 2795–9. doi:10.1002/eji.1830221107. PMID 1425907. S2CID 35096818.
^ ^a ^b Förster R, Mattis AE, Kremmer E, Wolf E, Brem G, Lipp M (December 1996). "A putative chemokine receptor, BLR1, directs B cell migration to defined lymphoid organs and specific anatomic compartments of the spleen". Cell. 87 (6): 1037–47. doi:10.1016/S0092-8674(00)81798-5. PMID 8978608. S2CID 17558174.
^ Honda, Kenya; Nakano, Hiroyasu; Yoshida, Hisahiro; Nishikawa, Satomi; Rennert, Paul; Ikuta, Koichi; Tamechika, Masakatsu; Yamaguchi, Kazuhito; Fukumoto, Tetsuo (2001-03-05). "Molecular Basis for Hematopoietic/Mesenchymal Interaction during Initiation of Peyer's Patch Organogenesis". The Journal of Experimental Medicine. 193 (5): 621–630. doi:10.1084/jem.193.5.621. ISSN 0022-1007. PMC 2193398. PMID 11238592.
^ Finke, D; Acha-Orbea, H; Mattis, A; Lipp, M; Kraehenbuhl, J.P (September 2002). "CD4+CD3− Cells Induce Peyer's Patch Development". Immunity. 17 (3): 363–373. doi:10.1016/S1074-7613(02)00395-3. PMID 12354388.
^ ^a ^b Junt, Tobias; Fink, Katja; Förster, Reinhold; Senn, Beatrice; Lipp, Martin; Muramatsu, Masamichi; Zinkernagel, Rolf M.; Ludewig, Burkhard; Hengartner, Hans (2005-12-01). "CXCR5-dependent seeding of follicular niches by B and Th cells augments antiviral B cell responses". Journal of Immunology. 175 (11): 7109–7116. doi:10.4049/jimmunol.175.11.7109. ISSN 0022-1767. PMID 16301613.
^ Hardtke, S. (2005-09-15). "Balanced expression of CXCR5 and CCR7 on follicular T helper cells determines their transient positioning to lymph node follicles and is essential for efficient B-cell help". Blood. 106 (6): 1924–1931. doi:10.1182/blood-2004-11-4494. ISSN 0006-4971. PMID 15899919.
^ Chevalier N, Jarrossay D, Ho E, Avery DT, Ma CS, Yu D, Sallusto F, Tangye SG, Mackay CR (May 2011). "CXCR5 expressing human central memory CD4 T cells and their relevance for humoral immune responses". Journal of Immunology. 186 (10): 5556–68. doi:10.4049/jimmunol.1002828. PMID 21471443.
^ He R, Hou S, Liu C, Zhang A, Bai Q, Han M, Yang Y, Wei G, Shen T, Yang X, Xu L, Chen X, Hao Y, Wang P, Zhu C, Ou J, Liang H, Ni T, Zhang X, Zhou X, Deng K, Chen Y, Luo Y, Xu J, Qi H, Wu Y, Ye L (August 2016). "Follicular CXCR5- expressing CD8(+) T cells curtail chronic viral infection". Nature. 537 (7620): 412–428. Bibcode:2016Natur.537..412H. doi:10.1038/nature19317. PMID 27501245. S2CID 4469688.
^ Moser B (2015). "CXCR5, the Defining Marker for Follicular B Helper T (TFH) Cells". Frontiers in Immunology. 6: 296. doi:10.3389/fimmu.2015.00296. PMC 4459225. PMID 26106395.
^ Biswas S, Sengupta S, Roy Chowdhury S, Jana S, Mandal G, Mandal PK, Saha N, Malhotra V, Gupta A, Kuprash DV, Bhattacharyya A (January 2014). "CXCL13-CXCR5 co-expression regulates epithelial to mesenchymal transition of breast cancer cells during lymph node metastasis". Breast Cancer Research and Treatment. 143 (2): 265–76. doi:10.1007/s10549-013-2811-8. PMID 24337540. S2CID 2937341.
^ Mitkin NA, Hook CD, Schwartz AM, Biswas S, Kochetkov DV, Muratova AM, Afanasyeva MA, Kravchenko JE, Bhattacharyya A, Kuprash DV (March 2015). "p53-dependent expression of CXCR5 chemokine receptor in MCF-7 breast cancer cells". Scientific Reports. 5 (5): 9330. Bibcode:2015NatSR...5E9330M. doi:10.1038/srep09330. PMC 4365401. PMID 25786345.
^ Mitkin NA, Muratova AM, Schwartz AM, Kuprash DV (Nov 2016). "The A Allele of the Single-Nucleotide Polymorphism rs630923 Creates a Binding Site for MEF2C Resulting in Reduced CXCR5 Promoter Activity in B-Cell Lymphoblastic Cell Lines". Frontiers in Immunology. 7 (515): 515. doi:10.3389/fimmu.2016.00515. PMC 5112242. PMID 27909439.
^ ^a ^b Singh, Shailesh; Singh, Rajesh; Singh, Udai P.; Rai, Shesh N.; Novakovic, Kristian R.; Chung, Leland W.K.; Didier, Peter J.; Grizzle, William E.; Lillard, James W. (2009-11-15). "Clinical and biological significance of CXCR5 expressed by prostate cancer specimens and cell lines". International Journal of Cancer. 125 (10): 2288–2295. doi:10.1002/ijc.24574. PMC 3600527. PMID 19610059.

External links

Human CXCR5 genome location and CXCR5 gene details page in the UCSC Genome Browser.

Lipp M, Müller G (2006). "Shaping up adaptive immunity: the impact of CCR7 and CXCR5 on lymphocyte trafficking". Verhandlungen der Deutschen Gesellschaft für Pathologie. 87: 90–101. PMID 16888899.
Barella L, Loetscher M, Tobler A, Baggiolini M, Moser B (August 1995). "Sequence variation of a novel heptahelical leucocyte receptor through alternative transcript formation". The Biochemical Journal. 309 ( Pt 3) (3): 773–9. doi:10.1042/bj3090773. PMC 1135699. PMID 7639692.
Legler DF, Loetscher M, Roos RS, Clark-Lewis I, Baggiolini M, Moser B (February 1998). "B cell-attracting chemokine 1, a human CXC chemokine expressed in lymphoid tissues, selectively attracts B lymphocytes via BLR1/CXCR5". The Journal of Experimental Medicine. 187 (4): 655–60. doi:10.1084/jem.187.4.655. PMC 2212150. PMID 9463416.
Gunn MD, Ngo VN, Ansel KM, Ekland EH, Cyster JG, Williams LT (February 1998). "A B-cell-homing chemokine made in lymphoid follicles activates Burkitt's lymphoma receptor-1". Nature. 391 (6669): 799–803. Bibcode:1998Natur.391..799G. doi:10.1038/35876. PMID 9486651. S2CID 4373691.
Müller G, Lipp M (September 2001). "Signal transduction by the chemokine receptor CXCR5: structural requirements for G protein activation analyzed by chimeric CXCR1/CXCR5 molecules". Biological Chemistry. 382 (9): 1387–97. doi:10.1515/BC.2001.171. PMID 11688722. S2CID 21366051.
Schaerli P, Loetscher P, Moser B (December 2001). "Cutting edge: induction of follicular homing precedes effector Th cell development". Journal of Immunology. 167 (11): 6082–6. doi:10.4049/jimmunol.167.11.6082. PMID 11714765.
Kim CH, Johnston B, Butcher EC (July 2002). "Trafficking machinery of NKT cells: shared and differential chemokine receptor expression among V alpha 24(+)V beta 11(+) NKT cell subsets with distinct cytokine-producing capacity". Blood. 100 (1): 11–6. doi:10.1182/blood-2001-12-0196. PMID 12070001. S2CID 37076470.
Carlsen HS, Baekkevold ES, Johansen FE, Haraldsen G, Brandtzaeg P (September 2002). "B cell attracting chemokine 1 (CXCL13) and its receptor CXCR5 are expressed in normal and aberrant gut associated lymphoid tissue". Gut. 51 (3): 364–71. doi:10.1136/gut.51.3.364. PMC 1773345. PMID 12171958.
Battle TE, Yen A (October 2002). "Ectopic expression of CXCR5/BLR1 accelerates retinoic acid- and vitamin D(3)-induced monocytic differentiation of U937 cells". Experimental Biology and Medicine. 227 (9): 753–62. doi:10.1177/153537020222700906. PMID 12324654. S2CID 26070911.
Lisignoli G, Toneguzzi S, Piacentini A, Cattini L, Lenti A, Tschon M, Cristino S, Grassi F, Facchini A (January 2003). "Human osteoblasts express functional CXC chemokine receptors 3 and 5: activation by their ligands, CXCL10 and CXCL13, significantly induces alkaline phosphatase and beta-N-acetylhexosaminidase release". Journal of Cellular Physiology. 194 (1): 71–9. doi:10.1002/jcp.10188. PMID 12447991. S2CID 8031523.
Chan CC, Shen D, Hackett JJ, Buggage RR, Tuaillon N (February 2003). "Expression of chemokine receptors, CXCR4 and CXCR5, and chemokines, BLC and SDF-1, in the eyes of patients with primary intraocular lymphoma". Ophthalmology. 110 (2): 421–6. doi:10.1016/S0161-6420(02)01737-2. PMID 12578791.
Flynn G, Maru S, Loughlin J, Romero IA, Male D (March 2003). "Regulation of chemokine receptor expression in human microglia and astrocytes". Journal of Neuroimmunology. 136 (1–2): 84–93. doi:10.1016/S0165-5728(03)00009-2. PMID 12620646. S2CID 39725685.
Lisignoli G, Piacentini A, Toneguzzi S, Grassi F, Tschon M, Cristino S, Facchini A, Mariani E (2004). "Age-associated changes in functional response to CXCR3 and CXCR5 chemokine receptors in human osteoblasts". Biogerontology. 4 (5): 309–17. doi:10.1023/A:1026203502385. PMID 14618028. S2CID 20511946.
Aust G, Sittig D, Becherer L, Anderegg U, Schütz A, Lamesch P, Schmücking E (February 2004). "The role of CXCR5 and its ligand CXCL13 in the compartmentalization of lymphocytes in thyroids affected by autoimmune thyroid diseases". European Journal of Endocrinology. 150 (2): 225–34. doi:10.1530/eje.0.1500225. PMID 14763921.
Howard OM, Dong HF, Su SB, Caspi RR, Chen X, Plotz P, Oppenheim JJ (June 2005). "Autoantigens signal through chemokine receptors: uveitis antigens induce CXCR3- and CXCR5-expressing lymphocytes and immature dendritic cells to migrate". Blood. 105 (11): 4207–14. doi:10.1182/blood-2004-07-2697. PMC 1895027. PMID 15713799.
Steinmetz OM, Panzer U, Kneissler U, Harendza S, Lipp M, Helmchen U, Stahl RA (April 2005). "BCA-1/CXCL13 expression is associated with CXCR5-positive B-cell cluster formation in acute renal transplant rejection". Kidney International. 67 (4): 1616–21. doi:10.1111/j.1523-1755.2005.00244.x. PMID 15780119.
Hu C, Xiong J, Zhang L, Huang B, Zhang Q, Li Q, Yang M, Wu Y, Wu Q, Shen Q, Gao Q, Zhang K, Sun Z, Liu J, Jin Y, Tan J (August 2004). "PEG10 activation by co-stimulation of CXCR5 and CCR7 essentially contributes to resistance to apoptosis in CD19+CD34+ B cells from patients with B cell lineage acute and chronic lymphocytic leukemia". Cellular & Molecular Immunology. 1 (4): 280–94. PMID 16225771.

Cytokine receptors

Chemokine receptor
(GPCRs)

CC	CCR1 / CCRL1 CCR2 CCRL2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9 CCR10
CXC	IL-8 CXCR1 CXCR2 CXCR3 CXCR4 CXCR5 CXCR6 CXCR7
Other	CX3C CX3CR1 XC XCR1 CCBP2 CMKLR1

TNF receptor

1-10	TNFR1 (TNFRSF1A) TNFR2 (TNFRSF1B) LTBR (TNFRSF3) CD134 (TNFRSF4) CD40 (TNFRSF5) Fas receptor (TNFRSF6) DcR3 (TNFRSF6B) CD27 (TNFRSF7) CD30 (TNFRSF8) CD137 (TNFRSF9)
11-20	DR4 (TNFRSF10A) DR5 (TNFRSF10B) DcR1 (TNFRSF10C) DcR2 (TNFRSF10D) RANK (TNFRSF11A) Osteoprotegerin (TNFRSF11B) TweakR (TNFRSF12A) TACI (TNFRSF13B) BAFFR (TNFRSF13C) HVEM (TNFRSF14) NGFR (TNFRSF16) BCMA (TNFRSF17) GITR (TNFRSF18) TAJ/TROY (TNFRSF19)
21-27	DR6 (TNFRSF21) DR3 (TNFRSF25) EDA2R (TNFRSF27)

JAK-STAT

Type I

γ-chain	Interleukin receptors IL2R / IL2RA/IL2RB / IL15R IL4R / IL13R / IL13RA1 / IL13RA2 IL7R / IL7RA IL9R IL21R
β-chain	Interleukin receptors IL3R / IL3RA IL5R / IL5RA GM-CSF
gp130	Interleukin receptors IL6RA 11/IL11RA 27/IL27RA OSMR LIFR CNTFR
IL12RB1	Interleukin receptors IL12R/IL12RB1/IL12RB2 IL23R23
Other	other CSF receptors EPO G-CSF Thrombopoietin hormone receptor: GH prolactin

Type II

Interleukin receptors
- IL10R / IL10RA / IL10RB / IL22R / IL22RA1 / IL22RA2
- IL20R / IL20RA / IL20RB
- IL28R
Interferon receptors
- -α/β / IFNAR1/IFNAR2
- -γ/IFNGR1 / IFNGR2

Ig superfamily

IL1
- IL1R1
- IL1R2
IL18R / IL18R1

IL 17 family

IL17
- IL17RA
- IL17RB
- IL17RC
- IL17RD
- IL17RE

Enzyme-linked receptor

Tyr
- CSF1R
- KIT
Ser/Thr: TGF-beta
- TGFBR1
- TGFBR2
- family

v t e Proteins: clusters of differentiation (see also list of human clusters of differentiation)
1–50	CD1 a-c 1A 1B 1D 1E CD2 CD3 γ δ ε CD4 CD5 CD6 CD7 CD8 a CD9 CD10 CD11 a b c d CD13 CD14 CD15 CD16 A B CD18 CD19 CD20 CD21 CD22 CD23 CD24 CD25 CD26 CD27 CD28 CD29 CD30 CD31 CD32 A B CD33 CD34 CD35 CD36 CD37 CD38 CD39 CD40 CD41 CD42 a b c d CD43 CD44 CD45 CD46 CD47 CD48 CD49 a b c d e f CD50
51–100	CD51 CD52 CD53 CD54 CD55 CD56 CD57 CD58 CD59 CD61 CD62 E L P CD63 CD64 A B C CD66 a b c d e f CD68 CD69 CD70 CD71 CD72 CD73 CD74 CD78 CD79 a b CD80 CD81 CD82 CD83 CD84 CD85 a d e h j k CD86 CD87 CD88 CD89 CD90 CD91 - CD92 CD93 CD94 CD95 CD96 CD97 CD98 CD99 CD100
101–150	CD101 CD102 CD103 CD104 CD105 CD106 CD107 a b CD108 CD109 CD110 CD111 CD112 CD113 CD114 CD115 CD116 CD117 CD118 CD119 CD120 a b CD121 a b CD122 CD123 CD124 CD125 CD126 CD127 CD129 CD130 CD131 CD132 CD133 CD134 CD135 CD136 CD137 CD138 CD140b CD141 CD142 CD143 CD144 CD146 CD147 CD148 CD150
151–200	CD151 CD152 CD153 CD154 CD155 CD156 a b c CD157 CD158 (a d e i k) CD159 a c CD160 CD161 CD162 CD163 CD164 CD166 CD167 a b CD168 CD169 CD170 CD171 CD172 a b g CD174 CD177 CD178 CD179 a b CD180 CD181 CD182 CD183 CD184 CD185 CD186 CD191 CD192 CD193 CD194 CD195 CD196 CD197 CDw198 CDw199 CD200
201–250	CD201 CD202b CD204 CD205 CD206 CD207 CD208 CD209 CDw210 a b CD212 CD213a 1 2 CD217 CD218 (a b) CD220 CD221 CD222 CD223 CD224 CD225 CD226 CD227 CD228 CD229 CD230 CD233 CD234 CD235 a b CD236 CD238 CD239 CD240CE CD240D CD241 CD243 CD244 CD246 CD247 - CD248 CD249
251–300	CD252 CD253 CD254 CD256 CD257 CD258 CD261 CD262 CD263 CD264 CD265 CD266 CD267 CD268 CD269 CD271 CD272 CD273 CD274 CD275 CD276 CD278 CD279 CD280 CD281 CD282 CD283 CD284 CD286 CD288 CD289 CD290 CD292 CDw293 CD294 CD295 CD297 CD298 CD299
301–350	CD300A CD301 CD302 CD303 CD304 CD305 CD306 CD307 CD309 CD312 CD314 CD315 CD316 CD317 CD318 CD320 CD321 CD322 CD324 CD325 CD326 CD327 CD328 CD329 CD331 CD332 CD333 CD334 CD335 CD336 CD337 CD338 CD339 CD340 CD344 CD349 CD350

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin-like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3
Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)
Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)
Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine D1 D2 D3 D4 D5 GHB receptor Histamine H1 H2 H3 H4 Melatonin (1A 1B 1C) TAAR (1 2 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 1 2 FPRL1 OXE Prostaglandin DP (1 2), EP (1 2 3 4), FP Prostacyclin Thromboxane
Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Hydroxycarboxylic acids 1 2 3 Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide

B/W (1
2)
FF (1
2)
S
Y (1
2
4
5)
Neuromedin (B
U (1
2))
Neurotensin (1
2)

Other

Anaphylatoxin (C3a
C5a (1
2))
Angiotensin (1
2)
Apelin
Bombesin
- BRS3
- GRPR
- NMBR)
- Bradykinin (B1
- B2)
Chemokine
Cholecystokinin (A
B)
Endothelin
- A
- B
Formyl peptide (1
2
3)
FSH
Galanin (1
2
3)
Gonadotropin-releasing hormone (1
2)
Ghrelin
Kisspeptin
Luteinizing hormone/choriogonadotropin
MAS (1
1L
D
E
F
G
X1
X2
X3
X4)
Melanocortin (1
2
3
4
5)
MCHR (1
2)
Motilin
Opioid (Delta
Kappa
Mu
Nociceptin & Zeta, but not Sigma)
Orexin (1
2)
Oxytocin
Prokineticin (1
2)
Prolactin-releasing peptide
Relaxin (1
2
3
4)
Somatostatin (1
2
3
4
5)
Tachykinin (1
2
3)
Thyrotropin
Thyrotropin-releasing hormone
Urotensin-II
Vasopressin (1A
1B
2)

Miscellaneous

Taste, bitter	TAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor type 1
Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)
Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin-like

Adhesion	ADGRB Brain-specific angiogenesis inhibitor 1 2 3 ADGRC Cadherin 1 2 3 ADGRE EMR 1 2 3 CD97 ADGRG 1 2 3 4 5 6 7 ADGRL Latrophilin 1 2 3 ELTD1
Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)
Other	Calcitonin CALCRL Corticotropin-releasing hormone (1 2) Glucagon (GR GIPR GLP1R GLP2R) Growth-hormone-releasing hormone PACAPR1 GPR Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste, sweet	TAS1R 1 2 3 Vomeronasal receptor, type 2
Other	Calcium-sensing receptor GABA_B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled & Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)
Smoothened	Smoothened

Chemokine receptor modulators

CCR1	Agonists: CCL4 (MIP-1β) CCL5 (RANTES) CCL6 CCL9 (CCL10) CCL14 CCL15 CCL16 CCL23
CCR2	Agonists: CCL2 CCL8 CCL12 CCL16 NAMs: Cenicriviroc (TAK-652, TBR-652)
CCR3	Agonists: CCL5 (RANTES) CCL7 CCL11 CCL13 CCL15 CCL18 CCL24 CCL26 CCL28
CCR4	Agonists: CCL3 (MIP-1α) CCL5 (RANTES) CCL17 CCL22 Antibodies: Mogamulizumab (against CCR4)
CCR5	Agonists: CCL3 (MIP-1α) CCL4 (MIP-1β) CCL5 (RANTES) CCL8 CCL11 CCL13 CCL14 CCL16 NAMs: Aplaviroc Cenicriviroc (TAK-652, TBR-652) INCB009471 Maraviroc Vicriviroc Antibodies: PRO-140
CCR6	Agonists: CCL20
CCR7	Agonists: CCL19 CCL21
CCR8	Agonists: CCL1 CCL16
CCR9	Agonists: CCL25
CCR10	Agonists: CCL27 CCL28
CCR11	Agonists: CCL19 CCL21 CCL25
Ungrouped	Antibodies: Bertilimumab (against CCL11) Carlumab (against CCL2)

CXC

CXCR1 (IL-8Rα)	Agonists: CXCL6 Emoctakin Interleukin-8 (CXCL8, GCP-1) Antagonists: Navarixin NAMs: Ladarixin Reparixin (repertaxin)
CXCR2 (IL-8Rβ)	Agonists: CXCL1 (MGSA) CXCL2 CXCL3 CXCL5 CXCL6 CXCL7 Emoctakin Garnocestim Interleukin-8 (CXCL8, GCP-1) Antagonists: Danirixin Elubrixin Navarixin NAMs: Ladarixin Reparixin (repertaxin)
CXCR3	Agonists: CXCL4 (PF4) CXCL9 (MIG) CXCL10 (IP-10) CXCL11 (I-TAC) Iroplact Antibodies: Eldelumab (against CXCL10)
CXCR4	Agonists: MIF SDF-1 (CXCL12) Ubiquitin Antagonists: Mavorixafor Plerixafor (AMD3100) Antibodies: Ulocuplumab (against CXCR4)
CXCR5	Agonists: CXCL13
CXCR6	Agonists: CXCL16
CXCR7	Agonists: CXCL11 (I-TAC) SDF-1 (CXCL12) PAMs: Plerixafor (AMD3100)