THE SCIENCE.
NOVAPEP’S NOVEL POLYPEPTIDE STRUCTURES HERALD A FIRST-IN-CLASS PEPTIDE DRUG FOR THE TREATMENT OF INDICATIONS WHERE THERE ARE UNMET MEDICAL NEEDS.
Activated Protein C:
Activated Protein C ('APC') has demonstrated anti-inflammatory and cytoprotective effects.
Protease-activated receptors (PARs) are a subfamily of four G protein coupled receptors (GPCR) activated by APC proteolytic cleavage of their N-terminal extracellular tail. PARs are expressed in many cell types, including endothelial cells, platelets, fibroblasts, immune cells, myocytes, neurons, and gastrointestinal tract cells.
APC has potent anti-inflammatory, cytoprotective and regenerative properties and has been shown to be an effective therapeutic in numerous animal disease models.
Figure A. below illustrates APC’s effective mechanisms of action on Protease-activated Receptors PAR-1 and PAR-3.
Figure B. below illustrates the P1 and P3 agonist peptides which mimic APC’s anti-inflammatory mechanisms of action.
Figure C. below shows the linked form of P1 and P3 peptides called NVP-202, which generates synergistic cell-signalling effects significantly greater than P1 and P3 individually.
Figure D. The PAR3 derived (P3) peptide reduces caspase-1 activity synergistically in the presence of the PAR1 peptide (P1) or when it is covalently linked to P1 in the bivalent G10 peptide (aka NVP202) and G10 is proven to reduce activation of the NLPR3 inflammasome reflected by the reduction of caspase-1 activity.
