Current Pharmaceutical Design - Volume 14, Issue 24, 2008

The production of new molecular entities endowed with salutary medicinal properties is a formidable challenge; synthetic molecules that can bind with high sequence specificity to a chosen target in a protein or gene sequence are of major interest in medicinal and biotechnological contexts. The general awareness of the importance of peptides in physiology and pathophysiology has markedly increased over the last few years Read More

Radiometal labeled peptide hormones are promising tools for a new generation of radiopharmaceuticals, because their receptors frequently are overexpressed in many human tumors. Furthermore, peptide hormones are characterized by different advantages for clinical application, such as high tumor-to-background ratios as well as rapid blood clearance. Peptidic tumor targeting agents can be subdivided into the following s Read More

Radiolabelled peptides and monoclonal antibodies are an emerging class of radiopharmaceuticals for imaging inflammation with clinical implications for several chronic inflammatory disorders for diagnosis, therapy decision making and follow up. In the last decades, a number of novel monoclonal antibodies and peptides have been introduced for the treatment of different inflammatory disorders and also labelled Read More

Cell penetrating peptides (CPPs) are a relatively new class of peptides that have the promising capability to cross cell membranes. While details remain to be resolved, various non-receptor-mediated endocytic pathways likely contribute most to the cell penetrating properties of these peptides. CPPs have been used to deliver many different cargos - ranging from radionuclides and other peptides to antibodies and nano Read More

Peptide microarrays have become increasingly accessible in recent years and as a result, more widely applied. Beyond its initial utility in substrate profiling, researchers are adopting peptide microarrays for the comparative screening of many different classes of enzymes, proteins/ proteomes and even living cells. Understanding the basis of peptide interactions at these diverse levels provides an unprecedented window into diss Read More

The peptide nucleic acids (PNAs) constitute a remarkable new class of synthetic nucleic acids analogs, based on peptide-like backbone. This structure gives to PNAs the capacity to hybridize with high affinity and specificity to complementary RNA and DNA sequences, and a great resistance to nucleases and proteinases. Originally conceived as ligands for the study of double stranded DNA, the unique physico-chemi Read More

The early identification of susceptibility to adverse cardiovascular outcomes and risk stratification amongst asymptomatic individuals, as well as amongst those with overt disease continues to be one of the major priorities of clinically-orientated research in the field of atherothrombosis. Available data from epidemiological studies indicate that traditional risk factors do not fully explain the predisposition to cardiovascular d Read More

Over two decades of research on venom peptides derived from cone snails (“conopeptides or conotoxins”) has led to several compounds that have reached human clinical trials, most of them for the treatment of pain. Remarkably, none of the conopeptides in clinical development mediate analgesia through the opioid receptors, underlying the diverse and novel neuropharmacology evolved by Conus snails. These predatory Read More

Many peptides are potent and highly selective blockers or modulators of calcium channel function, and as such are valuable pharmacological tools and potentially valuable leads for the development of human therapeutics. Cone shells and spiders are rich sources of such peptides, although they are also found in scorpions and insects. In this article we compare the amino acid sequences of toxins active against calcium channels a Read More

Throughout millions of years of evolution, nature has supplied various organisms with a massive arsenal of venoms to defend themselves against predators or to hunt prey. These venoms are rich cocktails of diverse bioactive compounds with divergent functions, extremely effective in immobilizing or killing the recipient. In fact, venom peptides from various animals have been shown to specifically act on ion channels a Read More

Animal venoms are rich natural sources of bioactive compounds, including peptide toxins acting on the various types of ion channels, i.e. K+, Na+, Cl- and Ca2+. Among K+ channel-acting toxins, those selective for voltage-gated K+ (Kv) channels are widely represented and have been isolated from the venoms of numerous animal species, such as scorpions, sea anemones, snakes, marine cone snails and spiders. The toxins cha Read More