Browse Items · NEOMED Bibliography Database

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

Novel multifunctional anti-Alzheimer drugs with various CNS neurotransmitter targets and neuroprotective moieties.

Traditionally, drug design programs are focused on optimizing the specificity of lead compounds against a carefully selected drug target. Disappointingly, this approach to discover a "magic bullet" drug has not met with the expected success for CNS…

Novel thiazolidinedione mitoNEET ligand-1 acutely improves cardiac stem cell survival under oxidative stress.

Ischemic heart disease (IHD) is a leading cause of death worldwide, and regenerative therapies through exogenous stem cell delivery hold promising potential. One limitation of such therapies is the vulnerability of stem cells to the oxidative…

Osteoactivin inhibition of osteoclastogenesis is mediated through CD44-ERK signaling.

Osteoactivin is a heavily glycosylated protein shown to have a role in bone remodeling. Previous studies from our lab have shown that mutation in Osteoactivin enhances osteoclast differentiation but inhibits their function. To date, a classical…

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

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.…

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

Polycyclic compounds: ideal drug scaffolds for the design of multiple mechanism drugs?

Recently there has been a resurging interest in developing multi-functional drugs to treat diseases with complex pathological mechanisms. Such drug molecules simultaneously target multiple etiologies that have been found to be important modulators in…

Tags: *Drug Design, 2009, Adamantane/chemistry/pharmacology, Animals, Central Nervous System Diseases/*drug therapy, Geldenhuys Werner J, Humans, Molecular Structure, Neuroprotective Agents/chemistry/*pharmacology/therapeutic use, Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, Polycyclic Compounds/*chemistry/pharmacology/therapeutic use, Psychotropic Drugs/chemistry/*pharmacology/therapeutic use, Quantitative Structure-Activity Relationship, Van der Schyf Cornelis J

Primary cilia regulates the directional migration and barrier integrity of endothelial cells through the modulation of hsp27 dependent actin cytoskeletal organization.

Cilia are mechanosensing organelles that communicate extracellular signals into intracellular responses. Altered functions of primary cilia play a key role in the development of various diseases including polycystic kidney disease. Here, we show that…

Role of serotonin in Alzheimer's disease: a new therapeutic target?

Mounting evidence accumulated over the past few years indicates that the neurotransmitter serotonin plays a significant role in cognition. As a drug target, serotonin receptors have received notable attention due in particular to the role of several…

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

Screening and identification of novel compounds with potential anti-proliferative effects on gallium-resistant lung cancer through an AXL kinase pathway.

The clinical application of gallium compounds as anticancer agents is hampered by development of resistance. As a potential strategy to overcome the limitation, eight series of compounds were identified through virtual screening of AXL kinase…

Tags: 2014, Alazizi Adnan, Antineoplastic Agents/chemical synthesis/chemistry/*pharmacology, Antitumor, AXL, Bioorganic & medicinal chemistry letters, Cell Line, Cell Proliferation/drug effects, Cell Survival/drug effects, Department of Pharmaceutical Sciences, Dose-Response Relationship, Drug, Drug Resistance, Drug Screening Assays, Gallium, Gallium-resistance, Gallium/pharmacology, Geldenhuys Werner J, Humans, Lin Li, Liva Sophia, Lung cancer, Lung Neoplasms/drug therapy/*enzymology/*pathology, Molecular Structure, Naphthalenes/chemistry/*pharmacology, NEOMED College of Pharmacy, Neoplasm/drug effects, Oyewumi Moses O, Proto-Oncogene Proteins/*antagonists & inhibitors/metabolism, Pyrazoles/chemistry/*pharmacology, Quinolines/chemistry/*pharmacology, Receptor Protein-Tyrosine Kinases/*antagonists & inhibitors/metabolism, Structure-Activity Relationship, Tetrazoles/chemistry/*pharmacology, Tumor, Virtual screening

Serotonin 5-HT6 receptor antagonists for the treatment of Alzheimer's disease.

Recently, the serotonin 5-HT(6) receptor has been identified as a drug target for attenuating cognitive deficits associated with Alzheimer's disease (AD). Additionally, this receptor may also play a role in schizophrenia, anxiety and obesity. Reports…

Tags: 2008, Alzheimer Disease/*drug therapy, Current topics in medicinal chemistry, Geldenhuys Werner J, Humans, Molecular Structure, Nootropic Agents/chemistry/*therapeutic use, Receptors, Serotonin Antagonists/chemistry/*therapeutic use, Serotonin/*metabolism, Van der Schyf Cornelis J

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…

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…

Structure-activity relationships of pentacycloundecylamines at the

Prompted by our interest in neuroprotective agents with multiple mechanisms of action, we assessed the structure-activity relationship of a series of pentacycloundecylamine derivatives previously shown to have both L-type calcium channel blocking…

Structure-based design of a thiazolidinedione which targets the mitochondrial protein mitoNEET.

Several PPAR-gamma agonists containing a thiazolidinedione moiety (referred to as glitazones) have been proposed to be neuroprotective and appear to alter mitochondrial function. Recently, a search for mitochondrial proteins that bind pioglitazone…

Synthesis and Biological Evaluation of Pentacycloundecylamines and Triquinylamines as Voltage-Gated Calcium Channel Blockers.

Preclinical studies for neurodegenerative diseases have shown a multi-targeted approach to be successful in the treatment of these complex disorders with several pathoetiological pathways. Polycyclic compounds, such as NGP1-01 (7a), have demonstrated…

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

The emergence of designed multiple ligands for neurodegenerative disorders.

The incidence of neurodegenerative diseases has seen a constant increase in the global population, and is likely to be the result of extended life expectancy brought about by better health care. Despite this increase in the incidence of…

Tags: *Drug Design, *Ligands, 2011, Amyloid beta-Peptides/metabolism, Antiparkinson Agents/therapeutic use, Carroll Richard T, Clinical Trials as Topic, Geldenhuys Werner J, Humans, Molecular Structure, Neurodegenerative Diseases/*drug therapy, Neuroprotective Agents/*therapeutic use, Progress in neurobiology, Van der Schyf Cornelis J, Youdim Moussa B H

The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease.

The serotonin 6 receptor is attracting attention as an etiological contributor in cognition deficits in diseases such as Alzheimer's disease, anxiety/depression and schizophrenia. In this review, we discuss the role of this recently discovered G…

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

Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.

The NK(3) subtype of tachykinin receptor is a G protein-coupled receptor that is a potential therapeutic target for several neurological diseases, including schizophrenia. In this study, we have screened compound databases for novel NK(3) receptor…

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