|The Prestwick Chemical Library (R), A Valuable Tool for Screening|
Jean-Marie Contreras1, Christophe Morice1, Jean-Marc Simon1, Bruno Didier2, Marie-Louise Jung1 and Thierry Langer3
The Prestwick Chemical Library® (PCL) is Prestwick’s flagship product dedicated to screening. It is a collection of 1280 molecules comprising 100% approved drugs (FDA, EMEA and other agencies) selected for their high chemical and pharmacological diversity. The PCL was designed to reduce the risk of "low quality" hits and therefore the cost of the initial screening, and appears to be an efficient smart library for hit discovery. The PCL comes with an extended fully-annotated database.
|Scale up of Atorvastatin Delayed Release Nanoparticles for Treatment of Hyperlipidemia: Quality by Design (QbD) Approach|
Gite S. M., Mirani A. G., Patravale V.B.
The studies describes the implementation of QbD approach in the systematic development of optimized Atorvastatin calcium delayed release nanoparticles (ACDRNPs) employing simple, efficient and cost-effectual technique.
|Direct Targets Identification of a Bioactive Compound|
Sylvain Blanc, Paul Bradley, Marie-Edith Gourdel, Michael Cholay, Gisèle Guimèse, Mike Mckenzie, George Nasi, Jean-Christophe and Barbara Ruggiero
Identifying protein partners of a small bioactive molecule is of great
interest in many aspects of life sciences and specifically in the drug
discovery and development process cycle. It is a support to (i) decipher
the mechanism of action after for example a “High Content” screening,
(ii) study “off-target” effects, (iii) adjust therapeutic indications and
clinical regimens of a drug and (iv) consider drug repositioning.
|Fighting Blindness with 3D-NET "Drug Discovery & Development of Novel Eye Therapeutics"|
Pilar Ventosa-Andrés, Nils Ohnesorge, Yolanda Fernández, Yolanda Alvarez and Breandán Kennedy
3D-NET, “Drug Discovery & Development of Novel Eye Therapeutics”, is a new European research consortium of industry and academic partners focusing efforts to enhance the discovery and development of drugs targeting ocular pathologies that lead to blindness.
|Automated detection and control of controlled substances|
Joe Bradley, Ian Johns
Scitegrity, in conjunction with the Pistoia Alliance and a number of pharmaceutical companies, have developed Controlled Substances Squared to scan large chemical libraries (millions of compounds) and determine whether a compound is considered as controlled in a selected country.
|Antioxidant and Free Radicals Scavenging Activity of Biomolecules: Hydroxamic Acids|
Bharati Verma and Rama Pande
In the present poster attention is focused towards the investigation of antioxidant and free radicals scavenging activity of N-aryl substituted hydroxamic acids by DPPH method which is based on the reduction of alcoholic DPPH solutions in presence of a hydrogen donating antioxidant, hydroxamic acids.
|Enabling Epigenetics Studies from HTS to SAR : A Novel HTRF® Platform to Identify and Characterize Reader Domain Inhibitors|
T. Roux1, M. Badol1, N. Douayry1, L. Sergeant1, E.Trinquet1, F. Degorce1, S. Milhas2, S. Betzi2, C. Derviaux2, C. Eydoux3, J. Letienne2, A. Lugari2, Y. Collette2, J-C. Guillemot3 et X. Morelli2
Discover a novel HTRF platform to identify and characterize the vast variety of epigenetic binding domain.
|Characterization of Proteins and Protein Self Association (Oligomerization) with SEC-MALS|
Michel Terray, Mark Pothecary
In this poster, a series of proteins and their oligomers were characterized using SEC-MALS with UV and RI detection. The monomer molecular weights are measured and compared with those from column calibration. The molecular weights of their oligomers are also compared with column calibration and the differences explored.
|High Throughput Screening in the European Lead Factory|
S.P. van Helden, W.H. Rutjes, C.A.A. van Boeckel and J.H.M. van den Broek
This paper describes workflows that have been implemented at the screening centre of the European Lead Factory and presents screening statistics on the first 18 months of operation.
|Novel Gpr39 Agonists: Correlation Of Binding Affinity Using Label-Free Back-Scattering Interferometry With Potency In Functional Assays|
Daniel Brown (1), Niklas Larsson (2), Ola Fjellström (3), Anders Johansson (3), Sara Lundqvist (2), Johan Brengdahl (2), and Richard J. Isaacs (1)
We describe the application of back-scattering interferometry (BSI) to the characterization of small molecule ligand binding to human GPR39 (a GPCR targeted for type-2 diabetes therapy) overexpressed in crude membrane fractions in free solution, including how BSI-derived affinity and functional assay-derived potency correlate for compounds of varying scaffolds.
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