• Treatment of transfected cells either with the Ca2+ ionophore A23187, or with the ER Ca2+-ATPase inhibitor thapsigargin, resulted in a five- to sevenfold increase of the expression of chloramphenicol acetyltransferase protein. (nih.gov)
  • Previously, we reported that emptying of intracellular Ca(2+) pools with endoplasmatic Ca(2+)-ATP-ase inhibitor thapsigargin leads to the Na(+) influx in human lymphocytes (M. Tepel et al. (semanticscholar.org)
  • Intravesicular 45 Ca transport was measured after the addition of glycolytic substrates and cofactors specific for each of the glycolytic reactions being studied or after the addition of exogenous ATP and was expressed as transport sensitive to the specific Ca 2+ -ATPase inhibitor thapsigargin. (ahajournals.org)
  • Due to its ability to kill mammalian cells, thapsigargin has been used as a therapeutic target to induce apoptosis in cancer cells with a low rate of cell proliferation, thus with resistance to standard anti-proliferative chemotherapy. (biomedcentral.com)
  • The cells were incubated at 37°C for 1h in media containing different concentrations of ab120286 (thapsigargin) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. (abcam.com)
  • As thapsigargin has been frequently applied at concentrations up to 2 microM, its inhibitory action on plasma-membrane Ca2+ fluxes deserves consideration. (biochemj.org)
  • In this study, the influence of external calcium concentrations and thapsigargin on the phagocytosis of polystyrene latex beads by the macrophage-like cell lines MH-S (murine) and differentiated U937 (human) was analyzed. (biomedcentral.com)
  • It appears to act intracellularly, as incubation of isolated rat liver microsomes with thapsigargin induces a rapid, dose-dependent release of stored Ca2+. (pnas.org)
  • Analysis of the promoter deletion constructs revealed that A23187- and thapsigargin-responsive regions are confined to two regions (-115 to -260 and -685 to -1,763) in the calreticulin promoter that contain the CCAAT nucleotide sequences. (nih.gov)
  • The thapsigargin-releasable pool of microsomal Ca2+ includes the pools sensitive to inositol 1,4,5-trisphosphate and GTP. (pnas.org)
  • Thapsigargin and DBHQ did not potentiate protein kinase C-mediated signals such as direct phosphorylation of myristoylated alanine-rich C-kinase substrate, activation of mitogen-activated protein kinase, and tyrosine phosphorylation of bands 110,000-130,000 and 70,000-80,000. (mysciencework.com)
  • A23187- and thapsigargin-dependent increase in calreticulin mRNA levels (A) and protein levels (B). (A) Nontransfected NIH/3T3 cells were incubated for 16 h with 7 μM A23187, 100 nM thapsigargin, or DMSO. (nih.gov)
  • Molecularly, while both Rab7 and Vps16 are essential regulatory components for endocytic fusion with lysosomes, we found that Rab7 but not Vps16 is required for complete autophagy flux, and that thapsigargin blocks recruitment of Rab7 to autophagosomes. (dundee.ac.uk)
  • One of these prodrugs termed G202 consists of an analog of the highly toxic natural product thapsigargin coupled to a peptide recognized as a substrate by the protease Prostate-Specific Membrane Antigen. (wikipedia.org)
  • Another mechanism, reported here for the first time, deals with RX871024-induced mobilization of Ca 2+ from nonmitochondrial thapsigargin-sensitive intracellular stores. (diabetesjournals.org)
  • The implications of this mechanism of action for the application of thapsigargin in the analysis of Ca2+ homeostasis and possible forms of Ca2+ control are discussed. (pnas.org)
  • In the present study we examined the mechanism underlying the thapsigargin-induced Na(+) entry. (semanticscholar.org)
  • Thapsigargin does not affect autophagosome formation but leads to accumulation of mature autophagosomes by blocking autophagosome fusion with the endocytic system. (dundee.ac.uk)
  • Queen's University researchers have successfully synthesized the anticancer agent thapsigargin, which could now open the door to the creation of new cancer drugs. (phys.org)
  • in another, stores were partially emptied using thapsigargin plus caffeine, after which syntillas were decreased. (rupress.org)
  • Their effects are mimicked by the pharmacological agent, thapsigargin, which is sometimes used in fluid secretion assays when a kinin is not available. (wikipedia.org)
  • Strikingly, thapsigargin has no effect on endocytosis-mediated degradation of epidermal growth factor receptor. (dundee.ac.uk)
  • This paradigm shift away from the ER derives from seminal studies, again in sea urchin egg, that showed NAADP-mediated Ca2+ release was sensitive to agents that target acidic organelles (e.g. bafilomycin A1) but was less sensitive to ones that interfere with ER Ca2+ storage (e.g. thapsigargin). (wikipedia.org)