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Peroxisome proliferator-activated receptor-β/δ

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Target not currently curated in GtoImmuPdb

Target id: 594

Nomenclature: Peroxisome proliferator-activated receptor-β/δ

Systematic Nomenclature: NR1C2

Family: 1C. Peroxisome proliferator-activated receptors

Gene and Protein Information Click here for help
Species AA Chromosomal Location Gene Symbol Gene Name Reference
Human 441 6p21.31 PPARD peroxisome proliferator activated receptor delta 33
Mouse 440 17 14.64 cM Ppard peroxisome proliferator activator receptor delta 20
Rat 440 20p12 Ppard peroxisome proliferator-activated receptor delta 40
Previous and Unofficial Names Click here for help
NUCII | PPARβ/δ | NUC1 | Pparb | Pparb/d | PPARδ
Database Links Click here for help
Alphafold
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  PPAR-δ ligand binding domain - cocrytallised with agonist
PDB Id:  1GWX
Ligand:  GW2433
Resolution:  2.5Å
Species:  Human
References:  41
Natural/Endogenous Ligands Click here for help
tretinoin
Comments: Fatty acids and eisosanoids are natural ligands

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists Click here for help
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
L-783483 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.0 pKd 4
pKd 9.0 [4]
tretinoin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.8 pKd 34
pKd 7.8 [34]
L-796449 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.7 pKi 4,16
pKi 8.7 [4,16]
L-165041 Small molecule or natural product Ligand has a PDB structure Hs Full agonist 8.2 pKi 4,39
pKi 8.2 [4,39]
GW501516 Small molecule or natural product Ligand has a PDB structure Hs Full agonist 9.0 pEC50 29
pEC50 9.0 [29]
seladelpar Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 8.7 pEC50 44
pEC50 8.7 (EC50 1.9x10-9 M) [44]
Description: Agonist activity determined by cell based transactivation assay.
GW2433 Small molecule or natural product Ligand has a PDB structure Hs Full agonist 6.6 pEC50 6,39
pEC50 6.6 [6,39]
(R)-16 [PMID: 32267688] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 6.1 pEC50 14
pEC50 6.1 (EC50 8.1x10-7 M) [14]
Description: Measuring nuclear receptor modulation in Gal4-hybrid reporter gene assays conducted in transiently transfected HEK293T cells.
lanifibranor Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 6.1 pEC50 5
pEC50 6.1 (EC50 8.66x10-7 M) [5]
GW9578 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.9 pEC50 7
pEC50 5.9 [7]
compound 25 [PMID: 32687365] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Agonist 5.8 pEC50 32
pEC50 5.8 (EC50 1.5x10-6 M) [32]
GW0742X Small molecule or natural product Ligand has a PDB structure Hs Full agonist 9.0 pIC50 13,36
pIC50 9.0 [13,36]
Agonist Comments
Endogenous fatty acid full agonists have also been reported with pIC50 values of 5.2 for the human isoform [41].
Antagonists Click here for help
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK0660 Small molecule or natural product Hs Antagonist 6.5 pIC50 35
pIC50 6.5 (IC50 3x10-7 M) [35]
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Tissue repair
Main Co-regulators Click here for help
Name Activity Specific Ligand dependent AF-2 dependent Comments References
NCOA1 Co-activator No No Yes 31
NCOA3 Co-activator No No Yes 28
NCOA6 Co-activator No Yes Yes 8
NCOR2 Co-repressor No No No 18,42
NCOR1 Co-repressor No No No 18,21,43
PPARGC1A Co-activator No No No 38
Main Target Genes Click here for help
Name Species Effect Technique Comments References
ANGPTL4 angiopoietin-like 4 (FIAF: fast-induced adipose factor) Human Activated EMSA 25
Pdpk1 Mouse Activated EMSA, ChIP 12
Ilk Mouse Activated EMSA, ChIP 12
Pink1 Mouse Repressed EMSA, ChIP 12
Dffa (DFF45) Mouse Activated EMSA 11
Tissue Distribution Click here for help
Ubiquitous
Expression level:  Medium
Species:  Human
Technique:  Northern blot, Q-PCR.
References:  10
Functional Assays Click here for help
Adipogenesis assay
Species:  Mouse
Tissue:  3T3-C2 fibroblasts
Response measured:  Staining of lipids with oil Red O and GDPH activity for detection of terminal differentiation
References:  3
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0000003 abnormal adipose tissue morphology PMID: 11756685 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0002152 abnormal brain morphology PMID: 10866668 
Ppardtm1Dgen Ppardtm1Dgen/Ppardtm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:101884  MP:0000822 abnormal brain ventricle morphology
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0005450 abnormal energy expenditure PMID: 10866668 
Ppardtm1Mtz|Tg(KRT14-cre)1Ipc Ppardtm1Mtz/Ppardtm1Mtz,Tg(KRT14-cre)1Ipc/0
involves: C57BL/6 * SJL
MGI:101884  MGI:2177412  MP:0001216 abnormal epidermal layer morphology PMID: 16751185 
Ppardtm2Rev Ppardtm2Rev/Ppardtm2Rev
involves: 129S4/SvJae
MGI:101884  MP:0002086 abnormal extraembryonic tissue morphology
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0009115 abnormal fat cell morphology PMID: 11756685 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0005335 abnormal gonadal fat pad morphology PMID: 10866668 
Ppardtm1Wwah Ppardtm1Wwah/Ppardtm1Wwah
Not Specified
MGI:101884  MP:0003704 abnormal hair follicle development PMID: 15713628 
Ppardtm1Mtz|Tg(KRT14-cre)1Ipc Ppardtm1Mtz/Ppardtm1Mtz,Tg(KRT14-cre)1Ipc/0
involves: C57BL/6 * SJL
MGI:101884  MGI:2177412  MP:0002655 abnormal keratinocyte morphology PMID: 16751185 
Ppard+|Ppardtm1Wwah Ppardtm1Wwah/Ppard+
Not Specified
MGI:101884  MP:0003453 abnormal keratinocyte physiology PMID: 11514592 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0001547 abnormal lipid level PMID: 12056592 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0000920 abnormal myelination PMID: 10866668 
Ppardtm1Dsvg Ppardtm1Dsvg/Ppardtm1Dsvg
involves: 129S2/SvPas
MGI:101884  MP:0001712 abnormal placenta development PMID: 16581799 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0001712 abnormal placenta development PMID: 11756685 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0001716 abnormal placenta labyrinth morphology PMID: 11756685 
Ppardtm1Mtz|Tg(KRT14-cre)1Ipc Ppardtm1Mtz/Ppardtm1Mtz,Tg(KRT14-cre)1Ipc/0
involves: C57BL/6 * SJL
MGI:101884  MGI:2177412  MP:0001191 abnormal skin condition PMID: 16751185 
Ppardtm1Mtz|Tg(KRT14-cre)1Ipc Ppardtm1Mtz/Ppardtm1Mtz,Tg(KRT14-cre)1Ipc/0
involves: C57BL/6 * SJL
MGI:101884  MGI:2177412  MP:0002060 abnormal skin morphology PMID: 16751185 
ApcMin|Ppardtm1.1Rev ApcMin/ApcMin,Ppardtm1.1Rev/Ppardtm1.1Rev
involves: C57BL/6J
MGI:101884  MGI:88039  MP:0003269 colon polyps PMID: 11756685 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0009287 decreased abdominal fat pad weight PMID: 11756685 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0001265 decreased body size PMID: 10866668 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0000774 decreased brain size PMID: 10866668 
Ppardtm1Mtz|Tg(KRT14-cre)1Ipc Ppardtm1Mtz/Ppardtm1Mtz,Tg(KRT14-cre)1Ipc/0
involves: C57BL/6 * SJL
MGI:101884  MGI:2177412  MP:0003983 decreased cholesterol level PMID: 16751185 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0004200 decreased fetal size PMID: 10866668 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0009295 decreased interscapular fat pad weight PMID: 11756685 
Ppardtm1Wwah Ppardtm1Wwah/Ppardtm1Wwah
Not Specified
MGI:101884  MP:0009584 decreased keratinocyte proliferation PMID: 15713628 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0010026 decreased liver cholesterol level PMID: 15001574 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0009356 decreased liver triglyceride level PMID: 15001574 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0009299 decreased mesenteric fat pad weight PMID: 11756685 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0008844 decreased subcutaneous adipose tissue amount PMID: 11756685 
Ppard+|Ppardtm1Dgen Ppardtm1Dgen/Ppard+
involves: 129P2/OlaHsd * C57BL/6
MGI:101884  MP:0003998 decreased thermal nociceptive threshold
Ppard+|Ppardtm1Wwah Ppardtm1Wwah/Ppard+
Not Specified
MGI:101884  MP:0002908 delayed wound healing PMID: 11514592 
Ppardtm1Dsvg Ppardtm1Dsvg/Ppardtm1Dsvg
involves: 129S2/SvPas
MGI:101884  MP:0003984 embryonic growth retardation PMID: 16581799 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0003984 embryonic growth retardation PMID: 11756685 
Ppardtm1Dgen Ppardtm1Dgen/Ppardtm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:101884  MP:0006207 embryonic lethality during organogenesis
Ppardtm1Dsvg Ppardtm1Dsvg/Ppardtm1Dsvg
involves: 129S2/SvPas
MGI:101884  MP:0006207 embryonic lethality during organogenesis PMID: 16581799 
Ppardtm1.1Rev Ppardtm1.1Rev/Ppardtm1.1Rev
Not Specified
MGI:101884  MP:0006207 embryonic lethality during organogenesis PMID: 11756685 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0001222 epidermal hyperplasia PMID: 10866668 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0001552 increased circulating triglyceride level PMID: 15001574 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0005145 increased circulating VLDL cholesterol level PMID: 15001574 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0005281 increased fatty acid level PMID: 15001574 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0004499 increased incidence of chemically-induced tumors PMID: 15033975  15048110 
ApcMin|Ppardtm1.1Rev ApcMin/ApcMin,Ppardtm1.1Rev/Ppardtm1.1Rev
involves: C57BL/6J
MGI:101884  MGI:88039  MP:0002404 increased intestinal adenoma incidence PMID: 11756685 
Ppardtm1Wwah Ppardtm1Wwah/Ppardtm1Wwah
Not Specified
MGI:101884  MP:0009580 increased keratinocyte apoptosis PMID: 15713628 
Ppard+|Ppardtm1Wwah Ppardtm1Wwah/Ppard+
Not Specified
MGI:101884  MP:0009583 increased keratinocyte proliferation PMID: 11514592 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0010300 increased skin tumor incidence PMID: 15033975 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0010024 increased total body fat amount PMID: 15001574 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0002020 increased tumor incidence PMID: 15033975 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0002957 intestinal adenocarcinoma PMID: 15048110 
Apc+|ApcMin|Ppardtm1Jps ApcMin/Apc+,Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * AKR/J * C57BL/6 * C57BL/6J
MGI:101884  MGI:88039  MP:0002957 intestinal adenocarcinoma PMID: 15033975 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0008011 intestine polyps PMID: 15048110 
Apc+|ApcMin|Ppardtm1Jps ApcMin/Apc+,Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * AKR/J * C57BL/6 * C57BL/6J
MGI:101884  MGI:88039  MP:0008011 intestine polyps PMID: 15033975 
ApcMin|Ppardtm1.1Rev ApcMin/ApcMin,Ppardtm1.1Rev/Ppardtm1.1Rev
involves: C57BL/6J
MGI:101884  MGI:88039  MP:0008011 intestine polyps PMID: 11756685 
Ppardtm1Dsvg Ppardtm1Dsvg/Ppardtm1Dsvg
involves: 129S2/SvPas
MGI:101884  MP:0001732 postnatal growth retardation PMID: 16581799 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0002080 prenatal lethality PMID: 10866668 
Ppardtm1Wwah Ppardtm1Wwah/Ppardtm1Wwah
Not Specified
MGI:101884  MP:0002080 prenatal lethality PMID: 11514592 
Ppardtm2Rev Ppardtm2Rev/Ppardtm2Rev
involves: 129S4/SvJae
MGI:101884  MP:0002080 prenatal lethality
Ppardtm1Dsvg Ppardtm1Dsvg/Ppardtm1Dsvg
involves: 129S2/SvPas
MGI:101884  MP:0001921 reduced fertility PMID: 16581799 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0004947 skin inflammation PMID: 10866668 
Ppardtm1Jps Ppardtm1Jps/Ppardtm1Jps
involves: 129/Sv * C57BL/6N
MGI:101884  MP:0002051 skin papilloma PMID: 15033975 
Ppard+|Ppardtm1Wwah Ppardtm1Wwah/Ppard+
Not Specified
MGI:101884  MP:0001219 thickened epidermis PMID: 11514592 
Ppardtm1Wwah Ppardtm1Wwah/Ppardtm1Wwah
Not Specified
MGI:101884  MP:0004126 thin hypodermis PMID: 15713628 
Ppardtm1Wwah Ppardtm1Wwah/Ppardtm1Wwah
Not Specified
MGI:101884  MP:0001199 thin skin PMID: 15713628 
Ppardtm1Wwah Ppardtm1Wwah/Ppardtm1Wwah
Not Specified
MGI:101884  MP:0000382 underdeveloped hair follicles PMID: 15713628 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Atherosclerosis susceptibility
Disease Ontology: DOID:1936
OMIM: 108725
Role: 
Comments: 
References:  9,13,22-23
Gene Expression and Pathophysiology Click here for help
Overexpression in C2C12 myoblasts participates in their transdifferentiation into adipocytes
Tissue or cell type:  C2C12 myoblasts
Pathophysiology: 
Species:  Mouse
Technique:  Retroviral mediated gene transfer
References:  17
Overexpression of constitutively active PPARβ-VP16 fusion protein in white adipose tissue triggers FA mobilization and oxidation leading to mass reduction
Tissue or cell type:  Adipose tissue
Pathophysiology: 
Species:  Mouse
Technique:  Transgenesis
References:  38
Overexpression in skeletal muscle provokes a shift toward more oxidative fibers and general decrease of body fat content
Tissue or cell type:  Skeletal muscle
Pathophysiology: 
Species:  Mouse
Technique:  Transgenesis
References:  24
PPAβ heterozygous mice
Tissue or cell type:  Skin
Pathophysiology:  Delayed wound closure
Species:  Mouse
Technique:  Targeted disruption of one allele
References:  26-27,37
PPARβ knockout: decreased amount of brown and white adipose tissues
Tissue or cell type: 
Pathophysiology:  Enhanced sensitivity to skin carcinogenesis, exacerbated epithelial proliferation, delayed wound repair, enhanced colon carcinogenesis, LDL hypertriglyceridemia
Species:  Mouse
Technique:  Targeted disruption-germline knockout
References:  1-2,15,19,27,30

References

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1. Akiyama TE, Lambert G, Nicol CJ, Matsusue K, Peters JM, Brewer HB, Gonzalez FJ. (2004) Peroxisome proliferator-activated receptor beta/delta regulates very low density lipoprotein production and catabolism in mice on a Western diet. J Biol Chem, 279 (20): 20874-81. [PMID:15001574]

2. Barak Y, Liao D, He W, Ong ES, Nelson MC, Olefsky JM, Boland R, Evans RM. (2002) Effects of peroxisome proliferator-activated receptor delta on placentation, adiposity, and colorectal cancer. Proc Natl Acad Sci USA, 99 (1): 303-8. [PMID:11756685]

3. Bastie C, Holst D, Gaillard D, Jehl-Pietri C, Grimaldi PA. (1999) Expression of peroxisome proliferator-activated receptor PPARdelta promotes induction of PPARgamma and adipocyte differentiation in 3T3C2 fibroblasts. J Biol Chem, 274 (31): 21920-5. [PMID:10419513]

4. Berger J, Leibowitz MD, Doebber TW, Elbrecht A, Zhang B, Zhou G, Biswas C, Cullinan CA, Hayes NS, Li Y, Tanen M, Ventre J, Wu MS, Berger GD, Mosley R, Marquis R, Santini C, Sahoo SP, Tolman RL, Smith RG, Moller DE. (1999) Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. J Biol Chem, 274 (10): 6718-25. [PMID:10037770]

5. Boubia B, Poupardin O, Barth M, Binet J, Peralba P, Mounier L, Jacquier E, Gauthier E, Lepais V, Chatar M et al.. (2018) Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate. J Med Chem, 61 (6): 2246-2265. [PMID:29446942]

6. Brown PJ, Smith-Oliver TA, Charifson PS, Tomkinson NC, Fivush AM, Sternbach DD, Wade LE, Orband-Miller L, Parks DJ, Blanchard SG, Kliewer SA, Lehmann JM, Willson TM. (1997) Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library. Chem Biol, 4 (12): 909-18. [PMID:9427656]

7. Brown PJ, Stuart LW, Hurley KP, Lewis MC, Winegar DA, Wilson JG, Wilkison WO, Ittoop OR, Willson TM. (2001) Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. Bioorg Med Chem Lett, 11 (9): 1225-7. [PMID:11354382]

8. Caira F, Antonson P, Pelto-Huikko M, Treuter E, Gustafsson JA. (2000) Cloning and characterization of RAP250, a novel nuclear receptor coactivator. J Biol Chem, 275 (8): 5308-17. [PMID:10681503]

9. Desvergne B, Michalik L, Wahli W. (2004) Be fit or be sick: peroxisome proliferator-activated receptors are down the road. Mol Endocrinol, 18 (6): 1321-32. [PMID:15087471]

10. Desvergne B, Wahli W. (1999) Peroxisome proliferator-activated receptors: nuclear control of metabolism. Endocr Rev, 20 (5): 649-88. [PMID:10529898]

11. Di-Poï N, Michalik L, Tan NS, Desvergne B, Wahli W. (2003) The anti-apoptotic role of PPARbeta contributes to efficient skin wound healing. J Steroid Biochem Mol Biol, 85 (2-5): 257-65. [PMID:12943711]

12. Di-Poï N, Tan NS, Michalik L, Wahli W, Desvergne B. (2002) Antiapoptotic role of PPARbeta in keratinocytes via transcriptional control of the Akt1 signaling pathway. Mol Cell, 10 (4): 721-33. [PMID:12419217]

13. Graham TL, Mookherjee C, Suckling KE, Palmer CN, Patel L. (2005) The PPARdelta agonist GW0742X reduces atherosclerosis in LDLR(-/-) mice. Atherosclerosis, 181 (1): 29-37. [PMID:15939051]

14. Hanke T, Cheung SY, Kilu W, Heering J, Ni X, Planz V, Schierle S, Faudone G, Friedrich M, Wanior M et al.. (2020) A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode. J Med Chem, 63 (9): 4555-4561. [PMID:32267688]

15. Harman FS, Nicol CJ, Marin HE, Ward JM, Gonzalez FJ, Peters JM. (2004) Peroxisome proliferator-activated receptor-delta attenuates colon carcinogenesis. Nat Med, 10 (5): 481-3. [PMID:15048110]

16. Henke BR. (2004) Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. J Med Chem, 47 (17): 4118-27. [PMID:15293980]

17. Holst D, Luquet S, Kristiansen K, Grimaldi PA. (2003) Roles of peroxisome proliferator-activated receptors delta and gamma in myoblast transdifferentiation. Exp Cell Res, 288 (1): 168-76. [PMID:12878168]

18. Jackson TA, Richer JK, Bain DL, Takimoto GS, Tung L, Horwitz KB. (1997) The partial agonist activity of antagonist-occupied steroid receptors is controlled by a novel hinge domain-binding coactivator L7/SPA and the corepressors N-CoR or SMRT. Mol Endocrinol, 11 (6): 693-705. [PMID:9171233]

19. Kim DJ, Bility MT, Billin AN, Willson TM, Gonzalez FJ, Peters JM. (2006) PPARbeta/delta selectively induces differentiation and inhibits cell proliferation. Cell Death Differ, 13 (1): 53-60. [PMID:16021179]

20. Kliewer SA, Forman BM, Blumberg B, Ong ES, Borgmeyer U, Mangelsdorf DJ, Umesono K, Evans RM. (1994) Differential expression and activation of a family of murine peroxisome proliferator-activated receptors. Proc Natl Acad Sci USA, 91 (15): 7355-9. [PMID:8041794]

21. Krogsdam AM, Nielsen CA, Neve S, Holst D, Helledie T, Thomsen B, Bendixen C, Mandrup S, Kristiansen K. (2002) Nuclear receptor corepressor-dependent repression of peroxisome-proliferator-activated receptor delta-mediated transactivation. Biochem J, 363 (Pt 1): 157-65. [PMID:11903058]

22. Lee CH, Chawla A, Urbiztondo N, Liao D, Boisvert WA, Evans RM, Curtiss LK. (2003) Transcriptional repression of atherogenic inflammation: modulation by PPARdelta. Science, 302 (5644): 453-7. [PMID:12970571]

23. Li AC, Binder CJ, Gutierrez A, Brown KK, Plotkin CR, Pattison JW, Valledor AF, Davis RA, Willson TM, Witztum JL, Palinski W, Glass CK. (2004) Differential inhibition of macrophage foam-cell formation and atherosclerosis in mice by PPARalpha, beta/delta, and gamma. J Clin Invest, 114 (11): 1564-76. [PMID:15578089]

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How to cite this page

1C. Peroxisome proliferator-activated receptors: Peroxisome proliferator-activated receptor-β/δ. Last modified on 09/06/2023. Accessed on 10/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=594.