Browse Items (61 total)
- Tags: Geldenhuys Werner J
Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease.
Tags: 2012, Al-Baghdadi Osamah B, Alkaloids/*chemistry/isolation & purification/pharmacology, Animals, Benzodioxoles/*chemistry/isolation & purification/pharmacology, Binding Sites, Bioorganic & medicinal chemistry letters, Blood-Brain Barrier/drug effects, Bovine/metabolism, Cattle, Geldenhuys Werner J, Humans, Hydrogen Bonding, Molecular Docking Simulation, Monoamine Oxidase Inhibitors/*chemistry/isolation & purification/pharmacology, Monoamine Oxidase/*chemistry/metabolism, Parkinson Disease/metabolism/pathology, Piper nigrum/*chemistry, Piperidines/*chemistry/isolation & purification/pharmacology, Polyunsaturated Alkamides/*chemistry/isolation & purification/pharmacology, Prater Natalie I, Protein Binding, Protein Structure, Serum Albumin, Tertiary, Van der Schyf Cornelis J
Markers associated with testosterone enhancement of methamphetamine-induced striatal dopaminergic neurotoxicity.
Tags: 2012, Animals, Biomarkers/metabolism, Blotting, Body Temperature/drug effects, Body Weight/drug effects, Buletko A Blake, Corpus Striatum/*drug effects/metabolism, Darvesh Altaf S, Department of Pharmaceutical Sciences, Dluzen Dean E, Dopamine Plasma Membrane Transport Proteins/metabolism, Dopamine/*metabolism, Drug Synergism, Geldenhuys Werner J, HSP70 Heat-Shock Proteins/metabolism, Inbred Strains, Male, McDermott Janet L, Methamphetamine/*toxicity, Mice, NEOMED College of Pharmacy, Neurotoxicity Syndromes/*etiology/metabolism, Neurotoxicology and teratology, Oxidative Stress/drug effects, Testosterone Propionate/*pharmacology, Vesicular Monoamine Transport Proteins/metabolism, Western
Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.
Tags: 2011, Animals, Awale Prabha S, Bioorganic & medicinal chemistry letters, Carroll Richard T, Dluzen Dean E, Funk Max O, Geldenhuys Werner J, Humans, Inbred C57BL, Male, Mice, Models, Molecular, Molecular Structure, Monoamine Oxidase Inhibitors/chemical synthesis/chemistry/*pharmacology, Monoamine Oxidase/*metabolism, Stereoisomerism, Stinnett Hilary, Structure-Activity Relationship, Thiazolidinediones/chemical synthesis/chemistry/*pharmacology
Oxidative stress and Alzheimer's disease: dietary polyphenols as potential therapeutic agents.
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
Curcumin and neurodegenerative diseases: a perspective.
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
In vivo brain microdialysis: advances in neuropsychopharmacology and drug discovery.
4-Hydroxynonenal dependent alteration of TRPV1-mediated coronary microvascular signaling.
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
Parkinson's disease biomarker: a patent evaluation of WO2013153386.
Tags: 2014, Abdelmagid Samir M, Autophagy, Biomarkers/metabolism, clinical testing, Department of Anatomy & Neurobiology, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Disease Progression, Dopaminergic Neurons/pathology, Expert opinion on therapeutic patents, Gallegos Patrick J, Geldenhuys Werner J, Humans, Mitochondria/pathology, mitochondrial membrane potential, mitophagy, NEOMED College of Medicine, NEOMED College of Pharmacy, Parkinson Disease/*diagnosis/physiopathology, Patents as Topic, Phosphorylation, Protein Kinases/*metabolism, Safadi Fayez F, Ubiquitin-Protein Ligases/*metabolism
The blood-brain barrier choline transporter.
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
Novel models for assessing blood-brain barrier drug permeation.
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
3-D-QSAR and docking studies on the neuronal choline transporter.
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
A novel Lipoprotein lipase (LPL) agonist rescues the enzyme from inhibition by angiopoietin-like 4 (ANGPTL4).
Tags: 2014, Angiopoietin-like 4 Protein, Angiopoietins/*metabolism, ANGPTL4, Aring Danielle, Atherosclerosis, Benzamides/pharmacology, Bioorganic & medicinal chemistry letters, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Drug Discovery, Enzyme Activation/*drug effects, Geldenhuys Werner J, High-throughput screen, Homology model, Humans, Ibrolipim, Lipoprotein Lipase/*metabolism, LPL, Molecular Docking Simulation, NEOMED College of Graduate Studies, NEOMED College of Pharmacy, NO-1886, Organophosphorus Compounds/pharmacology, Sadana Prabodh
MitoNEET (CISD1) Knockout Mice Show Signs of Striatal Mitochondrial Dysfunction and a Parkinson's Disease Phenotype.
Tags: *Aging, *Disease Models, *drug discovery, *mitochondrial dysfunction, *mitoNEET, 2017, ACS chemical neuroscience, Animal, Animals, Benkovic Stanley A, Brown Candice M, Corpus Striatum/*metabolism/*pathology, Crish Samuel D, Darvesh Altaf S, Department of Pharmaceutical Sciences, Geldenhuys Werner J, Inbred C57BL, Iron-Binding Proteins/genetics/*metabolism, Knockout, Lin Li, Male, Membrane Proteins/genetics/*metabolism, Mice, Mitochondria/*metabolism/*pathology, NEOMED College of Pharmacy, Parkinson Disease/*metabolism/pathology, Richardson Jason R, Sullivan Patrick G, Yonutas Heather M
High-content screen using zebrafish (Danio rerio) embryos identifies a novel kinase activator and inhibitor.
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
Effects of a novel dopamine uptake inhibitor upon extracellular dopamine from superfused murine striatal tissue.
Tags: 2009, Animals, Bezuidenhout Lois-May, Biological Transport/drug effects, Buffers, Calcium Channels/metabolism, Dluzen Dean E, Dopamine Plasma Membrane Transport Proteins/metabolism, Dopamine Uptake Inhibitors/*pharmacology, Dopamine/*metabolism, European journal of pharmacology, Extracellular Space/*drug effects/*metabolism, Geldenhuys Werner J, In Vitro Techniques, Male, Methamphetamine/pharmacology, Mice, Neostriatum/*cytology/drug effects, PC12 Cells, Perfusion, Potassium Channel Blockers/pharmacology, Potassium Channels, Potassium Chloride/pharmacology, Rats, Voltage-Gated/antagonists & inhibitors
Natural products of dietary origin as lead compounds in virtual screening and drug design.
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
Structure-activity and in vivo evaluation of a novel lipoprotein lipase (LPL) activator.
Tags: *Diabetes, *High-fat diet, *Homology modeling, *Hyperlipidemia, *Lipoprotein lipase, *Liver cirrhosis, *Obesity, 2017, Animals, Benzeneacetamides/chemical synthesis/chemistry/*pharmacology, Bioorganic & medicinal chemistry letters, Caporoso Joel, Darvesh Altaf S, Department of Integrative Medical Sciences, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Dose-Response Relationship, Drug, Geldenhuys Werner J, Imidazoles/chemical synthesis/chemistry/*pharmacology, Lee Yoon-Kwang, Leeper Thomas C, Lin Li, Lipoprotein Lipase/*metabolism, Mice, Molecular Docking Simulation, Molecular Structure, NEOMED College of Graduate Studies, NEOMED College of Medicine, NEOMED College of Pharmacy, Sadana Prabodh, Structure-Activity Relationship
Evolution of a Natural Products and Nutraceuticals Course in the Pharmacy Curriculum.
Tags: *Biological Products/therapeutic use, *Clinical Competence, *Dietary Supplements, *Students, 2015, American journal of pharmaceutical education, course curriculum, Cudnik Michelle L, Curriculum/*trends, Darvesh Altaf S, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Dietary Supplements, Education, Educational Measurement/methods, Evidence-Based Medicine, Geldenhuys Werner J, herbal products, Humans, Krinsky Daniel L, NEOMED College of Pharmacy, Nutraceuticals, Pharmacy, Pharmacy/methods/*trends
Pharmacotherapy of Alzheimer's disease: current and future trends.
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
Dimebon attenuates methamphetamine, but not MPTP, striatal dopamine depletion.
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
Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening.
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
A novel binding assay identifies high affinity ligands to the rosiglitazone binding site of mitoNEET.
Tags: 2011, Awale Prabha S, Binding Sites/drug effects, Bioorganic & medicinal chemistry letters, Carroll Richard T, Dose-Response Relationship, Drug, Funk Max O, Geldenhuys Werner J, Ligands, Lin Li, Mitochondrial Proteins/*antagonists & inhibitors/metabolism, Molecular Structure, Recombinant Proteins/antagonists & inhibitors/metabolism, Rosiglitazone, Stereoisomerism, Structure-Activity Relationship, Thiazolidinediones/chemical synthesis/chemistry/*pharmacology
Structure-based design of a thiazolidinedione which targets the mitochondrial protein mitoNEET.
Tags: *Drug Design, 2010, Animals, Barnes Kendra F, Binding Sites/drug effects/physiology, Bioorganic & medicinal chemistry letters, Carroll Richard T, Dose-Response Relationship, Drug, Drug Delivery Systems/*methods, Funk Max O, Geldenhuys Werner J, Liver/drug effects/metabolism, Mitochondria, Mitochondrial Proteins/*metabolism, Protein Structure, Rats, Secondary, Structure-Activity Relationship, Thiazolidinediones/administration & dosage/*chemical synthesis/*metabolism
A scaffold hopping approach to identify novel monoamine oxidase B inhibitors.
Tags: *Monoamine Oxidase/chemistry/metabolism, 2012, Benzofurans/chemistry/pharmacology, Bioorganic & medicinal chemistry letters, Carroll Richard T, Enzyme Activation/drug effects, Flavonoids/chemistry/pharmacology, Funk Max O, Geldenhuys Werner J, Humans, Inhibitory Concentration 50, Models, Molecular, Molecular Structure, Monoamine Oxidase Inhibitors/*chemistry/*pharmacology, Protein Binding/drug effects, Small Molecule Libraries, Structure-Activity Relationship, Van der Schyf Cornelis J
A novel biomechanical analysis of gait changes in the MPTP mouse model of Parkinson's disease.
Exploring Adenosine Receptor Ligands: Potential Role in the Treatment of Cardiovascular Diseases.
Tags: *drug discovery, *Ligands, 2017, Adenosine/metabolism, Animals, Atherosclerosis, Cardiac death, Cardiovascular Diseases/drug therapy/metabolism, Cardiovascular System/metabolism, Department of Integrative Medical Sciences, Geldenhuys Werner J, Hanif Ahmad, Humans, Hydrogen Bonding, Models, Molecular, Molecular Structure, Molecules (Basel, Switzerland), myocardial infarction, Nayeem Mohammed A, NEOMED College of Medicine, Protein Binding, Purinergic P1/*chemistry/*metabolism, Receptors, Signal Transduction, Structure-Activity Relationship, Vascular tone, Yun June
Methyl Yellow: A Potential Drug Scaffold for Parkinson's Disease.
Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.
Tags: *Models, *Narcotic Antagonists, *Quantitative Structure-Activity Relationship, 2010, Animals, Binding, Calcium Signaling/drug effects, CHO Cells, Competitive, Cricetinae, Cricetulus, Databases, Factual, Geldenhuys Werner J, Humans, Journal of medicinal chemistry, Kuzenko Stephanie R, Ligands, Molecular, Neurokinin-3/*antagonists & inhibitors/chemistry, Opioid/chemistry, Quinolines/*chemistry/pharmacology, Radioligand Assay, Receptors, Simmons Mark A
mitoNEET as a novel drug target for mitochondrial dysfunction.
Emerging strategies of targeting lipoprotein lipase for metabolic and cardiovascular diseases.
Tags: 2017, Animals, Cardiovascular Diseases/drug therapy/*enzymology, Darvesh Altaf S, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Drug Discovery Today, Geldenhuys Werner J, Humans, Lin Li, Lipoprotein Lipase/chemistry/*metabolism, Metabolic Diseases/drug therapy/*enzymology, NEOMED College of Graduate Studies, NEOMED College of Pharmacy, Sadana Prabodh
Structure-activity relationships of pentacycloundecylamines at the
Tags: 2007, Amines/chemical synthesis/chemistry/*pharmacology, Animals, Bioorganic & medicinal chemistry, Bloomquist Jeffrey R, Brain/drug effects, Dizocilpine Maleate/pharmacology, Excitatory Amino Acid Antagonists/*pharmacology, Geldenhuys Werner J, Inbred ICR, Ion Channels, Malan Sarel F, Male, Mice, Models, Molecular, N-Methyl-D-Aspartate/*antagonists & inhibitors, Phencyclidine/analogs & derivatives, Piperidines/pharmacology, Radioligand Assay, Receptors, Structure-Activity Relationship, Synaptosomes/*drug effects, Thiophenes/pharmacology, Van der Schyf Cornelis J
Molecular determinants of blood-brain barrier permeation.
Tags: *Drug Delivery Systems, 2015, Adkins Chris E, Animals, Blood-Brain Barrier/*metabolism, Brain/drug effects, Computer Simulation, Geldenhuys Werner J, high-throughput, Humans, in silico, Lockman Paul R, logPS, Mohammad Afroz S, nutrient transporters, Permeability, Therapeutic delivery, Virtual screening
3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists.
3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (sigma1) receptor.
Tags: *Quantitative Structure-Activity Relationship, 2013, Amines/*chemistry/metabolism, Aza Compounds/chemistry, Binding Sites, Bioorganic & medicinal chemistry letters, Geldenhuys Werner J, Kinetics, Malan Sarel F, Molecular Docking Simulation, Novotny Nicholas, Protein Binding, Protein Structure, Receptors, sigma/*chemistry/metabolism, Tertiary, Van der Schyf Cornelis J
3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor.
Tags: *Quantitative Structure-Activity Relationship, 2011, Binding Sites, Bioorganic & medicinal chemistry letters, Computer Simulation, Drug Design, Geldenhuys Werner J, Humans, Ligands, Models, Molecular, Neurokinin-3/*chemistry/metabolism, Protein Structure, Quinolines/chemistry, Receptors, Simmons Mark A, Tertiary
Identification of a novel serum and glucocorticoid regulated kinase-1 (SGK1) ligand from virtual screening.
Tags: 2012, Binding Sites, Bioorganic & medicinal chemistry letters, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Drug Discovery, Geldenhuys Werner J, Humans, Immediate-Early Proteins/*antagonists & inhibitors/chemistry/metabolism, Ligands, Molecular Docking Simulation, NEOMED College of Graduate Studies, NEOMED College of Pharmacy, Protein Kinase Inhibitors/*chemistry/*pharmacology, Protein-Serine-Threonine Kinases/*antagonists & inhibitors/chemistry/metabolism, Sadana Prabodh, Talasila Phani K
Designing drugs with multi-target activity: the next step in the treatment of neurodegenerative disorders.
The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease.
Tags: 2009, Alzheimer Disease/*complications, Animals, Biological, Cognition Disorders/*drug therapy/*etiology, Drug Design, Expert review of neurotherapeutics, Geldenhuys Werner J, Humans, Models, Receptors, Serotonin Antagonists/chemistry/*therapeutic use, Serotonin/*metabolism, Structure-Activity Relationship, Van der Schyf Cornelis J
Role of serotonin in Alzheimer's disease: a new therapeutic target?
Tags: 2011, Alzheimer Disease/*drug therapy/*metabolism, Alzheimer's Disease – Drug Therapy, Alzheimer's Disease – Metabolism, Animals, Cell Surface – Metabolism, Clinical Trials, Clinical Trials as Topic, CNS drugs, Drug Evaluation, Geldenhuys Werner J, Humans, Preclinical, Receptors, Serotonin – Pharmacodynamics, Serotonin – Therapeutic Use, Serotonin/*metabolism, Serotonin/*pharmacology/*therapeutic use, Van der Schyf Cornelis J