Mini Reviews in Medicinal Chemistry - Volume 8, Issue 10, 2008

Alzheimer's disease is a complex neurodegenerative disorder with a multifaceted pathogenesis. This fact has long halted the development of effective anti-Alzheimer drugs. Recently, however, basis for a therapeutic strategy based on multi-target-directed ligands has been formed. In this context, dual binding site acetylcholinesterase inhibitors represent a suitable starting point. The rational modification of their structures t Read More

Zonisamide (ZNS), a sulfonamide antiepileptic drug, is indicated as an adjunct therapy for partial seizure disorders with and without secondary generalization. ZNS has a favorable pharmacokinetic profile because of its rapid absorption and high bioavailability. Its activity is related to the blockade of voltage gated sodium and calcium channels, modulation of central dopaminergic, GABAergic, and serotonergic functions, as Read More

Due to the lack of highly selective dopamine D1 or D5 receptor ligands, only few data about activation or blocking of these receptor subtypes are available. The present review collects the available information about molecules with notable affinity for D5 receptor subtype with the purpose to help the researchers to design novel D5 selective ligands, whose discovery may enrich the knowledge about the physiological function o Read More

Different series of fluorescent agonists and antagonists have been developed and characterized for argininevasopressin and oxytocin G protein-coupled receptors. Both cyclic and linear peptide analogs of the neurohypophysial hormones are useful tools for investigating receptor localization and trafficking, analysing receptor structural organization, and developing new receptor-selective high-throughput ligand screening assays.

Ototoxic drugs, intense sound or age-related hearing loss recruit most of the apoptotic pathways, but also several additional enzymatic pathways which eventually result in cell death. Here, we discuss therapeutic strategies based on the inhibition of regulators or executors of apoptotic cell death pathways and on the use of antioxidants.

Recent epidemiological studies have demonstrated that selenium may be an effective chemopreventive and anticancer agent with a broad spectrum against several human cancer cells (prostate, colon, bladder, lung, liver, ovarian, leukemia). A wide range of potential mechanisms have been proposed for the antitumorigenic effects of selenium and these include antiandrogen activity, growth inhibitory effects by regulatio Read More

The purpose of this review is to discuss the cellular and molecular mechanisms of action of flavonoids focusing on carbohydrate metabolism. The beneficial effects of flavonoids have been studied in relation to diabetes mellitus, either through their capacity to avoid glucose absorption or to improve glucose tolerance. Furthermore, flavonoids stimulate glucose uptake in peripheral tissues, regulate the activity and/or expressio Read More

Bacterial resistance to conventional antibiotics poses a challenge medicine to search for alternatives. Cationic antimicrobial peptides (AMPs) are promising for the development of a new class of antibiotics. This review focuses on the use of technetium-99m labeled synthetic AMPs, derived from human natural cationic AMPs, for target-delivery to and in vivo detection of infection sites caused by (drug-resistant) micro-organis Read More

Src family of protein tyrosine kinases (SFKs) play key roles in regulating signal transduction in cellular processes. However, hyper-activated SFKs lead to uncontrolled cell proliferation and cancers. Many SFKs inhibitors were designed and synthesized as anticancer agents in the past several years and great progress has been made. Herein, some predominant examples of SFKs inhibitors recently developed are reviewed and Read More

Due to an oversight incorrect reference [52] was published in the review entitled “Leukotrienes, Antileukotrienes and Asthma”, Mini Reviews in Medicinal Chemistry, June 2008, Vol. 8(7), pp. 647-656 . The correct reference is Kumlin, M. Am. J. Respir. Crit. Care Med., 2000, 161, S102. instead of Pavord, I.D.; Ward, R.; Woltmann, G.; Wardlaw, A.J.; Sheller, J.R.; Dworski, R. Am. J. Respir. Crit. Care Med., 1999, 160, 1905.