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
Brefeldin A affects growth, endoplasmic reticulum, Golgi bodies, tubular vacuole system, and secretory pathway in Pisolithus tinctorius.
AuthorsCole L, Davies D, Hyde GJ, Ashford AE
JournalFungal Genet Biol
PubMed ID10919378
'Brefeldin A (BFA) reduced radial growth in Pisolithus tinctorius at a concentration as low as 2 microM. Use of endoplasmic reticulum (ER)-Tracker dye, unconjugated BFA, and fluorescent BFA (BODIPY-BFA) allowed comparison of the effects of BFA on the endomembrane system of P. tinctorius at the light and electron microscope levels. ... More
Block copolymers modify the internalization of micelle-incorporated probes into neural cells.
AuthorsMaysinger D, Berezovska O, Savic R, Soo PL, Eisenberg A
JournalBiochim Biophys Acta
PubMed ID11420118
An important therapeutic concern is rate and extent of internalization of drugs into cells. Hydrophilic agents often internalize poorly and slowly, and highly lipophilic ones too rapidly. The incorporation of drugs into micelles allows regulation of their internalization parameters, and newly-described block copolymers can be selectively tailored to suit specific ... More
Fluorescent conjugates of brefeldin A selectively stain the endoplasmic reticulum and Golgi complex of living cells.
AuthorsDeng Y, Bennink JR, Kang HC, Haugland RP, Yewdell JW
JournalJ Histochem Cytochem
PubMed ID7543914
The fungal metabolite brefeldin A (BFA) interferes with vesicular trafficking in most animal cells. To gain insight into the mechanism of BFA action, we esterified it to the fluorophore, boron dipyromethene difluoride (BODIPY). BODIPY-BEA localized predominantly in the endoplasmic reticulum (ER) and Golgi complex of viable cells and was extracted ... More