A5086385428- Lymphoma Diagnosis and Treatment
- Chronic Lymphocytic Leukemia Research
- Multicomponent Synthesis of Heterocycles
- HER2/EGFR in Cancer Research
- Cytokine Signaling Pathways and Interactions
- Lung Cancer Treatments and Mutations
- Ubiquitin and proteasome pathways
- Protein Degradation and Inhibitors
- Acute Lymphoblastic Leukemia research
- Chemical Synthesis and Analysis
- Catalytic C–H Functionalization Methods
- Acute Myeloid Leukemia Research
- Synthesis and Reactivity of Heterocycles
- Synthesis and biological activity
- Quinazolinone synthesis and applications
- Cancer-related Molecular Pathways
- Microtubule and mitosis dynamics
- Epigenetics and DNA Methylation
- PI3K/AKT/mTOR signaling in cancer
- Synthesis and Catalytic Reactions
- Crystallization and Solubility Studies
- Histone Deacetylase Inhibitors Research
- Chronic Myeloid Leukemia Treatments
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
University of Arkansas for Medical Sciences
2016-2025
University of Arizona
2012-2020
University of Arizona Cancer Center
2014
Accumulating evidence suggests that glioma stem cells (GSCs) are important therapeutic targets in glioblastoma (GBM). In this study, we identified NIMA-related kinase 2 (NEK2) as a functional binding protein of enhancer zeste homolog (EZH2) plays critical role the posttranslational regulation EZH2 GSCs. NEK2 was among most differentially expressed kinase-encoding genes GSC-containing cultures (glioma spheres), and it required for vitro clonogenicity, vivo tumor propagation, radioresistance....
The use of kinase-directed precision medicine has been heavily pursued since the discovery and development imatinib. Annually, it is estimated that around ∼20 000 new cases tropomyosin receptor kinase (TRK) cancers are diagnosed, with majority exhibiting a TRK genomic rearrangement. In this Perspective, we discuss current clinical applications for by providing following: (1) biological background significance family, (2) compilation known inhibitors analysis their cocrystal structures, (3)...
A large variety of halogenated nitroarenes have been selectively reduced with hydrazine hydrate in the presence Pd/C to give corresponding (halogenated) anilines good yield.
An expeditious one-pot, ligand-free, Pd(OAc)2-catalyzed, three-component reaction for the synthesis of 2,3-diarylimidazo[1,2-a]pyridines was developed under microwave irradiation. With high availability commercial reagents and great efficiency in expanding molecule diversity, this methodology is superior to existing procedures analogues.
Abstract Oncogenic conversion of the RET (rearranged during transfection) tyrosine kinase is associated with several cancers. A fragment‐based chemical screen led to identification a novel inhibitor, Pz‐1. Modeling and kinetic analysis identified Pz‐1 as type II inhibitor that able bind “DFG‐out” conformation kinase. Importantly, from single‐agent polypharmacology standpoint, was shown be active on VEGFR2, which can block blood supply required for RET‐stimulated growth. In cell‐based assays,...
The first example of metal-free regioselective hydrazination imidazo[1,2-<italic>a</italic>]pyridine with diethyl azodicarboxylate is accomplished.
Development of a multicomponent reaction to functionalize the C-3 position imidazo[1,2-<italic>a</italic>]pyridines <italic>via</italic> three component, decarboxylation protocol.
Abstract Expression of the serine/threonine kinase never in mitosis gene A (NIMA)–related 2 (NEK2) is essential for entry into via its role facilitating centrosome separation. Its overactivity can lead to tumorigenesis and drug resistance through activation several oncogenic pathways, including AKT. Although cancer-enabling activities NEK2 are documented many malignancies, correlations with poor survival myeloma, breast, non–small cell lung cancer, little known about lymphoma. Here, tumors...
RET receptor tyrosine kinase is a driver oncogene in human cancer. We recently identified the clinical drug candidate Pz-1, which targets and VEGFR2. A key vivo metabolite of Pz-1 its less active demethylated pyrazole analogue. Using bioisosteric substitution methods, here, we report identification NPA101.3, lacking structural liability for demethylation. NPA101.3 showed selective inhibitory profile an concentration 50 (IC50) <0.003 μM both inhibited phosphorylation all tested oncoproteins...
Quantitative proteomics generates large datasets with increasing depth and quantitative information.