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MMK1. A Potent and Selective Agonist of FPR2 G-Protein Coupled Receptors.
Chemotactic factors from both Gram-positive and Gram-negative bacteria are short peptides with N-formyl methionine at the N-terminus (extensively reviewed in reference 1). These peptides are released from bacteria during infection and activate formyl peptide receptor (FPR), a member of G-protein coupled receptors (GPCRs). In human, the FPR family consists mainly of three receptors, FPR1, FPR2/ALX (formerly FPRL1), and FPR3 (formerly FPRL2) which all couple to the G\\_i\\ subtype of G-proteins and ultimately lead to the activation of phospholipase C and intracellular Ca²⁺ increase.
MMK1 is a selective and potent agonist of the Formylpeptide receptor FPR2, which was originally derived from a random peptide library and was identified by a novel autocrine selection method in yeasts engineered to express human FPR2.
FPR2 is expressed in the promyelocytic leukemia cell line HL-60 as well as in the chronic myelogenous leukemia cell line K562. In human neutrophils, 1 μM MMK1 induces Ca²⁺ influx which is blocked by the specific FPR2 antagonist WRW4.

Resveratrol, a constituent of grape seeds, induces Ca²⁺ influx in human monocytes which is blocked by10 nM MMK1, demonstrating that the inhibition of chemoattractant receptors contribute to the anti-inflammatory properties of resveratrol. G-Protein Coupled Receptor Ligands; Formylpeptide Receptor Ligands.

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