Research Article

PPARβ/δ Agonism with GW501516 Increases Myotube PGC-1α Content and Reduces BCAA Media Content Independent of Changes in BCAA Catabolic Enzyme Expression

Table 1

Summary of experimental model, treatment conditions, and related findings to present report.

ModelDose of GW501516DurationEffectReference

C2C12 Myotubes10 nM16 hours↑ Glucose uptakeKramer et al. [29]
100 nM24 hours↑ Cpt1, Pdk4, Ucp3 mRNAKleiner et al. [42]
1 μM24 hours↑ Pdk4 mRNA expressionAoki et al. [43]
1 μM24 hours↑ Cpt1, Pdk4, Ucp3 mRNA and ↔mitochondrial functionTumova et al. [28]
1 μM24 hours↑ PPAR and PGC-1α promoter activity and Ppargc1a and Cpt1 mRNA expressionHondares et al. [26]
1 μM24 hours↑ PPAR and PGC-1α promoter activity and Ppargc1a and Ucp2 mRNA expressionMiura et al. [25]
1 μM*24 hours↑ PPAR and PGC-1α promoter activity and Ucp1, Ucp2, Ucp3 mRNA expressionDressel et al. [44]
1 μM + BMS691 at 10 μM16 hours↑ Ppargc1a mRNASchuler et al. [8]
1 μM + PAL at 500 μM16 hours↑ pAMPK, PDK4, and CPT1 protein expression and rescued palmitate oxidationColl et al. [45]
1 μM48 hours↑ PPAR reporter activityRemels et al. [31]
5 μM16 hours↑ Or rescued Cpt1 mRNA expression/rescued palmitate oxidation (TNFα suppressed)Zizola et al. [27]
10 μM24 hours↑ Cpt-1b, Acadm, and Acox mRNA expression and pAMPK protein expressionAguilar-Recarte et al. [46]
L6 Myotubes30, 100, and 300 nM (L6 myotubes)24 hours↑ Ppargc1a, Ucp2, Ucp3, and Cpt1 mRNA expression and palmitate oxidationTanaka et al. [1]
100 nM (L6 myotubes)5 days↑ UCP3 and ↓GLUT4 protein expressionHigashida et al. [47]
1 μM (L6 myotubes)24 hours↑ PGC-1α and CPT1 with ↔ PPARδ protein expression and ↑ palmitate oxidationDimopoulos et al. [48]
1 μM (L6 myotubes)24 hours↑ Palmitate oxidation and Cpt1 mRNA expressionHondares et al. [26]

*Indicates effects were enhanced by concurrent RXR agonism. Abbreviations: Cpt1: carnitine palmitoyl transferase 1; Glut4: glucose transporter 4; Ppargc1a: peroxisome proliferator-activated receptor gamma coactivator 1-alpha; Ppar: peroxisome proliferator-activated receptor; Ppard: peroxisome proliferator-activated receptor delta; Pdk4: pyruvate dehydrogenase kinase 4; Ucp: uncoupling protein.