Current Medicinal Chemistry - Volume 16, Issue 23, 2009

Dipeptidyl peptidase-4 (DPP4) or adenosine deaminase complexing protein 2 (ADCP 2) or T-cell activation antigen CD26 (EC 3.4.14.5.) is a serine exopeptidase belonging to the S9B protein family that cleaves X-proline dipeptides from the N-terminus of polypeptides, such as chemokines, neuropeptides, and peptide hormones. The enzyme is a type II transmembrane glycoprotein, expressed on the surface of many cell typ Read More

Obesity, the excess accumulation of adipose tissue, is one of the most pressing health problems in both the Western world and in developing countries. Adipose tissue growth results from two processes: the increase in number of adipocytes (hyperplasia) that develop from precursor cells, and the growth of individual fat cells (hypertrophy) due to incorporation of triglycerides. Adipogenesis, the process of fat cell developme Read More

The tripeptide, glutathione (γ-glutamylcysteinylglycine) is the primary endogenous free radical scavenger in the human body. When glutathione (GSH) levels are reduced there is an increased potential for cellular oxidative stress, characterised by an increase and accruement of reactive oxygen species (ROS). Oxidative stress has been implicated in the pathology of schizophrenia and bipolar disorder. This could partly be c Read More

Prophylactic approaches against intoxication with organophosphates (OP)/nerve agents can be based on following principles: keeping acetylcholinesterase (AChE), the key enzyme for toxic action of OP/nerve agents, intact (protection of cholinesterases) is a basic requirement for effective prophylaxis. It can be reached using simple chemicals such as reversible inhibitors (preferably carbamates), which are able to i Read More

The Estrogen Receptor (ER) is a ligand activated transcription factor involved in numerous fundamental biological processes as in many important diseases and malfunctions. Since 1998, when the first structure of the ER ligand binding domain complexed with 17 β-estradiol (E2) was released, the number of ERα and ERβ crystallographic structures constantly increased. Nevertheless, little is still known about several fundamenta Read More

Heparins are used in “therapeutic doses” for systemic anticoagulation to treat patients who have confirmed venous thromboembolism, or in “prophylactic doses ”for the prevention of venous thromboembolism : they are generally lower doses and are employed once a day. Structure-function relationships are strongly influenced by the chain length of the molecules. In fact, unfractionated heparin (UFH) binds to ATIII ly Read More

Drug-induced liver injury (DILI) has become a leading cause of severe liver disease in Western countries and therefore poses a major clinical and regulatory challenge. Whereas previously drug-specific pathways leading to initial injury of liver cells were the main focus of mechanistic research and classifications, current concepts see these as initial upstream events and appreciate that subsequent common downstream pathwa Read More

Mesoporous silica particles (MSP) are a new development in nanotechnology. Covalent modification of the surface of the silica is possible both on the internal pore and on the external particle surface. It allows the design of functional nanostructured materials with properties of organic, biological and inorganic components. Research and development are ongoing on the MSP, which have applications in catalysis, drug deli Read More

Traditional Chinese medicine (TCM) contains a large number of herbal medicine and Chinese patent medicine, each of which contains many compounds that may be relevant to the medicine's putative activity. The homonym and synonym are very popular in TCM for its source complex. How to identify species and control the quality of TCM has become urgent, and fingerprint techniques have now been widely used in TC Read More