Browse Items · NEOMED Bibliography Database

Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening.

Parkinson's disease is a severe debilitating neurodegenerative disorder. Recently, it was shown that the peroxisome proliferating-activator receptor-gamma agonist pioglitazone protected mice from

Tags: 2010, Bioorganic & medicinal chemistry letters, Carroll Richard T, Darvesh Altaf S, Department of Pharmaceutical Sciences, Funk Max O, Geldenhuys Werner J, Models, Molecular, Monoamine Oxidase Inhibitors/chemistry/*pharmacology, Monoamine Oxidase/*drug effects, NEOMED College of Pharmacy, Structure-Activity Relationship, Van der Schyf Cornelis J

Dimebon attenuates methamphetamine, but not MPTP, striatal dopamine depletion.

Dimebon is an anti-histamine with central nervous system activity. In this report the effects of dimebon as a neuroprotectant in animal models of Parkinson's disease were tested as assessed in methamphetamine- and MPTP-induced striatal dopaminergic…

Tags: 2012, Animals, Corpus Striatum/*drug effects/metabolism, Darvesh Altaf S, Department of Pharmaceutical Sciences, Dluzen Dean E, Dopamine/*metabolism, Drug Synergism, Geldenhuys Werner J, Inbred C57BL, Indoles/*pharmacology, Methamphetamine/*pharmacology, Mice, NEOMED College of Pharmacy, Neurochemistry international

Pharmacotherapy of Alzheimer's disease: current and future trends.

Alzheimer's disease (AD) and its related dementia has shown an alarming rise in the global population. Although considerable efforts have been made to develop effective therapeutic agents for AD therapy, drug development has not met significant…

Tags: 2015, Alzheimer Disease/*drug therapy, Alzheimer's disease, Anti-Inflammatory Agents, Antioxidants, cholinesterase inhibitors, Darvesh Altaf S, dementia, Department of Pharmaceutical Sciences, Drug Therapy/*methods/*trends, Expert review of neurotherapeutics, Geldenhuys Werner J, Humans, immunotherapy, memantine, multi-targeted drugs, natural products, NEOMED College of Pharmacy, Pharmacotherapy

Evolution of a Natural Products and Nutraceuticals Course in the Pharmacy Curriculum.

Objective. To develop, implement, and modify a required, second-year pharmacy course that provides an understanding of the scientific, therapeutic, and clinical principles, as well as the evidence-based medicine underlying the use of natural…

Structure-activity and in vivo evaluation of a novel lipoprotein lipase (LPL) activator.

Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in…

Natural products of dietary origin as lead compounds in virtual screening and drug design.

Natural products have been found to be useful in the treatment of several diseases across the ages. In this article, we review the use of natural products, obtained from dietary sources, as lead compounds in developing novel therapeutic agents. These…

Tags: *Biological Products/pharmacology, *Drug Design, 2012, Animals, Bishayee Anupam, Caffeine/pharmacology, Carroll Richard T, Curcumin/pharmacology, Current pharmaceutical biotechnology, Darvesh Altaf S, Department of Pharmaceutical Sciences, Diet, Geldenhuys Werner J, Genistein/pharmacology, Humans, NEOMED College of Pharmacy, Resveratrol, Stilbenes/pharmacology

Effects of a novel dopamine uptake inhibitor upon extracellular dopamine from superfused murine striatal tissue.

The dopamine transporter (DAT) plays an important role in substance abuse, schizophrenia, and dopaminergic toxicity associated with the Parkinsonian animal model toxin, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Accordingly, the DAT serves…

High-content screen using zebrafish (Danio rerio) embryos identifies a novel kinase activator and inhibitor.

In this report we utilized zebrafish (Danio rerio) embryos in a phenotypical high-content screen (HCS) to identify novel leads in a cancer drug discovery program. We initially validated our HCS model using the flavin adenosine dinucleotide (FAD)…

Tags: *Cancer, *Compound library, *Kinase, *Notochord, *Phenotypic screen, *Somites, *Zebrafish, 2017, Aljammal Rowaa, Animals, Antineoplastic Agents/chemistry/pharmacology, Antitumor/methods, Benzoic Acid/chemistry/pharmacology, Bergeron Sadie A, Bioorganic & medicinal chemistry letters, Chen Wei-Chi, Death-Associated Protein Kinases/metabolism, Department of Integrative Medical Sciences, Drug Discovery/*methods, Drug Screening Assays, Embryo, Enzyme Activation/drug effects, Enzyme Activators/*chemistry/*pharmacology, Gaasch Briah L, Geldenhuys Werner J, Hazlehurst Lori A, Mullins Jackie E, NEOMED College of Medicine, Neoplasms/drug therapy/enzymology, Nonmammalian/*drug effects/enzymology, Protein Kinase Inhibitors/*chemistry/*pharmacology, Protein-Serine-Threonine Kinases/antagonists & inhibitors/metabolism, Yun June, Zebrafish Proteins/antagonists & inhibitors/metabolism, Zebrafish/*embryology

MitoNEET (CISD1) Knockout Mice Show Signs of Striatal Mitochondrial Dysfunction and a Parkinson's Disease Phenotype.

Mitochondrial dysfunction is thought to play a significant role in neurodegeneration observed in Parkinson's disease (PD), yet the mechanisms underlying this pathology remain unclear. Here, we demonstrate that loss of mitoNEET (CISD1), an iron-sulfur…

A novel Lipoprotein lipase (LPL) agonist rescues the enzyme from inhibition by angiopoietin-like 4 (ANGPTL4).

Lipoprotein lipase (LPL) is a key physiological regulator of triglycerides and atherosclerosis risk. Random screening identified a compound designated C10, showing greater LPL agonist activity than NO-1886, a known LPL agonist. Structure-activity…

3-D-QSAR and docking studies on the neuronal choline transporter.

The high affinity neuronal choline transporter (CHT1) is responsible for the uptake of choline into the pre-synaptic terminal of cholinergic neurons. Considering our past experience with modeling the blood-brain barrier choline transporter (BBBCHT)…

Tags: 2010, Allen David D, Binding Sites, Bioorganic & medicinal chemistry letters, Blood-Brain Barrier/metabolism, Computer Simulation, Geldenhuys Werner J, Lockman Paul R, Membrane Transport Proteins/*chemistry/metabolism, Models, Molecular, Neurons/*metabolism, Quantitative Structure-Activity Relationship, Quaternary Ammonium Compounds/chemistry

Novel models for assessing blood-brain barrier drug permeation.

INTRODUCTION: The blood-brain barrier (BBB) is a selectively permeable micro-vascular unit which prevents many central nervous system (CNS)-targeted compounds from reaching the brain. A significant problem in CNS drug development is the ability to…

Tags: *Capillary Permeability, 2012, Allen David D, Animal, Animals, Blood-Brain Barrier/*metabolism, Bloomquist Jeffrey R, Drosophila melanogaster/metabolism, Expert opinion on drug metabolism & toxicology, Geldenhuys Werner J, Grasshoppers/metabolism, High-Throughput Screening Assays, Humans, Models, Pharmaceutical Preparations/*metabolism, Zebrafish/metabolism

The blood-brain barrier choline transporter.

Drug delivery to the brain is made difficult by the blood-brain barrier (BBB) which is selectively permeable to organic drug compounds. Several membrane solute and nutrient transporters are expressed in the BBB vasculature, which may be utilized as…

Tags: 2012, Allen David D, Animals, Blood-Brain Barrier/drug effects/*metabolism, Central nervous system agents in medicinal chemistry, Drug Delivery Systems/*methods, Geldenhuys Werner J, Humans, Membrane Transport Proteins/*metabolism, Organic Cation Transport Proteins/metabolism, Organic Cation Transporter 1/metabolism, Organic Cation Transporter 2

Parkinson's disease biomarker: a patent evaluation of WO2013153386.

INTRODUCTION: Parkinson's disease (PD) is a neurodegenerative movement disorder resultant from the loss of dopaminergic neurons in the brain. There is an urgent need for effective biomarkers that can be used in the early diagnosis of PD.…

4-Hydroxynonenal dependent alteration of TRPV1-mediated coronary microvascular signaling.

We demonstrated previously that TRPV1-dependent regulation of coronary blood flow (CBF) is disrupted in diabetes. Further, we have shown that endothelial TRPV1 is differentially regulated, ultimately leading to the inactivation of TRPV1, when exposed…

Tags: *4-Hydroxynonenal, *Coronary regulation, *Lipid peroxidation, *Post-translational modification, *Protein Processing, *Reactive oxygen species, *Signal Transduction, *TRPV1, 2016, Action Potentials/drug effects, Aldehydes/antagonists & inhibitors/metabolism/*pharmacology, Animal, Animals, Blood Flow Velocity, Bratz Ian N, Calcium Signaling/drug effects, Cappelli Holly C, Capsaicin/*pharmacology, Cardiovascular Agents/*pharmacology, Connell Patrick J, Coronary Circulation/drug effects, Coronary Vessels/metabolism/physiopathology, Cysteine/genetics/metabolism, Damron Derek S, DelloStritto Daniel J, Department of Integrative Medical Sciences, Diabetes Mellitus/drug therapy/*metabolism/physiopathology, Disease Models, Fahmy Joseph N, Femoral Artery/metabolism/physiopathology, Free radical biology & medicine, Geldenhuys Werner J, HEK293 Cells, Humans, Inbred C57BL, Lipid Peroxidation, Male, Mice, NEOMED College of Medicine, Patch-Clamp Techniques, Post-Translational, Sinharoy Pritam, Thodeti Charles K, TRPV Cation Channels/genetics/*metabolism, Vasodilation/drug effects

In vivo brain microdialysis: advances in neuropsychopharmacology and drug discovery.

INTRODUCTION: Microdialysis is an important in vivo sampling technique, useful in the assay of extracellular tissue fluid. The technique has both pre-clinical and clinical applications but is most widely used in neuroscience. The in vivo…

Tags: 2011, Carroll Richard T, Darvesh Altaf S, Department of Pharmaceutical Sciences, Expert opinion on drug discovery, Geldenhuys Werner J, Gudelsky Gary A, Klein Jochen, Meshul Charles K, NEOMED College of Pharmacy, Van der Schyf Cornelis J

Curcumin and neurodegenerative diseases: a perspective.

INTRODUCTION: Curcumin, a dietary polyphenol found in the curry spice turmeric, possesses potent antioxidant and anti-inflammatory properties and an ability to modulate multiple targets implicated in the pathogenesis of chronic illness. Curcumin has…

Tags: 2012, Animals, Bishayee Anupam, Carroll Richard T, Curcumin/adverse effects/pharmacokinetics/*pharmacology/*therapeutic use, Darvesh Altaf S, Department of Pharmaceutical Sciences, Drug Evaluation, Expert opinion on investigational drugs, Geldenhuys Werner J, Humans, NEOMED College of Pharmacy, Neurodegenerative Diseases/*drug therapy/metabolism, Neuroprotective Agents/adverse effects/pharmacokinetics/*pharmacology/*therapeutic use, Novotny Nicholas A, Oxidative Stress/drug effects, Preclinical, Van der Schyf Cornelis J

Oxidative stress and Alzheimer's disease: dietary polyphenols as potential therapeutic agents.

Oxidative stress has been strongly implicated in the pathophysiology of neurodegenerative disorders such as Alzheimer's disease (AD). In recent years, antioxidants - especially those of dietary origin - have been suggested as possible agents useful…

Tags: 2010, Alzheimer Disease/*physiopathology/*therapy, Animals, Antioxidants/*administration & dosage/chemistry/pharmacology, Bishayee Anupam, Carroll Richard T, Darvesh Altaf S, Department of Pharmaceutical Sciences, Expert review of neurotherapeutics, Flavonoids/*administration & dosage/chemistry/pharmacology, Geldenhuys Werner J, Humans, Mitochondria/drug effects/physiology, NEOMED College of Pharmacy, Neurodegenerative Diseases/physiopathology, Oxidative Stress/drug effects/*physiology, Phenols/*administration & dosage/chemistry/pharmacology, Polyphenols, Van der Schyf Cornelis J

Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.

The neuroprotective activity of pioglitazone and rosiglitazone in the MPTP parkinsonian mouse prompted us to evaluate a set of thiazolidinedione (TZD) type compounds for monoamine oxidase A and B inhibition activity. These compounds were able to…

Markers associated with testosterone enhancement of methamphetamine-induced striatal dopaminergic neurotoxicity.

Intact male CD-1 mice received an injection of testosterone propionate (TP–5 ug), progesterone (P–5 mg), the oil vehicle or remained untreated (control). At 24 hours after hormonal treatments the mice received an injection of methamphetamine (MA–40…

Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease.

A series of compounds related to piperine and antiepilepsirine was screened in a monoamine oxidase A and B assay. Piperine is an alkaloid from the source plant of both black and white pepper grains, Piper nigrum. Piperine has been shown to have a…

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