Synthesis and protein degradation capacity of photoactivated enediynes

[structure: see text] The viability of proteins as targets of thermally and photoactivated enediynes has been confirmed at the molecular level. Model studies using a labeled substrate confirmed the efficacy of atom transfer from diyl radicals produced from enediynes to form captodatively stabilized carbon centered aminoacyl radicals, which then undergo either fragmentation or dimerization. To exploit this finding, a family of enediynes was developed using an intramolecular coupling strategy. Derivatives were prepared and used to target specific proteins, showing good correlation between affinity and photoinduced protein degrading activity. The findings have potential applications in the design of artificial chemical proteases and add to our understanding of the mechanism of action of the clinically important enediyne antitumor antibiotics.     

Tailor-made domain structures on the x- and y-face of lithium niobate crystals

Ferroelectric domains are engineered in lithium niobate crystals by scanning strongly absorbed UV laser light across the crystal surface. Focused UV laser light can not only write, but also erase previously written domains on the non-polar faces of lithium niobate, which allows tailoring of domain patterns. Such domain pattern was generated and afterward investigated by piezoresponse force microscopy and hydrofluoric acid etching. It was found that domains with dimensions down to 2 μm can be engineered, which was ～30 % of the focus beam diameter (7 μm) used for writing the domains. Additionally, it was found that an unique domain depth profile can be formed, which is inclined to the crystallographic axes and can be described as ‘half-crescent-shaped’.     

Ti-free optical waveguiding regions produced by LiNbO3 etching during the indiffusion of Ti

We report the observation, first to our knowledge, of optical waveguiding found beneath trenches etched in congruent lithium niobate using the recently reported etching during the indiffusion of Ti process. Observations of multi-mode and single-mode guiding at visible wavelengths and preliminary measurements of waveguide insertion losses are presented.     

A Practical method for preparation of β-glycosides of N-acetylglucosamine

A mild and efficient method for preparation of GlcNAc derivatives by reaction of glycosyl acceptors with glycosyl oxazolines has been developed. The key feature is use of Yb(OTf)₃ as promoter, requiring moderate reaction times and equivalence stoichiometry. We anticipate application in the preparation of a wide range of derivatives of this biologically important class of building blocks.     

The photocurrent response of human cones is fast and monophasic

Background  

The precise form of the light response of human cone photoreceptors in vivo has not been established with certainty. To investigate the response shape we compare the predictions of a recent model of transduction in primate cone photoreceptors with measurements extracted from human cones using the paired-flash electroretinogram method. As a check, we also compare the predictions with previous single-cell measurements of ground squirrel cone responses.     

Multi-component assembly of the bicyclic core associated with the tRNA synthetase inhibitors SB-203207 and SB-203208. Application to the synthesis of biologically active analogues

The ketone (+/-)-5, which embodies the bicyclic core associated with the title tRNA synthetase inhibitors 1 and 2, has been prepared via a three-component coupling reaction involving 2-(hydroxymethyl)cyclopent-2-enone (15), methylamine (6) and propiolamide (10); straightforward elaboration of the readily derived acetates (-)-21 and (+)-21 has provided the biologically active analogues 23 and 24, respectively, of the title compounds.