Current Bioactive Compounds - Volume 9, Issue 1, 2013

p38α MAPK, initially discovered as a target for inhibition of proinflammatory cytokines, has been linked to several CNS disorders in preclinical animal models of CNS diseases, including Alzheimer's disease, Amyotrophic Lateral Sclerosis (ALS), cerebral ischemia and neuropathic pain. Here we describe pharmacophore and similarity-based virtual screenings of more than 18.3 million compounds based on correlation between Read More

Alzheimer's Disease (AD) is the major cause of senile dementia, flawing out 10% of 65 years old population and 50% of 85 years old, globally. The major physiopathology of AD is the deposition of extracellular neuritic plaques in memory related areas of the brain. These plaques are composed of the β-amyloid peptide resulting from the amyloidogenic pathway, that starts with the β-secretase enzyme. BACE-1 (β-secretase 1) is c Read More

An intracellular hallmark of Alzheimer's Disease (AD) is accumulation of hyperphosphorylated tau as paired helical filaments (PHF). A significant advance in understanding the behavior of tau occurred when it was reported that VQIVYK hexapeptide motif is responsible for initiating the process of aggregation. In the last years, a great number of Tau aggregation inhibitors have been developed, including flavonoids. However, the Read More

Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by marked atrophy of cortex and loss of cortical and subcortical neurons. At least two Casein Kinase 1 isoforms have been implicated in the pathogenesis of AD. The ligand-based virtual screening (LBVS) technique uses the information of a set of actives, focusing on the activity of this group of molecules against the desired target. Read More

The role of various structural features, namely basic scaffolds and substituents of small molecule inhibitors of the self-assembly of amyloid-beta (Aβ) peptide, a key process in Alzheimer's disease, is described. The literature analysis in this update extends to the past 5 years, thus the past 15 year period is covered. In addition, while our previous review was limited to anti-fibril agents the current update includes compounds wit Read More

In recent years, considerable research efforts have focused on the role of serotonin in various pathological states, as well as on the identification of the respective serotonin receptors involved. Among serotonin receptors, 5-HT6R is the most recently discovered sub-class. Despite the development of multiple selective ligands, the functional role of this receptor has thus far remained elusive. Available in vitro and in vivo Read More