Urokinase receptor derived peptides as potent inhibitors of the formyl peptide receptor type 1-triggered cell migration
Copyright policy )Urokinase receptor derived peptides as potent inhibitors of the formyl peptide receptor type 1-triggered cell migration
The receptor for the urokinase-type plasminogen activator (uPAR) is a widely recognized master regulator of cell migration. We and others have previously documented that the uPAR(84-95) sequence, interacts with the formyl peptide receptors (FPR)s, henceforth inducing cell migration of several cell lines, including leukocytes, and the synthetic shorter peptide (Ser88-Arg-Ser-Arg-Tyr92, SRSRY) retains chemotactic activity in vitro and in vivo. Recently, we have developed the head-to-tail cyclic analog [SRSRY], a new potent and stable inhibitor of monocyte trafficking. This prompted us to develop novel cyclic and linear analogs of [SRSRY] with the aim to broaden the knowledge about structure-activity relationships of peptide [SRSRY]. Herein we report their synthesis, effects on cell migration, conformational and docking analyses which served to envisage a new pharmacophore model for inhibitors of FPR1-triggered cell migration.
Formyl peptide receptors; Peptide conformational analysis; Peptide inhibitors of cell migration; Peptide structure-activity relationships; Urokinase-type plasminogen activator receptor; Animals; Cell Line, Tumor; Cell Movement; Dose-Response Relationship, Drug; Humans; Molecular Structure; Peptides; Rats; Receptors, Formyl Peptide; Receptors, Urokinase Plasminogen Activator; Structure-Activity Relationship; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry, Cell Line, Receptors, Urokinase Plasminogen Activator, Dose-Response Relationship, Structure-Activity Relationship, Peptide conformational analysis, Cell Movement, Cell Line, Tumor, Receptors, Animals, Humans, Pharmacology, Tumor, Dose-Response Relationship, Drug, Molecular Structure, Drug Discovery3003 Pharmaceutical Science, Organic Chemistry, Receptors, Formyl Peptide, Peptide structure-activity relationships, Rats, Urokinase Plasminogen Activator, Peptide inhibitors of cell migration, Urokinase-type plasminogen activator receptor, Drug, Formyl Peptide, Peptides, Formyl peptide receptors
Formyl peptide receptors; Peptide conformational analysis; Peptide inhibitors of cell migration; Peptide structure-activity relationships; Urokinase-type plasminogen activator receptor; Animals; Cell Line, Tumor; Cell Movement; Dose-Response Relationship, Drug; Humans; Molecular Structure; Peptides; Rats; Receptors, Formyl Peptide; Receptors, Urokinase Plasminogen Activator; Structure-Activity Relationship; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry, Cell Line, Receptors, Urokinase Plasminogen Activator, Dose-Response Relationship, Structure-Activity Relationship, Peptide conformational analysis, Cell Movement, Cell Line, Tumor, Receptors, Animals, Humans, Pharmacology, Tumor, Dose-Response Relationship, Drug, Molecular Structure, Drug Discovery3003 Pharmaceutical Science, Organic Chemistry, Receptors, Formyl Peptide, Peptide structure-activity relationships, Rats, Urokinase Plasminogen Activator, Peptide inhibitors of cell migration, Urokinase-type plasminogen activator receptor, Drug, Formyl Peptide, Peptides, Formyl peptide receptors
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