Journal: Scientific Reports

Article Title: Characterization of a novel non-steroidal glucocorticoid receptor agonist optimized for topical treatment

doi: 10.1038/s41598-022-05471-w

Figure Lengend Snippet: Pharmacological activity of LEO 134310A vs CP and BMV in human skin assessed by gene expression levels of FKBP5 . Effective doses (API concentrations in dosing solution) of CP (n = 6 studies), BMV (n = 3 studies) and LEO 134310A (n = 5 studies) to induce FKBP5 levels to 50% of maximum response (ED 50 ). FKBP5 levels were normalised to vehicle-treated controls and E max and ED 50 were estimated in a sigmoid E max model. Weighted geometric mean ± standard deviation. Statistical comparison (T-test) against BMV ( NS not significant).

Article Snippet: RNA was extracted and qPCR was performed using TaqMan gene expression assays ( FKBP5 -Hs01561006_m1, TSC22D3 (GILZ) -Hs00608272_m1, TXNIP -Hs01006900_g1, ACTB -Hs99999903_m1, PPIA -Hs99999904_m1, GAPDH -Hs99999905_m1).

Techniques: Activity Assay, Gene Expression, Standard Deviation, Comparison, Control

Journal: Scientific Reports

Article Title: Characterization of a novel non-steroidal glucocorticoid receptor agonist optimized for topical treatment

doi: 10.1038/s41598-022-05471-w

Figure Lengend Snippet: LEO 134310 does not induce skin atrophy in minipigs. H&E staining of minipig skin biopsy samples from untreated skin ( a ), test fields treated with LEO vehicle ( b ), Dermovate cream 0.05% CP ( c ), Betnovate cream 0.1% BMV ( d ), and LEO 134310 2% ( e ). The bar represents 100 µm. Epidermal thickness in skin biopsies from minipigs after 4 weeks treatment ( f ) (n = 5). Statistical significance was determined by one-way ANOVA with Dunnett’s multiple comparisons test versus vehicle. *p < 0.05; **p < 0.01; ***p < 0.001; NS: not significant. Fold changes of FKBP5 expression in relation untreated control, measured by qRT-PCR in skin biopsies from minipigs treated for 4 weeks ( g ) (n = 5). The differences were modelled in a paired manner applying a linear mixed effects model, with Dunnett’s post hoc testing (*p < 0.05; **p < 0.01; ***p < 0.001). Error bars represent standard errors of the paired differences.

Article Snippet: RNA was extracted and qPCR was performed using TaqMan gene expression assays ( FKBP5 -Hs01561006_m1, TSC22D3 (GILZ) -Hs00608272_m1, TXNIP -Hs01006900_g1, ACTB -Hs99999903_m1, PPIA -Hs99999904_m1, GAPDH -Hs99999905_m1).

Techniques: Staining, Cream, Expressing, Control, Quantitative RT-PCR

Journal: Scientific Reports

Article Title: Characterization of a novel non-steroidal glucocorticoid receptor agonist optimized for topical treatment

doi: 10.1038/s41598-022-05471-w

Figure Lengend Snippet: In vivo efficacy versus systemic side effects of LEO 134310, CP and BMV in the TPA-induced skin inflammation mouse model. Dose–response curves for effect of CP ( a ), BMV ( b ) and LEO 134310 ( c ) on ear biopsy weight, spleen weight and osteocalcin plasma concentration in the TPA mouse model. All values are normalized to vehicle/TPA controls. Body weight vs. dose ( d ), blood concentration at 2 h after dosing vs. dose ( e ) and mRNA levels of Fkbp5 vs ear biopsy weight ( f ) (R = correlation coefficient). Vehicle, ( a ) CP, ( b ) BMV, ( c ) LEO 134310. Mean values at each dose (n = 2) in ( a – e ) and individual values in ( f ).

Article Snippet: RNA was extracted and qPCR was performed using TaqMan gene expression assays ( FKBP5 -Hs01561006_m1, TSC22D3 (GILZ) -Hs00608272_m1, TXNIP -Hs01006900_g1, ACTB -Hs99999903_m1, PPIA -Hs99999904_m1, GAPDH -Hs99999905_m1).

Techniques: In Vivo, Clinical Proteomics, Concentration Assay

Journal: Scientific Reports

Article Title: Effects of a single application of hydrolyzed fish collagen on dermal protein expression and tissue architecture in human skin models

doi: 10.1038/s41598-025-11372-5

Figure Lengend Snippet: Relative gene expression of Elastin (ELN) and Aquaporin-3 (AQP3), Dermis thickness measurement, and representative images in 3D EpiDerm FT models treated for 24 h with S-HFC (a, b, c, g) and F-HFC (d, e, f, h) respectively, at different concentrations (47.00; 28.20; 23.50 µg Hyp /mL, corresponding to 0.1%; 0.06% and 0.05% w/v of HFC), with respect to negative controls (CTRL for S-HFC, consisting in vehicle, and 0.00 µg Hyp /mL for F-HFC, consisting in the cream without addition of HFC). For each treatment, dermis thickness was measured cutting five different hematoxylin-eosin stained sections of 5 μm thickness. In the box-and-whisker plots, the horizontal line indicates the median, the box reflects values from the first to the third quartile, and the whiskers represent the furthest points that are not outliers. Values come from at least 2 independent experiments performed in triplicate. The significant differences are indicated by symbols on bars (**** p ≤ 0.0001, *** p ≤ 0.001, ** p ≤ 0.01, * p ≤ 0.05 vs. CTRL).

Article Snippet: Expression of the following biomarkers was evaluated: Aquaporin (AQP3) (proteins involved in the transport of water, glycerol and urea across cell membrane) Collagen Type III Alpha 1 Chain (COL3A1), Collagen Type I Alpha 1 Chain (COL1A1) (both involved in the regulation of collagen expression) and Elastin (ELN) (involved in the assembly of elastic fibers) (Bio-Rad Laboratories, Hercules, CA, USA) .

Techniques: Gene Expression, Cream, Staining, Whisker Assay