Journal: Methods (San Diego, Calif.)

Article Title: Quantifying Membrane Protein Oligomerization with Fluorescence Cross-Correlation Spectroscopy

doi: 10.1016/j.ymeth.2018.02.002

Figure Lengend Snippet: fc values of the FKBP controls obtained from PIE-FCCS measurements in live Cos-7 cells. The three columns on the left side show the results of FKBP constructs without their dimerizer to induce interaction. The three columns on the right side show the results of FKBP constructs treated with the dimerizer (AP20187) which induces dimerization/oligomerization of the proteins. Each data point was the average of five 10 s FCS measurements performed on one cell. The purple numbers beside the box plots are the median values of the fc values. The grey numbers on top the plots are the total number of cells used. The one-way ANOVA tests were performed to obtain the p values (****: p<0.0001, **: p<0.01, ns: not significant).

Article Snippet: For the dimerizer assay, cells were incubated with AP20187 (HY-13992, MedChemExpress, Monmouth Junction, NJ) for 1 hour at a final concentration of 100 nM before imaging.

Techniques: Construct

Journal: Frontiers in Pharmacology

Article Title: FKBP Ligands—Where We Are and Where to Go?

doi: 10.3389/fphar.2018.01425

Figure Lengend Snippet: Structures of the selective bivalent dimerizer AP20187 and its monomeric precursors.

Article Snippet: Mice, transfected with colorectal cancer stem cells containing iCasp9 in their genome, were found to have strongly decreased tumor sizes after treatment with AP20187 (Kemper et al., ).

Techniques:

Journal: Nature Aging

Article Title: IL-23R is a senescence-linked circulating and tissue biomarker of aging

doi: 10.1038/s43587-024-00752-7

Figure Lengend Snippet: a , Treatment groups (top) and senotherapeutic treatment timeline (bottom) of young and old mice that received either vehicle or AP20187 (AP) by i.p. injection and either vehicle or one of four senolytic drugs (VEN, NAV, FIS or LUT) by oral gavage. Beginning on week 1, mice were treated once daily for 5 days, followed by 2 weeks without treatment, followed by 5 days of further treatment, followed by 1 week without treatment before necropsy. b – k , Plasma protein levels are demonstrated for all biomarkers that differed by age and at least one senolytic intervention significantly reversed the age-related change in at least one sex. This criterion was met for IL-23R ( b , c ), CCL5 ( d , e ), GCG ( f , g ), IL-17A ( h , i ) and CA13 ( j , k ). Pink, female groups; blue, male groups. Protein values were measured by Olink PEAs and are reported as NPX. Bars summarize median values. Samples sizes: YNG CON female, n = 6; OLD CON female, n = 6; OLD AP female, n = 5; OLD VEN female, n = 5; OLD NAV female, n = 7; OLD FIS female, n = 7; OLD LUT female, n = 7; YNG CON male, n = 5; OLD CON male, n = 8; OLD AP male, n = 8; OLD VEN male, n = 6; OLD NAV male, n = 7; OLD FIS male, n = 7; OLD LUT male, n = 7. YNG CON versus OLD CON reflect statistics provided in Fig. with exact P values provided. Kruskal–Wallis tests with multiple comparison correction were used for comparison of old treatment groups with OLD CON. We report * P < 0.05. See for additional description of the two-step statistical approach. a , Created with BioRender.com .

Article Snippet: AP20187 was acquired from WuXi AppTec.

Techniques: Injection, Clinical Proteomics, Comparison