Current Drug Discovery Technologies - Volume 4, Issue 3, 2007

Chemical breakthrough generates large numbers of prospective drug molecules; the use of ADMET (absorption, distribution, metabolism, excretion and toxicity) properties is flattering progressively more imperative in the drug discovery, assortment, development and promotion processes. Due to the inauspicious ADMET properties a huge amount of molecules in the development stage got failure. In the past years several author Read More

This study sought to assess by computer modeling the interactions between dentinal collagen and primer monomer ligands used to promote bonding of restorations to tooth. Modeling was carried out both by direct and indirect methods to probe interaction mechanisms. Ligands studied in this investigation conformed chemically to methacrylate phosphates of alkane diol, with changes in the number of methylene spacer gr Read More

Thrombocytopenia is a frequent finding in several clinical settings, including bone marrow failure associated with various disorders, immune-mediated thrombocytopenia, and chronic liver diseases. Currently, there is an unmet need for thrombopoietic agents to treat this condition. Thrombopoietin (TPO) is the key cytokine involved in thrombopoiesis, and is the endogenous ligand for the thrombopoietin receptor that Read More

Survivin, a member of the IAP family is an attractive target for cancer treatment due to it's over expression in most cancers and low or no expression in most differentiated adult tissues. Survivin expression is a poor prognostic marker in a number of cancers. Clinical trials are currently underway evaluating anti-sense oligonucleotides against Survivin, immunotherapy using Survivin primed dentritic cells and peptide mimi Read More

Omeprazole (OME), a proton pump inhibitor used to treat acid reflux disease and gastric ulcers presents a formulation challenge due to its rapid decomposition at acidic and neutral pHs. Thus, the aim of this project was to investigate whether interaction with sulfobutylether-β-cyclodextrin (Captisol®-CD) could improve omeprazole stability and provide more efficient oral liquid formulations. A stability-indicating high perform Read More

A series of new C-3 and N1-substituted 4-fluorotryptamides have been prepared and tested for their ability to activate pigment granule aggregation in Xenopus laevis melanophores and bind to the recombinant human MT1 and MT2 melatonin receptor subtypes expressed in NIH 3T3 cells. Planar sp2 geometry at C-3-βC seems to decrease the population of the preferred conformation as it renders 4-fluoroindoles 4b-d weaker anta Read More

Cervical cancer is the second most common malignancy in women worldwide. Two HPV strains, HPV-16 and 18, occur in the 70% of untreated cancers. Expression of viral oncogenes E6 and E7 disrupt the cell cycle by interfering with p53 and p107Rb. It is known that HPV infection is necessary but insufficient to cause malignancy. Furthermore, persistence of HPV-16 or 18 in women does not necessarily result in cance Read More