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Friday, October 31, 2014
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Anti-inflammatory activity of Dalbergia sissoo Roxb. heart-wood
Ohm Devani, S. K. Lahiri, D. D. Santani, M. B. Shah

The heart-wood of Dalbergia sissoo Roxb. is reported to be used in traditional medicinal practices, of which anti-inflammatory is one. The present work evaluates the effect of the heart-wood extract on the carrageenan induced rat paw edema. The drug was found to be active at lowest of 3 doses tried. the drug can be said to posses anti-inflamatory activity but needs further evaluation of discover the pathway of the same.

Necessity of quantum mechanics for predicting binding free energy
Ting Zhou, Danzhi Huang, Amedeo Caflisch

We demonstrate the necessity of quantum mechanics (QM) for predicting binding free energy by comparing the results of the linear interaction energy model with continuum model (LIECE) and the equivalent model with QM (QMLIECE).

Resorufin - a lead for a new protein kinase CK2 inhibitor
Iben Skjøth Sandholt1, Birgitte Brinkmann Olsen1, Barbara Guerra1, Olaf-Georg Issinger1, Brigitte Boldyreff2

Screening of a natural compound library led to the identification of resorufin, as a highly selective and potent inhibitor for protein kinase CK2. Out of 52 kinases tested only CK2 was inhibited. The IC50 values determined for the CK2 holoenzymes were 1.5 µM and for the free catalytic subunits ca. 4 µM. In different cancer cell lines treatment with resorufin led to cell death and endogenous CK2 was inhibited.

MED-SuMo and MED-Hybridise: exploit all PDB macromolecule structures to design/optimize innovative leads
Moriaud F., Oguievetskaia K., Adcock S.A., Vorotynsev A.M., Martin L., Doppelt-Azeroual O. and Delfaud F.

Obtaining structural information on fragment-protein target is a key factor and also a major limitation. We’ve used MED-SuMo and MED-Hybridise to query and mine the PDB seeking for similar interaction surfaces. MED-portions were used to design novel scaffolds (GPCR) and decorate a given scaffold (kinase). We have analysed the scaffolds in regard to their diversity, their presence in PubChem, PDB and other libraries.

Production of prostanoids in the plant Arabidopsis thaliana
Maged E. Mohamed and Colin M. Lazarus.

Prostanoids originate from PGHS action on the 20-carbon polyunsaturated fatty acid: DGLA, AA and EPA. We used cDNA expression in Saccharomyces cerevisiae and enzyme immunoassays to compare the activities of two mouse PGHS isoforms and cDNAs encoding mouse prostaglandin I synthase and thromboxane A synthase and genomic DNA encoding Trypanosoma brucei prostaglandin F synthase. All genes were active and were put in Transgenic Arabidopsis thaliana plants producing DGLA.

Biosynthesis of Very Long Chain Polyunsaturated Fatty Acids in Chicory
Hattem Mekky1, Michael R. Davey1, J. Brian Power1 , Maged E. Mohamed2 and Colin M. Lazarus2

Very long chain polyunsaturated fatty acids (VLCPUFAs) are declining in reserves, since they are produced by oily fish. VLCPUFAs are important in human nutrition because they are responsible for the production of inflammatory mediators such as prostaglandins, the regulation of cholesterol synthesis and its transport, and the maintenance of cellular membranes. This research aims to produce VLCPUFAs in edible plants.

qPCRas a primary screen in drug discovery
GauravJaggi, Frank Boeckler, Andreas Joerger and Alan Fersht

We report the use of qPCR technique to follow the thermal unfolding of proteins by the binding of the dye SYPRO Orange, and exploit its potential as a robust and high-throughput primary screen for small molecule drug discovery.

Heterochromatin structure is induced by siRNA targeting HIV-1 promoter region
K Suzuki1, H Lim1,3, T Ishida2, T Watanabe2, D Cooper1,3, A Kelleher1,3

We transfected siRNA targeting HIV-1 promoter region into a cell line productively infected with HIV-1. ChIP analysis revealed that the RNA duplex induced transcriptional gene silencing and enrichment of Ago1, H3K9me2, and HDAC1 in HIV promoter region to form heterochromatin structure. The data indicates RNA duplex induces the latent phase of HIV infection, since the chromosome formation is very similar to the state of HIV latently infected cell lines

Evolution of the Contact Phase of Vertebrate Blood Coagulation
M. B. Ponczek, D. Gailani and R. F. Doolittle

Three proteases involved in the contact phase of vertebrate blood coagulation were searched in genomes of amphibians, birds and mammals. Several data sources were used during this bioinformatics analysis. Our survey confirmed that the vertebrate contact phase has occurred by way of a series of gene duplications during the course of several hundred million years of evolution, beginning with the appearance of fXII and a PK-fXI predecessor in amphibians.

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Showing Results 71 - 80 of 160
Scientific News
MS Drug Candidate Shows Promise for Ulcerative Colitis
Positive new clinical data were released today on a drug candidate for ulcerative colitis that was first discovered and synthesized at The Scripps Research Institute.
New Technique has Profound Implications for Drug Development
The method, developed by Scripps Research Institute chemists, expands options for making pure batches of ‘one-handed’ molecules.
Team Discovers How Microbes Build a Powerful Antibiotic
Researchers discovery opens up new avenues of research into thousands of similar molecules.
Misfolded Proteins Clump Together in a Surprising Place
Stowers researchers create new framework for protein aggregation under acute stress.
Nanoparticle Research Could Enhance Drug Delivery Through Skin
A milestone study from the University of Southampton could have major implications for the delivery of drugs.
Chemists Recruit Anthrax to Deliver Cancer Drugs
With some tinkering, a deadly protein becomes an efficient carrier for antibody drugs.
Protein ‘Map’ Could Lead to Potent New Cancer Drugs
Findings will help scientists to design drugs that could target NMT enzyme.
Animal Testing can Mislead Drug Discovery and Development
Several blockbuster drugs would not be on the market, if scientists had relied solely on drug-uptake in animal trials, according to new research.
Synthesis and Bioactivity of Analogues of Tropodithietic Acid
The study suggests that the sulfur atoms in the marine antibiotic TDA are not essential for bioactivity, but different modes of action for TDA and its sulfur-free analogue cannot be excluded.
Cancer-Fighting Drugs Might Also Stop Malaria Early
A number of compounds have been identified which could be used to fight malaria.
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