Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists
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Structural optimization of a peptidomimetic antagonist of formyl peptide receptor 2 (FPR2) was explored by an approach involving combination of elements from the two most potent FPR2 antagonists described: a Rhodamine B-conjugated 10-residue gelsonin-derived peptide (i.e., PBP10, RhB-QRLFQVKGRR-OH) and the palmitoylated α-peptide/β-peptoid hybrid Pam-(Lys-βNspe)6-NH2. This generated an array of hybrid compounds from which a new subclass of receptor-selective antagonists was identified. The most potent representatives displayed activity in the low nanomolar range. The resulting stable and potent FPR2-selective antagonists (i.e., RhB-(Lys-βNphe)n-NH2; n = 4–6) are expected to become valuable tools in further elucidation of the physiological role of FPR2 in health and disease.
Original language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 60 |
Issue number | 16 |
Pages (from-to) | 6991-6997 |
ISSN | 0022-2623 |
DOIs | |
Publication status | Published - 2017 |
ID: 182521174