Current Drug Targets - Volume 13, Issue 4, 2012

The philosophy of enzymatic catalysis runs earth lives from generation to generation. Slightly structural alteration has allowed various physiological roles of these enzymes that belong to the same class. The substrate specificity distinguishes enzymes from one species to others, forming the base to design drugs specific for human and pesticides specific for pests. This characteristic even benefits the study of organic evolution and Read More

Plants utilized for agricultural productions interact with insects, fungi, and bacteria under the field conditions, affecting thereby their productivity. Since chitin and its derivatives play important roles in the interactions between these organisms, chitin-related enzymes are effective tools or drug targets for controlling the interactions. Thus, the molecular biology, protein chemistry, and enzymology of the chitin-related enzymes ha Read More

Insect pests are responsible for human suffering and financial losses worldwide. New and environmentally safe insecticides are urgently needed to cope with these serious problems. Resistance to current insecticides has resulted in a resurgence of insect pests, and growing concerns about insecticide toxicity to humans discourage the use of insecticides for pest control. The small market for insecticides has hampered insecti Read More

Ladostigil [(N-propargyl-(3R) aminoindan-5yl)-ethyl methyl carbamate] is a dual acetylcholine-butyrylcholineesterase and brain selective monoamine oxidase (MAO)-A and -B inhibitor in vivo (with little or no MAO inhibitory effect in the liver and small intestine), intended for the treatment of dementia co-morbid with extrapyramidal disorders and depression (presently in a Phase IIb clinical study). This suggests th Read More

Acetylcholinesterase (AChE; EC 3.1.1.7) is a primary target of many insecticides including organophosphates (OP) and carbamates (CB). Because AChE is expressed in all invertebrate and vertebrate animals as a key enzyme of the cholinergic system, the toxicity of anticholinesterase insecticides to mammals and non-target species such as beneficial insects has been a great concern. In addition, the intensive use of OP Read More

Chitinases belong to family 18 glycosyl hydrolases that can hydrolyze chitin by cleaving β-1,4-glycosidic bond, and are at key points in the life cycles of organism. The inhibitors of chitinases not only have chemotherapeutic potential against fungi, insects, but also hold anti-inflammatory efficacy against asthma and allergic disease in human. This review summarizes the structural characters of chitinases, the proposed catalytic m Read More

Glycosyl hydrolase family 3, 20 and 84 β-N-acetyl-D-hexosaminidases are widely distributed enzymes that function in energy metabolism, cell proliferation, signal transduction as well as in pathogen-related inflammation and autoimmune diseases. Sharing the same retaining catalytic mechanism, they are distinguished from each other in terms of structure rather than substrate-enzyme transition state. Selective inhibit Read More

The globally rising incidence of Type 1 diabetes (T1D) is no longer restricted to individuals with higher risk genotypes, but is now significantly increasing in a population with lower risk genotypes, likely as the result of environmental factors. In this review, we discuss the potential of advanced glycation end products (AGEs) as environmental contributors to the development of T1D. AGEs are nonenzymatically formed Read More

Breast cancer is the most common non-cutaneous cancer diagnosed in women in the United States and the second most common cause of cancer-related mortality. Over the past two decades, the progress in screening and adjuvant systemic therapies noticeably improved the survival rate. However, traditional methods of characterizing tumors are imprecise and create heterogeneous groupings of tumors and patients. As a Read More

Antipsychotic medicines are the cornerstone pharmacotherapy for patients with psychotic disorders. Early and continuous management of psychoses improves the quality of life, decreases hospitalization and reduces medical costs. However, many psychotic patients are not fully compliant with treatment, and thus they more often experience a relapsing course with a suboptimal clinical outcome. Long-term paren Read More

The bone marrow-derived mesenchymal stem cells or mesenchymal stromal cells (MSCs), with pluripotent differentiation capacity, present an ideal source for cell transplantation or tissue engineering therapies, but exact understanding of regulating mechanism underling MSC proliferation and differentiation remains a critical issue in securing their safe and efficient clinical application. This review outlines current knowledge rega Read More