Amphiphilic stilbene derivatives attenuate the neurotoxicity of soluble Aβ oligomers by controlling their interactions with cell membranes.

The misfolded proteins or polypeptides commonly observed in neurodegenerative diseases, including Alzheimer's disease (AD), are promising drug targets for developing therapeutic agents. To target the amyloid-β (Aβ) peptide plaques and oligomers, the hallmarks of AD, we have developed twelve amphiphilic small molecules with different hydrophobic and hydrophilic fragments. fluorescence binding assays demonstrate that these amphiphilic compounds show high binding affinity to both Aβ plaques and oligomers, and six of them exhibit selective binding toward Aβ oligomers.

Turn-on fluorescent sensors for Cu-rich amyloid β peptide aggregates.

Protein misfolding and metal dishomeostasis are two key pathological factors of Alzheimer's disease. Previous studies have shown that Cu-mediated amyloid β (Aβ) peptide aggregation leads to the formation of neurotoxic Aβ oligomers. Herein, we report a series of picolinic acid-based Cu-activatable sensors, which can be used for the fluorescence imaging of Cu-rich Aβ aggregates.

A five-coordinate Ni(I) complex supported by 1,4,7-triisopropyl-1,4,7-triazacyclononane.

An isolated Ni(II)-nitrosyl complex supported by the bulky tridentate 1,4,7-triisopropyl-1,4,7-triazacyclononane (iPrTACN) ligand was obtained from the reaction of a Ni(II) dimethyl complex with NOPF, suggesting the formation of a Ni(I) species that reacts with the resulting NO product. Use of a π-acceptor ancillary isocyanide ligand led to the isolation and characterization of an uncommon 5-coordinate Ni(I) complex supported by the iPrTACN ligand and -butylisocyanide.

Electrocatalytic H evolution promoted by a bioinspired (N2S2)Ni(II) complex.

A bioinspired (N2S2)Ni(II) electrocatalyst is reported that produces H from CFCOH with a turnover frequency (TOF) of ∼1250 s at low acid concentration (<0.043 M) in MeCN. A mechanism for the H production by this electrocatalyst is proposed and its activity is benchmarked against those of other reported molecular Ni H evolution electrocatalysts.

Metal-chelating benzothiazole multifunctional compounds for the modulation and Cu PET imaging of Aβ aggregation.

While Alzheimer's Disease (AD) is the most common neurodegenerative disease, there is still a dearth of efficient therapeutic and diagnostic agents for this disorder. Reported herein are a series of new multifunctional compounds (MFCs) with appreciable affinity for amyloid aggregates that can be potentially used for both the modulation of Aβ aggregation and its toxicity, as well as positron emission tomography (PET) imaging of Aβ aggregates. Firstly, among the six compounds tested is shown to be capable to reroute the toxic Cu-mediated Aβ oligomerization into the formation of less toxic amyloid fibrils.

Insights into the Electronic Structure of Ozone and Sulfur Dioxide from Generalized Valence Bond Theory: Bonding in O3 and SO2.

There are many well-known differences in the physical and chemical properties of ozone (O3) and sulfur dioxide (SO2). O3 has longer and weaker bonds than O2, whereas SO2 has shorter and stronger bonds than SO. The O-O2 bond is dramatically weaker than the O-SO bond, and the singlet-triplet gap in SO2 is more than double that in O3.

Synthesis of Polyglycerol, Porphyrin-Cored Dendrimers Using Click Chemistry.

Polyglycerol, porphyrin-cored dendrimers were synthesized by the click reaction of azide-cored polyglycerol dendrons and octaazidoporphyrin . The dendrons were synthesized divergently starting with TBDPS protected allyl alcohol . Two, three and four cycles of dihydroxylation-allyl etherification gave dendrons [G-2.

Development of a novel strategy for engineering high-affinity proteins by yeast display.

Yeast display provides a system for engineering high-affinity proteins using a fluorescent-labeled ligand and fluorescence-activated cell sorting (FACS). In cases where it is difficult to obtain purified ligands, or to access FACS instrumentation, an alternative selection strategy would be useful. Here we show that yeast expressing high-affinity proteins against a mammalian cell surface ligand could be rapidly selected by density centrifugation.