Search Results - "Silverman, Richard"
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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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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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Design of Selective Neuronal Nitric Oxide Synthase Inhibitors for the Prevention and Treatment of Neurodegenerative Diseases
Published in Accounts of chemical research (17-03-2009)“…Nitric oxide (NO), which is produced from l-arginine by the nitric oxide synthase (NOS) family of enzymes, is an important second-messenger molecule that…”
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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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Inactivators of Ornithine Aminotransferase for the Treatment of Hepatocellular Carcinoma
Published in ACS medicinal chemistry letters (13-01-2022)“…Hepatocellular carcinoma (HCC) is the second or third leading cause of cancer mortality worldwide (depending on which statistics are used), yet there is no…”
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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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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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American Academy of Orthopaedic Surgeons Clinical Practice Guideline Case Study: Management of Anterior Cruciate Ligament Injuries
Published in Journal of the American Academy of Orthopaedic Surgeons (01-06-2023)“…Considering the frequency of anterior cruciate ligament (ACL) tears, optimal management of these injuries was the subject of a 2022 clinical practice guideline…”
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The 2011 E. B. Hershberg Award for Important Discoveries in Medicinally Active Substances: (1S,3S)-3-Amino-4-difluoromethylenyl-1-cyclopentanoic Acid (CPP-115), a GABA Aminotransferase Inactivator and New Treatment for Drug Addiction and Infantile Spasms
Published in Journal of medicinal chemistry (26-01-2012)Get full text
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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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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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Synthesis of (2R,4S)‑4-Amino-5-hydroxybicyclo[3.1.1]heptane-2-carboxylic Acid via an Asymmetric Intramolecular Mannich Reaction
Published in Journal of organic chemistry (21-06-2024)“…Inhibition of human ornithine aminotransferase interferes with glutamine and proline metabolism in hepatocellular carcinoma, depriving tumors of essential…”
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Improved synthesis and anticancer activity of a potent neuronal nitric oxide synthase inhibitor
Published in Bioorganic & medicinal chemistry letters (15-06-2023)“…[Display omitted] An improved synthesis of 4-methyl-7-(3-((methylamino)methyl)phenethyl)quinolin-2-amine (1) is reported. A scalable, rapid, and efficient…”
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OV329, a novel highly potent γ‐aminobutyric acid aminotransferase inactivator, induces pronounced anticonvulsant effects in the pentylenetetrazole seizure threshold test and in amygdala‐kindled rats
Published in Epilepsia (Copenhagen) (01-12-2021)“…Summary Objective An attractive target to interfere with epileptic brain hyperexcitability is the enhancement of γ‐aminobutyric acidergic (GABAergic)…”
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Optimization of Blood–Brain Barrier Permeability with Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibitors Having a 2‑Aminopyridine Scaffold
Published in Journal of medicinal chemistry (14-03-2019)“…Effective delivery of therapeutic drugs into the human brain is one of the most challenging tasks in central nervous system drug development because of the…”
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2-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors
Published in Bioorganic & medicinal chemistry (01-09-2022)“…[Display omitted] A series of potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors (hnNOS) based on the 2-aminopyridine…”
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First Contact: 7‑Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate
Published in Journal of medicinal chemistry (14-05-2020)“…Inhibition of neuronal nitric oxide synthase (nNOS), an enzyme implicated in neurodegenerative disorders, is an attractive strategy for treating or preventing…”
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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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Editorial Commentary: Preoperative Patient-Reported Outcomes Measurement Information System Scores Predict Which Patients Will Benefit From Arthroscopic Meniscectomy: To Scope or Not to Scope?
Published in Arthroscopy (01-03-2021)“…Despite its widespread use and low complication rates, arthroscopic meniscectomy has not been uniformly successful in all patients, especially in those with…”
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Interaction of Candida albicans Cell Wall Als3 Protein with Streptococcus gordonii SspB Adhesin Promotes Development of Mixed-Species Communities
Published in Infection and Immunity (01-11-2010)“…Candida albicans colonizes human mucosa and prosthetic surfaces associated with artificial joints, catheters, and dentures. In the oral cavity, C. albicans…”
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