Peptides-to-Drugs (P2D)

Our proprietary Peptides-to-Drugs (P2D) platform enables the efficient discovery of both peptidomimetic and small molecule drug candidates against protein targets which are difficult to approach with conventional drug discovery methods. The ability to discover both peptidomimetic and small molecule drug candidates allows us to address both acute and chronic disease indications that are related to the same protein target. Our P2D platform combines novel peptide chemistry technologies with state-of-the-art medicinal chemistry and computer-aided drug design capabilities. Our P2D platform is based on our proprietary technologies SPOT™ and PepMed™.

SPOT™

SPOT™ is a fully-automated high-throughput-synthesis (HTS) and screening process to generate peptides and peptidomimetics. With SPOT™ thousands of molecules can be synthesized at once and are then screened for binding to a target protein. The molecules are screened either directly on membranes or they are released from the membrane for HTS screening. SPOT™ strongly supports extensive pharmacophore mapping. It synthesizes and screens thousands of derivatives of a peptide lead molecule before transforming it into a peptidomimetic or small molecule. SPOT™ is protected by global patents.

PepMed™

PepMed™ is a proprietary medicinal chemistry platform which systematically transforms peptide leads into peptidomimetics or small molecules. After lead peptides have been identified with biological and chemical methods, their pharmacophore information is extracted from SPOT™ arrays. Subsequently, the pharmacophore information is used to identify small molecules with drug-like properties. With PepMed™, Jerini can transform the pharmacophore data of lead peptides or peptidomimetics directly into small molecules. This is an important advance over historical attempts to produce small molecules from peptides. In a virtual screen, small molecule scaffolds matching the pharmacophore model derived from the peptide-based structure-activity-relationship (SAR) data are selected from an extensive library of compounds. The small molecule scaffolds are subsequently optimized using medicinal chemistry methodology. The PepMed™ transformation is supported by advanced NMR and X-ray techniques.