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The use of the IV microtracer technique to drive formulation optimisation
Vanessa Zann, Paul Dickinson, Wang Wang Lee, George Kirk, Owen Jones, Andy Gray, Davindera Singh Sanghera, Mark Seymour, Jo Collier, Lloyd Stevens, Julie Dent

Strategy: Use IV microtracer techniquer to de risk compounds with PK issues and drive formulation development

Addressing the challenges of poor solubility: Rapid development and clinical evaluation of a lipid based formulation to enhance oral bioavailability of amuvatinib (MP-470)
P.D. Scholes, J. McDermott, J. Vertommen, J-L Colin, G Choy, M Azab, R Joshi and S. Redkar

Physiochemical and biopharmaceutical properties of new chemical entities are presenting increasing challenges to successful oral drug delivery. Here we present data on amuvatinib, a novel multi-targeted tyrosine kinase inhibitor specifically designed to be a potent inhibitor of mutant c-Kit and PDGFRalpha.

Elucidation of the Relative Bioavailability of a Drug Candidate from Different Regions of the Human Gastrointestinal Tract
David Harris, Ph.d. , Joanne Collier, MBCHB, Alyson Connor, Ph. D. , Tomoko Freshwater, Ph. D. , David Goldfarb, Ph. D. , Ann Horowitsz Ph. D. , Xuewen Ma, Ph. D. , Paul Statkevich, Ph. D.

This poster describes a pharmacokinetic study to investigate the relative absorption of an NCE from different regions of the human gastrointestinal tract, to support potential development of a sustained-release formulation.

Evaluation Of Single Point And IC50 Shift Assays For Measuring Time-Dependent Inhibition Of Drug Discovery Compounds
Katie Fox, Rosey Pearson, Phillip Butler, Clive Dilworth

The aim of this study is to evaluate different assay designs, and data analysis methodology for measuring the extent of TDI for known inhibitors. We propose a reversible inhibition and TDI screening platform to cover early phase compounds, which enables accurate decisions to be made regarding development of compounds which could cause DDIs.

Nitric Oxide Decreases the Expression and Activity of the Ubiquitin-Conjugating Enzyme UbcH10
Nick D. Tsihlis, PhD, Chris S. Oustwani, BA, Ashley K. Vavra, MD, Qun Jiang, MD and Melina R. Kibbe, MD

Nitric oxide (NO) has been shown to limit the formation of neointimal hyperplasia in animal models of arterial injury. Ubiquitination proceeds via formation of thioester bonds and NO can act to disrupt those bonds. We report that NO decreases the activity and expression of UbcH10 in vitro, and decreases the expression of UbcH10 following arterial injury in vivo. Therefore, UbcH10 may be a promising therapeutic target for inhibiting neointimal hyperplasia.

SuperNatural: A Database of Available Natural Compounds
Melanie Füllbeck, Mathias Dunkel and Robert Preissner

The majority of marketed drugs are natural compounds or derivatives thereof. The compounds availability is often unclear. Therefore we have compiled a database of ~50,000 natural compounds. Starting point for in silico screenings are about 2,500 well-known, classified natural compounds or imported molecules. Possible medical applications can be detected and about three million conformers computed to account for the flexibility during usage of the 3D-superposition algorithm.

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.

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Showing Results 81 - 90 of 182
Scientific News
Drugs that Activate Brain Stem Cells May Reverse Multiple Sclerosis
NIH-funded study identifies over-the-counter compounds that may replace damaged cells.
Allergy Drug Inhibits Hepatitis C in Mice
NIH study suggests alternative drug to treat virus.
Saccharin Shows Promise as Cancer Inhibitor
Researchers have found that the artificial sweetener can inhibit cancer cell growth.
Treating Canine Periodontal Disease
The class of compounds, designed to resolve inflammation, has potential to treat chronic disease in animals and humans.
‘Warhead’ Molecule Targets Deadly Bacteria
Boston college chemists target bacterial lipids to label deadly bacteria, spare healthy cells.
Garlic Could Aid Cystic Fibrosis Fight
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.
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