Publications

Showing 1–12 of 35 results

Publications Detection of Cellular Target Engagement for Small-Molecule Modulators of Striatal-Enriched Protein Tyrosine Phosphatase (STEP)

Striatal-enriched protein tyrosine phosphatase (STEP) is a brain-specific enzyme that regulates the signaling molecules that control synaptic plasticity and neuronal…

Publications Discovery of Potent Agonists for the Predominant Variant of the Orphan MAS-Related GPCR X4 (MRGPRX4)

The MAS-related Gq protein-coupled receptor X4 (MRGPRX4) is poorly investigated. MRGPRX4 has been proposed to be involved in pain transmission,…

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 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 Multiplex quantitative assays indicate a need for reevaluating reported small-molecule TrkB agonists

Brain-derived neurotrophic factor (BDNF) and its receptor, tropomyosin-related kinase B (TrkB), have emerged as key regulators of brain plasticity and…

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 Development of Selective Phosphatidylinositol 5‑Phosphate 4‑Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode

Phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are emerging as attractive therapeutic targets in diseases, such as cancer, immunological disorders, and neurodegeneration, owing…

Publications Sorafenib activity and disposition in liver cancer does not depend on organic cation transporter 1 (OCT1).

Systemic therapy of advanced hepatocellular carcinoma (HCC) with the small molecule multi-kinase inhibitor sorafenib is associated with large inter-individual pharmacokinetic…

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 Activation of TrkB with TAM-163 results in opposite effects on body weight in rodents and non-human primates.

Strong genetic data link the Tyrosine kinase receptor B (TrkB) and its major endogenous ligand brain-derived neurotrophic factor (BDNF) to…

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 The Identification of Potent, Selective, and Brain Penetrant PI5P4Kγ Inhibitors as In Vivo-Ready Tool Molecules

Owing to their central role in regulating cell signaling pathways, the phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are attractive therapeutic targets in…