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peroxisome proliferator; PPAR agonist; PPAR gamma agonist
Function:
- large class of structurally dissimilar molecules, originally identified as inducers of both the size & number of peroxisomes in rat & mouse hepatocytes
- peroxisome proliferators bind to peroxisome proliferator activated receptors (PPAR)
- binding specificity with PPAR varies with perxisome proliferator
- most bind to PPAR-gamma
- only a few seem to bind PPAR-beta/delta
- chronic exposure causes an increased incidence of liver tumors in mice & rats
Pharmacology:
- the PPAR gamma agonist pioglitazone causes fewer cancer stem cells to remain dormant, thereby rendering them more vulnerable to chemotherapy with imatinib [2]
Related
peroxisome
peroxisome proliferator-activated receptor (PPAR)
Specific
5,8,11,14-eicosatetraynoic acid
fenoprofen (Nalfon)
fibrate
glitazar
ibuprofen (Motrin, Advil, Nuprin, Rufen, NeoProfen, Caldolor)
indomethacin (Indocin)
lanifibranor
pioglitazone (Actos)
piroxicam (Feldene)
rosiglitazone (Avandia)
troglitazone (Rezulin)
General
bioagent
References
- Corton et al Annu Rev Pharmacol Toxicol 40:491, 2000
- Prost S et al.
Erosion of the chronic myeloid leukaemia stem cell pool by
PPAR-gamma agonists.
Nature 2015 Sep 17; 525:380.
PMID: 26331539
- Holyoake T and Vetrie D.Cancer:
Repositioned to kill stem cells.
Nature 2015 Sep 17; 525:328
PMID: 26331538