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Thursday, September 18, 2014
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Microwave chemistry in SiC Reaction Vials
D. Obermayer, B. Gutmann, B. Reichart, C. O. Kappe

Using novel SiC-technology to mimic conventional heated autoclave experiments.

Enzyme kinetic measurements performed on BMG LABTECH´s FLUOstar OPTIMA

BMG LABTECH has developed a new evaluation software feature able to calculate the Km value as well as the maximal velocity (Vmax) from an enzymatic kinetic measurement. Enzymes differ in their affinity to specific substrates and this affinity is represented by the Michaelis-Menten constant Km. The new software feature for enzyme kinetic offers fast and easy calculation of Km and Vmax. Available plots are the common Michaelis-Menten, Lineweaver-Burk, Eadie-Hofstee, Scatchard and Hanes kinetic f

Automated Microreactor Optimisation of the Swern-Moffatt Oxidation at Elevated Temperatures
Pieter J. Nieuwland, Kaspar Koch, Noud van Harskamp, Ron Wehrens, Jan C.M. van Hest and Floris P.J.T. Rutjes

Optimisation of the selective Swern-Moffatt oxidation of benzyl alcohol to benzaldehyde by varying five experimental parameters in an automated microreactor setup.

Organic azide synthesis in microreactors: from optimization to lab scale production
Pieter J. Nieuwland, Bo Hanssen, Kaspar Koch, Paul Janssen, Marielle M.E. Delville, Anton Lunshof and Floris P.J.T. Rutjes

The formation of benzyl azide by diazotransfer to benzyl amine was screened and subsequently scaled up using continuous flow chemistry.

Five noncovalent peptidic ligands show different affinity rankings in solution and gas phase
Andrey Dyachenko , Michael Goldflam , Marta Vilaseca , Ernest Giralt

Stability of noncovalent complexes of VEGF protein with 5 peptidic ligands is studied. Experiments were conducted in solution (NMR CSP, ITC) and in gas phase (CID TOF MS). Each ligand differs from others in chirality of one amino acid. It was shown, that trend of stability of the studied noncovalent complexes is reversed in the gas phase relatively to the solution. An explanation of this behavior is presented.

Synthesis and trafficking of the tonoplast potassium channel AtTPK1
Marie Maitrejean (1,2), Michael Wudick (2), Camilla Voelker (2), Katrin Czempinski (2), Emanuela Pedrazzini (1), Alesandro Vitale (1)

Sorting signals of tonoplast proteins and the pathway they follow through the endomembrane system are still poorly characterized. Using Brefeldin A (an inhibitor of the Golgi-mediated traffic) we showed that a Golgi-dependent pathway for tonoplast delivery may exist. Then we generated various chimeric TPK1-TPK4 fusions, exchanging various domains. We observed that the cytosolic, C-terminal domain of TPK1 is sufficient to re-direct the plasma membrane TPK4 to the tonoplast.

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.

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Showing Results 51 - 60 of 146
Scientific News
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.
Collaboration Leads to Possible Shortcut to New Drugs
The reaction, reported in Science, demonstrates how a carboxylic acid can be transformed into a very reactive site through use of a novel photoredox catalyst.
Catalysts That Mimic Enzymes Could Revolutionize Pharmaceutical Manufacturing
Structures made of polymer chains allow the catalysts to work in water.
Discovery of How Taxol Works Could Lead to Better Anticancer Drugs
The drug’s interference with the normal function of microtubules could help in designing better anticancer drugs.
Chemists Discover Cancer Drug Candidate Structure
Chemists at The Scripps Research Institute have determined the correct structure of a highly promising anticancer compound approved by the U.S. FDA for clinical trials in cancer patients.
Novel Drug Targets for Allergy Identified
Researchers have identified several target molecules which are suitable for the development of new allergy drugs.
Drug Does Not Improve Set of Cardiovascular Outcomes for Diastolic Heart Failure
NIH-supported study finds drug does appear to reduce hospitalizations for diastolic heart failure.
Entirely Novel Strategy to Molecular Anticancer Therapy Tricks Malignant Cells
New drug prevents tumour growth by inhibiting the nucleotide sanitizing enzyme MTH1.
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