You searched for AR - Page 2 of 19

Publications Use of pharmacotrafficking assays therapeutically beneficial for Type 2 Diabetes

Type 2 diabetes (T2D) affects Latinos at twice the rate seen in populations of European descent. We recently identified a…

Publications Type 2 Diabetes Variants Disrupt Function of SLC16A11 through Two Distinct Mechanisms

Type 2 diabetes (T2D) affects Latinos at twice the rate seen in populations of European descent. We recently identified a…

Publications Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors.

A series of substituted indoles were examined as selective inhibitors of tropomyosin-related kinase receptor A (TrkA), a therapeutic target for…

Publications Structural characterization of nonactive site, TrkA-selective kinase inhibitors

Current therapies for chronic pain can have insufficient efficacy and lead to side effects, necessitating research of novel targets against…

Publications PathHunter Pharmacotrafficking: Review how customers used a pharmacochaperone-based high-throughput screening assay approach to discover chemical probes of orphan GPCRs

G-protein-coupled receptors (GPCRs) have varying and diverse physiological roles, transmitting signals from a range of stimuli, including light, chemicals, peptides,…

Publications A Pharmacochaperone-Based High-Throughput Screening Assay for the Discovery of Chemical Probes of Orphan Receptors.

G-protein-coupled receptors (GPCRs) have varying and diverse physiological roles, transmitting signals from a range of stimuli, including light, chemicals, peptides,…

Publications InCELL Target Engagement: A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1

A persistent problem in early small-molecule drug discovery is the frequent lack of rank-order correlation between biochemical potencies derived from…

Publications A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

Publications A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors

The non-receptor protein tyrosine phosphatase (PTP) SHP2 is encoded by the proto-oncogene PTPN11 and is a ubiquitously expressed key regulator…

Publications Measurement of β-Arrestin Recruitment for GPCR Targets.

β-Arrestins are ubiquitously expressed in all cell types, and function in the desensitization of G- protein coupled receptors (GPCRs), the…

Publications Navigating CYP1A induction and arylhydrocarbon receptor agonism in drug discovery. A case history with S1P1 agonists.

This article describes the finding of substantial upregulation of mRNA and enzymes of the cytochrome P450 1A family during a…

Publications Comparison of four in vitro cytotoxicity assays for assessing the potency of CD3-bispecific antibodies redirecting T cells to kill tumor target cells

Evaluation of cytotoxicity is a critical step in the selection of CD3-bispecific antibodies (BsAbs) for cancer immunotherapy.

Search results: “AR”