Current Topics in Medicinal Chemistry - Volume 16, Issue 2, 2016

Multiple Gαi protein-coupled somatostatin receptors (SSTRs) are expressed in human kidney and liver tissues. Also, aberrant cAMP signaling has been shown to play a critical role in cysto-genesis and enlargement of the human kidney and liver. Thus, somatostatin (SST) analogs become potential and promising alternatives in treating human polystic kidney disease (PKD) and polycystic liver disease (PLD) via interacting wit Read More

Morphine and the other alkaloids found in the opium poppy plant still represent the preferred therapeutic tools to treat severe pain in first aid protocols, as well as chronic pain. The use of the opiate alkaloids is accompanied by several unwanted side effects; additionally, some forms of pain are resistant to standard treatments (e.g. neuropathic pain from cancer). For these reasons, there is currently renewed interest in the d Read More

α-Conotoxins (α-Ctxs) are the major class of Ctxs extracted from the venom of marine cone snails. Most α-Ctxs specifically target various subtypes of the nicotinic acetylcholine receptors (nAChRs) with high affinity and potency as antagonists. Therefore, they may be used for the treatment of numerous diseases that nAChRs involved. The subtype affinity and selectivity of α-Ctxs arise from their amino acid composition and geo Read More

Three classes of membrane active peptides (MAPs) are considered in this review: cell penetrating peptides (CPPs); anti-microbial peptides (AMPs), and amyloidal peptides. We summarize both experimental and theoretical results for several representative peptides in these different classes, which highlight commonalities in their interactions with model lipid membranes. While it is clear that no fixed set of mechanisms comple Read More

With the continued rise in antibiotic-resistant bacteria, there is an immense need for the development of new therapeutic agents. Host-defense peptides (HDPs) offer a unique alternative to many of the current approved antibiotics. By targeting the host rather than the pathogen, HDPs offer several benefits over traditional small molecule drug treatments, such as a slower propensity towards resistance, broad-spectrum activi Read More

Defensins are small cationic cysteine rich peptides, which usually contain 18-45 amino acids and possess amphiphilic properties. The term "defensin" was coined as the sequences of rabbit and human leukin/phagocytin molecules were first reported in 1985. Since then, various defensins were isolated and characterized from insects, plants and vertebrates. Using vertebrate defensins as examples, defensins are categorize Read More

With the growing concerns in the scientific and health communities over increasing levels of antibiotic resistance, antimicrobial peptide bacteriocins have emerged as promising alternatives to conventional small molecule antibiotics. A substantial attention has recently focused on the utilization of bacteriocins in food preservation and health safety. Despite the fact that a large number of bacteriocins have been reported, only a few Read More

Melanoma is a highly malignant tumor. Prognoses of melanoma patients are often unsatisfactory due to poor operational and chemoradiational efficacy. Recently, researches for melanoma treatment have found multipeptide vaccines a favorite and possible breakthrough as they are stable in chemical property and easy to be synthesized, have no carcinogenecity and dispense with virus vector. Studies have shown that the im Read More