Journal: Journal of medicinal chemistry

Article Title: A novel N-substituted valine derivative with unique PPARγ binding properties and biological activities

doi: 10.1021/acs.jmedchem.0c01555

Figure Lengend Snippet: Effect of 7j on PPARγ phosphorylation. (A) Percentage of in vitro PPARγ Ser273 phosphorylation by CDK5 in the presence of 0.1 μM of 7j or Rosi. (B) Phosphorylation of PPARγ Ser273 in 3T3-L1 adipocyte incubated for 60 minutes with 5 μM of Rosi, 7j or Roscovitine (Rsv) before TNFα stimulation (50 ng/ml; 90 minutes). Two independent experiments are shown. Phosphospecific antibodies were from Rockland or New England Peptide (NEP). Arrow heads indicate phosphorylated PPARγ and PPARγ2. (C) RT-PCR analysis of the expression levels of a selection of genes known to be regulated by CDK5-dependent phosphorylation of PPARγ. Values are means ± SD (n = 5) expressed relative to the mean of control. **p < 0.01, ***p < 0.001 vs. control (one-way ANOVA followed by Dunnett’s post hoc test).

Article Snippet: PPARγ phospho Ser273 antibodies were from Rockland (Limerick, PA, USA) or custom produced by New England Peptide (Gardner, MA, USA).

Techniques: Phospho-proteomics, In Vitro, Incubation, Reverse Transcription Polymerase Chain Reaction, Expressing, Selection, Control

Journal: Bioactive Materials

Article Title: A foam cell-targeted lipophagy restoration strategy stabilizes vulnerable atherosclerotic plaques

doi: 10.1016/j.bioactmat.2026.02.041

Figure Lengend Snippet: Schematic of the anti-atherosclerotic mechanism of OPN-HMCN@MLT. ( A ) The study commenced with the synthesis of mesoporous carbon nanospheres (MCN) functionalized with an OPN-binding peptide and hyaluronic acid to construct the OPN-HMCN nanoplatform. The OPN-binding peptide was designed to recognize OPN enriched in the extracellular matrix and on the surface of foam cells, thereby enabling selective accumulation in OPN-rich pathological regions. Following OPN recognition, OPN-HMCN@MLT undergoes CD44-dependent endocytosis. Melatonin (MLT), a lipid autophagy–promoting agent, was subsequently encapsulated within the nanocarrier to form OPN-HMCN@MLT. Firstly, the released MLT can bind to and upregulate the expression of PPARα and PPARγ, which then promote the expression of downstream genes (ABCA1, ABCG1, ACOX-1, and CTP1A) and trigger the lipophagy. ( B ) Subsequently, its lipophagy-enhancing effects, including ABCA1/G1-mediated cholesterol efflux and CTP1A/ACOX-1-mediated mitochondrial fatty acid oxidation, were studied to confirm the reversal of foam cell formation. ( C ) These effects eventually promote foam cells to reverse into macrophages. Abbreviations: MCN, mesoporous carbon nanoparticle; OPN, osteopontin; MLT, melatonin; LDL, low-density lipoprotein; ox-LDL, oxidized low-density lipoprotein; PA, Photoacoustic.

Article Snippet: To block nonspecific binding, membranes were incubated with 5% skim milk for 1 h. Thereafter, membranes were incubated overnight at 4 °C with primary antibodies against ABCA1, ABCG1, ACOX1, CPT1A, LC3 (ab192890, 1:2000, abcam), LAMP1 (84658-5-RR, 1:8000, Proteintech), PPARα (66826-1-Ig, 1:3000, Proteintech), PPARγ (66936-1-Ig, 1:10000, Proteintech), P62 (18420-1-AP, 1:10000, Proteintech), MCAD (55210-1-AP, 1:3000, Proteintech), LCAD (17526-1-AP, 1:10000, Proteintech), tubulin (80762-1-RR, 1:10000, Proteintech), GAPDH (60004-1-Ig, 1:50000, Proteintech), and β-actin (66009-1-Ig, 1:20000, Proteintech).

Techniques: Binding Assay, Construct, Expressing

Journal: Drug Design, Development and Therapy

Article Title: Asiatic acid protests against myocardial ischemia/reperfusion injury via modulation of glycometabolism in rat cardiomyocyte

doi: 10.2147/DDDT.S175116

Figure Lengend Snippet: Asiatic acid increases PPARγ levels and promotes GLUT4 translocation to plasma membrane in ischemic rats. Notes: The myocardium was isolated from vehicle-, asiatic acid (AA)-, and asiatic acid plus LY294002 (AA+LY)-treated rats under normal condition and following 1 hour of myocardial ischemia and 24 hours of reperfusion, respectively. The mRNA levels of ( A ) PPARγ and ( B ) GLUT4 were determined by real-time PCR. ( C ) PPARγ, GLUT4 from plasma membrane (PM GLUT4), GLUT4, and GAPDH levels were determined by Western blot. ( D ) Quantitative analysis of PPARγ levels were normalized to GAPDH levels, and ( E ) GLUT4 translocation levels (PM GLUT4) were normalized to total GLUT4. # P <0.05, ## P <0.01 vs the sham group; ** P <0.01 vs the vehicle group; && P <0.01 vs the asiatic acid-treated group. Abbreviation: MI/R, myocardial ischemia/reperfusion.

Article Snippet: The anti-Akt and anti-phosphor-Akt antibodies were obtained from Santa Cruz Biotechnology, Inc. (Santa Cruz, CA, USA); the anti-GSK-3β and anti-phospho-GSK-3β (Ser9) antibodies were from Cell Signaling Technology, Inc. (Danvers, MA, USA); the anti-GLUT4 and anti-PPARγ antibody was from Boster Biological Technology, Ltd. (Wuhan, China); and the anti-glyceraldehyde phosphate dehydrogenase (GAPDH) antibody was obtained from KangChen Bio-tech Inc. (Shanghai, China).

Techniques: Translocation Assay, Clinical Proteomics, Membrane, Isolation, Real-time Polymerase Chain Reaction, Western Blot

Journal: PLoS ONE

Article Title: Expression of Obesity Markers and Persistent Organic Pollutants Levels in Adipose Tissue of Obese Patients: Reinforcing the Obesogen Hypothesis?

doi: 10.1371/journal.pone.0084816

Figure Lengend Snippet: Data represent mean (±SE) of the serum concentrations of leptin and adiponectin (A) and gene expression of leptin, adiponectin, TNFα and PPARγ normalised to the gene expression of TBP gene*1000 of AT samples (B, C, D, E). Significant differences between men (n = 17) and women (n = 33) (B, C), diabetic (n = 8) and non diabetic patients (n = 42) (D, E) are indicated with asterisks (Mann Whitney U-test; *p≤0.05; **p≤0.01).

Article Snippet: Template standards and primers were obtained from OriGene Technologies (Rockville, MD) for every measured gene: PPARγ (HK210365), TNFα (HK208349), ADIPOQ (HK209573) and LEP (HK204316).

Techniques: Expressing, MANN-WHITNEY

Journal: eLife

Article Title: Bladder-cancer-associated mutations in RXRA activate peroxisome proliferator-activated receptors to drive urothelial proliferation

doi: 10.7554/eLife.30862

Figure Lengend Snippet:

Article Snippet: recombinant DNA reagent , pCMV6-XL4 PPARG (plasmid) , OriGene , OriGene:SC108192 , .

Techniques: Generated, Plasmid Preparation, Infection, In Vitro, Recombinant, Mutagenesis, Clone Assay, Sequencing, Luciferase, Software