Medicinal Chemistry Reviews - Online (Discontinued) - Volume 2, Issue 4, 2005

Bifunctional Penicillin-Binding Proteins (PBPs) catalyze bacterial peptidoglycan synthesis; their glycosyltransferase (GT) activity carries out glycan chain polymerization and the transpeptidase domain allows stem peptide crosslinking. The latter domain is the target of β-lactam antibiotics, while the glycosyltransfer region is a potential target for the design of novel antibacterial drugs. This review aims at presenting recent advanc Read More

Cancer is characterized by cell cycle deregulation, progressive loss of cell differentiation and uncontrolled growth. Since cancer cells are particularly sensitive to oxidative stress, we took advantage of this poor antioxidant status to develop an experimental approach to selectively expose cancer cells to an oxidant insult induced by the association of vitamins C and K3 (CK3). The results we obtained reinforce the ma Read More

Cysteine proteases are widespread in nature. Their implication in numerous vital processes and pathologies make them highly attractive targets for drug design. The proper functioning and regulation of activity of cysteine proteases is a delicate balance of many factors, one of the most crucial being the protease inhibitors. In this review the basic principles of physiological protease inhibition by protein inhibitors are discussed wit Read More

An increase in the frequency of allergic diseases during last several decades has been linked to improved hygienic conditions. This review focuses on a few recent findings in this extensive field. Accumulative data suggest that a spectrum of CD4+T cells, including type 3 T helper cells, T regulatory 1 cells, CD25+T cells, and natural killer T cells, has a crucial role in the regulation of allergic inflammation. Farming environm Read More

Less than a decade ago, the ability to generate proteins with unnatural modifications was a Herculean task available only to specialty labs. Recent advances make it possible to generate reasonable quantities of protein with unnatural amino acids both in vitro and in vivo . The combination of solid-phase peptide synthesis and enzymatic or chemoselective ligation now permits construction of entirely-synthetic proteins as large Read More

Human telomeres are several kilobases of repeated (TTAGGG)n sequences at the ends of chromosomes, a short fragment of which is lost with each cell division. This shortening serves as a "mitotic clock", limiting the number of divisions which normal somatic cells can undergo. Cells undergoing continuous division need some method of bypassing this clock. One such method is the expression of telomerase, a ribonucleoprotein th Read More

Proteoglycans (PG) are complex macromolecules which consist structurally of a core protein and associated glycosaminoglycan (GAG) chains. The different GAG chains of PG, heparan sulfate/heparin, dermatan/chondroitin sulfate, keratan sulfate are synthesized as polymers of repeating disaccharide units. The structures of GAG chains are highly diverse and confer to them a variety of structures and functions. Without co Read More

Amyloid beta (Aβ) protein in Alzheimer's disease and scrapie prion protein (PrPsc) in Scrapie is the key component of amyloid plaques in brain whereas stefin B is an intracellular cysteine proteinase inhibitor, broadly distributed in different tissue and recently reported to form amyloid fibrils in vitro. By reducing the pH to around 4.6, the native conformation of both polypeptides is changed into less ordered, metastable interm Read More