Detailed entry information

Protein Information (annotations from UniProt)

Database IDHIV0008749
UniProt IDP25116
Primary gene name(s)F2R
Synonym gene name(s)CF2R, PAR1, TR
Protein nameProteinase-activated receptor 1
Protein functionHigh affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development. {ECO:0000269|PubMed:10079109}.
Subcellular locationCell membrane;
Multi-pass membrane protein.
ECO codeClick here for more information.
Amino acid sequence
FASTA format: P25116
Gene Ontology
(Biological Process)
Complete annatation
activation of cysteine-type endopeptidase activity involved in apoptotic process [GO:0006919];
activation of MAPKK activity [GO:0000186];
anatomical structure morphogenesis [GO:0009653];
blood coagulation [GO:0007596];
connective tissue replacement involved in inflammatory response wound healing [GO:0002248];
establishment of synaptic specificity at neuromuscular junction [GO:0007529];
G-protein coupled receptor signaling pathway [GO:0007186];
homeostasis of number of cells within a tissue [GO:0048873];
inflammatory response [GO:0006954];
negative regulation of cell proliferation [GO:0008285];
negative regulation of glomerular filtration [GO:0003105];
negative regulation of neuron apoptotic process [GO:0043524];
negative regulation of renin secretion into blood stream [GO:1900134];
phospholipase C-activating G-protein coupled receptor signaling pathway [GO:0007200];
platelet activation [GO:0030168];
platelet dense granule organization [GO:0060155];
positive regulation of blood coagulation [GO:0030194];
positive regulation of calcium ion transport [GO:0051928];
positive regulation of cell migration [GO:0030335];
positive regulation of cell proliferation [GO:0008284];
positive regulation of collagen biosynthetic process [GO:0032967];
positive regulation of cysteine-type endopeptidase activity involved in apoptotic process [GO:0043280];
positive regulation of cytosolic calcium ion concentration [GO:0007204];
positive regulation of cytosolic calcium ion concentration involved in phospholipase C-activating G-protein coupled signaling pathway [GO:0051482];
positive regulation of ERK1 and ERK2 cascade [GO:0070374];
positive regulation of I-kappaB kinase/NF-kappaB signaling [GO:0043123];
positive regulation of interleukin-6 secretion [GO:2000778];
positive regulation of interleukin-8 secretion [GO:2000484];
positive regulation of JAK-STAT cascade [GO:0046427];
positive regulation of MAPK cascade [GO:0043410];
positive regulation of phosphatidylinositol 3-kinase signaling [GO:0014068];
positive regulation of release of sequestered calcium ion into cytosol [GO:0051281];
positive regulation of Rho protein signal transduction [GO:0035025];
positive regulation of smooth muscle contraction [GO:0045987];
positive regulation of transcription, DNA-templated [GO:0045893];
positive regulation of vasoconstriction [GO:0045907];
protein kinase C-activating G-protein coupled receptor signaling pathway [GO:0007205];
regulation of blood coagulation [GO:0030193];
regulation of interleukin-1 beta production [GO:0032651];
regulation of sensory perception of pain [GO:0051930];
release of sequestered calcium ion into cytosol [GO:0051209];
response to lipopolysaccharide [GO:0032496];
response to wounding [GO:0009611];
STAT protein import into nucleus [GO:0007262];
tyrosine phosphorylation of STAT protein [GO:0007260]
Gene Ontology
(Molecular Function)
Complete annatation
G-protein alpha-subunit binding [GO:0001965];
G-protein beta-subunit binding [GO:0031681];
G-protein coupled receptor activity [GO:0004930];
receptor binding [GO:0005102];
thrombin receptor activity [GO:0015057]
Gene Ontology
(Cellular Component)
Complete annatation
caveola [GO:0005901];
cell surface [GO:0009986];
cytosol [GO:0005829];
early endosome [GO:0005769];
extracellular region [GO:0005576];
Golgi apparatus [GO:0005794];
integral component of plasma membrane [GO:0005887];
late endosome [GO:0005770];
neuromuscular junction [GO:0031594];
plasma membrane [GO:0005886];
platelet dense tubular network [GO:0031094];
postsynaptic membrane [GO:0045211]
Protein-protein interaction108448
Phylogenetic treeP25116
HIV replication factor status Zhou et al., Cell. Host. Microbe., 2008
Brass et al., Science, 2008
Smith et al., J. Immunol, 2010
gene status
Lu et al., J. Virol., 2011
      Folds changes 8h: unknown; Folds changes 16h: unknown; Tested: unknown;
Schoggins JW and Rice CM, Curr. Opin. Virol., 2011
      Targeted viruses: unknown
      Viral life cycle: unknown
      Mechanism related to antiviral activity: unknown
Anti-viral restriction factor Liu et al., Retrovirology, 2011
      unknown (Triplicates)

Gene Expression Profile       top

            Up-regulated;            Down-regulated

For brief introduction to each study, please go to the help page.

Gene expression during HIV latency

(1). Mohammadi et al., PLoS Pathog., 2014

Differentially expressed transcripts (Pairwise) during latency and subsequent viral reactivation using several agents - Primary CD4+ T-cell based model

DMSO: Dimethyl suloxyde (negative control) - 0.0033% final
SAHA: Vorinostat (Histone deacetylase inhibitor) - 0.5 μM
CD3: TCR Stimulation by IL-2+ antiCD3/anti-CD28 antibodies
IL7: Interleukin-7 based stimulation
DISU: Disulfiram (alcohol dehydrogenase inhibitor) - 0.5 μM
AZA: 5-azacytidine (AZA; DNA methylation inhibitor) - 1 μM
Experimental Condition Log2 Fold Change P value Adjusted P value
AZA vs. CD3-2.12621488004951.89124193084034e-071.71097229181426e-06
AZA vs. DISU-0.05155968302772570.8405755483178560.986800805932004
AZA vs. IL7-0.3604867134151880.1845065140235290.952505417553304
AZA vs. SAHA0.3653068016185840.1404757455698840.476170764272639
DISU vs. CD32.062307319688061.64932265733775e-071.91324935244661e-06
DISU vs. IL7-0.3197187607747070.2114542791903430.59173440853804
DISU vs. SAHA0.4190358080859270.154677632066290.506267268089952
DMSO vs. AZA-0.02368429777183530.9082519347265881
DMSO vs. CD32.094720963885784.1004553563706e-073.15009484669674e-06
DMSO vs. DISU0.02707202075198830.9128091404489350.988283279918411
DMSO vs. IL7-0.3302886068444590.216417963094840.724804783238115
DMSO vs. SAHA0.3827230323799710.110197825515210.393925860611889
HIV vs. Mock in Activation0.3077932896400770.7107407883790330.999983755607037
HIV vs. Mock in Latency0.5927688245911650.0004748781363325130.0352626257491443
IL7 vs. CD31.770970110486054.85015438281833e-050.000309379504918412
SAHA vs. CD32.467749955079262.62409427520538e-105.03759244934332e-09
SAHA vs. IL70.7233537880962990.00356658151373690.0302547269206922
(2). Iglesias-Ussel et al., J. Virol., 2013

Up and Downregulated transcripts during Latency (Latently infected CD4+ T cells vs Uninfected)- Primary CD4+Tcell based model
Log2 Fold Change P Value
unknown unknown

Gene expression during HIV infection and replication

(1). Imbeault et al., PloS Pathog., 2012

Transcriptomic profiling of HIV-1 infected CD4+ T cells - Primary CD4+ T cells
Experiment type Log2 Fold Change P Value Adjusted P Value
Infected vs. Mock 1.447 1.53E-11 3.79E-09
Infected vs. Bystander 1.572 2.75E-12 5.17E-10
(2). Lefebvre et al., J. Virol., 2011

Transcriptome analysis of T-cell line (Sup T1)
Log2 Fold Change unknown
(3). Li et al., J. Immunol., 2013

Lymphatic tissue
Acute Fold Change Acute P Value Asymt Fold Change Asypt P Value AIDS Fold Change AIDS P Value
-1.2 0.151418693 -1.5 0.002281862 -2 0.001337595
(4). Chang et al., MBio., 2011

Transcriptome analysis of T-cell line (Sup T1)

Derived from Sherrill-Mix et al., BMC Retrovirol., 2015 cross validation
Up-regulated (True) unknown
(5). Sherrill-Mix et al., BMC Retrovirol., 2015

Deep RNA-seq analysis of primary human T cell infected with low passage HIV isolate HIV89.6 - Primary CD4+ T cell based
Test Status Log2 Fold Change P Value
OK 2.33771 0.000305467
(6). Rotger et al., PLoS Pathog., 2010

Genome-wide mRNA expression of CD4+ T cells from HIV-infected patient
(Genes differentially expressed (at adjusted p<0.01) according to the empirical Bayes approach)
Log2 Fold Change P Value
unknown unknown

Proteomic/Transcriptomics studies indicating differentially expressed genes mediated by HIV

(1). Greenwood et al., Elife, 2016

Activated (CD3/CD28) Primary human CD4+ T cells infected with pNL4-3-dE-EGFP. The table shows the complete (unfiltered) TMT (tandem mass tag)-based proteomic time course dataset
6 h 24 h 48 h 72 h RTi
unknown unknown unknown unknown unknown
(2). Navare et al., Virology, 2012

SUP-T1 cell line
FC-4hpi P-value FC-8hpi P-value FC-20hpi P-value Category
unknown unknown unknown unknown unknown unknown unknown
(3). Hyrcza et al., J. Virolo., 2007

Primary human CD4+ and CD8+ T Cells
Affymetrix Prob ID Fold Change In CD8? Category
unknown unknown unknown unknown

Protein Overview       top

Drug-protein Interaction       (annotations from DrugBank)      top

Drugbank ID Drug Name Drug Status Pharmacological Action Drug Action
DB00086 Streptokinase approved unknown cleavage
DB05361 SR-123781A investigational unknown unknown
DB05692 SCH-530348 investigational unknown unknown
DB09030 Vorapaxar approved yes antagonist

Protein Secondary Structure       (annotations from PDB)      top

PDB Accession Method Resolution Chain Structure Preview
1NRN X-ray 3.1Å R=38-60.
1NRO X-ray 3.1Å R=38-64.
1NRP X-ray 3.0Å R=38-60.
1NRQ X-ray 3.5Å R=40-60.
1NRR X-ray 2.4Å R=43-60.
3BEF X-ray 2.2Å C/F=49-57.
3HKI X-ray 2.2Å C/F=42-62.
3HKJ X-ray 2.6Å C/F=42-62.
3LU9 X-ray 1.8Å C/F=33-57.
3VW7 X-ray 2.2Å A=86-395.

HIV-1 Interaction       (annotations from NCBI HIV-1 Interaction Database)      top

HIV Partner Interaction Type PubMed
Envelope surface glycoprotein gp160; precursor inhibited by 26283733
Envelope transmembrane glycoprotein gp41 inhibits 26283733
Vpr blocks 26283733
HIV-1 virus replication inhibited by expression of human gene 26283733

Metabolic/Signalling Pathway       (annotations from KEGG database)      top

Pathway Accession Number Description
hsa04015 Rap1 signaling pathway - Homo sapiens (human)
hsa04020 Calcium signaling pathway - Homo sapiens (human)
hsa04024 cAMP signaling pathway - Homo sapiens (human)
hsa04072 Phospholipase D signaling pathway - Homo sapiens (human)
hsa04080 Neuroactive ligand-receptor interaction - Homo sapiens (human)
hsa04144 Endocytosis - Homo sapiens (human)
hsa04151 PI3K-Akt signaling pathway - Homo sapiens (human)
hsa04610 Complement and coagulation cascades - Homo sapiens (human)
hsa04611 Platelet activation - Homo sapiens (human)
hsa04810 Regulation of actin cytoskeleton - Homo sapiens (human)
hsa05200 Pathways in cancer - Homo sapiens (human)