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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.

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.

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Showing Results 81 - 90 of 175
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A chemical in garlic kills bacteria that cause deadly infections in people with cystic fibrosis, University of Edinburgh research shows.
UGA Researchers Discover Potential Treatment for Drug-resistant Tuberculosis
Researchers have developed a new small molecule drug as a treatment against multi-drug resistant tuberculosis.
A Protein's Novel Role In Several Types Of Cancers Discovered
Stanford ChEM-H scientists are helping to develop a novel cancer therapy based on a new finding of a protein that inadvertently promotes cancer growth.
Cancer Treatment with KU Origins Enters Second Clinical Trial
Cleave Biosciences has begun a Phase 1 clinical trial to evaluate CB-5083.
Grant will Help Develop More Powerful Disinfectants
$200,000 grant awarded to develop the next generation of antibacterial cleansers and disinfectants.
Artificially-intelligent Robot Scientist ‘Eve’ Could Boost Search for New Drugs
Eve, an artificially-intelligent ‘robot scientist’ could make drug discovery faster and much cheaper, say researchers writing in the Royal Society journal Interface.
Novogen Announces Important Discovery in Regenerative Medicine Program
A key proof-of-concept step to develop drugs capable of stimulating the function of brain tissue stem cells.
Stanford Chemists Take Step Toward Solving Mystery of How Enzymes Work
Steven Boxer and his students have found that the electrostatic field within an enzyme accounts for the lion's share of its success.
New Class of Synthetic Molecules Mimics Antibodies
A Yale University lab has crafted the first synthetic molecules that have both the targeting and response functions of antibodies.
The Hunt for Botanicals
Herbal medicine can be a double-edged sword and should be more rigorously investigated for both its beneficial and harmful effects, say researchers writing in a special supplement of Science.
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