Publications

Showing 1–12 of 33 results

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 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 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 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 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…

Publications Examining Ligand-Based Stabilization of Proteins in Cells with MEK1 Kinase Inhibitors

In this study, we describe the evaluation of a cell-based protein stability assay using β-galactosidase fragment complementation technology performed in…

Publications Development of Three Orthogonal Assays Suitable for the Identification and Qualification of PIKfyve Inhibitors

FYVE-type zinc finger-containing phosphoinositide kinase (PIKfyve) catalyzes the formation of phosphatidylinositol 3,5-bisphosphate (PI(3,5)P2) from phosphatidylinositol 3-phosphate (PI(3)P).