Although more than 50% of current therapeutics modulates GPCR activities, only few of these pharmaceuticals target peptide-activated GPCRs. This investigation is aimed to design and develop the peptidomimetic agonists for formyl peptide receptor (FPR), one of the peptide-activated GPCRs. The proposed peptidomimetics will be designed to mimic the natural peptide ligand of FPR, N-formyl-methionine-leucine-phenylalanine (fMLF). These peptidomimetics have potential to be drug leads, as they resist to the degradation by proteases and peptidases, thereby increase the bioavailability over the natural peptides.
(a) To design and generate peptidomimetics mimic FPR ligand.
(b) To determine the ability of the compounds synthesized in (a) to bind to FPR.
(c) To test the compounds synthesized in (a) for their ability to elicit FPR signaling responses.
(d) To test of the resistance of compounds against degradation by proteases or peptidases (if necessary).
