AzaGly‐Appended Peptidomimetics Structurally Related to PTR6154 as Potential PKB/Akt Inhibitors

We report the synthesis and biological and physiochemical properties of a series of azaGly‐appended peptidomimetics. We have developed a simple and facile synthesis for azapeptides on solid support without any side reaction. The azaGly is inserted by in situ reaction of disuccinimidyl carbonate with free amine followed by treatment of hydrazine hydrate at room temperature. The new series of peptidomimetics was prepared by azaGly scanning of heptapeptide Arg‐Pro‐Arg‐Nle‐Tyr‐Dap‐Nle ( Akt‐01 ), a GSK‐3β‐derived Akt inhibitor. The azaGly‐appended peptides showed significant improvement in biological activity and serum stability, with retention of conformation as evidenced by NMR and CD studies. The results clearly demonstrate that azaGly‐appended peptides are new peptidomimetics. Their synthesis makes this approach highly useful for the development of novel peptidomimetics of therapeutic potential.     

Phototactic supersmarticles

Smarticles or smart active particles are small robots equipped with only basic movement and sensing abilities that are incapable of rotating or displacing individually. We study the ensemble behavior of smarticles, i.e., the behavior a collective of these very simple computational elements can achieve, and how such behavior can be implemented using minimal programming. We show that an ensemble of smarticles constrained to remain close to one another (which we call a supersmarticle), achieves directed locomotion toward or away from a light source, a phenomenon known as phototaxing. We present experimental and theoretical models of phototactic supersmarticles that collectively move with a directed displacement in response to light. The motion of the supersmarticle is stochastic, performing approximate free diffusion, and is a result of chaotic interactions among smarticles. The system can be directed by introducing asymmetries among the individual smarticle’s behavior, in our case, by varying activity levels in response to light, resulting in supersmarticle-biased motion.     

Ring‐opening polymerization of lactones using RuCl2(PPh3)3 as initiator: Effect of hydroxylic transfer agents

ε‐Caprolactone and δ‐valerolactone were polymerized in bulk at 150°C using the ruthenium(II) complex RuCl₂(PPh₃)₃ as initiator in the presence of 1,3‐propanediol (PD) with a series of alcohols as coinitiators. Polymerization of lactones proceeds via ruthenium(II) alkoxide active centers. ¹H‐NMR analysis revealed that the ruthenium complex reacted with the alcohol, generating in situ a ruthenium alkoxide. This species became a more active initiator of ring‐opening polymerization than was RuCl₂(PPh₃)₃. The obtained polylactones were characterized by ¹H‐ and ¹³C‐NMR and matrix‐assisted laser desorption ionization time‐of‐flight (MALDI‐TOF). The results showed the formation had occurred of α,ω‐telechelic PCL and PVL diols, in which PD had been incorporated into the polymer backbone. Depending on the nature of the alcohol used as coinitiator, PCLs with different end groups could be synthesized. Insertion of an alcohol as an end group (benzyl alcohol, n‐octanol, or isopropanol) or into the polymeric backbone (propanediol) provided support for the conclusion that a classical coordination–insertion mechanism was operating during lactone polymerization. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci, 2006     

Microwave dielectrics: solid solution,ordering and microwave dielectric properties of $$(1{-}x)\hbox {Ba}(\hbox {Mg}_{1/3}\hbox {Nb}_{2/3})\hbox {O}_{3}{-}x\hbox {Ba(Mg}_{1/8}\hbox {Nb}_{3/4})\hbox {O}_{3}$$ ceramics

The effect of Ba(\(\hbox {Mg}_{1/8}\hbox {Nb}_{3/4})\hbox {O}_{3}\) phase on structure and dielectric properties of \(\hbox {Ba(Mg}_{1/3}\hbox {Nb}_{2/3})\hbox {O}_{3}\) was studied by synthesizing \((1{-}x)\hbox {Ba(Mg}_{1/3}\hbox {Nb}_{2/3})\hbox {O}_{3}{-}x\hbox {Ba}(\hbox {Mg}_{1/8}\hbox {Nb}_{3/4})\hbox {O}_{3}\) (\(x = 0\), 0.005, 0.01 and 0.02) ceramics. Superlattice reflections due to 1:2 ordering appear as low as \(1000^{\circ }\hbox {C}\). \(\hbox {Ba}(\hbox {Mg}_{1/3}\hbox {Nb}_{2/3})\hbox {O}_{3}\) forms solid solution with \(\hbox {Ba}(\hbox {Mg}_{1/8}\hbox {Nb}_{3/4})\hbox {O}_{3}\) for all ‘x’ values studied until \(1350^{\circ }\hbox {C}\). Ordering was confirmed by powder X-ray diffraction pattern, Raman study and HRTEM. Ceramic pucks can be sintered to density \({>}92\%\) of theoretical density. Temperature and frequency-stable dielectric constant and nearly zero dielectric loss (tan \(\delta \)) were observed at low frequencies (20 MHz). The sintered samples exhibit dielectric constant (\(\varepsilon _{\mathrm{r}})\) between 30 and 32, high quality factor between 37000 and 74000 GHz and temperature coefficient of resonant frequency (\(\tau _{\mathrm{f}})\) between 21 and \(24\hbox { ppm }^{\circ }\hbox {C}^{-1}\).     

Fold change based approach for identification of significant network markers in breast,lung and prostate cancer

Cancer belongs to a class of highly aggressive diseases and a leading cause of death in the world. With more than 100 types of cancers, breast, lung and prostate cancer remain to be the most common types. To identify essential network markers (NMs) and therapeutic targets in these cancers, the authors present a novel approach which uses gene expression data from microarray and RNA‐seq platforms and utilises the results from this data to evaluate protein–protein interaction (PPI) network. Differentially expressed genes (DEGs) are extracted from microarray data using three different statistical methods in R, to produce a consistent set of genes. Also, DEGs are extracted from RNA‐seq data for the same three cancer types. DEG sets found to be common in both platforms are obtained at three fold change (FC) cut‐off levels to accurately identify the level of change in expression of these genes in all three cancers. A cancer network is built using PPI data characterising gene sets at log‐FC (LFC)>1, LFC>1.5 and LFC>2, and interconnection between principal hub nodes of these networks is observed. Resulting network of hubs at three FC levels highlights prime NMs with high confidence in multiple cancers as validated by Gene Ontology functional enrichment and maximal complete subgraphs from CFinder.Inspec keywords: cancer, proteins, RNA, bioinformatics, statistical analysis, genetics, molecular biophysics, ontologies (artificial intelligence), lungOther keywords: cancer network, PPI data, gene sets, multiple cancers, Gene Ontology functional enrichment, prostate cancer, gene expression data, RNA‐seq platforms, protein–protein interaction network, DEG, microarray data, RNA‐seq data, cancer types, lung cancer, diseases, breast cancer, network markers, differentially expressed genes, fold change based approach, CFinder, statistical methods     

Reaching the goal of Universal Salt Iodization (USI): experience of Uttar Pradesh, India

BACKGROUND: In 2002, the percentage of households consuming iodized salt in the state of Uttar Pradesh (UP) in India dropped to as low as 6%. This implied that 3.5 million newborns in this non-salt producing state, with 180 million population, were at risk of brain damage unless universal accessibility and consumption of iodized salt was ensured and sustained. OBJECTIVES: Urgent measures were introduced in 3 phases in the statefor accelerating procurement, distribution and consumption of iodized salt. METHODS: In the first phase, a study on mapping of salt wholesalers and understanding the salt trading system--including understanding the knowledge, attitudes, and practices of salt traders was undertaken to accelerate efforts to influence availability, marketing, and accessibility of iodized salt. The study revealed that a total of only 344 primary wholesalers supplied salt to the entire state. Of these, 126 wholesalers marketed 80% of salt and were located in only 15 of the total 70 districts of the state. This finding became a very strong basis for the program in phase II, which focused on the critical group of wholesalers and set up a system to frequently interact with them. The salt wholesalers were equipped with Salt Testing Kits (STKs) to ensure adequate iodine content in the salt procured by them and adherence to the legal ban on the sale of non-iodized salt for human consumption. Simultaneously, a "child-to-community" approach was launched through involvement of middle and high school children to create demand and monitor consumption of iodized salt at the household level. Over 217,000 salt samples (about 26,000 samples per quarter) were brought in by school children and tested for iodine content. RESULTS: The school activities resulted not only in influencing consumption of iodized salt, but also galvanized the entire chain linking consumers, retailers, and wholesalers. In less than 2 years, salt procured with nil iodine decreased from 38% to 15.3%, and salt marketed with adequate iodine level increased from 28.6% to 64.9%. School data revealed an increase in consumption of iodized salt from 6% to 46.7%. In phase 3, additional standardized activities at the school level were included and the program was taken to scale in the state. CONCLUSION: The findings revealed that identification and inclusion of salt wholesalers-not only the salt manufacturers-was important for achieving a rapid positive shift in iodized salt marketing and consumption practices.     

Combining pores and ridges with minutiae for improved fingerprint verification

This paper presents a fast fingerprint verification algorithm using level-2 minutiae and level-3 pore and ridge features. The proposed algorithm uses a two-stage process to register fingerprint images. In the first stage, Taylor series based image transformation is used to perform coarse registration, while in the second stage, thin plate spline transformation is used for fine registration. A fast feature extraction algorithm is proposed using the Mumford–Shah functional curve evolution to efficiently segment contours and extract the intricate level-3 pore and ridge features. Further, Delaunay triangulation based fusion algorithm is proposed to combine level-2 and level-3 information that provides structural stability and robustness to small changes caused due to extraneous noise or non-linear deformation during image capture. We define eight quantitative measures using level-2 and level-3 topological characteristics to form a feature supervector. A 2ν-support vector machine performs the final classification of genuine or impostor cases using the feature supervectors. Experimental results and statistical evaluation show that the feature supervector yields discriminatory information and higher accuracy compared to existing recognition and fusion algorithms.     

Robust circuit implementation of 4-bit 4-tube CNFET based ALU at 16-nm technology node

Analog Integrated Circuits and Signal Processing - Tremendous and inescapable application of full adder adds impetus to its optimization till high-end performance. Use of full adder propels the...