|Identification and Characterisation of Novel Positive Allosteric Modulators of the Galanin 2 Receptor|
An HTS against GalR2 was carried out to find novel PAMs to treat neuropathic pain.
|The Longest Way Round is the Shortest Way Home: HTS Assay Development for Complex Multi-domain Protein Kinases|
Doris Hafenbrandl, Vanessa Nardese, Maria Cristina Sidoli, Valeria Wanke, Mariantonietta Rubino and Daniele Carettoni
This study strongly supports the possibility to overcome the major bottlenecks in the production of long kinase recombinant forms, in order to perform drug discovery programmes with proteins more closely preserving the structural and functional properties of the native enzymes.
|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.
|Artificial Multi-Gene Expression Systems Design Service for Natural Compound Formation and Hetero Protein Complexes|
Bernauer, Hubert, Gregor Zipf and Josef Maier
Drug discovery of natural compounds drug development and drug target analyses as well as bioproduction can benefit from artificial genetic systems and constructions. The direction in which genes are to be developed is written in the genomes. Synthesis oriented genomic analyses of codon bias and tRNA adaption analyses are prerequisites for generating adaptive, highly functional genes.
|Validation of a 3-Dimensional Human Liver Microtissue Model for Long-term Hepatotoxicity Studies|
Brad Larson1, Stewart Hunt2, Timothy Moeller3, Diana Long4, and Peter Banks1
Non-steroidal anti-inflammatory drugs (NSAIDs) are a class of drug commonly used as analgesics and antipyretics, as well as for management of rheumatological disorders. They are one of the most highly prescribed drug families around the world, and consequently, along with antimicrobial agents, are the most frequent causes of druginduced liver injury (DILI) (Bjornsson et al., 2010).
|Amino-Coated Metallofullerene Nanoparticles for Glioblastoma Mutiforme Tumor Detection|
Tinghui Li , Susan. Murphy, Kanwarpal Bakshi, Steven LaConte, Zhi Sheng, and Harry Dorn
We report the preparation of a new functionalized trimetallic nitride endohedral metallofullerene, with a cage surface consisting of positively charged amino groups, which is expected to bind more efficiently to negatively charged cell phospholipid bi-layer cellular surfaces and will more readily undergo endocytosis. We now report that this Gd-nanoplatform when subsequently conjugated with an IL-13 peptide, (IL-13-Gd3N@C80(OH)x(NH2)y) exhibits enhanced targeting of U-251 GBM cell lines.
|Performance of a hybrid gamma-optical camera for improved utility in diagnostic imaging|
L.K. Jambi1, J.E. Lees1, S.L. Bugby1, B.S. Bhatia1,2, M.S. Alqahtani1, W.R. McKnight1, A.H. Ng3 and A.C. Perkins3
Performance of a hybrid gamma-optical camera for improved utility in diagnostic imaging
|Side by Side: An Evaluation of 2D vs. 3D Cell Culture for High Throughput Screening in Drug Discovery|
Sophie Quick 1,2, Sinead Knight 1, Jon Winter 3
•3D cell culture has the potential to provide a more physiologically relevant model compared to standard tissue culture plastic.
•From a screening perspective the technology offers the possibility of more predictive drug responses but has an increased cost.
•The question: is it possible and, more importantly, is it worthwhile moving towards screening in High Throughput using a 3D model?
|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.