Target Information
Target General Infomation | |||||
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Target ID |
T91480
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Former ID |
TTDS00331
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Target Name |
Sulfonylurea receptor 1
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Gene Name |
ABCC8
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Synonyms |
SUR1; ATPbinding cassette subfamily C member 8; Sulfonylurea receptor 1; Kir6.2/SUR1; SUR1-type K(ATP) channel; ABCC8
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Target Type |
Successful
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Disease | Atrial fibrillation [ICD9: 272, 427.31; ICD10: E78, I48] | ||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Non-insulin dependent diabetes [ICD10: E11.9] | |||||
Type 1 diabetes [ICD9: 250; ICD10: E10] | |||||
Function |
Putative subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
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BioChemical Class |
ABC transporter
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Target Validation |
T92305
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UniProt ID | |||||
Sequence |
MPLAFCGSENHSAAYRVDQGVLNNGCFVDALNVVPHVFLLFITFPILFIGWGSQSSKVHI
HHSTWLHFPGHNLRWILTFMLLFVLVCEIAEGILSDGVTESHHLHLYMPAGMAFMAAVTS VVYYHNIETSNFPKLLIALLVYWTLAFITKTIKFVKFLDHAIGFSQLRFCLTGLLVILYG MLLLVEVNVIRVRRYIFFKTPREVKPPEDLQDLGVRFLQPFVNLLSKGTYWWMNAFIKTA HKKPIDLRAIGKLPIAMRALTNYQRLCEAFDAQVRKDIQGTQGARAIWQALSHAFGRRLV LSSTFRILADLLGFAGPLCIFGIVDHLGKENDVFQPKTQFLGVYFVSSQEFLANAYVLAV LLFLALLLQRTFLQASYYVAIETGINLRGAIQTKIYNKIMHLSTSNLSMGEMTAGQICNL VAIDTNQLMWFFFLCPNLWAMPVQIIVGVILLYYILGVSALIGAAVIILLAPVQYFVATK LSQAQRSTLEYSNERLKQTNEMLRGIKLLKLYAWENIFRTRVETTRRKEMTSLRAFAIYT SISIFMNTAIPIAAVLITFVGHVSFFKEADFSPSVAFASLSLFHILVTPLFLLSSVVRST VKALVSVQKLSEFLSSAEIREEQCAPHEPTPQGPASKYQAVPLRVVNRKRPAREDCRGLT GPLQSLVPSADGDADNCCVQIMGGYFTWTPDGIPTLSNITIRIPRGQLTMIVGQVGCGKS SLLLAALGEMQKVSGAVFWSSLPDSEIGEDPSPERETATDLDIRKRGPVAYASQKPWLLN ATVEENIIFESPFNKQRYKMVIEACSLQPDIDILPHGDQTQIGERGINLSGGQRQRISVA RALYQHANVVFLDDPFSALDIHLSDHLMQAGILELLRDDKRTVVLVTHKLQYLPHADWII AMKDGTIQREGTLKDFQRSECQLFEHWKTLMNRQDQELEKETVTERKATEPPQGLSRAMS SRDGLLQDEEEEEEEAAESEEDDNLSSMLHQRAEIPWRACAKYLSSAGILLLSLLVFSQL LKHMVLVAIDYWLAKWTDSALTLTPAARNCSLSQECTLDQTVYAMVFTVLCSLGIVLCLV TSVTVEWTGLKVAKRLHRSLLNRIILAPMRFFETTPLGSILNRFSSDCNTIDQHIPSTLE CLSRSTLLCVSALAVISYVTPVFLVALLPLAIVCYFIQKYFRVASRDLQQLDDTTQLPLL SHFAETVEGLTTIRAFRYEARFQQKLLEYTDSNNIASLFLTAANRWLEVRMEYIGACVVL IAAVTSISNSLHRELSAGLVGLGLTYALMVSNYLNWMVRNLADMELQLGAVKRIHGLLKT EAESYEGLLAPSLIPKNWPDQGKIQIQNLSVRYDSSLKPVLKHVNALIAPGQKIGICGRT GSGKSSFSLAFFRMVDTFEGHIIIDGIDIAKLPLHTLRSRLSIILQDPVLFSGTIRFNLD PERKCSDSTLWEALEIAQLKLVVKALPGGLDAIITEGGENFSQGQRQLFCLARAFVRKTS IFIMDEATASIDMATENILQKVVMTAFADRTVVTIAHRVHTILSADLVIVLKRGAILEFD KPEKLLSRKDSVFASFVRADK |
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Drugs and Mode of Action | |||||
Drug(s) | Acetohexamide | Drug Info | Approved | Diabetes | [538241], [541874] |
Glibenclamide | Drug Info | Approved | Diabetes | [537022], [539544] | |
Gliclazide | Drug Info | Approved | Diabetes | [549819] | |
Glimepiride | Drug Info | Approved | Diabetes | [536554], [541902] | |
Repaglinide | Drug Info | Approved | Diabetes | [538328], [541921] | |
Tolbutamide | Drug Info | Approved | Non-insulin dependent diabetes | [551871] | |
NN-414 | Drug Info | Phase 1 | Type 1 diabetes | [521917] | |
Modulator | Acetohexamide | Drug Info | |||
Glibenclamide | Drug Info | [556264] | |||
NN-414 | Drug Info | ||||
NS-11757 | Drug Info | [539957] | |||
Blocker | Gliclazide | Drug Info | [535269], [535457] | ||
Glimepiride | Drug Info | [537007] | |||
Repaglinide | Drug Info | [535457], [535492], [537390] | |||
Tolbutamide | Drug Info | [536969] | |||
Inhibitor | HBR-985 | Drug Info | [535148] | ||
Pathways | |||||
KEGG Pathway | ABC transporters | ||||
Insulin secretion | |||||
Type II diabetes mellitus | |||||
Pathway Interaction Database | FOXA2 and FOXA3 transcription factor networks | ||||
PathWhiz Pathway | Muscle/Heart Contraction | ||||
Pancreas Function | |||||
Reactome | ABC-family proteins mediated transport | ||||
Regulation of insulin secretion | |||||
WikiPathways | Potassium Channels | ||||
Integration of energy metabolism | |||||
References | |||||
Ref 521917 | ClinicalTrials.gov (NCT00400283) A Study Looking Into the Effect of NNC 55-0414 in Subjects With Type 2 Diabetes. U.S. National Institutes of Health. | ||||
Ref 536554 | Clinical utilization of combined rosiglitazone and glimepiride in the treatment of type 2 diabetes mellitus. Orv Hetil. 2007 Dec 9;148(49):2331-5. | ||||
Ref 537022 | Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets. 2009 Jan;10(1):71-87. | ||||
Ref 538241 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071893. | ||||
Ref 538328 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077571. | ||||
Ref 539544 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2414). | ||||
Ref 541874 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6793). | ||||
Ref 541902 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6820). | ||||
Ref 535148 | Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas. J Med Chem. 2001 Mar 29;44(7):1085-98. | ||||
Ref 535269 | Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes. 2001 Oct;50(10):2253-9. | ||||
Ref 535492 | Clinical pharmacokinetics and pharmacodynamics of repaglinide. Clin Pharmacokinet. 2002;41(7):471-83. | ||||
Ref 536969 | Expression of an activating mutation in the gene encoding the KATP channel subunit Kir6.2 in mouse pancreatic beta cells recapitulates neonatal diabetes. J Clin Invest. 2009 Jan;119(1):80-90. doi: 10.1172/JCI35772. Epub 2008 Dec 8. | ||||
Ref 537007 | Mechanism of disopyramide-induced hypoglycaemia in a patient with Type 2 diabetes. Diabet Med. 2009 Jan;26(1):76-8. | ||||
Ref 537390 | Metformin/Repaglinide (PrandiMet) for type 2 diabetes. Med Lett Drugs Ther. 2009 Jun 1;51(1313):41-3. |
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