The rate of cleavage was observed to be a function of the conformation of the dipeptide promoiety and the strength of the cyclization nucleophile.
Through the careful selection of chemical functionality, a set of GLP ester prodrugs of variable half-lives has been identified. (C) 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 448-456,2010.”
“Systematic structure-activity RepSox price relationship studies of caprazamycin (CPZ) analogs, including the aminoribose-truncated 5 and the uridine-truncated 6, have been carried out. Both 5 and 6 were synthesized efficiently via diazepanone ring construction by intramolecular reductive alkylation of aminoaldehyde derivatives. The antibacterial activity of a range of analogs,
including 5 and 6, against Mycobacteriumosis was evaluated, and it was found that the uridine, the aminoribose, and the fatty acyl side chains are crucial for antibacterial activity. This study would be a guide for designing novel anti-tuberculosis agents based on the 6′-N-alkyl-5′-beta-O-aminoribosyl-glycyluridine class of antibiotics including the CPZs. (C) 2008 Elsevier Ltd. All rights reserved.”
“Extracellular carbonic anhydrase was purified from Pseudomonas fragi isolated from CaCO(3) enriched soil samples. The enzyme is induced in presence of CaCO(3) and is envisaged to play an important role in bicarbonate ion transport. The 75% ammonium sulphate dialysate was purified by single step affinity Gamma-secretase inhibitor chromatography with
86% yield. It is a trimeric protein having a subunit molecular weight of 31.0 kDa and was stable at pH 7.0-8.5 and temperature 35-45 degrees C. Lead, mercury and EDTA had an inhibitory effect on CA activity, whereas zinc, iron and cadmium increased it. The presence of esterase activity along with IC(50) of sulphonamides and anionic inhibitors indicated that CA from P. fragi belonged to a-class. The CA stability in presence of different Ro 61-8048 salts, as well as in alkaline pH and high temperature makes it a potential candidate to be exploited for biomimetic CO(2) sequestration. (C) 2009 Elsevier Ltd. All rights reserved.”
“Tracking eye-movements provides easy access to cognitive processes involved in visual and sensorimotor processing. More recently, the underlying neural mechanisms have been examined by combining eye-tracking and functional neuroimaging methods. Apart from extracting visual information, gaze also serves important functions in social interactions. As a deictic cue, gaze can be used to direct the attention of another person to an object. Conversely, by following other persons’ gaze we gain access to their attentional focus, which is essential for understanding their mental states. Social gaze has therefore been studied extensively to understand the social brain.