Search Results - "Silverman, Richard B."
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Inducible nitric oxide synthase: Regulation, structure, and inhibition
Published in Medicinal research reviews (01-01-2020)“…A considerable number of human diseases have an inflammatory component, and a key mediator of immune activation and inflammation is inducible nitric oxide…”
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Development of nitric oxide synthase inhibitors for neurodegeneration and neuropathic pain
Published in Chemical Society reviews (07-10-2014)“…Nitric oxide (NO) is an important signaling molecule in the human body, playing a crucial role in cell and neuronal communication, regulation of blood…”
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3
From Basic Science to Blockbuster Drug: The Discovery of Lyrica
Published in Angewandte Chemie (International ed.) (28-04-2008)“…The anticonvulsant drug (S)‐(+)‐3‐isobutyl‐γ‐aminobutyric acid ((S)‐(+)‐3‐isobutyl‐GABA, Lyrica; see structure) was developed from a study of fundamental…”
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4
The Sirtuin 2 Inhibitor AK-7 Is Neuroprotective in Huntington’s Disease Mouse Models
Published in Cell reports (Cambridge) (27-12-2012)“…Inhibition of sirtuin 2 (SIRT2) deacetylase mediates protective effects in cell and invertebrate models of Parkinson’s disease and Huntington’s disease (HD)…”
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5
Potent, Selective, and Membrane Permeable 2‑Amino-4-Substituted Pyridine-Based Neuronal Nitric Oxide Synthase Inhibitors
Published in Journal of medicinal chemistry (27-07-2023)“…A series of potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors (hnNOS), based on a difluorobenzene ring linked to a…”
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6
CaV1.3-selective L-type calcium channel antagonists as potential new therapeutics for Parkinson's disease
Published in Nature communications (23-10-2012)“…L-type calcium channels expressed in the brain are heterogeneous. The predominant class of L-type calcium channels has a Ca V 1.2 pore-forming subunit. L-type…”
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The sirtuin-2 inhibitor AK7 is neuroprotective in models of Parkinson's disease but not amyotrophic lateral sclerosis and cerebral ischemia
Published in PloS one (21-01-2015)“…Sirtuin deacetylases regulate diverse cellular pathways and influence disease processes. Our previous studies identified the brain-enriched sirtuin-2 (SIRT2)…”
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8
Revisiting Heme Mechanisms. A Perspective on the Mechanisms of Nitric Oxide Synthase (NOS), Heme Oxygenase (HO), and Cytochrome P450s (CYP450s)
Published in Biochemistry (Easton) (26-02-2008)“…Despite the essential biological importance of reactions that involve heme, mechanisms of heme reactions in enzymes like nitric oxide synthase (NOS), heme…”
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9
Inhibition of interferon-gamma-stimulated melanoma progression by targeting neuronal nitric oxide synthase (nNOS)
Published in Scientific reports (01-02-2022)“…Interferon-gamma (IFN-γ) is shown to stimulate melanoma development and progression. However, the underlying mechanism has not been completely defined. Our…”
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10
Physiological involvement of presynaptic L‐type voltage‐dependent calcium channels in GABA release of cerebellar molecular layer interneurons
Published in Journal of neurochemistry (01-11-2020)“…While high threshold voltage‐dependent Ca2+ channels (VDCCs) of the N and P/Q families are crucial for evoked neurotransmitter release in the mammalian CNS, it…”
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11
Total Synthesis of Tambromycin Enabled by Indole C–H Functionalization
Published in Organic letters (20-04-2018)“…The total synthesis of tambromycin (1), a recently isolated tetrapeptide, is reported. This unusual natural product possesses a highly modified…”
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12
Stereospecific Total Syntheses of Proteasome Inhibitors Omuralide and Lactacystin
Published in Journal of organic chemistry (21-10-2011)“…Omuralide, a transformation product of the microbial metabolite lactacystin, was the first molecule discovered as a specific inhibitor of the proteasome and is…”
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13
Activation of heat shock and antioxidant responses by the natural product celastrol: transcriptional signatures of a thiol-targeted molecule
Published in Molecular biology of the cell (01-03-2008)“…Stress response pathways allow cells to sense and respond to environmental changes and adverse pathophysiological states. Pharmacological modulation of…”
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14
Structural and Mechanistic Basis for the Inactivation of Human Ornithine Aminotransferase by (3 S ,4 S )-3-Amino-4-fluorocyclopentenecarboxylic Acid
Published in Molecules (Basel, Switzerland) (23-01-2023)“…Ornithine aminotransferase (OAT) is overexpressed in hepatocellular carcinoma (HCC), and we previously showed that inactivation of OAT inhibits the growth of…”
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Ornithine Aminotransferase versus GABA Aminotransferase: Implications for the Design of New Anticancer Drugs
Published in Medicinal research reviews (01-03-2015)“…Ornithine aminotransferase (OAT) and γ‐aminobutyric acid aminotransferase (GABA‐AT) are classified under the same evolutionary subgroup and share a large…”
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NU-9 improves health of hSOD1G93A mouse upper motor neurons in vitro, especially in combination with riluzole or edaravone
Published in Scientific reports (30-03-2022)“…Even though amyotrophic lateral sclerosis (ALS) is a disease of the upper and lower motor neurons, to date none of the compounds in clinical trials have been…”
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Hydrophilic, Potent, and Selective 7‑Substituted 2‑Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors
Published in Journal of medicinal chemistry (24-08-2017)“…Neuronal nitric oxide synthase (nNOS) is a target for development of antineurodegenerative agents. Most nNOS inhibitors mimic l-arginine and have poor…”
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Design and Mechanism of GABA Aminotransferase Inactivators. Treatments for Epilepsies and Addictions
Published in Chemical reviews (11-04-2018)“…When the brain concentration of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) diminishes below a threshold level, the excess neuronal excitation…”
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19
Structural and biological studies on bacterial nitric oxide synthase inhibitors
Published in Proceedings of the National Academy of Sciences - PNAS (05-11-2013)“…Nitric oxide (NO) produced by bacterial NOS functions as a cytoprotective agent against oxidative stress in Staphylococcus aureus , Bacillus anthracis, and…”
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20
Celastrols as Inducers of the Heat Shock Response and Cytoprotection[boxs]
Published in The Journal of biological chemistry (31-12-2004)“…Alterations in protein folding and the regulation of conformational states have become increasingly important to the functionality of key molecules in…”
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