Concentration | 2mL,0.5mg/mL |
EntrezGeneNumber | |
EntrezGeneSummary | ThisgeneencodesaCXCchemokinereceptorspecificforstromalcell-derivedfactor-1.Theproteinhas7transmembraneregionsandislocatedonthecellsurface.ItactswiththeCD4proteintosupportHIVentryintocellsandisalsohighlyexpressedinbreastcancercells.MutationsinthisgenehavebeenassociatedwithWHIM(warts,hypogammaglobulinemia,infections,andmyelokathexis)syndrome.Alternatetranscriptionalsplicevariants,encodingdifferentisoforms,havebeencharacterized. |
GeneSymbol | - CXCR4
- WHIM
- NPY3R
- NPYY3R
- FB22
- LAP3
- Fusin
- CXCR-4
- LCR1
- NPYR
- HM89
- fusin
- HSY3RR
- CXC-R4
- NPYY3
- NPYRL
- D2S201E
- CD184
- LESTR
|
GPCRClass | A |
HostCells | Chem-1 |
ProteinTarget | CXCR4 |
TargetSub-Family | Chemokine |
UniProtNumber | |
UniProtSummary | FUNCTION:SwissProt:P61073#ReceptorfortheC-X-CchemokineCXCL12/SDF-1.Transducesasignalbyincreasingtheintracellularcalciumionslevel.Involvedinhaematopoiesisandincardiacventricularseptumformation.Playsalsoanessentialroleinvascularizationofthegastrointestinaltract,probablybyregulatingvascularbranchingand/orremodelingprocessesinendothelialcells.Couldbeinvolvedincerebellardevelopment.IntheCNS,couldmediatehippocampal-neuronsurvival.Actsasacoreceptor(CD4beingtheprimaryreceptor)forHIV-1X4isolatesandasaprimaryreceptorforsomeHIV-2isolates.PromotesEnv-mediatedfusionofthevirus. SIZE:352aminoacids;39746Da SUBUNIT:InteractswithHIV-1surfaceproteingp120andTat. SUBCELLULARLOCATION:Cellmembrane;Multi-passmembraneprotein. TISSUESPECIFICITY:Expressedinnumeroustissues,suchasperipheralbloodleukocytes,spleen,thymus,spinalcord,heart,placenta,lung,liver,skeletalmuscle,kidney,pancreas,cerebellum,cerebralcortexandmedulla(inmicrogliaaswellasinastrocytes),brainmicrovascular,coronaryarteryandumbilicalcordendothelialcells.Isoform1ispredominantinalltissuestested. DOMAIN:SwissProt:P61073Theamino-terminusiscriticalforligandbinding.ResiduesinallfourextracellularregionscontributetoHIV-1coreceptoractivity. PTM:Sulfated. DISEASE:SwissProt:P61073#DefectsinCXCR4areacauseofWHIMsyndrome[MIM:193670];alsocalledwarts,hypogammaglobulinemia,infections,andmyelokathexis.WHIMsyndromeisanimmunodeficiencydiseasecharacterizedbyneutropenia,hypogammaglobulinemiaandextensivehumanpapillomavirus(HPV)infection.Despitetheperipheralneutropenia,bonemarrowaspiratesfromaffectedindividualscontainabundantmaturemyeloidcells,aconditiontermedmyelokathexis. SIMILARITY:BelongstotheG-proteincoupledreceptor1family. |
IncubationConditions | RECOMMENDEDASSAYCONDITIONS:Membranesaremixedwithradioactiveligandandunlabeledcompetitor(seeFigures1and2forconcentrationstested)inbindingbufferinanonbinding96-wellplate,andincubatedfor1-2h.Priortofiltration,aGF/C96-wellfilterplateiscoatedwith0.33%polyethyleneiminefor30min,thenwashedwith50mMHEPES,pH7.4,0.5%BSA.Bindingreactionistransferredtothefilterplate,andwashed3times(1mLperwellperwash)withWashBuffer.Theplateisdriedandcounted.
Bindingbuffer:50mMHepes,pH7.4,5mMMgCl2,1mMCaCl2,0.2%BSA,filteredandstoredat4°C
Radioligand:[125I]SDF-1alpha(Perkinelmer#:NEX346)
WashBuffer:50mMHepes,pH7.4,500mMNaCl,0.1%BSA,filteredandstoredat4°C.
Onevialcontainsenoughmembranesforatleast200assays(units),whereanunitistheamountofmembranethatwillyieldgreaterthan4-foldsignal:backgroundwith125I-labeledSDF-1alphaat0.13nM. |