Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| 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 | [1], [2] |
| Glibenclamide | Drug Info | Approved | Diabetes | [3], [4] | |
| Gliclazide | Drug Info | Approved | Diabetes | [5] | |
| Glimepiride | Drug Info | Approved | Diabetes | [6], [7] | |
| Repaglinide | Drug Info | Approved | Diabetes | [8], [9] | |
| Tolbutamide | Drug Info | Approved | Non-insulin dependent diabetes | [10] | |
| NN-414 | Drug Info | Phase 1 | Type 1 diabetes | [11] | |
| Modulator | Acetohexamide | Drug Info | |||
| Glibenclamide | Drug Info | [12] | |||
| NN-414 | Drug Info | ||||
| NS-11757 | Drug Info | [13] | |||
| Blocker | Gliclazide | Drug Info | [14], [15] | ||
| Glimepiride | Drug Info | [16] | |||
| Repaglinide | Drug Info | [15], [17], [18] | |||
| Tolbutamide | Drug Info | [19] | |||
| Inhibitor | HBR-985 | Drug Info | [20] | ||
| 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 1 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071893. | ||||
| REF 2 | (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 3 | 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 4 | (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 5 | Cefradine - FDA approved drug information (drug label) from DailyMed. | ||||
| REF 6 | 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 7 | (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 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077571. | ||||
| REF 9 | (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: 6841). | ||||
| REF 10 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 11 | 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 12 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
| REF 13 | (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: 2944). | ||||
| REF 14 | Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes. 2001 Oct;50(10):2253-9. | ||||
| REF 15 | Pharmacological modulation of K(ATP) channels. Biochem Soc Trans. 2002 Apr;30(2):333-9. | ||||
| REF 16 | Mechanism of disopyramide-induced hypoglycaemia in a patient with Type 2 diabetes. Diabet Med. 2009 Jan;26(1):76-8. | ||||
| REF 17 | Clinical pharmacokinetics and pharmacodynamics of repaglinide. Clin Pharmacokinet. 2002;41(7):471-83. | ||||
| REF 18 | Metformin/Repaglinide (PrandiMet) for type 2 diabetes. Med Lett Drugs Ther. 2009 Jun 1;51(1313):41-3. | ||||
| REF 19 | 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 20 | Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas. J Med Chem. 2001 Mar 29;44(7):1085-98. | ||||
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