Crystal-Grade Kinase Protein and Structures Platform Established

Two companies have jointly established a crystal-grade kinase protein and structures platform, which was optimized and quality-controlled for successful crystallization.

One of the first targets was Pim1, a kinase that has been implicated in the progression of several hematological malignancies. The joint technology platform combines ZoBio's (Leiden, The Netherlands) proprietary Target Immobilized NMR Screening (TINS) technology with Crelux's (Martinsried, Germany) 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 were soaked into protein crystals. Thirty-seven 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.

Crelux has used its 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.

"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 Schaffer, CEO of Crelux.

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ZoBio
Crelux