background: protozoa related to trypanosome family including leishmania , synthesize enzymes to escape from drug therapy. one of them is ptr1 that its enzymatic activity is similar to dihydrofolate reductase (dhfr). dihydrofolate reductase - thymidylate synthase has a major role in dna synthesis, if it is inhibited, the result would be the death of parasite. since ptr1 activity is similar to dh...

Purpose: Despite their preclinical promise, previous MEK inhibitors have shown little benefit for patients. This likely reflects the narrow therapeutic window for MEK inhibitors due to the essential role of the P42/44 MAPK pathway in many nontumor tissues. GSK1120212 is a potent and selective allosteric inhibitor of theMEK1 andMEK2 (MEK1/2) enzymes with promising antitumor activity in a phase I...

PURPOSE Despite their preclinical promise, previous MEK inhibitors have shown little benefit for patients. This likely reflects the narrow therapeutic window for MEK inhibitors due to the essential role of the P42/44 MAPK pathway in many nontumor tissues. GSK1120212 is a potent and selective allosteric inhibitor of the MEK1 and MEK2 (MEK1/2) enzymes with promising antitumor activity in a phase ...

The study of human protoporphyrinogen oxidase (hPPO) inhibition can contribute significantly to a better understanding some pathogeneses (e.g., porphyria, herbicide exposure) and the development anticancer agents. Therefore, we prepared new potential inhibitors with Schiff base structural motifs (2-hydroxybenzaldehyde-based bases 9–13 chromanone derivatives 17–19) as structurally relevant PPO h...

introduction: non-enzymatic glycosylation of proteins which is the major cause of diabetic complications, cardiovascular diseases retinopathy, nephropathy and neuropathy can effectively be inhibted by antioxidants. materials and method: the antioxidant effects of several flavonoids, such as rutin, kaempferol, quercetin, apigenin, naringin, morin and biochanin a were studied  on glycosylation of...

Achievement of appropriate precision is a major challenge for the clinical laboratory, particularly in specialized fields such as enzymology and immunochemistry. Especially in immunochemistry, where accuracy can only poorly be checked because of a lack of reference methods and a multitude of detectable epitopes, precision remains an important index of quality. In immunochemical methods there ar...

11 HASSID and ABRAHAM, Chemical Procedures for Analysis of Polysaccharides, in: Methods of Enzymology, Vol . 3, Academic Press, New York 1957. 12 F. W. FALES, J. biol. Chemistry 193, 113 [1951] . 13 N. NELSON and M. SOMOGYI, as cited in Practical clinical B i o c h e m i s t r y , H . V A R L E Y , 4 t h e d i t i o n , W . HEINEMANN, Medical Book Ltd., London 1967. 14 O. FOLIN and H. Wu, as ci...

This review describes the life of Sir John Cornforth AC CBE FRS, who was awarded the Nobel Prize for Chemistry in 1975. It covers his early life in Australia, his work in Oxford, the National Institute for Medical Research, the Milstead Laboratory of Chemical Enzymology and the University of Sussex, together with the contributions made by his wife, Lady Rita Cornforth.

Single-chain urokinase-type plasminogen activator (scu-PA) possesses enzymatic activity that increases by 2-3 orders of magnitude upon binding to its cellular cofactor, the u-PA receptor (u-PAR), hence activating an enzymatic cascade initially composed of zymogens. The present study demonstrates that plasminogen activator inhibitor type 3 (PAI-3) reversibly inhibits scu-PA in solution, maintain...

DNA glycosylases safeguard the genome by locating and excising a diverse array of aberrant nucleobases created from oxidation, alkylation, and deamination of DNA. Since the discovery 28years ago that these enzymes employ a base flipping mechanism to trap their substrates, six different protein architectures have been identified to perform the same basic task. Work over the past several years ha...