Focused on services around an integrated structure guided Lead Generation Process and on distinct services in the fields of protein production, biophysical and thermodynamic profiling and protein structure analysis to accelerate drug discovery. Proteros is also highly committed to its own R&D activities leveraging its capabilities to drive R&D projects and to fuel Proteros’ Discovery Pipeline of truly novel lead compounds with first-in-class/best-in-class potential in areas with proven medical needs such as oncology and neurology.
- Meet the need for de-novo or highly challenging protein structure analysis
- Guarantee best of core competencies
- Provide high quality scientific validation
- Ensure market relevance
Proteros' own R&D projects are based on the huge experience of its scientists and technicians in integrated target identification and lead generation and can draw on the existing equipment and proprietary technologies. The huge amount of already existing information in Proteros’ compound databases and libraries as well as outstanding relationships to key opinion leaders in universities and institutions around the world are cornerstones when generating high-quality leads for challenging targets in the areas of kinases, epigenetic targets and G-protein-coupled receptors (GPCRs).
Protein Kinases are key regulators of cell functions that constitute one of the largest and most functionally diverse gene families. By adding phosphate groups to substrate proteins, they direct the activity, localization and overall functions of many proteins, and serve to coordinate the activities of almost all cellular processes. Despite numerous kinase inhibitors, currently in early discovery and pre-clinical development, the number of approved drugs based on kinase inhibition remains very low. This discrepancy reflects the challenges of developing ATP-competitive kinase inhibitors, including low specificity and off-target binding that can cause severe side-effects and limited use for oncology indications. Allosteric regulation of kinases by binding an effector molecule provides the opportunity to identify selective inhibitors providing the therapeutic window.
- Huge experience in Kinase Structural Biology
- Unique assay technologies for Kinases
Epigenetic mechanisms are seen as key regulators of genomic information. Epigenetic factors are observable as DNA methylation, histone modification and small regulatory RNAs. In recent years the field of epigenetics has grown into one of the most dynamic areas of biological research, and is increasingly the focus of drug screening activities with the potential to address disease-causing dysfunctions with small molecules in essentially all fields of indication.
- Proprietary technologies to generate homogenously modified nucleosomes – the universal substrate for all epigenetic enzymes.
- RDA assay technology to select long residence time compounds to explore the full potential of epigenetic targets.
- Kinetic and thermodynamic profiling using nucleosomal substrates supported by high-resolution structures of on- and off-target isoenzymes to develop selective compounds.
G-protein-coupled receptors (GPCRs), the largest family of cell-surface molecules responsible for cellular signal transmission are involved in a wide variety of physiological processes and are associated with many diseases including various cancers. As a consequence, GPCRs worked as target molecules of approximately 40% of all modern medicinal drugs. A structure-based approach offers tremendous potential to accelerate the identification of selective small molecules to modify GPCRs. Proteros’ unique expertise and proprietary technical platforms allow for high-quality
- Quantification of functional GPCR expression
- Screening for GPCR conformations
- Crystallization of GPCR proteins
- Structure analysis