Drug Design Reviews - Online (Discontinued) - Volume 2, Issue 6, 2005

Recent advances in computation-based protein engineering offer opportunities to introduce or modify the biophysical characteristics of proteins at will. The power of computational design comes from the ability to surpass the combinatorial and physical limitations inherent to laboratory-based high-throughput or trial-and-error methods. As a result, modifications that require significant changes to the amino acid sequence of a p Read More

Tuberculosis (TB) is a growing international health concern and the appearance of multidrug-resistant (MDR) TB has greatly contributed to the increased incidence of TB. Because of the increasing rate of MDR-TB and the high rate of a co-infection with HIV, the development of potent new anti-TB drugs without cross-resistance with known antimycobacterial agents is urgently needed. This article deals with the following area Read More

Genomics projects elucidating the molecular mechanisms of osteoarthritis are complicated by the simultaneous appearance of many different and in part contrary pathways in diseased cartilage. To view a potential function of genes being differentially expressed in osteoarthritis, it has proven extremely useful to investigate their expression patterns in the developing skeleton. There, counteractive processes such as cartilage sy Read More

Memantine is an uncompetitive antagonist with moderate affinity for NMDA receptors, and it demonstrates voltage-dependency and relatively fast on/off receptor kinetics. Agents such as memantine which mimic some of the features of the endogenous antagonist magnesium may be an optimal treatment combining both neuroprotective activity with symptomatological improvement. The latter can be explained on the ba Read More

Mannose-binding lectin (MBL) has attracted great interest as potential target for passive immunotherapy to prevent or reduce infection in a variety of clinical settings. MBL is a multimeric serum lectin that recognises a broad array of pathogens and initiates complement activation independently of antibody. MBL2, the gene encoding MBL, contains several polymorphisms that influence synthesis, assembly or stability of functional Read More

Drug design is a complex process that requires a good command of several disciplines including organic and physical chemistry, biochemistry and metabolism, pharmacology, pharmacodynamics and pharmacokinetics. The process starts with the synthesis of compound libraries and their evaluation toward pharmacological targets for biological activity. This first step allows to identify lead compounds characterized by a des Read More