C-C chemokine receptor type 5; C-C CKR-5; CC-CKR-5; CCR-5; CCR5; HIV-1 fusion coreceptor; CHEMR13; sCD195 (CCR5, CMKBR5)
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Function
- receptor for a number of inflammatory CC-chemokines including MIP-1-alpha, MIP-1-beta & RANTES
- transduces a signal by increasing the intracellular Ca+2
- may play a role in the control of granulocytic lineage proliferation or differentiation
- interacts with PRAF2
- efficient ligand binding to CCL3/MIP-1alpha & CCR4/MIP-1beta requires sulfation, O-glycosylation & sialic acid modifications
- interacts with ADRBK1
- phosphorylation on Ser in the C-terminal is stimulated by binding CC chemokines especially by APO-RANTES
Structure
- glycosylation on Ser-6 is required for efficient
- sulfated on at least 2 of the N-terminal tTyr binding of CCL4.
- sulfation is required for efficient binding of chemokines, CCL3 & CCL4
- O-glycosylated, but not N-glycosylated; Ser-6 appears to be the major site
- Thr-16 & Ser-17 may also be glycosylated
- also sialylated glycans present which contribute to chemokine binding
- palmitoylation in the C-terminal is important for cell surface expression
- belongs to the G-protein coupled receptor 1 family
Compartment
Expression
- expressed in spleen, thymus, in myeloid cell line THP-1, in promyeloblastic cell line KG-1A & on CD4+ & CD8+ T-cells > peripheral blood leukocytes, small intestine > ovary & lung
Pathology
- coreceptor for HIV-1 (CD4 is primary receptor)
- interacts with HIV-1 surface protein gp120
- sulfation contributes to the efficiency of HIV-1 entry
- palmitoylation in the C-terminal may have role in HIV entry
Polymorphism
- variations in CCR5 are associated with susceptibility or resistance to HIV1
- Ser-60 variant (in 1st intracellular domain of CCR5) results in diminished amounts in the membrane & thus diminished susceptibility to infection by microbes that depend on CCR5 as their receptors
- variations in CCR5 are associated with susceptibility to West Nile virus
Pharmacology
More general terms
Additional terms
References
- ↑ UniProt http://www.uniprot.org/uniprot/P51681.html
- ↑ Wikipedia; CC chemokine receptors entry http://en.wikipedia.org/wiki/CC_chemokine_receptors
- ↑ Wikipedia; CCR5 receptor entry http://en.wikipedia.org/wiki/CCR5
Database
- Kegg: http://www.genome.jp/dbget-bin/www_bget?hsa:1234
- Kegg: http://www.genome.jp/dbget-bin/www_bget?hsa:7277
- OMIM: https://mirror.omim.org/entry/601373
- OMIM: https://mirror.omim.org/entry/609423
- OMIM: https://mirror.omim.org/entry/610379
- UniProt: http://www.uniprot.org/uniprot/P51681.html
- Entrez gene: http://www.ncbi.nlm.nih.gov/sites/entrez?db=gene&cmd=Retrieve&dopt=Graphics&list_uids=1234