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Homogeneous time-resolved G protein-coupled receptor-ligand binding assay based on fluorescence cross-correlation spectroscopy.
This work demonstrates the suitability of the homogeneous and time-resolved FCCS assay format for a robust, high-throughput determination of receptor-ligand binding affinities and kinetic rate constants for various therapeutically relevant GPCRs. Expand
Simultaneous detection of intracellular target and off‐target binding of small molecule cancer drugs at nanomolar concentrations
A combination of fluorescence correlation spectroscopy (FCS) and fluorescence cross‐correlation spectroscope (FCCS) is presented as a solution to the problem of off‐target binding and membrane permeability in vitro assays. Expand
The in vitro biological activity of the HLA-DR-binding clinical IgG4 antibody 1D09C3 is a consequence of the disruption of cell aggregates and can be abrogated by Fab arm exchange.
The results indicate that the activity of 1D09C3 in vitro may have been a consequence of assay design rather than an ability to induce HLA-DR-dependent cell death, and this antibody undergoes Fab arm exchange in the presence of IgG4. Expand
Identification of Methionine Aminopeptidase-2 (MetAP-2) inhibitor M8891, a Clinical Compound for the Treatment of Cancer.
The recently disclosed next generation of reversible, selective and potent MetAP-2 inhibitors introduced a cyclic tartronic diamide scaffold. However, the lead compound 1a suffered from enterohepaticExpand
Structural and functional insights into the fly microRNA biogenesis factor Loquacious.
The structure of the third double-stranded RNA-binding domain (dsRBD) of Loqs is solved and specific structural elements that interact with dmDcr1 are defined and it is suggested that dimerization might be a general feature of dsRBD proteins in gene silencing. Expand
XPO1 target occupancy measurements confirm the selinexor recommended phase 2 dose
In vivo mouse studies showed XPO1 occupancy could be measured in tumors and was dose-dependent, with >90% target saturation at 10 mg/kg, and findings confirm the selinexor RP2D of 60 mg for achieving target occupancy and inhibition up to 48 hours. Expand
Abstract LB-B09: Application of Fluorescence Correlation Spectroscopy as a novel tool to quantify target occupancy in cells and tumor tissue
The quantification of Target Occupancy (TO) in cells after application of an inhibitor is an important parameter to correlate the biochemical features of a drug with its in vivo efficacy.Expand
Development of a Pharmacodynamic Assay for XPO1 Occupancy Using Fluorescence Cross Correlation Spectroscopy (FCCS)
Comparison of cytotoxicity and XPO1 binding in hematological cell lines treated with increasing concentrations of selinexor in vitro indicated that XPO 1 occupancy by se linexor occurred to the same extent regardless of drug sensitivity, but there were two observations that distinguished the selineXor-resistant cell line THP-1 from the other 3 sensitive cell lines. Expand
Although focal and segmental glomerulosclerosis (FSGS) has been in the scientific focus for many years, it is still a massive burden for patients with no causal therapeutic option. In FSGS,Expand