Combinatorial Chemistry & High Throughput Screening - Volume 15, Issue 9, 2012

Due to the numerous challenges in hit identification from random RNAi screening, we have examined current practices with a discovery of a variety of methodologies employed and published in many reports; majority of them, unfortunately, do not address the minimum associated criteria for hit nomination, as this could potentially have been the cause or may well be the explanation as to the lack of confirmation and follow up stu Read More

Silica nanoparticles were synthesized from rice husk ash at room temperature by sonochemical method. The feeding rate of percipiteting agent and time of sonication were investigated. The nanostructure of the synthesized powder was realized by the FE-SEM photomicrograph, FT-IR spectroscopy, XRD and XRF analyses. These analytical observations have revealed that the nano-sized amorphous silica particles are for Read More

Congenital Insensitivity to Pain (CIP) is a loss of function mutation resulting in a truncated NaV1.7 protein, suggesting a pivotal role in pain signaling and rendering it an important pharmaceutical target for multiple pain conditions. The structural homology in the NaV-channel family makes it challenging to design effective analgesic compounds without inducing for example cardiotoxicity or seizure liabilities. An additional appr Read More

Autophagy is an evolutionally conserved process in cells for cleaning abnormal proteins and organelles in a lysosome dependent manner. Growing studies have shown that defects or induced autophagy contributes to many diseases including aging, neurodegeneration, pathogen infection, and cancer. However, the precise involvement of autophagy in health and disease remains controversial because the theories are built on li Read More

Optimization of the experimental conditions of a novel HPLC method for determination of the impurity levels with ziprasidone (in bulk substance and pharmaceutical dosage forms) was performed with use of Multi-Layer Perceptron (MLP) Artificial Neural Networks (ANN) and Response Surface Plots. The obtained experimental conditions were further used to test a set of 20 reversed-phase columns for their selectivity towards zi Read More

N-alkyl 2-[(2-oxo-2-aryl ethyl)amino] benzamide derivatives have been synthesized in high yields. This involves three-component reaction of isatoic anhydride, primary amines in the presence of 2-bromoacethophenone derivatives. The reaction workup is simple and the products can be easily separated from the reaction mixture.

Virtual screening (VS) is becoming an increasingly important approach for identifying and selecting biologically active molecules against specific pharmaceutically relevant targets. Compared to conventional high throughput screening techniques, in silico screening is fast and inexpensive, and is increasing in popularity in early-stage drug discovery endeavours. This paper reviews and discusses recent trends and developments i Read More

Prediction of promiscuous coupling between G-protein coupling receptors (GPCRs) and various G-proteins is one of the challenges for current research. In this article, a novel method that based on the optimization of the coupling regions is proposed. The cross validation results demonstrate that it can achieve an average accuracy of over 80% for promiscuous coupling prediction. The results further suggest that Read More