Bridged peptide macrocycles as ligands for PDZ domain proteins

[reaction: see text] Conformationally constrained side chain-bridged cyclic peptides were prepared using bis-carboxylic acid ring spacers. These macrocyles were designed to inhibit protein-protein interactions mediated by the third PDZ domain (PDZ3) of a mammalian neuronal protein, PSD-95. Isothermal titration calorimetry (ITC) experiments measured dissociation constants in the low micromolar range. For each compound, the change in entropy (TdeltaS) of binding either is comparable in magnitude to the enthalpy change (deltaH) or is the predominant driving force for association.     

用真比重分离法研究一种飞灰残炭的生成途径和再燃特性

根据煤在足够高温度下，停留时间越长，分子结构的晶格化程度越高，因而反应活性越低，同时真比重也越大的原理，采用重液将一种链条锅炉飞灰中的残炭颗粒富集并按不同真比重分开。各比重组颗粒表面积测定结果符合不同燃尽度焦炭比表面积变化规律；小流化床燃烧实验证明随真比重增大，残炭颗粒本征反应活性降低。说明真比重分离法对于判断飞灰残炭颗粒的形成途径和再燃特性很有效。实验结果表明，链条炉飞灰残炭并不主要由原煤中的细小颗粒形成，由中等和大颗粒原煤形成的飞灰残炭占相当比例；在真比重最大的残炭组中，细小颗粒所拥有的总碳量最大。估计它们是由大颗粒或大块原煤经过炉内高温区、停留时间长，燃烧后期碎裂形成的。     

Thermodynamic analysis of a hydrophobic binding site: probing the PDZ domain with nonproteinogenic peptide ligands

[structure: see text] Isothermal titration calorimetry (ITC) is used to study the thermodynamic consequences of systematically modifying the hydrophobic character of a single residue in a series of protein-binding ligands. By substituting standard and nonproteinogenic aliphatic amino acids for the C-terminal valine of the hexapeptide KKETEV, binding to the third PDZ domain (PDZ3) of the PSD-95 protein is characterized by distinct changes in the Gibbs free energy (DeltaG), enthalpy (DeltaH), and entropy (TDeltaS) parameters. One notable observation is that peptide binding affinity can be improved with a nonstandard residue.     

用真比重分离法研究一种习灰残炭的生成途径和再燃特性

根据煤在足够高温度下，停留时间越长，分子结构的晶格化程度越高，因而反应活性越低，同时真比重也越大的原理，采用重液将一种链条锅炉飞灰中的残炭颗粒富集并按不同真比重分开。各比重组颗粒表面积测定结果符合不同燃尽度灰比表面积变化规律；小流化床燃烧实验证明随真比重增大，残炭颗粒本征反应活性降低。说明真比重分离法对于判断飞灰残炭颗料的形成和再燃特性很有效。