Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T58921 | Target Info | |||
| Target Name | Peroxisome proliferator-activated receptor gamma (PPAR-gamma) | ||||
| Synonyms |
PPAR-gamma; Nuclear receptor subfamily 1 group C member 3; NR1C3
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| Target Type | Successful Target | ||||
| Gene Name | PPARG | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Peroxisome proliferator-activated receptor alpha (PPARA) | Successful Target | ||||
| UniProt ID | PPARA_HUMAN | |||||
| Gene Name | PPARA | |||||
| Synonyms |
Peroxisome proliferater-activated receptor alpha; PPARalpha; PPAR-alpha; PPAR; Nuclear receptor subfamily 1 group C member 1; NR1C1
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| Representative Drug(s) | GW-409544 | Drug Info | EC50 = 2 nM | Click to Show More | [1] | |
| 2 | Imiglitazar | Drug Info | EC50 = 5 nM | [2] | ||
| 3 | TESAGLITAZAR | Drug Info | EC50 = 37 nM | [3] | ||
| 4 | MURAGLITAZAR | Drug Info | EC50 = 40 nM | [4] | ||
| 5 | FARGLITAZAR | Drug Info | EC50 = 122 nM | [6] | ||
| 6 | Ragaglitazar | Drug Info | IC50 = 980 nM | [8] | ||
| Co-Target Name | Platelet-derived growth factor receptor beta (PDGFRB) | Successful Target | ||||
| UniProt ID | PGFRB_HUMAN | |||||
| Gene Name | PDGFRB | |||||
| Synonyms |
Platelet-derived growth factor receptor 1; PDGFR1; PDGFR-beta; PDGFR-1; PDGFR; PDGF-R-beta; CD140b antigen; CD140b; CD140 antigen-like family member B; Beta-type platelet-derived growth factor receptor; Beta-PDGFR; Beta platelet-derived growth factor receptor
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| Representative Drug(s) | Rosiglitazone + metformin | Drug Info | IC50 = 50 nM | [5] | ||
| Co-Target Name | Vascular endothelial growth factor receptor 2 (KDR) | Successful Target | ||||
| UniProt ID | VGFR2_HUMAN | |||||
| Gene Name | KDR | |||||
| Synonyms |
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
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| Representative Drug(s) | Rosiglitazone + metformin | Drug Info | IC50 = 135 nM | [7] | ||
| Co-Target Name | Vascular endothelial growth factor receptor 1 (FLT-1) | Clinical trial Target | ||||
| UniProt ID | VGFR1_HUMAN | |||||
| Gene Name | FLT1 | |||||
| Synonyms |
Vascular permeability factor receptor; VEGFR1; VEGFR-1; VEGF-1 receptor; Tyrosine-protein kinase receptor FLT; Tyrosine-protein kinase FRT; Fms-like tyrosine kinase 1; FRT; FLT
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| Representative Drug(s) | Rosiglitazone + metformin | Drug Info | IC50 = 28 nM | [7] | ||
| Co-Target Name | Aurora kinase B (AURKB) | Clinical trial Target | ||||
| UniProt ID | AURKB_HUMAN | |||||
| Gene Name | AURKB | |||||
| Synonyms |
Serine/threonine-protein kinase aurora-B; Serine/threonine-protein kinase 5; Serine/threonine-protein kinase 12; Serine/threonine protein kinase 12; STK5; STK12; Aurora/IPL1-related kinase 2; Aurora-related kinase 2; Aurora-B; Aurora-2 kinase; Aurora-2; Aurora- and Ipl1-like midbody-associated protein 1; Aurora 1; ARK2; ARK-2; AIRK2; AIM1; AIM-1; AIK2
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| Representative Drug(s) | Rosiglitazone + metformin | Drug Info | IC50 = 35 nM | [9] | ||
| Co-Target Name | Aurora kinase C (AURKC) | Clinical trial Target | ||||
| UniProt ID | AURKC_HUMAN | |||||
| Gene Name | AURKC | |||||
| Synonyms |
Serine/threonine-protein kinase aurora-C; STK13; Aurora/Ipl1/Eg2 protein 2; Aurora/Ipl1-related kinase 3; Aurora-related kinase 3; Aurora-C; Aurora 3; ARK3; ARK-3; AIRK3; AIK3; AIE2
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| Representative Drug(s) | Rosiglitazone + metformin | Drug Info | IC50 = 210 nM | [9] | ||
| Co-Target Name | Alpha glucosidase (AGL) | Co-Target | ||||
| UniProt ID | MGA_HUMAN; MGAL_HUMAN; SUIS_HUMAN; LYAG_HUMAN | |||||
| Gene Name | MGAM; MGAM2; SI; GAA | |||||
| Representative Drug(s) | Thiazolidinedione | Drug Info | IC50 = 540 nM | [10] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. J Med Chem. 2004 Aug 12;47(17):4118-27. | ||||
| REF 2 | Design and synthesis of novel bis-oximinoalkanoic acids as potent PPAR alpha agonists. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1156-61. | ||||
| REF 3 | 4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1617-22. | ||||
| REF 4 | Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma ... Bioorg Med Chem Lett. 2008 Jun 15;18(12):3545-50. | ||||
| REF 5 | 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50. | ||||
| REF 6 | Anti-diabetic activity of fused PPARgamma-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression. Eur J Med Chem. 2017 Sep 8;137:310-26. | ||||
| REF 7 | The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. | ||||
| REF 8 | Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar. J Med Chem. 2003 Apr 10;46(8):1306-17. | ||||
| REF 9 | The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. | ||||
| REF 10 | Synthetic heterocyclic candidates as promising alpha-glucosidase inhibitors: An overview. Eur J Med Chem. 2019 Aug 15;176:343-377. | ||||
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