Property Summary

NCBI Gene PubMed Count 531
Grant Count 156
R01 Count 51
Funding $27,476,238.56
PubMed Score 285.22
PubTator Score 2867.06

Knowledge Summary

Patent (33,607)

TINX Plot

  Disease Relevance (53)

Disease Z-score Confidence
Donohue Syndrome 6 5.599 2.8
Polycystic Ovary Syndrome 332 4.349 2.2
Acanthosis nigricans 14 4.239 2.1
diabetes mellitus 1,663 4.221 2.1
Hyperinsulinism 63 4.065 2.0
Obesity 616 3.763 1.9
Hyperglycemia 120 3.703 1.9
Hypertrichosis 23 3.208 1.6
Cancer 2,346 3.121 1.6
Hyperandrogenism 32 3.058 1.5
Alzheimer's disease 644
Breast cancer 3,094
Carcinoma 2,147 1.0
Congenital diaphragmatic hernia 43
Diabetes Mellitus, Experimental 106
Diabetes Mellitus, Insulin-Resistant, wi... 1 
Diabetes Mellitus, Non-Insulin-Dependent 157
Diabetes mellitus type 1 1
Diabetes mellitus type 2 69
Diabetic Neuropathies 13
Gout 93 2.0
Hyperalgesia 71
Hyperinsulinemic Hypoglycemia, Familial,... 1 
Impaired glucose tolerance 12
Insulin Resistance 48
Insulin resistance - type A 1
Lewy Body Disease 19
Lung diseases 48
Multiple myeloma 1,327
Parkinson Disease 102
Rabson-Mendenhall Syndrome 1
Retinal disease 16 1.0
Substance-Related Disorders 114
Type 2 diabetes mellitus with acanthosis... 1 
adult high grade glioma 2,148
astrocytoma 1,493
atypical teratoid / rhabdoid tumor 4,369
dermatomyositis 933
ependymoma 2,514
esophageal adenocarcinoma 737
glioblastoma 5,572
intraductal papillary-mucinous adenoma (... 2,956 
intraductal papillary-mucinous neoplasm ... 3,289 
malignant mesothelioma 3,162
medulloblastoma, large-cell 6,234
osteosarcoma 7,933
ovarian cancer 8,484
pancreatic cancer 2,300
pancreatic carcinoma 567
primary Sjogren syndrome 789
primary pancreatic ductal adenocarcinoma 1,271
psoriasis 6,685
spina bifida 1,064

Expression

  Differential Expression (21)

Disease log2 FC p
pancreatic cancer -1.400 0.003
Multiple myeloma 1.672 0.012
malignant mesothelioma 1.700 0.000
astrocytoma 2.200 0.007
ependymoma -1.100 0.003
esophageal adenocarcinoma 1.800 0.022
psoriasis -2.700 0.000
osteosarcoma -2.019 0.000
atypical teratoid / rhabdoid tumor -1.200 0.004
glioblastoma -1.400 0.003
medulloblastoma, large-cell -2.200 0.000
primary pancreatic ductal adenocarcinoma -1.341 0.004
intraductal papillary-mucinous adenoma (... -1.300 0.016
intraductal papillary-mucinous neoplasm ... -1.400 0.027
Breast cancer 2.900 0.037
adult high grade glioma -1.200 0.004
primary Sjogren syndrome -1.500 0.000
pancreatic carcinoma 1.100 0.030
spina bifida -1.577 0.047
ovarian cancer -1.200 0.001
dermatomyositis 1.600 0.000

Synonym

Accession P06213 Q17RW0 Q59H98 Q9UCB7 Q9UCB8 Q9UCB9 IR
Symbols HHF5
CD220

Gene

PDB

3W11   3W12   3W13   4OGA   4XSS   2Z8C   2B4S   1GAG   1I44   1IR3   1IRK   1P14   1RQQ   2AUH   2HR7   2MFR   3BU3   3BU5   3BU6   3EKK   3EKN   3ETA   3W14   4IBM   4XLV   4XST   4ZXB   5E1S   5HHW   5J3H  

  TechDev Info (1)

Gary Johnson Kinome profile via MIB/MS Technology

MLP Assay (2)

AID Type Active / Inconclusive / Inactive Description
1982 other 0 / 0 / 0 Kinase inhibition selectivity assay for compound SID-48409448
652206 other 0 / 0 / 0 ML-187 activity in a kinase panel for Extended probe characterization for beta-cell apoptosis Measured in Biochemical System

Gene RIF (282)

PMID Text
27172637 results indicate a significant correlation between T132903C and C109869T single nucleotide polymorphisms in the insulin receptor and solute carrier family 6 member 14 amino acid transporter (SLC6A14) genes with idiopathic infertility in Persian males
26874853 A novel insertion/deletion (indel) mutation was found in INSR gene.
26862994 Data indicate that a highly specific qRT-PCR assay to quantify levels of the insulin-like growth factor receptor and insulin receptor isoforms (IR-A, IR-B, and IGF-1R) on the same scale to provide a critical diagnostic and predictive tool.
26850678 Given the limited number of patients treated with KW-2450 in our study, it is not possible to make a meaningful comparison of efficacy with other IGF-1R/IR dual kinases inhibitors
26760116 Low-oxygen tension can modify the IGF-1 or IGF-2 signaling via the IGF-1R and IR in placental mesenchymal stem cells.
26721804 C1008T SNP at exon 17 of INSR is associated with insulin resistance in Indian women with polycystic ovarian syndrome.
26584640 mTORC2 promotes rapamycin- and ligand-induced type I insulin-like growth factor receptor / insulin receptor phosphorylation.
26438154 remarkable therapeutic window observed for BI 885578 is achieved by virtue of the distinctive pharmacokinetic properties of the compound capitalizing on the physiologic mechanism of glucose homeostasis and differential levels of IGF1R and INSR expression
26406954 The results demonstrate an increased IR-A:IR-B ratio in all clinical stages of breast cancer
26297026 Down-regulation of IR and IGF1R, achieved by insulin + fructose and monoclonal antibody treatments, results in decreased downstream signaling.
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AA Sequence

MATGGRRGAAAAPLLVAVAALLLGAAGHLYPGEVCPGMDIRNNLTRLHELENCSVIEGHLQILLMFKTRP      1 - 70
EDFRDLSFPKLIMITDYLLLFRVYGLESLKDLFPNLTVIRGSRLFFNYALVIFEMVHLKELGLYNLMNIT     71 - 140
RGSVRIEKNNELCYLATIDWSRILDSVEDNYIVLNKDDNEECGDICPGTAKGKTNCPATVINGQFVERCW    141 - 210
THSHCQKVCPTICKSHGCTAEGLCCHSECLGNCSQPDDPTKCVACRNFYLDGRCVETCPPPYYHFQDWRC    211 - 280
VNFSFCQDLHHKCKNSRRQGCHQYVIHNNKCIPECPSGYTMNSSNLLCTPCLGPCPKVCHLLEGEKTIDS    281 - 350
VTSAQELRGCTVINGSLIINIRGGNNLAAELEANLGLIEEISGYLKIRRSYALVSLSFFRKLRLIRGETL    351 - 420
EIGNYSFYALDNQNLRQLWDWSKHNLTITQGKLFFHYNPKLCLSEIHKMEEVSGTKGRQERNDIALKTNG    421 - 490
DQASCENELLKFSYIRTSFDKILLRWEPYWPPDFRDLLGFMLFYKEAPYQNVTEFDGQDACGSNSWTVVD    491 - 560
IDPPLRSNDPKSQNHPGWLMRGLKPWTQYAIFVKTLVTFSDERRTYGAKSDIIYVQTDATNPSVPLDPIS    561 - 630
VSNSSSQIILKWKPPSDPNGNITHYLVFWERQAEDSELFELDYCLKGLKLPSRTWSPPFESEDSQKHNQS    631 - 700
EYEDSAGECCSCPKTDSQILKELEESSFRKTFEDYLHNVVFVPRKTSSGTGAEDPRPSRKRRSLGDVGNV    701 - 770
TVAVPTVAAFPNTSSTSVPTSPEEHRPFEKVVNKESLVISGLRHFTGYRIELQACNQDTPEERCSVAAYV    771 - 840
SARTMPEAKADDIVGPVTHEIFENNVVHLMWQEPKEPNGLIVLYEVSYRRYGDEELHLCVSRKHFALERG    841 - 910
CRLRGLSPGNYSVRIRATSLAGNGSWTEPTYFYVTDYLDVPSNIAKIIIGPLIFVFLFSVVIGSIYLFLR    911 - 980
KRQPDGPLGPLYASSNPEYLSASDVFPCSVYVPDEWEVSREKITLLRELGQGSFGMVYEGNARDIIKGEA    981 - 1050
ETRVAVKTVNESASLRERIEFLNEASVMKGFTCHHVVRLLGVVSKGQPTLVVMELMAHGDLKSYLRSLRP   1051 - 1120
EAENNPGRPPPTLQEMIQMAAEIADGMAYLNAKKFVHRDLAARNCMVAHDFTVKIGDFGMTRDIYETDYY   1121 - 1190
RKGGKGLLPVRWMAPESLKDGVFTTSSDMWSFGVVLWEITSLAEQPYQGLSNEQVLKFVMDGGYLDQPDN   1191 - 1260
CPERVTDLMRMCWQFNPKMRPTFLEIVNLLKDDLHPSFPEVSFFHSEENKAPESEELEMEFEDMENVPLD   1261 - 1330
RSSHCQREEAGGRDGGSSLGFKRSYEEHIPYTHMNGGKKNGRILTLPRSNPS                     1331 - 1382
//

Text Mined References (558)

PMID Year Title
27172637 Four Single Nucleotide Polymorphisms in INSR, SLC6A14, TAS2R38, and OR2W3 Genes in Association with Idiopathic Infertility in Persian Men.
26874853 2016 First molecular diagnosis of Donohue syndrome in Africa: novel unusual insertion/deletion mutation in the INSR gene.
26862994 2016 Development of a Quantitative PCR Assay for Detection of Human Insulin-Like Growth Factor Receptor and Insulin Receptor Isoforms.
26850678 2016 Preclinical and first-in-human phase I studies of KW-2450, an oral tyrosine kinase inhibitor with insulin-like growth factor receptor-1/insulin receptor selectivity.
26760116 2016 Low Oxygen Tension Modulates the Insulin-Like Growth Factor-1 or -2 Signaling via Both Insulin-Like Growth Factor-1 Receptor and Insulin Receptor to Maintain Stem Cell Identity in Placental Mesenchymal Stem Cells.
26721804 2016 Single-Nucleotide Polymorphism on Exon 17 of Insulin Receptor Gene Influences Insulin Resistance in PCOS: A Pilot Study on North Indian Women.
26584640 2016 mTORC2 promotes type I insulin-like growth factor receptor and insulin receptor activation through the tyrosine kinase activity of mTOR.
26438154 2015 BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.
26406954 2015 Quantification of insulin receptor mRNA splice variants as a diagnostic tumor marker in breast cancer.
26297026 2015 Insulin and IGF1 signalling pathways in human astrocytes in vitro and in vivo; characterisation, subcellular localisation and modulation of the receptors.
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