2m3n | pdb_00002m3n
Peptide leucine arginine
Structural highlights
Function[PLR_RANPI] Mast cell degranulating peptide. Antiproliferative activity against human breast and ovarian tumor cell lines in vitro. Inhibits granulopoiesis in rat in vitro. Causes histamine release from rat peritoneal mast cells in vitro. Has antibacterial activity against Gram-positive bacteria B.megaterium Bm11, S.lentus and M.luteus, and antifungal activity against C.tropicalis, C.guiller-mondii and P.nicotianae spores. Has hemolytic activity. The mature peptide inserts into the hydrophobic core of the bacterial cell membrane and increases permeability without disrupting membrane integrity. Probably binds to the outer membrane surface before aggregating to form transmembrane pores.[1] [2] [3] Publication Abstract from PubMedThe peptide leucine arginine (pLR) belongs to a new class of cyclic peptides isolated from frog skin. Its primary sequence is similar to the reactive loop of plant Bowman-Birk inhibitors (BBI), and the recently discovered circular sunflower trypsin inhibitor-1 (SFTI-1). The conformational properties of pLR in solution were determined by NMR spectroscopy and revealed excellent structural similarity to BBI and SFTI-1. Moreover, pLR is a highly potent trypsin inhibitor, with Ki values in the nanomolar range, and, due to its small size, a potential inhibitor of the serine protease tryptase. Since tryptase plays a crucial role in the development of allergic airway inflammation, the therapeutic potential of pLR in a murine asthma model was investigated. Treatment of ovalbumin-sensitized mice with pLR during allergen challenge reduced the acute asthma phenotype. Most importantly, application even at the end of a long-lasting chronic asthma model decreased the development of chronic airway inflammation and tissue remodeling. Therapeutic Potential of the Peptide Leucine Arginine As a New Nonplant Bowman-Birk-Like Serine Protease Inhibitor.,Rothemund S, Sonnichsen FD, Polte T J Med Chem. 2013 Aug 29. PMID:23988198[4] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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