D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A(2) (IIa) with antiinflammatory activity

Few reported inhibitors of secretory phospholipase A(2) enzymes inhibit the IIa human isoform (hnpsPLA(2)-IIa) noncovalently at submicromolar concentrations. Herein, the simple chiral precursor D-tyrosine was derivastised to give a series of potent new inhibitors of hnpsPLA(2)-IIa. A 2.2-Angstrom crystal structure shows an inhibitor bound in the active site of the enzyme, chelated to a Ca2+ ion through carboxylate and amide oxygen atoms, H bonded through an amide NH group to His48, with multiple hydrophobic contacts and a T-shaped aromatic-group-His6 interaction. Antiinflammatory activity is also demonstrated for two compounds administered orally to rats.

Probabilistic world modelling for distributed team planning

This paper describes an application of decoupled probabilistic world modeling to achieve team planning. The research is based on the principle that tbe action selection mechanism of a member in a robot team cm select am effective action if a global world model is available to all team members. In the real world, the sensors are imprecise, and are individual to each robot, hence providing each robot a partial and unique view about the environment. We address this problem by creating a probabilistic global view on each agent by combining the perceptual information from each robot. This probsbilistie view forms the basis for selecting actions to achieve the team goal in a dynamic environment. Experiments have been carried ont to investigate the effectiveness of this principle using custom-built robots for real world performance, in addition, to extensive simulation results. The results show an improvement in team effectiveness when using probabilistic world modeling based on perception sharing for team planning.