mutLBSgeneDB

mutLBSgeneDB
mutated Ligand Binding Site gene DataBase

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Gene Summary

Ligand Binding Site Mutation Information

Protein Structure Related Information

Gene Expression and Gene-Gene Network

Phenotype Information

Pharmacological Information

Conservation Information for LBS

Gene summary for F2R
Gene summary
Basic gene Info.Gene symbolF2R
Gene namecoagulation factor II (thrombin) receptor
SynonymsCF2R|HTR|PAR-1|PAR1|TR
CytomapUCSC genome browser: 5q13
Type of geneprotein-coding
RefGenesNM_001992.3,
Descriptionprotease-activated receptor 1proteinase-activated receptor 1
Modification date20141222
dbXrefs MIM : 187930
HGNC : HGNC
Ensembl : ENSG00000181104
HPRD : 01763
Vega : OTTHUMG00000131299
ProteinUniProt: P25116
go to UniProt's Cross Reference DB Table
ExpressionCleanEX: HS_F2R
BioGPS: 2149
PathwayNCI Pathway Interaction Database: F2R
KEGG: F2R
REACTOME: F2R
Pathway Commons: F2R
ContextiHOP: F2R
ligand binding site mutation search in PubMed: F2R
UCL Cancer Institute: F2R
Assigned class in mutLBSgeneDBB: This gene belongs to targetable_mutLBSgenes.

Gene ontology having evidence of Inferred from Direct Assay (IDA) from Entrez
GO IDGO TermPubMed ID
GO:0002248connective tissue replacement involved in inflammatory response wound healing9639571
GO:0006919activation of cysteine-type endopeptidase activity involved in apoptotic process10692450
GO:0007200phospholipase C-activating G-protein coupled receptor signaling pathway20164183
GO:0007260tyrosine phosphorylation of STAT protein10692450
GO:0007262STAT protein import into nucleus10692450
GO:0008285negative regulation of cell proliferation10692450
GO:0009611response to wounding9639571
GO:0030168platelet activation9038223
GO:0030193regulation of blood coagulation17848177
GO:0030194positive regulation of blood coagulation9038223
GO:0032967positive regulation of collagen biosynthetic process9639571
GO:0043280positive regulation of cysteine-type endopeptidase activity involved in apoptotic process10692450
GO:0043410positive regulation of MAPK cascade17848177
GO:0045893positive regulation of transcription, DNA-templated17848177
GO:0046427positive regulation of JAK-STAT cascade10692450
GO:0051281positive regulation of release of sequestered calcium ion into cytosol1672265
GO:2000484positive regulation of interleukin-8 secretion17404307
GO:2000778positive regulation of interleukin-6 secretion11447194


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Ligand binding site mutations for F2R

Cancer type specific mutLBS sorted by frequency
LBSAAchange of nsSNVCancer type# samples
H336H336DCOAD1
L333L333QSKCM1
H336A335VSTAD1
Y187M186IUCEC1
cf) Cancer type abbreviation. BLCA: Bladder urothelial carcinoma, BRCA: Breast invasive carcinoma, CESC: Cervical squamous cell carcinoma and endocervical adenocarcinoma, COAD: Colon adenocarcinoma, GBM: Glioblastoma multiforme, LGG: Brain lower grade glioma, HNSC: Head and neck squamous cell carcinoma, KICH: Kidney chromophobe, KIRC: Kidney renal clear cell carcinoma, KIRP: Kidney renal papillary cell carcinoma, LAML: Acute myeloid leukemia, LUAD: Lung adenocarcinoma, LUSC: Lung squamous cell carcinoma, OV: Ovarian serous cystadenocarcinoma, PAAD: Pancreatic adenocarcinoma, PRAD: Prostate adenocarcinoma, SKCM: Skin cutaneous melanoma, STAD: Stomach adenocarcinoma, THCA: Thyroid carcinoma, UCEC: Uterine corpus endometrial carcinoma.


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Protein structure related information for F2R
Relative protein structure stability change (ΔΔE) using Mupro 1.1
Mupro score denotes assessment of the effect of mutations on thermodynamic stability.
  (ΔΔE<0: mutation decreases stability, ΔΔE>0: mutation increases stability)
: nsSNV at non-LBS: nsSNV at LBS

nsSNVs sorted by the relative stability change of protein structure by each mutation
Blue: mutations of positive stability change. and red : the most recurrent mutation for this gene.
LBSAAchange of nsSNVRelative stability change
H336H336D-1.2850537
L333L333Q-1.2039434
Y187M186I-0.88598603
H336A335V-0.83427508
(MuPro1.1: Jianlin Cheng et al., Prediction of Protein Stability Changes for Single-Site Mutations Using Support Vector Machines, PROTEINS: Structure, Function, and Bioinformatics. 2006, 62:1125-1132)

Structure image for F2R from PDB

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Differential gene expression and gene-gene network for F2R
Differential gene expression between mutated and non-mutated LBS samples in all 16 major cancer types

Differential co-expressed gene network based on protein-protein interaction data (CePIN)
* Left PPI network was created from samples with mutations in the LBS of F2R and the right PPI network was created from samples without mutations in the LBS of F2R. Only genes with p-value < 0.05 are shown.
Red circle: input gene. Orange circle: LBSgene. Blue circle: other gene.


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Phenotype information for F2R
Gene level disease information (DisGeNet)
Disease IDDisease name# PubMedAssociation type
umls:C0015695Fatty Liver3Biomarker
umls:C0021368Inflammation2Biomarker
umls:C0023890Liver Cirrhosis2Biomarker, GeneticVariation
umls:C0019158Hepatitis1Biomarker
umls:C0027659Neoplasms, Experimental1Biomarker
umls:C0038356Stomach Neoplasms1Biomarker

Mutation level pathogenic information (ClinVar annotation)
Allele IDAA changeClinical significanceOriginPhenotype IDs

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Pharmacological information for F2R
Gene expression profile of anticancer drug treated cell-lines (CCLE)
Heatmap showing the correlation between gene expression and drug response across all the cell-lines. We chose the top 20 among 138 drugs.We used Pearson's correlation coefficient.

Gene-centered drug-gene interaction network
Drug information targeting mutLBSgene (Approved drugs only)
Drug statusDrugBank IDNameTypeDrug structure
ApprovedDB00086StreptokinaseBiotech
InvestigationalDB05361SR-123781ASmall molecule
InvestigationalDB05692SCH-530348Small molecule
ApprovedDB09030VorapaxarSmall molecule

Gene-centered ligand-gene interaction network

Ligands binding to mutated ligand binding site of F2R go to BioLip
Ligand IDLigand short nameLigand long namePDB IDPDB namemutLBS
VPXVORAPAXARETHYL [(1R,3AR,4AR,6R,8AR,9S,9AS)-9-{(E)-2-[5-(3- FLUOROPHENYL)PYRIDIN-2-YL]ETHENYL}-1-METHYL-3- OXODODECAHYDRONAPHTHO[2,3-C]FURAN-6-YL]CARBAMATE3vw7AY187 L333 H336


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Conservation information for LBS of F2R
Multiple alignments for P25116 in multiple species
LBSAA sequence# speciesSpecies
A349STTEAAYFAYL1Homo sapiens
A349PGTEAAYFAYL1Mus musculus
A349PMTEAAYFAYL1Bos taurus
F271YYAYYFSAFSA1Homo sapiens
F271FYSYYFSAFSA1Mus musculus
F271YYSYYFSAFSA1Bos taurus
G233ALAIAGVVPLL1Homo sapiens
G233VMAIMGVVPLL1Mus musculus
G233AMAIAGVAPLL1Bos taurus
H336VLLIAHYSFLS1Homo sapiens
H336VLLIVHYLFLS1Mus musculus
H336ILLLLHYAFLS1Bos taurus
L237AGVVPLLLKEQ1Homo sapiens
L237MGVVPLLLKEQ1Mus musculus
L237AGVAPLLLQEQ1Bos taurus
L332GPTNVLLIAHY1Homo sapiens
L332GPTNVLLIVHY1Mus musculus
L332GPTNILLLLHY1Bos taurus
L333PTNVLLIAHYS1Homo sapiens
L333PTNVLLIVHYL1Mus musculus
L333PTNILLLLHYA1Bos taurus
L340AHYSFLSHTST1Homo sapiens
L340VHYLFLSDSPG1Mus musculus
L340LHYAFLSSDPM1Bos taurus
P236IAGVVPLLLKE1Homo sapiens
P236IMGVVPLLLKE1Mus musculus
P236IAGVAPLLLQE1Bos taurus
Y183VTAAFYCNMYA1Homo sapiens
Y183ATAAFYGNMYA1Mus musculus
Y183VTAAFYGNMYA1Bos taurus
Y187FYGNMYASIML2Mus musculus, Bos taurus
Y187FYCNMYASILL1Homo sapiens
Y337LLIAHYSFLSH1Homo sapiens
Y337LLIVHYLFLSD1Mus musculus
Y337LLLLHYAFLSS1Bos taurus
Y350TTEAAYFAYLL1Homo sapiens
Y350GTEAAYFAYLL1Mus musculus
Y350MTEAAYFAYLL1Bos taurus
Y353AAYFAYLLCVC3Homo sapiens, Mus musculus, Bos taurus


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