Browse Items · NEOMED Bibliography Database

Identification of small molecules that bind to the mitochondrial protein mitoNEET.

MitoNEET (CISD1) is a 2Fe-2S iron-sulfur cluster protein belonging to the zinc-finger protein family. Recently mitoNEET has been shown to be a major role player in the mitochondrial function associated with metabolic type diseases such as obesity and…

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

Development and validation of an LC-MS/MS method for determination of the L-type voltage-gated calcium channel/NMDA receptor antagonist NGP1-01 in mouse serum.

NGP1-01 (8-benzylamino-8,11-oxapentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecane) is a heterocyclic cage compound with multifunctional calcium channel blocking activity that has been demonstrated to be neuroprotective in several neurodegenerative…

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…

Generation and characterization of ATP analog-specific protein kinase Cdelta.

To better study the role of PKCdelta in normal function and disease, we developed an ATP analog-specific (AS) PKCdelta that is sensitive to specific kinase inhibitors and can be used to identify PKCdelta substrates. AS PKCdelta showed nearly 200…

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…

Alteration of hepatic proinflammatory cytokines is involved in the resveratrol-mediated chemoprevention of chemically-induced hepatocarcinogenesis.

Hepatocellular carcinoma (HCC), one of the most common cancers in the world, is a leading cause of cancerrelated mortality. HCC develops most frequently in the background of oxidative stress and chronic hepatic inflammation due to viral infections,…

Engineering triiodothyronine (T3) nanoparticle for use in ischemic brain stroke.

A potential means of pharmacological management of ischemic stroke is rapid intervention using potent neuroprotective agents. Thyroid hormone (T3) has been shown to protect against ischemic damage in middle cerebral artery occlusion (MCAO) model of…

Tags: 2013, Blood-brain barrier, Brain stroke, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Drug delivery and translational research, Geldenhuys Werner J, Mdzinarishvili Alexander, Nanoparticles, NEOMED College of Graduate Studies, NEOMED College of Pharmacy, Neuroprotection, Sadana Prabodh, Sutariya Vijaykumar, Talasila Phani K, Thyroid hormone

Novel compounds that target lipoprotein lipase and mediate growth arrest in acute lymphoblastic leukemia.

Over the past decade, the therapeutic strategies employed to treat B-precursor acute lymphoblastic leukemia (ALL) have been progressively successful in treating the disease. Unfortunately, the treatment associated dyslipidemia, either acute or…

Tags: *Acute lymphoblastic leukemia, *Cancer, *Co-culture model, *Lipids, *Lipoprotein lipase, *Metabolism, 2018, Amides/chemistry/metabolism/pharmacology, Antineoplastic Agents/*chemistry/metabolism/pharmacology, Binding Sites, Bioorganic & medicinal chemistry letters, Cell Line, Cell Proliferation/drug effects, Coculture Techniques, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Dyslipidemias/complications/metabolism/pathology, Geldenhuys Werner J, Gibson Laura F, Humans, Lipoprotein Lipase/antagonists & inhibitors/*metabolism, Mesenchymal Stem Cells/cytology/metabolism, Molecular Docking Simulation, Nair Rajesh R, NEOMED College of Graduate Studies, NEOMED College of Pharmacy, Piktel Debbie, Precursor Cell Lymphoblastic Leukemia-Lymphoma/complications/metabolism/pathology, Protein Binding, Protein Structure, Sadana Prabodh, Serum Albumin/chemistry/metabolism, Tertiary, Tumor

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

A quantitative LC-MS/MS method for determination of thiazolidinedione mitoNEET ligand NL-1 in mouse serum suitable for pharmacokinetic studies.

Thiazolidinedione (TZD) compounds have shown promise as antidiabetic, antibiotics, antifungal and neuroprotective agents. The mitochondrial effect of a novel mitoNEET ligand, NL-1…

Tags: %CV, %RE, 1-Methyl-4-phenyl-1, 2, 2014, 3, 3-thiazolidine-2, 4-dione, 5-[3, 5-[4-hydroxy-3, 5-di-tert-butyl-4-hydroxyphenyl)methyl]-1, 5-dimethyl-phenyl)methyl]thiazolidine-2, 6-tetrahydropyridine, Anderson David J, Animals, Carroll Richard T, Carry-over, Chromatography, Department of Internal Medicine, Geldenhuys Werner J, High Pressure Liquid/*methods, internal standard, IS, Jogiraju Harini, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, LC-MS/MS, Limit of Detection, Lin Li, LLOQ, lower limit of quantification, Methanol, Mice, mitoNEET, Mouse serum, MPTP, MRM, multiple reaction monitoring, NEOMED College of Medicine, NL-1, NL-2, Pedada Kiran K, percent coefficient of variation, peroxisome proliferator activated receptor-gamma, pharmacokinetic, PK, PPAR-gamma, QC, Quality Control, relative error, relative matrix effect, RME, SD, standard deviation, Tandem Mass Spectrometry/*methods, thiazolidinedione, Thiazolidinedione (TZD), Thiazolidinediones/*blood, TZD, Zhou Xiang

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…

Development and validation of a novel RP-HPLC method for the analysis of reduced glutathione.

The objective of this study was the development, optimization, and validation of a novel reverse-phase high-pressure liquid chromatography (RP-HPLC) method for the quantification of reduced glutathione in pharmaceutical formulations utilizing simple…

Tags: 2012, Chromatography, Geldenhuys Werner J, Glutathione/*analysis, High Pressure Liquid/*methods, Journal of chromatographic science, Limit of Detection, Linear Models, Nanoparticles/chemistry, Pharmaceutical Preparations/chemistry, Reproducibility of Results, Reverse-Phase/*methods, Spectrophotometry, Sutariya Vijaykumar, Ultraviolet, Wehrung Daniel

Multimodal drugs and their future for Alzheimer's and Parkinson's disease.

This chapter discusses the rationale for developing multimodal or multifunctional drugs (also called designed multiple ligands or DMLs) aimed at disease-modifying treatment strategies for the most common neurodegenerative diseases Alzheimer's and…

Tags: 2011, Alzheimer Disease/*drug therapy/*enzymology/prevention & control, Animals, Combined Modality Therapy/*methods, Forecasting, Geldenhuys Werner J, Humans, International review of neurobiology, Monoamine Oxidase Inhibitors/*pharmacology/therapeutic use, Parkinson Disease/*drug therapy/*enzymology/prevention & control, Van der Schyf Cornelis J

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

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…

Identification of Novel Agents for the Treatment of Brain Metastases of Breast Cancer.

BACKGROUND: Brain cancer from metastasized breast cancer has a high mortality rate in women. The treatment of lesions is hampered in large part by the blood-brain barrier (BBB), which prevents adequate distribution of anti-cancer compounds to brain…

Antitumor efficacy and tolerability of systemically administered gallium acetylacetonate-loaded gelucire-stabilized nanoparticles.

The widespread clinical success with most gallium compounds in cancer therapy is markedly hampered by lack of tumor specific accumulation, poor tumor permeability and undesirable toxicity to healthy tissues. The aim of this work was to investigate…

Biocompatibility, efficacy and biodistribution of Gelucire-stabilized nanoparticles engineered for docetaxel delivery.

Docetaxel is a potent anticancer agent that will benefit greatly from alternative delivery systems that can overcome several reported adverse effects due to the drug itself and/or the solvent system in the current clinical formulation. In this…

Tags: *Biocompatible Materials, *Nanoparticles, 2012, Animals, Antineoplastic Agents/*administration & dosage/pharmacokinetics/pharmacology, Bi Lipeng, Department of Pharmaceutical Sciences, Docetaxel, Geldenhuys Werner J, Journal of nanoscience and nanotechnology, Macrophage Activation/drug effects, NEOMED College of Pharmacy, Oyewumi Moses O, Platelet Aggregation/drug effects, Rats, Reactive Oxygen Species/metabolism, Taxoids/*administration & dosage/pharmacokinetics/pharmacology, Tissue Distribution, Wehrung Daniel

Effects of gelucire content on stability, macrophage interaction and blood circulation of nanoparticles engineered from nanoemulsions.

The main objective of the study is to investigate the efficacy of Gelucire 44/14 (gelucire) in facilitating formation of cetyl alcohol (CA)-based nanoparticle (NP) and to assess the effects on key NP properties and functions. NPs from oil-in-water…

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…

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