Kinetics of penetration influence the apparent potency of vanilloids on TRPV1.
AuthorsLazar J, Braun DC, Tóth A, Wang Y, Pearce LV, Pavlyukovets VA, Blumberg PM, Garfield SH, Wincovitch S, Choi HK, Lee J,
JournalMol Pharmacol
PubMed ID16418338
'Evidence that the ligand binding site of TRPV1 lies on the inner face of the plasma membrane and that much of the TRPV1 itself is localized to internal membranes suggests that the rate of ligand entry into the cell may be an important determinant of the kinetics of ligand action. ... More
Antimicrobial peptides: the LPS connection.
AuthorsGiuliani A, Pirri G, Rinaldi AC,
JournalMethods Mol Biol
PubMed ID20094863
'An expanding body of evidence is rendering manifest that many cationic antimicrobial peptides are endowed with different properties and activities, well beyond their direct action on microbes. One of the most interesting and potentially important research avenue on the alternative use of antimicrobial peptides grounds on their affinity toward lipopolysaccharide ... More
Self-delivering nanoemulsions for dual fluorine-19 MRI and fluorescence detection.
AuthorsJanjic JM, Srinivas M, Kadayakkara DK, Ahrens ET,
JournalJ Am Chem Soc
PubMed ID18266363
We report the design, synthesis, and biological testing of highly stable, nontoxic perfluoropolyether (PFPE) nanoemulsions for dual 19F MRI-fluorescence detection. A linear PFPE polymer was covalently conjugated to common fluorescent dyes (FITC, Alexa647 and BODIPy-TR), mixed with pluronic F68 and linear polyethyleneimine (PEI), and emulsified by microfluidization. Prepared nanoemulsions (<200 ... More
Probing the cathepsin D using a BODIPY FL-pepstatin A: applications in fluorescence polarization and microscopy.
AuthorsChen CS, Chen WN, Zhou M, Arttamangkul S, Haugland RP
JournalJ Biochem Biophys Methods
PubMed ID10737220
Redistribution of cathepsin D, a major lysosomal aspartic endopeptidase, has been related to various pathological progressions during tumor formation and oxidation stress. We have synthesized a fluorescent probe for cathepsin D, where the pepstatin A was covalently conjugated with the BODIPY (Boron dipyrromethene difluoride) fluorophore. In vitro, BODIPY FL-pepstatin A ... More
Anti-endotoxin agents. 1. Development of a fluorescent probe displacement method optimized for the rapid identification of lipopolysaccharide-binding agents.
AuthorsWood SJ, Miller KA, David SA
JournalComb Chem High Throughput Screen
PubMed ID15134530
Lipopolysaccharides (LPS), otherwise termed 'endotoxins', are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of 'Septic Shock', a major cause of mortality in the critically ill patient. Therapeutic options aimed at limiting downstream systemic inflammatory processes by targeting lipopolysaccharide do not exist at the present ... More