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…

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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,…

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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…

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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…

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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…

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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…

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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…

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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…

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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…

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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…

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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,…

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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…

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