Details of the Target

General Information of Target

Target ID LDTP03840
Target Name Peroxisome proliferator-activated receptor gamma (PPARG)
Gene Name PPARG
Gene ID 5468
Synonyms
NR1C3; Peroxisome proliferator-activated receptor gamma; PPAR-gamma; Nuclear receptor subfamily 1 group C member 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR1 subfamily
Subcellular location
Nucleus
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 pro-inflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of BMAL1 in the blood vessels.; (Microbial infection) Upon treatment with M.tuberculosis or its lipoprotein LpqH, phosphorylation of MAPK p38 and IL-6 production are modulated, probably via this protein.
TTD ID
T58921
Uniprot ID
P37231
DrugMap ID
TTZMAO3
Ensemble ID
ENST00000287820.10
HGNC ID
HGNC:9236
ChEMBL ID
CHEMBL235

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C313(3.04)  LDD3311  [1]
IPM
 Probe Info  		C198(0.00); C313(0.00)  LDD0147  [2]
TFBX
 Probe Info  		N.A.  LDD0148  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A-549 C198(1.62)  LDD2260  [1]
 LDCM0023  KB03 A2780 C313(2.57)  LDD2671  [1]
 LDCM0024  KB05 G361 C313(3.04)  LDD3311  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adenylate cyclase type 4 (ADCY4) Adenylyl cyclase class-4/guanylyl cyclase family Q8NFM4
Cyclin-dependent kinase 5 (CDK5) CMGC Ser/Thr protein kinase family Q00535
Mitogen-activated protein kinase 9 (MAPK9) CMGC Ser/Thr protein kinase family P45984
NAD-dependent protein deacetylase sirtuin-1 (SIRT1) Sirtuin family Q96EB6
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Oxysterols receptor LXR-alpha (NR1H3) Nuclear hormone receptor family Q13133
Transcription factor
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear receptor corepressor 1 (NCOR1) N-CoR nuclear receptor corepressors family O75376
Peroxisome proliferator-activated receptor gamma (PPARG) Nuclear hormone receptor family P37231
Retinoic acid receptor alpha (RARA) Nuclear hormone receptor family P10276
Retinoic acid receptor RXR-alpha (RXRA) Nuclear hormone receptor family P19793
Retinoic acid receptor RXR-beta (RXRB) Nuclear hormone receptor family P28702
Transcription factor GATA-5 (GATA5) . Q9BWX5
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Clusterin (CLU) Clusterin family P10909
Endothelial differentiation-related factor 1 (EDF1) . O60869
Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PPARGC1A) . Q9UBK2

The Drug(s) Related To This Target

Approved
Click To Hide/Show 31 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alpha-linolenic Acid Small molecular drug DB00132
Amiodarone Small molecular drug DB01118
Balsalazide Small molecular drug DB01014
Bezafibrate Small molecular drug DB01393
Cannabidiol Small molecular drug DB09061
Clofazimine Small molecular drug DB00845
Curcumin Small molecular drug DB11672
Dexibuprofen Small molecular drug DB09213
Doconexent Small molecular drug DB03756
Fenofibric Acid Small molecular drug DB13873
Fenoprofen Small molecular drug DB00573
Flufenamic Acid Small molecular drug DB02266
Glipizide Small molecular drug DB01067
Ibuprofen Small molecular drug DB01050
Icosapent Small molecular drug DB00159
Indomethacin Small molecular drug DB00328
Lobeglitazone Small molecular drug D04BCB
Mesalazine Small molecular drug DB00244
Nateglinide Small molecular drug DB00731
Oleic Acid Small molecular drug DB04224
Pioglitazone Small molecular drug D03OFF
Repaglinide Small molecular drug DB00912
Rosiglitazone Small molecular drug DB00412
Rosiglitazone Xr Small molecular drug D0K5ER
Telmisartan Small molecular drug DB00966
Thiazolidinedione Small molecular drug D0K8IX
Triclosan Small molecular drug DB08604
Troglitazone Small molecular drug D06XZW
Valproic Acid Small molecular drug DB00313
Fish Oil . DB13961
Omega-3 Fatty Acids . DB11133
Phase 4
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Glitazone Small molecular drug D0S2BV
Phase 3
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rosiglitazone + Metformin Combination drug (small molecular drug) D0A1AQ
Rosiglitazone + Simvastatin Combination drug (small molecular drug) D0Q6IW
Balaglitazone Small molecular drug D0F3NH
Cs-038 Small molecular drug D0F5JH
Farglitazar Small molecular drug D0M0SS
Imiglitazar Small molecular drug D0VU5M
Mbx-102 Small molecular drug D0X7VB
Muraglitazar Small molecular drug D0M3UT
Ragaglitazar Small molecular drug D02NHD
Rivoglitazone Small molecular drug D08PFA
Tesaglitazar Small molecular drug D0H1NL
Zyh-1 . D0T7MN
Phase 2
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fk-614 Small molecular drug D00PJJ
Naveglitazar Small molecular drug D04BPS
Netoglitazone Small molecular drug D02TGD
Chs-131 . D0P5SU
Ged-0507-34-levo . D0E6ME
Mbx-2044 . D08NPG
Oms405 . D0W0JP
Ono-5129 . D0PP8G
T3d-959 . D0ZT8A
Phase 1
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Englitazone Sodium Small molecular drug D08EEU
Gw-409544 Small molecular drug D0AX9S
Oxeglitazar Small molecular drug D03RJZ
Clx-0921 . D06TWE
Dsp-8658 . D07IGC
Preclinical
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ciglitazone Small molecular drug D03GWY
Mc-3002 . D08WOE
Investigative
Click To Hide/Show 46 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(2s)-2-(4-chlorophenoxy)-3-phenylpropanoic Acid Small molecular drug D0J3UU
(2s)-2-(4-ethylphenoxy)-3-phenylpropanoic Acid Small molecular drug D0H4US
(2s)-2-(Biphenyl-4-yloxy)-3-phenylpropanoic Acid Small molecular drug D06MDX
(2s)-2-ethoxy-3-{4-[2-(10h-phenoxazin-10-yl)Ethoxy]Phenyl}Propanoic Acid Small molecular drug DB07675
(9z,11e,13s)-13-hydroxyoctadeca-9,11-dienoic Acid Small molecular drug D0Z5TV
(9z11e13s)-13-hydroxyoctadeca-911-dienoic Acid Small molecular drug DB06926
15-deoxy-delta(12, 14)-prostaglandin J(2) Small molecular drug D01PGU
2-chloro-5-nitro-n-phenylbenzamide Small molecular drug D00ACX
3-(5-methoxy-1h-indol-3-yl)Propanoic Acid Small molecular drug D0E5HC
9(S)-hode Small molecular drug DB07302
9-hydroxyoctadecadienoic Acid Small molecular drug D0SZ4T
Aleglitazar Small molecular drug DB08915
Arhalofenate Small molecular drug DB11811
Capric Acid Small molecular drug DB03600
Darglitazone Small molecular drug DB14034
Ertiprotafib Small molecular drug DB06521
Gw-2331 Small molecular drug D01POG
Gw7845 Small molecular drug D0O2US
Mitiglinide Small molecular drug DB01252
Muraglitazar Small molecular drug DB06510
Nabiximols Small molecular drug DB14011
Phthalic Acid Small molecular drug DB02746
Reglitazar Small molecular drug DB04971
Resveratrol Small molecular drug DB02709
Tesaglitazar Small molecular drug DB06536
(2s)-3-(1-{[2-(2-chlorophenyl)-5-methyl-13-oxazol-4-yl]Methyl}-1h-indol-5-yl)-2-ethoxypropanoic Acid . DB06908
(4s5e7z10z13z16z19z)-4-hydroxydocosa-5710131619-hexaenoic Acid . DB07111
(5e14e)-11-oxoprosta-591214-tetraen-1-oic Acid . DB08435
(5r6e8z11z14z17z)-5-hydroxyicosa-68111417-pentaenoic Acid . DB07172
(8e10s12z)-10-hydroxy-6-oxooctadeca-812-dienoic Acid . DB07208
(8r9z12z)-8-hydroxy-6-oxooctadeca-912-dienoic Acid . DB07209
(S)-3-(4-(2-carbazol-9-yl-ethoxy)-phenyl)-2-ethoxy-propionic Acid . DB04270
2-[(24-dichlorobenzoyl)Amino]-5-(Pyrimidin-2-yloxy)Benzoic Acid . DB08402
2-{5-[3-(6-benzoyl-1-propylnaphthalen-2-yloxy)Propoxy]Indol-1-yl}Ethanoic Acid . DB04689
2-{5-[3-(7-propyl-3-trifluoromethylbenzo[D]Isoxazol-6-yloxy)Propoxy]Indol-1-yl}Ethanoic Acid . DB07053
3-fluoro-n-[1-(4-fluorophenyl)-3-(2-thienyl)-1h-pyrazol-5-yl]Benzenesulfonamide . DB08560
3-[5-(2-nitropent-1-en-1-yl)Furan-2-yl]Benzoic Acid . DB08302
Amg-131 . DB05490
Clinofibrate . DB09006
Curcumin Sulfate . DB14635
Db-900 . D01ARG
Difluoro(5-{2-[(5-octyl-1h-pyrrol-2-yl-kappan)Methylidene]-2h-pyrrol-5-yl-kappan}Pentanoato)Boron . DB07509
Elafibranor . DB05187
Isoflavone . DB12007
Medical Cannabis . DB14009
Zy H2 . D0Z4MH
Patented
Click To Hide/Show 24 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-(Biphenyl-4-yl-methyl)-1h-imidazole Derivative 1 Small molecular drug D0U6AW
3-phenyl Acrylic Acid Derivative 1 Small molecular drug D0SV6U
A-substituted Phenylpropionic Acid Derivative 1 Small molecular drug D0E9GF
A-substituted Phenylpropionic Acid Derivative 2 Small molecular drug D0M5YQ
Biaromatic Compound 1 Small molecular drug D0O8PR
Cannabinoid Quinone Derivative 1 Small molecular drug D0ZO0D
Crystalline Anhydrous Toluene Derivative 1 Small molecular drug D0M4RD
Flavonoid Derivative 8 Small molecular drug D0HW6Y
Fused Aromatic Compound 1 Small molecular drug D0UG1W
Fused Ring Compound 1 Small molecular drug D0SL0K
Mrl20 Small molecular drug D0PO7F
Mrl24 Small molecular drug D0H5FI
Phenylpropionic Acid Derivative 1 Small molecular drug D09OXG
Phenylpyridine Derivative 3 Small molecular drug D0NF8V
Pmid25416646-compound-figure2-j Small molecular drug D0UH5B
Pmid25416646-compound-figure2-k Small molecular drug D0G3KY
Pmid25416646-compound-figure2-n Small molecular drug D0GG5K
Pmid25416646-compound-figure5-a Small molecular drug D0O5IN
Pmid25416646-compound-figure5-c Small molecular drug D0V0JN
Pmid25416646-compound-figure5-e Small molecular drug D0LA6O
Pmid25416646-compound-figure5-h Small molecular drug D05AUY
Spirolaxine Derivative 1 Small molecular drug D03GFB
Sulfonamide Derivative 18 Small molecular drug D0HT9C
Thiazolidine Dione Crystalline Derivative 1 Small molecular drug D0TF0T
Discontinued
Click To Hide/Show 18 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ad-5075 Small molecular drug D0LB4T
Darglitazone Small molecular drug D0N1EF
Gsk-677954 Small molecular drug D0S6KX
Indeglitazar Small molecular drug D09OHP
Krp-297 Small molecular drug D02RAU
Ly-929 Small molecular drug D0B0EB
Sb-219994 Small molecular drug D00YGA
Sodelglitazar Small molecular drug D01JGG
Akp-320 . D04JVX
Ave-0847 . D0W2IU
Bvt-142 . D0I0RF
Cs-204 . D0V0TT
Ds-6930 . D0Z6OI
E-3030 . D06PHO
Edaglitazone . D08VKZ
Reglixane . D02ZKL
Sipoglitazar . D0OW6Z
Ym-440 . D0KL3K

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255