Current Medicinal Chemistry - Volume 19, Issue 21, 2012

The high distribution of CB2 receptors in immune cells suggests their important role in the control of inflammation. Growing evidence offers this receptor as an attractive therapeutic target: CB2 selective agonists are able to modulate inflammation without triggering psychotropic effects. This review will summarize the literature on the implication of CB2 in inflammation and CB2 selective agonists with anti-inflammatory activity.

DNA methyltransferases (DNMTs) are a family of epigenetic enzymes for which inhibition is an attractive strategy for the treatment of cancer and other diseases. In synergy with experimental approaches, computational methods are increasingly being used to identify and optimize the activity of inhibitors of DNMTs as well as to rationalize at the molecular level of the mechanism of established inhibitors. Recently, a crystallogra Read More

Camptothecins are still among the most widely prescribed and effective anticancer drugs. Unfortunately, important drawbacks including water insolubility, lactone instability, reversibility of the drug–target interaction, drug resistance and toxicity are responsible for treatment failure and often require suspension of the drug administration itself. In order to overcome such drawbacks, several options in chemical manipulati Read More

Cardio-renal-anemia syndrome is a combination of heart failure, kidney failure, and anemia. Many advanced chronic kidney disease patients have both anemia and chronic heart failure. They have often hyperhomocysteinemia, high dimethylarginine values and low erythropoietin levels. Nephrologists treat advanced chronic kidney disease patients with erythropoiesis stimulating agents to improve anemia, renal and heart Read More

Glaucoma is a chronic progressive optic neuropathy, which can result in visual impairment and blindness. Elevated intraocular pressure (IOP) is currently the only modifiable risk factor. Several recent studies have shown the benefits of IOP reduction in open-angle glaucoma. Therefore, current glaucoma drugs are IOP-lowering substances such as α2-adrenergic agonists, β2-adrenergic antagonists, carbonic anhydrase in Read More

There is evidence that Trigonella foenum-graecum L. (fenugreek), a traditional Chinese herb, and its components are beneficial in the prevention and treatment of diabetes and central nervous system disease. The pharmacological activities of trigonelline, a major alkaloid component of fenugreek, have been more thoroughly evaluated than fenugreek’s other components, especially with regard to diabetes and central ne Read More

The various physiological actions of the neurohormone melatonin are mediated mainly by two G-protein-coupled MT1 and MT2 receptors. The melatoninergic drugs on the market, ramelteon and agomelatine, as well as the most advanced drug candidates under clinical evaluation, tasimelteon and PD-6735, are high-affinity nonselective MT1 and MT2 agonists. However, exploring the exact physiological role of the M Read More

The emergence of bacterial strains with resistance to currently marketed antibacterial agents has spurred interest in the discovery of new antibacterial agents with novel modes of action. One set of potential novel targets are the family of bacterial aminoacyltRNA synthetases (AaRS). Aminoacyl-tRNA synthetases are the enzymes that catalyze the transfer of amino acids to their cognate tRNA. They play a pivotal role in Read More

Diketopiperazines are the smallest cyclic peptides known. 90% of Gram-negative bacteria produce diketopiperazines and they have also been isolated from Gram-positive bacteria, fungi and higher organisms. Biosynthesis of cyclodipeptides can be achieved by dedicated nonribosomal peptide synthetases or by a novel type of synthetases named cyclopeptide synthases. Since the first report in 1924 a large number of bi Read More

Sulfonyl group-containing compounds constitute an important class of therapeutical agents in medicinal chemistry presumably because of the tense chemical structure and functionality of the sulfonyl, which could not only form hydrogen bonding interactions with active site residues of biological targets but also, as incorporated into core ring structure, constrain the side chains and allowed their specific conformations th Read More

Cytochrome P450 (CYP450) has widely been implicated for drug-drug interactions (DDI) in the pharmaceutical industry. Inhibition or induction of this enzyme family has led to withdrawal of multiple drugs from the market leading to major time and financial losses for the pharmaceutical industry. CYP450 plays a prevailing role in the biotransformation of a large number of structurally diverse drugs. Few isoenzymes of the CYP enzy Read More

Hydrogen peroxide (H2O2) has entrapped the abundant concern of numerous researchers in the cutting edge of chemistry, biology and medicine since it is thought to be associated with various biological and pathological conditions. Fluorescent probes are the promising tools for the detection and understanding of the physiological roles of H2O2, considering that they are able to provide spatial and temporal information about t Read More

The antimicrobial and chemotherapeutic activities of a silver(I) glutamic acid complex with the synergistic concomitant generation of reactive oxygen species (ROS) were investigated here. The ROS generation system employed was via Fenton chemistry. The antimicrobial and chemotherapeutic activities were investigated on Staphylococcus aureus ATCC 43300 and Escherichia coli bacteria, and Vero and MCF-7 Read More

Recently, selected polyphenols were reported to exert proprotein convertase (PC) inhibitory activities on in vitro cleavage of a fluorogenic peptide substrate and it was concluded that this anti-protease activity might be responsible for the reported anti-cancer properties of these polyphenols. This prompted investigations to identify PC inhibiting polyphenols that could affect IGF-1R-mediated tumorigenesis since pro-IGF-1R is bi Read More