New source of evidence: Explosive traces in hair

This study examines the sorption of explosives [TNT, RDX, PETN, TATP] to hair during exposure to their vapors. In each test, three colors of hair were simultaneously exposed to explosive vapor. Washing, extracting, and gas Chromatographic quantification protocols were developed, and replication of quantitative data was confirmed. Results show that sorption of explosives, via vapor diffusion, to black hair is significantly greater than to blond, brown or bleached hair. Furthermore, the rate of sorption is directly related to the vapor density of the explosive: TATP ≪ TNT ≪ PETN \u3c RDX. Using TNT as the prototype, persistence of the explosive upon standing in air and upon repeated washing with sodium dodecyl sulfate was demonstrated. This study indicates that hair can be a useful indicator of explosive exposure/handling. Work is in progress to develop this technique into an effective forensic tool

A facile one-pot conversion of acetates of the Baylis-Hillman adducts to [E]-α-methylcinnamic acids

A simple and convenient stereoselective synthesis of [E]-α-methylcinnamic acids via the nucleophilic addition of hydride ion from sodium borohydride to methyl 3-acetoxy-3-aryl-2-methylenepropanoates followed by hydrolysis and crystallization is described. Efficacy of this methodology in the synthesis of [E]-p-(myristyloxy)-α-methylcinnamic acid, an active hypolipidemic agent, and [E]-p-(carbomethoxy)-α -methylcinnamic acid, a valuable synthon for an orally active serine protease inhibitor, is also demonstrated

Peptidomimetic targeting of critical androgen receptor-coregulator interactions in prostate cancer

Extent: 11 p.The growth of advanced prostate cancer depends on androgen receptor signalling, however treatment options are limited. Here we report the disruption of specific protein–protein interactions involving LXXLL motifs in androgen receptor–coregulator proteins such as PELP1 using a novel, small molecule peptidomimetic (D2). D2 is stable, non-toxic and efficiently taken up by prostate cancer cells. Importantly, D2 blocks androgen-induced nuclear uptake and genomic activity of the androgen receptor. Furthermore, D2 abrogates androgen-induced proliferation of prostate cancer cells in vitro with an IC50 of 40 nM, and inhibits tumour growth in a mouse xenograft model. D2 also disrupts androgen receptor–coregulator interactions in ex vivo cultures of primary human prostate tumours. These findings provide evidence that targeting androgen receptor–coregulator interactions using peptidomimetics may be a viable therapeutic approach for patients with advanced prostate cancer.Preethi Ravindranathan, Tae-Kyung Lee, Lin Yang, Margaret M. Centenera, Lisa Butler, Wayne D. Tilley, Jer-Tsong Hsieh, Jung-Mo Ahn and Ganesh V. Ra