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Chemical Compound Review

AC1NUQYJ     (3Z,5E,7R,8S,9S,11E,13E,15S,16 R)-16-[(2S...

Synonyms: NSC381866
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Disease relevance of NSC381866


High impact information on NSC381866


Chemical compound and disease context of NSC381866


Biological context of NSC381866

  • Bafilomycin A1 alone caused increased DNA laddering of genomic DNA and increased nuclear staining for fragmented DNA in neonatal cardiomyocyte apoptosis in a dose- and time-dependent manner [9].
  • The acidity of the Golgi lumen dissipated rapidly upon addition of bafilomycin A1, a blocker of vacuolar-type ATPases, pHG remained constant despite acidification of the cytosol by reversal of the plasmalemmal Na+/H+ antiport [15].
  • Treating cells with either U-18666A, a compound that creates an NPC-like phenotype, or with bafilomycin A1, a compound that raises late endosomal pH, has no effect on labeling of NPC1-YFP, suggesting that both drugs affect processes other than NPC1 binding to cholesterol [16].
  • In isolated rabbit ciliary body preparations examined under voltage-clamped conditions, bafilomycin A1 produced a concentration-dependent decrease in short-circuit current, and topical application of bafilomycin A1 reduced intraocular pressure in rabbits, indicating an essential role of the V-ATPase in ciliary epithelial ion transport [17].
  • Endosomal membrane potential was required for viral infection because cotreatment of cells with monensin partially overcame the inhibitory effect of bafilomycin A1 [18].

Anatomical context of NSC381866


Associations of NSC381866 with other chemical compounds


Gene context of NSC381866

  • Importantly, bafilomycin A1 reverses CAL-mediated CFTR degradation [27].
  • Blocking receptor trafficking to lysosomes with bafilomycin A1 had no effect on basal turnover of either subtype but blocked agonist-stimulated beta 2AR turnover [28].
  • Blocking TIMP-2 degradation with bafilomycin A1 significantly increased cell-associated TIMP-2 levels in the presence of high calcium [29].
  • U1 RNA-stimulated, but not TLR-3 ligand-stimulated, IFN-I was blocked by bafilomycin A1, indicating that immunostimulation by U1 RNA requires endosomal acidification [30].
  • High copy expression of STV1 partially restores vacuolar acidification in a delta vph1 mutant strain; solubilization and fractionation of membrane proteins from these vacuoles show that Stv1p co-purifies with bafilomycin A1-sensitive ATPase activity and with the 60- and 69-kDa V-ATPase subunits [31].

Analytical, diagnostic and therapeutic context of NSC381866


  1. Role of autophagy in temozolomide-induced cytotoxicity for malignant glioma cells. Kanzawa, T., Germano, I.M., Komata, T., Ito, H., Kondo, Y., Kondo, S. Cell Death Differ. (2004) [Pubmed]
  2. Identification of a gene for a polyamine transport protein in yeast. Tomitori, H., Kashiwagi, K., Sakata, K., Kakinuma, Y., Igarashi, K. J. Biol. Chem. (1999) [Pubmed]
  3. Active vacuolar H+ATPase is required for both endocytic and exocytic processes during viral infection of BHK-21 cells. Palokangas, H., Metsikkö, K., Väänänen, K. J. Biol. Chem. (1994) [Pubmed]
  4. Bafilomycin A1 inhibits bone resorption and tooth eruption in vivo. Sundquist, K.T., Marks, S.C. J. Bone Miner. Res. (1994) [Pubmed]
  5. Bafilomycin A1 inhibits Helicobacter pylori-induced vacuolization of HeLa cells. Papini, E., Bugnoli, M., De Bernard, M., Figura, N., Rappuoli, R., Montecucco, C. Mol. Microbiol. (1993) [Pubmed]
  6. pH-dependent perforation of macrophage phagosomes by listeriolysin O from Listeria monocytogenes. Beauregard, K.E., Lee, K.D., Collier, R.J., Swanson, J.A. J. Exp. Med. (1997) [Pubmed]
  7. Degradation of T cell receptor (TCR)-CD3-zeta complexes after antigenic stimulation. Valitutti, S., Müller, S., Salio, M., Lanzavecchia, A. J. Exp. Med. (1997) [Pubmed]
  8. Autophagy is involved in T cell death after binding of HIV-1 envelope proteins to CXCR4. Espert, L., Denizot, M., Grimaldi, M., Robert-Hebmann, V., Gay, B., Varbanov, M., Codogno, P., Biard-Piechaczyk, M. J. Clin. Invest. (2006) [Pubmed]
  9. Enhanced expression of p53 and apoptosis induced by blockade of the vacuolar proton ATPase in cardiomyocytes. Long, X., Crow, M.T., Sollott, S.J., O'Neill, L., Menees, D.S., de Lourdes Hipolito, M., Boluyt, M.O., Asai, T., Lakatta, E.G. J. Clin. Invest. (1998) [Pubmed]
  10. Specific inhibitors of vacuolar H(+)-ATPase trigger apoptotic cell death of osteoclasts. Okahashi, N., Nakamura, I., Jimi, E., Koide, M., Suda, T., Nishihara, T. J. Bone Miner. Res. (1997) [Pubmed]
  11. Activation of p38 and ERK signaling during adenovirus vector cell entry lead to expression of the C-X-C chemokine IP-10. Tibbles, L.A., Spurrell, J.C., Bowen, G.P., Liu, Q., Lam, M., Zaiss, A.K., Robbins, S.M., Hollenberg, M.D., Wickham, T.J., Muruve, D.A. J. Virol. (2002) [Pubmed]
  12. Adeno-associated virus type 2-mediated gene transfer: altered endocytic processing enhances transduction efficiency in murine fibroblasts. Hansen, J., Qing, K., Srivastava, A. J. Virol. (2001) [Pubmed]
  13. Inhibitory mechanisms of H(+)-ATPase inhibitor bafilomycin A1 and carbonic anhydrase II inhibitor acetazolamide on experimental bone resorption. Ohba, Y., Ohba, T., Sumitani, K., Tagami-Kondoh, K., Hiura, K., Miki, Y., Kakegawa, H., Takano-Yamamoto, T., Katunuma, N. FEBS Lett. (1996) [Pubmed]
  14. Vanadate and bafilomycin A1 are potent inhibitors of the ATPase activity of the reconstituted bacterial ATP-binding cassette transporter for maltose (MalFGK2). Hunke, S., Döse, S., Schneider, E. Biochem. Biophys. Res. Commun. (1995) [Pubmed]
  15. Dynamic measurement of the pH of the Golgi complex in living cells using retrograde transport of the verotoxin receptor. Kim, J.H., Lingwood, C.A., Williams, D.B., Furuya, W., Manolson, M.F., Grinstein, S. J. Cell Biol. (1996) [Pubmed]
  16. Binding between the Niemann-Pick C1 protein and a photoactivatable cholesterol analog requires a functional sterol-sensing domain. Ohgami, N., Ko, D.C., Thomas, M., Scott, M.P., Chang, C.C., Chang, T.Y. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  17. Vacuolar H+-ATPase in ocular ciliary epithelium. Wax, M.B., Saito, I., Tenkova, T., Krupin, T., Becker, B., Nelson, N., Brown, D., Gluck, S.L. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  18. pH-independent entry and sequential endosomal sorting are major determinants of hepadnaviral infection in primary hepatocytes. Funk, A., Mhamdi, M., Hohenberg, H., Will, H., Sirma, H. Hepatology (2006) [Pubmed]
  19. Acid extrusion is induced by osteoclast attachment to bone. Inhibition by alendronate and calcitonin. Zimolo, Z., Wesolowski, G., Rodan, G.A. J. Clin. Invest. (1995) [Pubmed]
  20. Role of ATP7B in biliary copper excretion in a human hepatoma cell line and normal rat hepatocytes. Harada, M., Sakisaka, S., Terada, K., Kimura, R., Kawaguchi, T., Koga, H., Taniguchi, E., Sasatomi, K., Miura, N., Suganuma, T., Fujita, H., Furuta, K., Tanikawa, K., Sugiyama, T., Sata, M. Gastroenterology (2000) [Pubmed]
  21. Base treatment corrects defects due to misfolding of mutant cystic fibrosis transmembrane conductance regulator. Namkung, W., Kim, K.H., Lee, M.G. Gastroenterology (2005) [Pubmed]
  22. Transport from late endosomes to lysosomes, but not sorting of integral membrane proteins in endosomes, depends on the vacuolar proton pump. van Weert, A.W., Dunn, K.W., Gueze, H.J., Maxfield, F.R., Stoorvogel, W. J. Cell Biol. (1995) [Pubmed]
  23. Cell entry and cAMP imaging of anthrax edema toxin. Dal Molin, F., Tonello, F., Ladant, D., Zornetta, I., Zamparo, I., Di Benedetto, G., Zaccolo, M., Montecucco, C. EMBO J. (2006) [Pubmed]
  24. Effect of vacuolar proton ATPase on pHi, Ca2+, and apoptosis in neonatal cardiomyocytes during metabolic inhibition/recovery. Karwatowska-Prokopczuk, E., Nordberg, J.A., Li, H.L., Engler, R.L., Gottlieb, R.A. Circ. Res. (1998) [Pubmed]
  25. Integrin Ligands Mobilize Ca2+ from Ryanodine Receptor-gated Stores and Lysosome-related Acidic Organelles in Pulmonary Arterial Smooth Muscle Cells. Umesh, A., Thompson, M.A., Chini, E.N., Yip, K.P., Sham, J.S. J. Biol. Chem. (2006) [Pubmed]
  26. Cathepsin D triggers Bax activation, resulting in selective apoptosis-inducing factor (AIF) relocation in T lymphocytes entering the early commitment phase to apoptosis. Bidère, N., Lorenzo, H.K., Carmona, S., Laforge, M., Harper, F., Dumont, C., Senik, A. J. Biol. Chem. (2003) [Pubmed]
  27. Modulation of mature cystic fibrosis transmembrane regulator protein by the PDZ domain protein CAL. Cheng, J., Wang, H., Guggino, W.B. J. Biol. Chem. (2004) [Pubmed]
  28. Resistance of the human beta 1-adrenergic receptor to agonist-mediated down-regulation. Role of the C terminus in determining beta-subtype degradation. Liang, W., Austin, S., Hoang, Q., Fishman, P.H. J. Biol. Chem. (2003) [Pubmed]
  29. Calcium regulation of matrix metalloproteinase-mediated migration in oral squamous cell carcinoma cells. Munshi, H.G., Wu, Y.I., Ariztia, E.V., Stack, M.S. J. Biol. Chem. (2002) [Pubmed]
  30. "Endogenous adjuvant" activity of the RNA components of lupus autoantigens Sm/RNP and Ro 60. Kelly, K.M., Zhuang, H., Nacionales, D.C., Scumpia, P.O., Lyons, R., Akaogi, J., Lee, P., Williams, B., Yamamoto, M., Akira, S., Satoh, M., Reeves, W.H. Arthritis Rheum. (2006) [Pubmed]
  31. STV1 gene encodes functional homologue of 95-kDa yeast vacuolar H(+)-ATPase subunit Vph1p. Manolson, M.F., Wu, B., Proteau, D., Taillon, B.E., Roberts, B.T., Hoyt, M.A., Jones, E.W. J. Biol. Chem. (1994) [Pubmed]
  32. Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, inhibits acidification and protein degradation in lysosomes of cultured cells. Yoshimori, T., Yamamoto, A., Moriyama, Y., Futai, M., Tashiro, Y. J. Biol. Chem. (1991) [Pubmed]
  33. Endocytosis of heparin-binding protein (CAP37) is essential for the enhancement of lipopolysaccharide-induced TNF-alpha production in human monocytes. Heinzelmann, M., Platz, A., Flodgaard, H., Polk, H.C., Miller, F.N. J. Immunol. (1999) [Pubmed]
  34. Bafilomycin A1 inhibits the action of tetanus toxin in spinal cord neurons in cell culture. Williamson, L.C., Neale, E.A. J. Neurochem. (1994) [Pubmed]
  35. Insulin-stimulated cytosol alkalinization facilitates optimal activation of glucose transport in cardiomyocytes. Yang, J., Gillingham, A.K., Hodel, A., Koumanov, F., Woodward, B., Holman, G.D. Am. J. Physiol. Endocrinol. Metab. (2002) [Pubmed]
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