Current Drug Discovery Technologies - Volume 13, Issue 1, 2016

Protein kinases are an important class of enzymes and drug targets. New opportunities to discover medicines for neglected diseases can be leveraged by the extensive kinase tools and knowledge created in targeting human kinases. A valuable tool for kinase drug discovery is an enzyme assay that measures catalytic function. The functional assay can be used to identify inhibitors, estimate affinity, characterize molecular Read More

Antigens of infectious agents share amino acid sequences with human proteins. Such a peptide matching may lead to autoimmunity through crossreactivity phenomena following pathogen infection and/or immunotherapeutic approaches. In this framework, we analyzed as a model the primary sequence of human cytomegalovirus (HCMV) glycoprotein B (gB) protein and searched for viral peptide sequences shared with Read More

Background: G2013 molecule is a novel non-steroidal anti-inflammatory agent with immunosuppressive property, which was investigated on determinants relative to the oxidative stress in animal model. Materials and Methods: The Sprague-Dawley rats were used for evaluating properties of G2013 on some oxidative stress enzymes including: Myeloperoxidase (MPO), Glutathione peroxidase (GPX1), mitochondrial Superoxid Read More

Background: Parthenolide (PN) has been reported to inhibit proliferation and induces apoptosis in a variety of cancer cells with different mechanisms. Nevertheless, to the best of our knowledge, its relative anticancer activity at lower doses has not been reported in HaCaT immortalized keratinocytes and A375 melanoma cells. Objective and Method: The present study aimed to investigate the relative antica Read More

Prompted by the ineptness of the currently used non-steroidal antiinflammatory drugs (NSAIDs) to control gastric mucosal and renal adverse reactions, several ester prodrugs of ketoprofen were synthesized and characterized by IR, 1H NMR and mass spectral data. Physicochemical properties such as aqueous solubility, octanol-water partition coefficient log P, chemical stability and enzymatic hydrolysis of the synthes Read More