Current Medicinal Chemistry - Volume 21, Issue 10, 2014

Phosphodiesterases (PDEs), as key regulators of cyclic nucleotides, and their inhibitors have been emerged as new pharmacological targets and promising drug candidates for many diseases, including central nervous system pathologies. The high level of PDE10A expression in the striatal medium spiny neurons suggests a prominent function role for the isoenzyme. Basal ganglia dysfunction is associated with neuropsychiat Read More

The use of synthetic peptides as HIV-1 inhibitors has been the object of research over recent years. A large number of peptides that affect different stages of the HIV-1 life cycle have been and continue to be studied due to their possible clinical application in the fight against HIV-1 infection. The main advantages of synthetic peptides as therapeutic agents are their low systemic toxicity, the fact that structural modifications can be Read More

Traumatic brain injury (TBI) is a major healthcare concern, constituting a major cause of death and disability throughout the world. Among the factors leading to TBI outcome are biochemical cascades which occur in response to primary and secondary injury. These mechanisms generate oxidative stress, an imbalance between oxidant and antioxidant agents that can result in neural dysfunction and death. After TBI, an ass Read More

Neuritin (also known as candidate plasticity gene 15, cpg15) is an activity-induced glycosylphosphatidylinositol- anchored axonal protein and is mainly expressed in the brain. Neuritin mRNA expression is modulated by neurotrophic factors, synaptic activity, hormones, sensory experience, and electroconvulsive seizure therapy. Neuritin has several effects in the nervous system, such as promoting neurite outgrowth, modulat Read More

It has been a long story of the development of anticancer metallopharmaceuticals since the identification of cisplatin. Advances in metallodrugs discovery during the past 40 years have made it an ever-growing area of research in medicinal inorganic chemistry. Meanwhile, the emerging of N-heterocyclic carbene (NHC) chemistry has stimulated the newly burgeoning interests in the biomedical applications of metal-NHC compl Read More

Human forkhead box class O (FoxO) transcription factors, activated in response to a wide range of external stimuli, like growth factors, insulin, nutrient levels and oxidative stress, are able to control several specific geneexpression programs. Besides their clear implication in metabolic processes, they appear to play a relevant role in tumour suppression by upregulation of genes involved in cell cycle arrest or apoptosis. Read More

Low molecular weight oligonucleotides have been discovered to have potential use for gene therapy by selectively inhibiting the expression of certain genes. Chemical conjugation of functional peptides to oligonucleotides can introduce desired properties to the oligonucleotides, such as cell-specific delivery, cellular uptake efficiency, and/or intracellular distribution. In this paper, targeting peptides are conjugated to antisense Read More

Epidemiological evidence has linked the development and progression of several cancers including melanoma with obesity. However, whether obesity impinges on responses of cancer cells to treatment remains less understood. Here we report that human adipocytes contribute to resistance of melanoma cells to various therapeutic agents. Exposure to media from adipocyte cultures (adipocyte media) increased cel Read More