DT-Web

DB01252 - Mitiglinide


Identification
Name Mitiglinide
Accession Number DB01252
Type small molecule
Description Mitiglinide is a drug for the treatment of type 2 diabetes .Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 315.4067
Groups approved
Monoisotopic Weight 315.183443671
Pharmacology
Indication For the treatment of type 2 diabetes.
Mechanism of action Mitiglinide is thought to stimulate insulin secretion by binding to and blocking ATP-sensitive K(+) (K(ATP)) channels (Kir6.2/SUR1 complex, KATP channels) in pancreatic beta-cells. Closure of potassium channels causes depolarization which stimulates calcium influx through voltage-gated calcium channels. High intracellular calcium subsequently triggers the exocytosis of insulin granules.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms Not Available
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


ATP-binding cassette transporter sub-family C member 8
Name ATP-binding cassette transporter sub-family C member 8
Gene Name ABCC8
Pharmacological action yes
Actions inhibitor
References
  • Sunaga Y, Gonoi T, Shibasaki T, Ichikawa K, Kusama H, Yano H, Seino S: The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol. 2001 Nov 9;431(1):119-25. - Pubmed
  • Nagamatsu S, Ohara-Imaizumi M, Nakamichi Y, Kikuta T, Nishiwaki C: Imaging docking and fusion of insulin granules induced by antidiabetes agents: sulfonylurea and glinide drugs preferentially mediate the fusion of newcomer, but not previously docked, insulin granules. Diabetes. 2006 Oct;55(10):2819-25. - Pubmed
  • Ogawa K, Ikewaki K, Taniguchi I, Takatsuka H, Mori C, Sasaki H, Okazaki F, Shimizu M, Mochizuki S: Mitiglinide, a novel oral hypoglycemic agent, preserves the cardioprotective effect of ischemic preconditioning in isolated perfused rat hearts. Int Heart J. 2007 May;48(3):337-45. - Pubmed
DTHybrid score 0.3636
Peroxisome proliferator-activated receptor gamma
Name Peroxisome proliferator-activated receptor gamma
Gene Name PPARG
Pharmacological action unknown
Actions agonist
References
  • Scarsi M, Podvinec M, Roth A, Hug H, Kersten S, Albrecht H, Schwede T, Meyer UA, Rucker C: Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: a combined virtual screening and biological assay approach. Mol Pharmacol. 2007 Feb;71(2):398-406. Epub 2006 Nov 2. - Pubmed
DTHybrid score 1.0076

Enzymes


UDP-glucuronosyltransferase 1-3
Name UDP-glucuronosyltransferase 1-3
Gene Name UGT1A3
Actions substrate
References
  • Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. - Pubmed
DTHybrid score 0.2209
UDP-glucuronosyltransferase 2B7
Name UDP-glucuronosyltransferase 2B7
Gene Name UGT2B7
Actions substrate
References
  • Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. - Pubmed
DTHybrid score 0.2271

Predictions


Id Partner name Gene Name Score
4757 Cytochrome P450 2C9 CYP2C9 0.126
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.1046
709 ATP-sensitive inward rectifier potassium channel 1 KCNJ1 0.0931
4924 Cytochrome P450 2C8 CYP2C8 0.0838
4512 Cytochrome P450 3A4 CYP3A4 0.0835
20 Prostaglandin G/H synthase 1 PTGS1 0.0751
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0695
6016 Cytochrome P450 2C19 CYP2C19 0.0686
1588 Multidrug resistance protein 1 ABCB1 0.0683
587 Serum albumin ALB 0.068
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0667
4209 ATP-sensitive inward rectifier potassium channel 8 KCNJ8 0.0569
1729 Solute carrier family 22 member 6 SLC22A6 0.0503
290 Prostaglandin G/H synthase 2 PTGS2 0.0463
6228 Nuclear receptor coactivator 1 NCOA1 0.0462
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0396
459 Retinoic acid receptor RXR-alpha RXRA 0.0389
6180 UDP-glucuronosyltransferase 2B4 UGT2B4 0.0381
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0377
4118 Cytochrome P450 3A5 CYP3A5 0.037
6177 UDP-glucuronosyltransferase 1-10 UGT1A10 0.0366
80 Peroxisome proliferator-activated receptor alpha PPARA 0.0345
4119 Cytochrome P450 2D6 CYP2D6 0.0322
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.031
70 Type-1 angiotensin II receptor AGTR1 0.0305
631 3-hydroxy-3-methylglutaryl-coenzyme A reductase HMGCR 0.0301
3387 3-hydroxy-3-methylglutaryl-coenzyme A reductase mvaA 0.0301
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0299
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0296
4200 Cytochrome P450 1A2 CYP1A2 0.0292
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0281
6241 Nuclear receptor coactivator 2 NCOA2 0.028
2164 Multidrug resistance-associated protein 4 ABCC4 0.0269
6181 UDP-glucuronosyltransferase 1-8 UGT1A8 0.0259
6107 Cytochrome P450 3A7 CYP3A7 0.0249
1974 Oligopeptide transporter, kidney isoform SLC15A2 0.0246
6030 Cytochrome P450 2B6 CYP2B6 0.024
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0235
183 Vascular endothelial growth factor A VEGFA 0.023
1502 Peroxisome proliferator-activated receptor delta PPARD 0.0225
6157 Solute carrier organic anion transporter family member 1B3 SLCO1B3 0.0209
862 Multidrug resistance-associated protein 1 ABCC1 0.0202
3802 Sodium channel protein type 2 subunit alpha SCN2A 0.0197
275 Arachidonate 5-lipoxygenase ALOX5 0.0186
5880 Thrombopoietin receptor MPL 0.0183
1457 Long-chain-fatty-acid--CoA ligase 4 ACSL4 0.0164
3233 Bile acid receptor NR1H4 0.0156
606 Cytochrome P450 27, mitochondrial CYP27A1 0.0154
5718 Cytochrome P450 2A6 CYP2A6 0.0154
588 Chromodomain-helicase-DNA-binding protein 1 CHD1 0.0144
890 Niemann-Pick C1-like protein 1 NPC1L1 0.0143
467 Delta-type opioid receptor OPRD1 0.0142
696 Kappa-type opioid receptor OPRK1 0.0142
847 Mu-type opioid receptor OPRM1 0.0135
838 Inosine-5'-monophosphate dehydrogenase 1 IMPDH1 0.0135
796 Inosine-5'-monophosphate dehydrogenase 2 IMPDH2 0.0135
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.013
1760 Aminopeptidase N ANPEP 0.0126
6843 Aminopeptidase N pepN 0.0126
6024 Cytochrome P450 1A1 CYP1A1 0.0125
117 Sterol O-acyltransferase 1 SOAT1 0.0123
6179 UDP-glucuronosyltransferase 2B17 UGT2B17 0.0123
703 NADPH azoreductase azr 0.0122
2184 Cystic fibrosis transmembrane conductance regulator CFTR 0.0121
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0121
6106 Cytochrome P450 2C18 CYP2C18 0.0118
4604 Liver carboxylesterase 1 CES1 0.0118
6142 Solute carrier family 22 member 8 SLC22A8 0.0114
2038 Inhibitor of nuclear factor kappa-B kinase subunit beta IKBKB 0.0113
521 ATP-binding cassette transporter sub-family C member 9 ABCC9 0.0108
738 Monocarboxylate transporter 1 SLC16A1 0.0107
6143 Solute carrier family 22 member 7 SLC22A7 0.0105
4164 Potassium voltage-gated channel subfamily KQT member 5 KCNQ5 0.0104
4163 Potassium voltage-gated channel subfamily KQT member 4 KCNQ4 0.0104
2021 Thrombomodulin THBD 0.0103
4162 Potassium voltage-gated channel subfamily KQT member 3 KCNQ3 0.0101
1024 Solute carrier family 22 member 11 SLC22A11 0.0101
776 Bile salt export pump ABCB11 0.0099
6141 Sodium/bile acid cotransporter SLC10A1 0.0099
1630 Integrin beta-2 ITGB2 0.0098
723 Cytosolic phospholipase A2 PLA2G4A 0.0095
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0095
267 Plasminogen activator inhibitor 1 SERPINE1 0.0095
6138 Multidrug resistance protein 3 ABCB4 0.0093
132 ATP-binding cassette sub-family A member 1 ABCA1 0.0091
6221 Steroid hormone receptor ERR1 ESRRA 0.0089
1629 Transcription factor AP-1 JUN 0.0084
6044 Serum paraoxonase/lactonase 3 PON3 0.0079
817 DNA topoisomerase 2-alpha TOP2A 0.0078
243 Ribosyldihydronicotinamide dehydrogenase [quinone] NQO2 0.0076
3961 G protein-activated inward rectifier potassium channel 4 KCNJ5 0.0076
572 Integrin alpha-L ITGAL 0.0073
1792 Tissue-type plasminogen activator PLAT 0.0073
3809 Estrogen-related receptor gamma ESRRG 0.0071
273 Apoptosis regulator Bcl-2 BCL2 0.0069
6085 Fatty acid-binding protein, intestinal FABP2 0.0068
6102 Arylamine N-acetyltransferase 2 NAT2 0.0068
590 5-hydroxytryptamine 2C receptor HTR2C 0.0068
4122 Histone deacetylase 2 HDAC2 0.0067
841 Gamma-aminobutyric-acid receptor subunit alpha-6 GABRA6 0.0066
530 Gamma-aminobutyric-acid receptor subunit alpha-4 GABRA4 0.0065
1039 Histone deacetylase 9 HDAC9 0.0064
6136 Multidrug resistance-associated protein 5 ABCC5 0.0064
811 Translocator protein TSPO 0.0063
580 Gamma-aminobutyric-acid receptor subunit alpha-3 GABRA3 0.0062
523 Gamma-aminobutyric-acid receptor subunit alpha-5 GABRA5 0.0062
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0062
423 Gamma-aminobutyric-acid receptor subunit alpha-2 GABRA2 0.0062
617 Muscarinic acetylcholine receptor M2 CHRM2 0.006
502 5-hydroxytryptamine 2A receptor HTR2A 0.006
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0058
492 Histamine H1 receptor HRH1 0.0058
1757 Myeloperoxidase MPO 0.0058
2222 Equilibrative nucleoside transporter 1 SLC29A1 0.0058
6220 Aryl hydrocarbon receptor AHR 0.0056
630 Short/branched chain specific acyl-CoA dehydrogenase, mitochondrial ACADSB 0.0055
789 Alpha-1D adrenergic receptor ADRA1D 0.0055
78 Acetyl-CoA acetyltransferase, mitochondrial ACAT1 0.0055
182 2-oxoglutarate dehydrogenase E1 component, mitochondrial OGDH 0.0054
759 Free fatty acid receptor 1 FFAR1 0.0054
1818 Long-chain-fatty-acid--CoA ligase 3 ACSL3 0.0054
54 Prothrombin F2 0.0053
2981 Phospholipase A2, membrane associated PLA2G2A 0.0051
6013 Cytochrome P450 2E1 CYP2E1 0.005
632 Alpha-1B adrenergic receptor ADRA1B 0.0049
340 Apoptotic protease-activating factor 1 APAF1 0.0049
170 Succinate semialdehyde dehydrogenase, mitochondrial ALDH5A1 0.0047
6042 Prostaglandin reductase 2 PTGR2 0.0047
1053 BC269730_2 FADS1 0.0047
1395 Sodium/calcium exchanger 1 SLC8A1 0.0047
3811 Cytochrome P450 19A1 CYP19A1 0.0046
1650 Heme carrier protein 1 SLC46A1 0.0044
3312 Fatty acid-binding protein, brain FABP7 0.0044
556 Alpha-1A adrenergic receptor ADRA1A 0.0044
1558 Transient receptor potential cation channel subfamily V member 1 TRPV1 0.0044
825 Arsenical pump-driving ATPase ASNA1 0.0043
3435 Arsenical pump-driving ATPase arsA 0.0043
2105 ATP-binding cassette sub-family G member 1 ABCG1 0.0043
510 Serine/threonine-protein kinase receptor R3 ACVRL1 0.0043
733 Activin receptor type 1B ACVR1B 0.0043
745 Anti-Muellerian hormone type-2 receptor AMHR2 0.0043
486 Serine/threonine-protein kinase ALS2CR7 CDK15 0.0043
483 A-Raf proto-oncogene serine/threonine-protein kinase ARAF 0.0043
21 Beta-adrenergic receptor kinase 2 ADRBK2 0.0043
377 Beta-adrenergic receptor kinase 1 ADRBK1 0.0043
154 AFG3-like protein 2 AFG3L2 0.0043
225 NEDD8-activating enzyme E1 regulatory subunit NAE1 0.0043
395 ALK tyrosine kinase receptor Not Available 0.0043
6043 Putative G-protein coupled receptor 44 GPR44 0.0042
280 4-aminobutyrate aminotransferase, mitochondrial ABAT 0.0042
33 Cystine/glutamate transporter SLC7A11 0.004
4217 Telomerase reverse transcriptase TERT 0.0039
292 Activin receptor type-1 ACVR1 0.0038
849 Activated CDC42 kinase 1 TNK2 0.0038
704 Long-chain-fatty-acid--CoA ligase 1 ACSL1 0.0038
297 Adenylate cyclase type 1 ADCY1 0.0038
821 Acetyl-coenzyme A synthetase 2-like, mitochondrial ACSS1 0.0038
386 Acetyl-coenzyme A synthetase, cytoplasmic ACSS2 0.0038
289 Cytosolic purine 5'-nucleotidase NT5C2 0.0038
341 5-hydroxytryptamine 3 receptor HTR3A 0.0037
1313 Lactoylglutathione lyase GLO1 0.0037
952 Dipeptidyl peptidase 4 DPP4 0.0036
748 5'-AMP-activated protein kinase catalytic subunit alpha-1 PRKAA1 0.0035
484 Tyrosine-protein kinase ABL2 ABL2 0.0035
6155 ATP-binding cassette transporter sub-family C member 11 ABCC11 0.0035
740 Argininosuccinate synthase ASS1 0.0032
865 Argininosuccinate synthase ASS1 0.0032
2680 Argininosuccinate synthase argG 0.0032
3194 Argininosuccinate synthase argG 0.0032
824 Sodium-dependent serotonin transporter SLC6A4 0.0032
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0031
2320 Thymidine kinase, cytosolic TK1 0.0031
6145 Solute carrier family 22 member 1 SLC22A1 0.0031
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0031
242 Asparagine synthetase [glutamine-hydrolyzing] ASNS 0.0031
476 RAC-alpha serine/threonine-protein kinase AKT1 0.0031
6021 Adenosine kinase ADK 0.003
6137 Multidrug resistance-associated protein 6 ABCC6 0.003
661 ADP/ATP translocase 1 SLC25A4 0.0029
118 Organic cation/carnitine transporter 2 SLC22A5 0.0029
17 Proto-oncogene tyrosine-protein kinase ABL1 ABL1 0.0025
389 Amiloride-sensitive cation channel 2, neuronal ACCN2 0.0022
3804 Sodium channel protein type 4 subunit alpha SCN4A 0.002
6031 Cytochrome P450 3A43 CYP3A43 0.0018
6144 Solute carrier family 22 member 2 SLC22A2 0.0018
6091 Gamma-aminobutyric acid receptor subunit theta GABRQ 0.0017
6086 Gamma-aminobutyric acid receptor subunit gamma-2 GABRG2 0.0016
6090 Gamma-aminobutyric acid receptor subunit pi GABRP 0.0016
6092 Gamma-aminobutyric acid receptor subunit rho-2 GABRR2 0.0016
6088 Gamma-aminobutyric acid receptor subunit gamma-3 GABRG3 0.0016
6115 Gamma-aminobutyric acid receptor subunit rho-3 GABRR3 0.0016
4100 Gamma-aminobutyric-acid receptor subunit beta-2 GABRB2 0.0016
6093 Gamma-aminobutyric acid receptor subunit delta GABRD 0.0016
6087 Gamma-aminobutyric acid receptor subunit gamma-1 GABRG1 0.0016
6089 Gamma-aminobutyric acid receptor subunit epsilon GABRE 0.0016
142 Gamma-aminobutyric-acid receptor subunit rho-1 GABRR1 0.0016
4098 Gamma-aminobutyric-acid receptor subunit beta-1 GABRB1 0.0015
4099 Gamma-aminobutyric-acid receptor subunit beta-3 GABRB3 0.0015
6158 Solute carrier organic anion transporter family member 1C1 SLCO1C1 0.0015
373 Transthyretin TTR 0.0013
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0012
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