Fragment Based Screening Service at CRELUX and ZoBio
One of the first targets, which also will be made accessible to customers, was Pim1, a kinase that has been implicated in the progression of several haematological malignancies. In addition to the "off the shelf" data on Pim1, tailor made fragment based screening projects are available for customers upon request.
The joint technology platform combines ZoBio's proprietary Target Immobilized NMR Screening (TINS) technology with CRELUX's high performance kinase crystallography platform. In the first campaign Pim1 was screened by TINS using ZoBio's fragment library, hits were assessed in an in vitro kinase assay and the top 50 hits have been soaked into protein crystals. 37 out of these 50 fragments showed defined binding modes. Together with this high hit rate the structural diversity within this group generated multiple points for optimization and clearly proved the power of this technology combination.
"We are delighted to have found a perfect partner for entering into high performance fragment based screening. The collaboration with ZoBio adds another crucial drug discovery technology to our service portfolio", commented Dr. Michael Schäffer, CEO of CRELUX.
"This project demonstrates the power of the combination of TINS with top notch crystallography. I am absolutely convinced that together we can provide our customers with critical starting point to jump start their challenging or failed targets." noted Dr. Gregg Siegal, CSO of ZoBio.
CRELUX has used its state-of-the-art structural biology platform to solve more than 270 crystal and co-crystal structures for pharma and biotech companies. This platform encompasses all steps - from target cloning and expression all the way to high-throughput protein crystallization and in-house x-ray crystallography.
ZoBio provides fragment discovery and characterization services to the pharmaceutical and biotech industries using its proprietary Target Immobilized NMR Screening (TINS) platform. TINS, with its unparalleled sensitivity and reliability, has been used to discovery highly diverse, efficient ligands for a variety of targets including kinases, protein-protein interactions, viral targets and membrane proteins.
ZoBio - www.zobio.com ZoBio develops innovative methods using Nuclear Magnetic Resonance to screen compound libraries for binding to a broad range of pharmacological targets. Using its TINS technology, ZoBio is capable of rapidly generating high affinity, high specificity lead compounds with optimal drug-like properties. Founded in 2004 as a spinout from Leiden University in the Netherlands, ZoBio has focussed on development of its proprietary TINS hardware and methods that allow rapid screening of drug fragment libraries for interaction with a target. TINS allows fragment based screening of a much broader array of targets than competing technologies. ZoBio concentrates on collaborative drug discovery projects with diverse biotech and pharmaceutical partners.
CRELUX provides fast and affordable access to co-crystal structures for biotech and pharma companies worldwide. Three dimensional structures of target-compound complexes are unique sources of information during the rational drug discovery process. Straightforward availability of structural data at an early stage of the drug development process significantly enhances productivity and success rates during hit selection, lead generation, and lead optimization. CRELUX has streamlined the processes of structure generation and solved hundreds of co-crystal structures using an integrated technology platform. In addition to customer designed projects crystallization conditions of numerous relevant therapeutic targets are available within the Off-The-Shelf Program of CRELUX. Off-The-Shelf target structures are delivered at a fixed price and short turn around times, facilitating affordable access to structural information.