Drug Discovery Approach | Taking clues from nature
We identify new drug sites for allosteric modulation of proteins and design new therapeutics
Proteins are complex three-dimensional molecules with tremendous degrees of freedom.
Proteins are in a constant state of flux and their precise folding topology is dictated by their micro-environment. Specific regions of a protein can be highly sensitive to external changes in the micro-environment. This is especially true for certain regions of the protein where specific binding ligands may alter the localized micro-environment in such a way as to allow (or disallow) the protein to adopt a different conformation.
Identification of these target regions, and specific binding ligands that alter protein conformation, is at the heart of the Serometrix platform.
Dynamic Drug Discoverysm Platform
Unraveling the complexities of protein-protein interactions is a challenging task.
Taking an entirely new approach, Serometrix developed the Dynamic Drug Discoverysm Platform which identifies:
- specific protein-protein interaction sites
- allosteric drug sites
- evolutionarily based prototype ligands that we call Peptimer™ compounds (Peptimer™ = Compound containing peptide bonds with MW <900Da)
Platform & Process Highlights
- Applicable to all proteins or complexes with a known structure
- Can provide both positive and negative modulators for the same target
- Typically shows more than one potential site per protein
- Offers new drug sites for old or intractable targets
- Provides greater selectivity where target is a member of a closely related protein family with similar functional sites
- Offers more subtle control possibilities other than “on/off”
- Efficiently Exposes Natural Regulatory Mechanism of Action (MOA)
- Rapidly Provides Prototype Ligands (Peptimer™ Compounds) without High Throughput Screening (HTS)
- Optimization of Peptimer™ Compounds to Small Molecule Leads
- Provides for robust Intellectual Property with composition-of-matter and general methods
- Focus on High-Value Protein Targets (validated by mAbs, GOF/LOF mutational data or strong understanding of biology)