Therapeutic Targets Database
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TTD Target ID: TTDS00292

Target Information
NameInsulin receptor    
Type of targetSuccessful target    
SynonymsCD220 antigen    
IR    
DiseaseDiabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[1]
Drug(s)Insulin Glargine recombinantApprovedDiabetes mellitus[2][3]
Insulin Lyspro recombinantApprovedDiabetes mellitus[4]
Insulin recombinantApprovedDiabetes mellitus[4]
Insulin, porcineApprovedDiabetes mellitus[5]
Insulin-aspartApprovedDiabetes mellitus[6]
Insulin-detemirApprovedDiabetes mellitus[7]
Insulin-glargineApprovedDiabetes mellitus[8]
Insulin-glulisineApprovedDiabetes mellitus[9]
Insulin-lisproApprovedDiabetes mellitus[10]
MeglitinidesApprovedHyperglycaemia in type 2 diabetes mellitus[11]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayAdherens junction
Insulin signaling pathway
Type II diabetes mellitus
UniProt IDP06213
PDB Structure1GAG; 1I44; 1IR3; 1IRK; 1P14; 1RQQ; 2AUH; 2B4S; 2DTG; 2HR7; 2Z8C; 3BU3; 3BU5; 3BU6; 3EKK; 3EKN; 3ETA; 3LOH; 3W11; 3W12; 3W13; 3W14.    
FunctionThis receptor binds insulin and has a tyrosine-protein kinase activity.    
SequenceMGTGGRRGAAAAPLLVAVAALLLGAAGHLYPGEVCPGMDIRNNLTRLHELENCSVIEGHL QILLMFKTRPEDFRDLSFPKLIMITDYLLLFRVYGLESLKDLFPNLTVIRGSRLFFNYAL VIFEMVHLKELGLYNLMNITRGSVRIEKNNELCYLATIDWSRILDSVEDNYIVLNKDDNE ECGDICPGTAKGKTNCPATVINGQFVERCWTHSHCQKVCPTICKSHGCTAEGLCCHSECL GNCSQPDDPTKCVACRNFYLDGRCVETCPPPYYHFQDWRCVNFSFCQDLHHKCKNSRRQG CHQYVIHNNKCIPECPSGYTMNSSNLLCTPCLGPCPKVCHLLEGEKTIDSVTSAQELRGC TVINGSLIINIRGGNNLAAELEANLGLIEEISGYLKIRRSYALVSLSFFRKLRLIRGETL EIGNYSFYALDNQNLRQLWDWSKHNLTTTQGKLFFHYNPKLCLSEIHKMEEVSGTKGRQE RNDIALKTNGDKASCENELLKFSYIRTSFDKILLRWEPYWPPDFRDLLGFMLFYKEAPYQ NVTEFDGQDACGSNSWTVVDIDPPLRSNDPKSQNHPGWLMRGLKPWTQYAIFVKTLVTFS DERRTYGAKSDIIYVQTDATNPSVPLDPISVSNSSSQIILKWKPPSDPNGNITHYLVFWE RQAEDSELFELDYCLKGLKLPSRTWSPPFESEDSQKHNQSEYEDSAGECCSCPKTDSQIL KELEESSFRKTFEDYLHNVVFVPRKTSSGTGAEDPRPSRKRRSLGDVGNVTVAVPTVAAF PNTSSTSVPTSPEEHRPFEKVVNKESLVISGLRHFTGYRIELQACNQDTPEERCSVAAYV SARTMPEAKADDIVGPVTHEIFENNVVHLMWQEPKEPNGLIVLYEVSYRRYGDEELHLCV SRKHFALERGCRLRGLSPGNYSVRIRATSLAGNGSWTEPTYFYVTDYLDVPSNIAKIIIG PLIFVFLFSVVIGSIYLFLRKRQPDGPLGPLYASSNPEYLSASDVFPCSVYVPDEWEVSR EKITLLRELGQGSFGMVYEGNARDIIKGEAETRVAVKTVNESASLRERIEFLNEASVMKG FTCHHVVRLLGVVSKGQPTLVVMELMAHGDLKSYLRSLRPEAENNPGRPPPTLQEMIQMA AEIADGMAYLNAKKFVHRDLAARNCMVAHDFTVKIGDFGMTRDIYETDYYRKGGKGLLPV RWMAPESLKDGVFTTSSDMWSFGVVLWEITSLAEQPYQGLSNEQVLKFVMDGGYLDQPDN CPERVTDLMRMCWQFNPKMRPTFLEIVNLLKDDLHPSFPEVSFFHSEENKAPESEELEME FEDMENVPLDRSSHCQREEAGGRDGGSSLGFKRSYEEHIPYTHMNGGKKNGRILTLPRSN PS
Related US Patent6,600,069
Target ValidationClick to Find Target Validation Information.    
Inhibitor4- ([12]
4- ([12]
Adenosine-5'-[Beta, Gamma-Methylene]Triphosphate[13]
NVP-AEW541[14]
NVP-TAE684[15]
StimulatorMeglitinides[11]
BinderHumulin (Human insulin isophane)[4]
Insulin Glargine recombinant[2][3]
Insulin Lispro[10]
Insulin Lyspro recombinant[4]
Insulin lispro recombinant[4]
Insulin recombinant[4]
Insulin, porcine[5]
Insulin-aspart[6]
Insulin-detemir[7]
Insulin-glargine[8]
Insulin-glulisine[9]
Insulin-lispro[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1New approaches in the treatment of type 2 diabetes. Curr Opin Chem Biol. 2000 Aug;4(4):461-7. To Reference
Ref 2Efficacy and safety of insulin glulisine in Japanese patients with type 1 diabetes mellitus. Diabetes Obes Metab. 2009 Jul 13. [Epub ahead of print] To Reference
Ref 3Use of insulin glargine and cancer incidence in Scotland: a study from the Scottish Diabetes Research Network Epidemiology Group. Diabetologia. 2009 Jul 15. [Epub ahead of print] To Reference
Ref 4Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 5Acidic residues on the N-terminus of proinsulin C-Peptide are important for the folding of insulin precursor. J Biochem. 2002 Jun;131(6):855-9. To Reference
Ref 6Comparison of insulin detemir and insulin glargine using a basal-bolus regimen in a randomized, controlled clinical study in patients with type 2 diabetes. Diabetes Metab Res Rev. 2009 Jun 29. [Epub ahead of print] To Reference
Ref 7The role of insulin detemir in overweight type 2 diabetes management. Vasc Health Risk Manag. 2009;5(3):553-60. Epub 2009 Jun 29. To Reference
Ref 8Safe and Simple Emergency Department Discharge Therapy for Type 2 Diabetes Patients with Severe Hyperglycemia. Endocr Pract. 2009 Jul 20:1-26. [Epub ahead of print] To Reference
Ref 9Insulin glulisine: a review of its use in the management of diabetes mellitus. Drugs. 2009;69(8):1035-57. doi: 10.2165/00003495-200969080-00006. To Reference
Ref 10Hope for insulin mimetic oral antidiabetic drugs. Eur J Endocrinol. 1999 Dec;141(6):561-2. To Reference
Ref 11New drugs for type 2 diabetes mellitus: what is their place in therapy? Drugs. 2008;68(15):2131-62. To Reference
Ref 12Eur J Pharmacol. 2007 May 7;562(1-2):1-11. Epub 2007 Feb 3.ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents. To Reference
Ref 13Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 14J Med Chem. 2009 Aug 27;52(16):4981-5004.Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. To Reference
Ref 15Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. Epub 2006 Dec 21.Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. To Reference



 

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