Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T58921
(Former ID: TTDS00338)
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| Target Name |
Peroxisome proliferator-activated receptor gamma (PPAR-gamma)
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| Synonyms |
PPAR-gamma; Nuclear receptor subfamily 1 group C member 3; NR1C3
Click to Show/Hide
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| Gene Name |
PPARG
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Acute diabete complication [ICD-11: 5A2Y] | |||||
| 2 | Alzheimer disease [ICD-11: 8A20] | |||||
| 3 | Type 2 diabetes mellitus [ICD-11: 5A11] | |||||
| Function |
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. ARF6 acts as a key regulator of the tissue-specific adipocyte P2 (aP2) enhancer. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated proinflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of ARNTL/BMAL1 in the blood vessels (By similarity).
Click to Show/Hide
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| BioChemical Class |
Nuclear hormone receptor
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| UniProt ID | ||||||
| Sequence |
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL LQVIKKTETDMSLHPLLQEIYKDLY Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A02556 ; BADD_A04820 ; BADD_A05675 | |||||
| HIT2.0 ID | T58J2Y | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 5 Approved Drugs | + | ||||
| 1 | Lobeglitazone | Drug Info | Approved | Type-2 diabetes | [2] | |
| 2 | Pioglitazone | Drug Info | Approved | Diabetic complication | [3], [4] | |
| 3 | Rosiglitazone XR | Drug Info | Approved | Type-2 diabetes | [5] | |
| 4 | Thiazolidinedione | Drug Info | Approved | Alzheimer disease | [6] | |
| 5 | Troglitazone | Drug Info | Approved | Diabetic complication | [7], [8] | |
| Clinical Trial Drug(s) | [+] 27 Clinical Trial Drugs | + | ||||
| 1 | Balaglitazone | Drug Info | Phase 3 | Type-1 diabetes | [9] | |
| 2 | CS-038 | Drug Info | Phase 3 | Type-2 diabetes | [10] | |
| 3 | FARGLITAZAR | Drug Info | Phase 3 | Type-1 diabetes | [11], [12] | |
| 4 | Imiglitazar | Drug Info | Phase 3 | Type-2 diabetes | [13], [14] | |
| 5 | Leriglitazone | Drug Info | Phase 3 | Cerebral X-linked adrenoleukodystrophy | [15] | |
| 6 | Ragaglitazar | Drug Info | Phase 3 | Type-1 diabetes | [16], [17] | |
| 7 | Rivoglitazone | Drug Info | Phase 3 | Ocular inflammation | [18] | |
| 8 | Rosiglitazone + metformin | Drug Info | Phase 3 | Diabetic complication | [19] | |
| 9 | Rosiglitazone + simvastatin | Drug Info | Phase 3 | Type-2 diabetes | [20] | |
| 10 | TESAGLITAZAR | Drug Info | Phase 3 | Type-1 diabetes | [21] | |
| 11 | ZYH-1 | Drug Info | Phase 3 | Lipid metabolism disorder | [22] | |
| 12 | MBX-102 | Drug Info | Phase 2/3 | Gout | [23] | |
| 13 | CHS-131 | Drug Info | Phase 2 | Multiple sclerosis | [24] | |
| 14 | FK-614 | Drug Info | Phase 2 | Type-2 diabetes | [25] | |
| 15 | GED-0507-34-Levo | Drug Info | Phase 2 | Inflammatory bowel disease | [26] | |
| 16 | MBX-2044 | Drug Info | Phase 2 | Type-2 diabetes | [27] | |
| 17 | Naveglitazar | Drug Info | Phase 2 | Diabetic complication | [28] | |
| 18 | Netoglitazone | Drug Info | Phase 2 | Non-alcoholic fatty liver disease | [29], [30] | |
| 19 | OMS405 | Drug Info | Phase 2 | Nicotine dependence | [31] | |
| 20 | ONO-5129 | Drug Info | Phase 2 | Diabetic complication | [32] | |
| 21 | T3D-959 | Drug Info | Phase 2 | Alzheimer disease | [33] | |
| 22 | T3D-959 | Drug Info | Phase 1/2 | Alzheimer disease | [34] | |
| 23 | CLX-0921 | Drug Info | Phase 1 | Type-2 diabetes | [35] | |
| 24 | DSP-8658 | Drug Info | Phase 1 | Type-2 diabetes | [36] | |
| 25 | Englitazone sodium | Drug Info | Phase 1 | Type-2 diabetes | [37] | |
| 26 | GW-409544 | Drug Info | Phase 1 | Hyperlipidaemia | [38], [39] | |
| 27 | Oxeglitazar | Drug Info | Phase 1 | Gout | [40] | |
| Discontinued Drug(s) | [+] 18 Discontinued Drugs | + | ||||
| 1 | AVE-0847 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [41] | |
| 2 | GSK-677954 | Drug Info | Discontinued in Phase 2 | Non-alcoholic fatty liver disease | [30] | |
| 3 | Indeglitazar | Drug Info | Discontinued in Phase 2 | Type-2 diabetes | [42] | |
| 4 | KRP-297 | Drug Info | Discontinued in Phase 2 | Type-2 diabetes | [43] | |
| 5 | Reglixane | Drug Info | Discontinued in Phase 2 | Diabetic complication | [44] | |
| 6 | Sodelglitazar | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [45] | |
| 7 | YM-440 | Drug Info | Discontinued in Phase 2 | Type-1 diabetes | [46] | |
| 8 | DS-6930 | Drug Info | Discontinued in Phase 1 | Diabetic complication | [47] | |
| 9 | E-3030 | Drug Info | Discontinued in Phase 1 | Hyperlipidaemia | [48] | |
| 10 | LY-929 | Drug Info | Discontinued in Phase 1 | Lipid metabolism disorder | [49], [50] | |
| 11 | AD-5075 | Drug Info | Terminated | Type-2 diabetes | [53], [54] | |
| 12 | AKP-320 | Drug Info | Terminated | Type-2 diabetes | [55] | |
| 13 | BVT-142 | Drug Info | Terminated | Type-2 diabetes | [56] | |
| 14 | CS-204 | Drug Info | Terminated | Metabolic disorder | [57] | |
| 15 | DARGLITAZONE | Drug Info | Terminated | Diabetic complication | [58] | |
| 16 | Edaglitazone | Drug Info | Terminated | Type-2 diabetes | [59] | |
| 17 | SB-219994 | Drug Info | Terminated | Diabetic complication | [60], [61] | |
| 18 | Sipoglitazar | Drug Info | Terminated | Diabetic complication | [62] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | Ciglitazone | Drug Info | Preclinical | Pulmonary fibrosis | [51] | |
| 2 | MC-3002 | Drug Info | Preclinical | Metabolic disorder | [52] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Agonist | [+] 53 Agonist drugs | + | ||||
| 1 | Lobeglitazone | Drug Info | [2] | |||
| 2 | Pioglitazone | Drug Info | [1], [63] | |||
| 3 | Rosiglitazone XR | Drug Info | [64] | |||
| 4 | Thiazolidinedione | Drug Info | [1] | |||
| 5 | Troglitazone | Drug Info | [1], [65], [66] | |||
| 6 | Glitazone | Drug Info | [67] | |||
| 7 | Leriglitazone | Drug Info | [75] | |||
| 8 | Rivoglitazone | Drug Info | [77] | |||
| 9 | Rosiglitazone + metformin | Drug Info | [64] | |||
| 10 | Rosiglitazone + simvastatin | Drug Info | [64] | |||
| 11 | MBX-102 | Drug Info | [27] | |||
| 12 | FK-614 | Drug Info | [25] | |||
| 13 | GED-0507-34-Levo | Drug Info | [79] | |||
| 14 | MBX-2044 | Drug Info | [27] | |||
| 15 | OMS405 | Drug Info | [82] | |||
| 16 | T3D-959 | Drug Info | [84] | |||
| 17 | CLX-0921 | Drug Info | [35] | |||
| 18 | Englitazone sodium | Drug Info | [37], [87] | |||
| 19 | 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative 1 | Drug Info | [88] | |||
| 20 | 3-phenyl acrylic acid derivative 1 | Drug Info | [88] | |||
| 21 | A-substituted phenylpropionic acid derivative 1 | Drug Info | [88] | |||
| 22 | A-substituted phenylpropionic acid derivative 2 | Drug Info | [88] | |||
| 23 | Biaromatic compound 1 | Drug Info | [88] | |||
| 24 | Crystalline anhydrous toluene derivative 1 | Drug Info | [88] | |||
| 25 | Flavonoid derivative 8 | Drug Info | [88] | |||
| 26 | Fused aromatic compound 1 | Drug Info | [88] | |||
| 27 | Fused ring compound 1 | Drug Info | [88] | |||
| 28 | MRL20 | Drug Info | [88] | |||
| 29 | MRL24 | Drug Info | [88] | |||
| 30 | Phenylpropionic acid derivative 1 | Drug Info | [88] | |||
| 31 | Phenylpyridine derivative 3 | Drug Info | [88] | |||
| 32 | PMID25416646-Compound-Figure2-J | Drug Info | [88] | |||
| 33 | PMID25416646-Compound-Figure2-K | Drug Info | [88] | |||
| 34 | PMID25416646-Compound-Figure2-N | Drug Info | [88] | |||
| 35 | PMID25416646-Compound-Figure5-A | Drug Info | [88] | |||
| 36 | PMID25416646-Compound-Figure5-C | Drug Info | [88] | |||
| 37 | PMID25416646-Compound-Figure5-E | Drug Info | [88] | |||
| 38 | PMID25416646-Compound-Figure5-H | Drug Info | [88] | |||
| 39 | Spirolaxine derivative 1 | Drug Info | [88] | |||
| 40 | Sulfonamide derivative 18 | Drug Info | [88] | |||
| 41 | Thiazolidine dione crystalline derivative 1 | Drug Info | [88] | |||
| 42 | GSK-677954 | Drug Info | [30] | |||
| 43 | Indeglitazar | Drug Info | [90] | |||
| 44 | Sodelglitazar | Drug Info | [92] | |||
| 45 | LY-929 | Drug Info | [96] | |||
| 46 | Ciglitazone | Drug Info | [97] | |||
| 47 | BVT-142 | Drug Info | [56], [99] | |||
| 48 | CS-204 | Drug Info | [100] | |||
| 49 | DARGLITAZONE | Drug Info | [101], [87] | |||
| 50 | SB-219994 | Drug Info | [102] | |||
| 51 | 15-deoxy-Delta(12, 14)-prostaglandin J(2) | Drug Info | [65] | |||
| 52 | DB-900 | Drug Info | [104] | |||
| 53 | GW7845 | Drug Info | [106] | |||
| Modulator | [+] 28 Modulator drugs | + | ||||
| 1 | Balaglitazone | Drug Info | [68] | |||
| 2 | CS-038 | Drug Info | [69], [70] | |||
| 3 | FARGLITAZAR | Drug Info | [71], [72] | |||
| 4 | Imiglitazar | Drug Info | [73], [74] | |||
| 5 | MURAGLITAZAR | Drug Info | [76] | |||
| 6 | Ragaglitazar | Drug Info | [17] | |||
| 7 | TESAGLITAZAR | Drug Info | [78] | |||
| 8 | ZYH-1 | Drug Info | [62] | |||
| 9 | CHS-131 | Drug Info | [24] | |||
| 10 | Naveglitazar | Drug Info | [80] | |||
| 11 | Netoglitazone | Drug Info | [81] | |||
| 12 | ONO-5129 | Drug Info | [83] | |||
| 13 | T3D-959 | Drug Info | [85] | |||
| 14 | DSP-8658 | Drug Info | [86] | |||
| 15 | GW-409544 | Drug Info | [39] | |||
| 16 | Oxeglitazar | Drug Info | [40] | |||
| 17 | AVE-0847 | Drug Info | [89] | |||
| 18 | KRP-297 | Drug Info | [91] | |||
| 19 | Reglixane | Drug Info | [83] | |||
| 20 | DS-6930 | Drug Info | [94] | |||
| 21 | E-3030 | Drug Info | [95] | |||
| 22 | MC-3002 | Drug Info | [83] | |||
| 23 | AD-5075 | Drug Info | [54] | |||
| 24 | AKP-320 | Drug Info | [98] | |||
| 25 | Edaglitazone | Drug Info | [59] | |||
| 26 | Sipoglitazar | Drug Info | [62] | |||
| 27 | GW-2331 | Drug Info | [105] | |||
| 28 | ZY H2 | Drug Info | [107] | |||
| Ligand | [+] 1 Ligand drugs | + | ||||
| 1 | Cannabinoid quinone derivative 1 | Drug Info | [88] | |||
| Inhibitor | [+] 8 Inhibitor drugs | + | ||||
| 1 | YM-440 | Drug Info | [93], [87] | |||
| 2 | (2S)-2-(4-chlorophenoxy)-3-phenylpropanoic acid | Drug Info | [103] | |||
| 3 | (2S)-2-(4-ethylphenoxy)-3-phenylpropanoic acid | Drug Info | [103] | |||
| 4 | (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid | Drug Info | [103] | |||
| 5 | (9Z,11E,13S)-13-hydroxyoctadeca-9,11-dienoic acid | Drug Info | [103] | |||
| 6 | 2-chloro-5-nitro-N-phenylbenzamide | Drug Info | [103] | |||
| 7 | 3-(5-methoxy-1H-indol-3-yl)propanoic acid | Drug Info | [103] | |||
| 8 | 9-hydroxyoctadecadienoic acid | Drug Info | [103] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Indomethacin | Ligand Info | |||||
| Structure Description | Human PPARgamma ligand-binding domain in complex with indomethacin and nitro-233 | PDB:3ADX | ||||
| Method | X-ray diffraction | Resolution | 1.95 Å | Mutation | No | [108] |
| PDB Sequence |
QLNPESADLR
212 ALAKHLYDSY222 IKSFPLTKAK232 ARAILTGKTT242 DKSPFVIYDM252 NSLMMGEDKI 262 KFKHITPLQE272 QSKEVAIRIF282 QGCQFRSVEA292 VQEITEYAKS302 IPGFVNLDLN 312 DQVTLLKYGV322 HEIIYTMLAS332 LMNKDGVLIS342 EGQGFMTREF352 LKSLRKPFGD 362 FMEPKFEFAV372 KFNALELDDS382 DLAIFIAVII392 LSGDRPGLLN402 VKPIEDIQDN 412 LLQALELQLK422 LNHPESSQLF432 AKLLQKMTDL442 RQIVTEHVQL452 LQVIKKTETD 462 MSLHPLLQEI472 YKDL
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ALA278
4.525
ILE281
3.493
PHE282
3.093
CYS285
3.632
GLN286
3.984
SER289
3.015
HIS323
2.880
ILE326
3.351
TYR327
3.109
LEU330
3.923
LEU353
3.662
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Glutathione | Ligand Info | |||||
| Structure Description | Human peroxisome proliferator-activated receptor gamma ligand binding domain complexed with glutathion conjugated 15-deoxy-delta12,14-prostaglandin J2 | PDB:2ZK2 | ||||
| Method | X-ray diffraction | Resolution | 2.26 Å | Mutation | No | [109] |
| PDB Sequence |
QLNPESADLR
212 ALAKHLYDSY222 IKSFPLTKAK232 ARAILTGKTT242 DKSPFVIYDM252 NSLMMGEDKI 262 KFKHITPLQE272 QSKEVAIRIF282 QGCQFRSVEA292 VQEITEYAKS302 IPGFVNLDLN 312 DQVTLLKYGV322 HEIIYTMLAS332 LMNKDGVLIS342 EGQGFMTREF352 LKSLRKPFGD 362 FMEPKFEFAV372 KFNALELDDS382 DLAIFIAVII392 LSGDRPGLLN402 VKPIEDIQDN 412 LLQALELQLK422 LNHPESSQLF432 AKLLQKMTDL442 RQIVTEHVQL452 LQVIKKTETD 462 MSLHPLLQEI472 YKDL
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LEU228
4.365
PHE264
3.738
ILE267
3.833
THR268
4.497
ARG280
3.628
ILE281
3.078
PHE282
4.922
GLN283
4.767
GLY284
2.935
CYS285
3.473
ARG288
2.887
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| PPAR signaling pathway | hsa03320 | Affiliated Target |
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| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| AMPK signaling pathway | hsa04152 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Longevity regulating pathway | hsa04211 | Affiliated Target |
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| Class: Organismal Systems => Aging | Pathway Hierarchy | ||
| Osteoclast differentiation | hsa04380 | Affiliated Target |
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| Class: Organismal Systems => Development and regeneration | Pathway Hierarchy | ||
| Thermogenesis | hsa04714 | Affiliated Target |
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| Class: Organismal Systems => Environmental adaptation | Pathway Hierarchy | ||
| Degree | 52 | Degree centrality | 5.59E-03 | Betweenness centrality | 4.21E-03 |
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| Closeness centrality | 2.58E-01 | Radiality | 1.45E+01 | Clustering coefficient | 9.95E-02 |
| Neighborhood connectivity | 3.50E+01 | Topological coefficient | 4.04E-02 | Eccentricity | 11 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7. | |||||
| REF 2 | Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-gamma agonist, after a single oral administration in healthy female subjects. Clin Drug Investig. 2014 Jul;34(7):467-74. | |||||
| REF 3 | URL: 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: 2694). | |||||
| REF 4 | 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 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 6 | Thiazolidinediones: a comparative review of approved uses. Diabetes Technol Ther. 2000 Autumn;2(3):429-40. | |||||
| REF 7 | URL: 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: 2693). | |||||
| REF 8 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 9 | ClinicalTrials.gov (NCT00515632) Efficacy and Safety of Treatment With Balaglitazone in Type 2 Diabetes Patients on Stable Insulin Therapy. U.S. National Institutes of Health. | |||||
| REF 10 | ClinicalTrials.gov (NCT02173457) Study of Chiglitazar Compare With Sitagliptin in Type 2 Diabetes Patients. U.S. National Institutes of Health. | |||||
| REF 11 | URL: 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: 2672). | |||||
| REF 12 | Clinical pipeline report, company report or official report of MacroGenics. | |||||
| REF 13 | URL: 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: 2675). | |||||
| REF 14 | Medicinal Chemistry and Actions of Dual and Pan PPAR Modulators. Open Med Chem J. 2011;5(Suppl 2):93-8. | |||||
| REF 15 | ClinicalTrials.gov (NCT05819866) A Clinical Study to Assess the Efficacy and Safety of Leriglitazone in Adult Male Subjects With Cerebral Adrenoleukodystrophy. U.S.National Institutes of Health. | |||||
| REF 16 | URL: 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: 2664). | |||||
| REF 17 | Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. J Clin Pharmacol. 2003 Nov;43(11):1244-56. | |||||
| REF 18 | ClinicalTrials.gov (NCT00571519) Randomized, Double-blind, Active-controlled, Study of Rivoglitazone in Type 2 Diabetes Mellitus. U.S. National Institutes of Health. | |||||
| REF 19 | ClinicalTrials.gov (NCT00499707) Efficacy and Safety Study of Rosiglitazone/Metformin Therapy vs Rosiglitazone and Metformin in Type 2 Diabetes Subjects. U.S. National Institutes of Health. | |||||
| REF 20 | Clinical pipeline report, company report or official report of GlaxoSmithKline. | |||||
| REF 21 | ClinicalTrials.gov (NCT00229710) GALLEX 9: Safety and Tolerability of Oral Tesaglitazar When Added to Insulin Therapy in Patients With Type 2 Diabetes. U.S. National Institutes of Health. | |||||
| REF 22 | A multicenter, prospective, randomized, double-blind study to evaluate the safety and efficacy of Saroglitazar 2 and 4 g compared with placebo in type 2 diabetes mellitus patients having hypertriglyceridemia not controlled with atorvastatin therapy (PRESS VI). Diabetes Technol Ther. 2014 Feb;16(2):63-71. | |||||
| REF 23 | ClinicalTrials.gov (NCT00353587) Safety and Efficacy Study of Metaglidasen in Type 2 Diabetes in Patients Suboptimally Controlled on Insulin. U.S. National Institutes of Health. | |||||
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