Michael DePasquale
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View article: Identification and Characterization of a Blood–Brain Barrier Penetrant Inositol Hexakisphosphate Kinase (IP6K) Inhibitor
Identification and Characterization of a Blood–Brain Barrier Penetrant Inositol Hexakisphosphate Kinase (IP6K) Inhibitor Open
Inositol hexakisphosphate kinases (IP6Ks) have been studied for their role in glucose homeostasis, metabolic disease, fatty liver disease, chronic kidney disease, neurological development, and psychiatric disease. IP6Ks phosphorylate inosi…
View article: The IP6K Inhibitor LI-2242 Ameliorates Diet-Induced Obesity, Hyperglycemia, and Hepatic Steatosis in Mice by Improving Cell Metabolism and Insulin Signaling
The IP6K Inhibitor LI-2242 Ameliorates Diet-Induced Obesity, Hyperglycemia, and Hepatic Steatosis in Mice by Improving Cell Metabolism and Insulin Signaling Open
Obesity and nonalcoholic fatty liver disease (NAFLD) are global health concerns, and thus, drugs for the long-term treatment of these diseases are urgently needed. We previously discovered that the inositol pyrophosphate biosynthetic enzym…
View article: Identification of Small-Molecule Inhibitors of Human Inositol Hexakisphosphate Kinases by High-Throughput Screening
Identification of Small-Molecule Inhibitors of Human Inositol Hexakisphosphate Kinases by High-Throughput Screening Open
Inositol hexakisphosphate kinases (IP6Ks) catalyze pyrophosphorylation of inositol hexakisphosphate (IP6) into inositol 5-diphospho-1,2,3,4,6-pentakisphosphate (IP7), which is involved in numerous areas of cell physiology including glucose…
View article: Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol <i>O</i>-Methyltransferase
Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol <i>O</i>-Methyltransferase Open
A series of bicyclic pyridones were identified as potent inhibitors of catechol O-methyltransferase (COMT). Substituted benzyl groups attached to the basic nitrogen of the core scaffold gave the most potent inhibitors within this series. R…
View article: Development of a PC12 Cell Based Assay for Screening Catechol- <i>O</i> -methyltransferase Inhibitors
Development of a PC12 Cell Based Assay for Screening Catechol- <i>O</i> -methyltransferase Inhibitors Open
The male rat adrenal pheochromocytoma cell-derived PC12 cell line can synthesize and release catecholamine neurotransmitters, and it has been widely used as a model system in cell biology and toxicology research. Catechol-O-methyltransfera…
View article: Development of a PC12 cell-based assay for<i>in vitro</i>screening of catechol-<i>O</i>-methyltransferase inhibitors
Development of a PC12 cell-based assay for<i>in vitro</i>screening of catechol-<i>O</i>-methyltransferase inhibitors Open
The male rat adrenal pheochromocytoma cell-originated PC12 cell line can synthesize and release catecholamine neurotransmitters, and it has been widely used as a model system in cell biology and toxicology research. Catechol- O -methyltran…
View article: Novel, non-nitrocatechol COMT inhibitors modulate dopamine neurotransmission in the frontal cortex and improve cognitive flexibility
Novel, non-nitrocatechol COMT inhibitors modulate dopamine neurotransmission in the frontal cortex and improve cognitive flexibility Open
Cognitive impairment is a primary feature of many neuropsychiatric disorders and there is a need for new therapeutic options. Catechol- O -methyltransferase (COMT) inhibitors modulate cortical dopaminergic function and have been proposed a…
View article: Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol <i>O</i> -Methyltransferase
Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol <i>O</i> -Methyltransferase Open
A series of 8-hydroxy quinolines were identified as potent inhibitors of catechol O-methyltransferase (COMT) with selectivity for the membrane-bound form of the enzyme. Small substituents at the 7-position of the quinoline were found to in…