brefeldin a


Summary: A fungal metabolite which is a macrocyclic lactone exhibiting a wide range of antibiotic activity.

Top Publications

  1. Ito Y, Uemura T, Shoda K, Fujimoto M, Ueda T, Nakano A. cis-Golgi proteins accumulate near the ER exit sites and act as the scaffold for Golgi regeneration after brefeldin A treatment in tobacco BY-2 cells. Mol Biol Cell. 2012;23:3203-14 pubmed publisher
    ..expressing multiple Golgi markers tagged by different fluorescent proteins and observed their responses to brefeldin A (BFA) treatment and BFA removal...
  2. Kim S, Bassham D. TNO1 is involved in salt tolerance and vacuolar trafficking in Arabidopsis. Plant Physiol. 2011;156:514-26 pubmed publisher
    ..The tno1 mutant had delayed formation of the brefeldin A (BFA) compartment in cotyledons upon application of BFA, suggesting less efficient membrane fusion processes in ..
  3. Pantazopoulou A, Peñalva M. Organization and dynamics of the Aspergillus nidulans Golgi during apical extension and mitosis. Mol Biol Cell. 2009;20:4335-47 pubmed publisher
    ..b>Brefeldin A transiently collapses late and early GEs into distinct aggregates containing Sec7/mRFP-PH(OSBP) and GrhA-GFP, ..
  4. Wlodkowic D, Skommer J, Pelkonen J. Brefeldin A triggers apoptosis associated with mitochondrial breach and enhances HA14-1- and anti-Fas-mediated cell killing in follicular lymphoma cells. Leuk Res. 2007;31:1687-700 pubmed
    ..Herein we report for the first time the effects of an ER-Golgi transport inhibitor, Brefeldin A (BFA), alone and in combination with a small molecule Bcl-2 inhibitor HA14-1 or agonistic anti-Fas mAb, in the ..
  5. Verheije M, Raaben M, Mari M, te Lintelo E, Reggiori F, van Kuppeveld F, et al. Mouse hepatitis coronavirus RNA replication depends on GBF1-mediated ARF1 activation. PLoS Pathog. 2008;4:e1000088 pubmed publisher
    ..We now show that MHV replication is sensitive to brefeldin A (BFA)...
  6. Cho M, Lee S, Cho H. P-glycoprotein4 displays auxin efflux transporter-like action in Arabidopsis root hair cells and tobacco cells. Plant Cell. 2007;19:3930-43 pubmed
    ..b>Brefeldin A partially interfered with the trafficking of PGP4 reversibly, and this was rescued by pretreatment with auxin...
  7. Reichardt I, Stierhof Y, Mayer U, Richter S, Schwarz H, Schumacher K, et al. Plant cytokinesis requires de novo secretory trafficking but not endocytosis. Curr Biol. 2007;17:2047-53 pubmed
    ..Our results suggest that during plant cytokinesis, unlike animal cytokinesis, protein secretion is absolutely essential, whereas endocytosis is not. ..
  8. Goueslain L, Alsaleh K, Horellou P, Roingeard P, Descamps V, Duverlie G, et al. Identification of GBF1 as a cellular factor required for hepatitis C virus RNA replication. J Virol. 2010;84:773-87 pubmed publisher
    ..Here, we used brefeldin A (BFA) to investigate cellular mechanisms involved in HCV infection...
  9. Soni K, Mardones G, Sougrat R, Smirnova E, Jackson C, Bonifacino J. Coatomer-dependent protein delivery to lipid droplets. J Cell Sci. 2009;122:1834-41 pubmed publisher
    ..Here we demonstrate that ATGL and ADRP, but not TIP47, are delivered to LDs by a pathway mediated by the COPI and COPII coatomer proteins and their corresponding regulators. ..

More Information


  1. Maruyama N, Okuda E, Tatsuhara M, Utsumi S. Aggregation of proteins having Golgi apparatus sorting determinant induces large globular structures derived from the endoplasmic reticulum in plant seed cells. FEBS Lett. 2008;582:1599-606 pubmed publisher
    ..These results indicate that aggregation of the Golgi protein blocks transport from the ER to the Golgi. ..
  2. Kleine Vehn J, Dhonukshe P, Sauer M, Brewer P, Wisniewska J, Paciorek T, et al. ARF GEF-dependent transcytosis and polar delivery of PIN auxin carriers in Arabidopsis. Curr Biol. 2008;18:526-31 pubmed publisher
    ..Our data suggest that an ARF GEF-dependent transcytosis-like mechanism is operational in plants and provides a plausible mechanism to trigger changes in PIN polarity and hence auxin fluxes during embryogenesis and organogenesis. ..
  3. Boal F, Guetzoyan L, Sessions R, Zeghouf M, Spooner R, Lord J, et al. LG186: An inhibitor of GBF1 function that causes Golgi disassembly in human and canine cells. Traffic. 2010;11:1537-51 pubmed publisher
    b>Brefeldin A-mediated inhibition of ADP ribosylation factor (Arf) GTPases and their guanine nucleotide exchange factors, Arf-GEFs, has been a cornerstone of membrane trafficking research for many years...
  4. Li J, Gao Z, Kehoe V, Xing J, King N, Sinoway L. Interstitial adenosine triphosphate modulates muscle afferent nerve-mediated pressor reflex. Muscle Nerve. 2008;38:972-7 pubmed publisher
    ..05 vs. control). In contrast, glibenclamide (an inhibitor of the ATP-binding cassette protein), monensin, and brefeldin A, which interfere with vesicular formation (or trafficking) and inhibit exocytosis, did not significantly affect ..
  5. Takáč T, Pechan T, Richter H, Muller J, Eck C, Böhm N, et al. Proteomics on brefeldin A-treated Arabidopsis roots reveals profilin 2 as a new protein involved in the cross-talk between vesicular trafficking and the actin cytoskeleton. J Proteome Res. 2011;10:488-501 pubmed publisher
    ..Here, proteomic and cell biology approaches were applied to study effects of brefeldin A (BFA), an inhibitor of vesicle recycling and secretion, in Arabidopsis roots...
  6. Silady R, Ehrhardt D, Jackson K, Faulkner C, Oparka K, Somerville C. The GRV2/RME-8 protein of Arabidopsis functions in the late endocytic pathway and is required for vacuolar membrane flow. Plant J. 2008;53:29-41 pubmed
    ..The GRV2-positive endosomes were sensitive to Wortmannin but not brefeldin A (BFA), consistent with GRV2 operating late in the endocytic pathway, prior to delivery of vesicles to the ..
  7. Greaves J, Salaun C, Fukata Y, Fukata M, Chamberlain L. Palmitoylation and membrane interactions of the neuroprotective chaperone cysteine-string protein. J Biol Chem. 2008;283:25014-26 pubmed publisher
    ..Palmitoylation of an ER-localized mutant could be rescued by brefeldin A treatment, which promotes the mixing of ER and Golgi membranes...
  8. Teh O, Moore I. An ARF-GEF acting at the Golgi and in selective endocytosis in polarized plant cells. Nature. 2007;448:493-6 pubmed the Golgi but is also required for selective internalization from the plasma membrane in the presence of brefeldin A (BFA)...
  9. Foresti O, De Marchis F, de Virgilio M, Klein E, Arcioni S, Bellucci M, et al. Protein domains involved in assembly in the endoplasmic reticulum promote vacuolar delivery when fused to secretory GFP, indicating a protein quality control pathway for degradation in the plant vacuole. Mol Plant. 2008;1:1067-76 pubmed publisher delivered to the vacuole and fragmented, in a process that is inhibited by the secretory traffic inhibitor brefeldin A. Moreover, a fusion between GFP and a domain of the maize storage protein gamma-zein involved in zein ..
  10. Cheng F, Zamski E, Guo W, Pharr D, Williamson J. Salicylic acid stimulates secretion of the normally symplastic enzyme mannitol dehydrogenase: a possible defense against mannitol-secreting fungal pathogens. Planta. 2009;230:1093-103 pubmed publisher
    ..After SA treatment, MTD was not detected in the Golgi apparatus, and its SA-induced secretion was resistant to brefeldin A, an inhibitor of Golgi-mediated protein transport...
  11. Verghese P, Arrese E, Howard A, Soulages J. Brefeldin A inhibits cholesterol efflux without affecting the rate of cellular uptake and re-secretion of apolipoprotein A-I in adipocytes. Arch Biochem Biophys. 2008;478:161-6 pubmed publisher
    ..the rates of apoA-I induced cholesterol efflux and apoA-I recycling in the presence and in the absence of Brefeldin A (BFA)...
  12. Chen L, Jondal M. Brefeldin A inhibits vesicular MHC class I processing in resting but not in CpG- and disruption-activated DC. Mol Immunol. 2008;46:158-65 pubmed publisher
    ..Here we investigate the sensitivity of this VP to Brefeldin A (BFA), a fungal metabolite which inhibits vesicular trafficking by preventing the activation of some ADP-..
  13. Ster J, de Bock F, Bertaso F, Abitbol K, Daniel H, Bockaert J, et al. Epac mediates PACAP-dependent long-term depression in the hippocampus. J Physiol. 2009;587:101-13 pubmed publisher
    ..Altogether these results provided evidence for a new form of hippocampal LTD. ..
  14. Kim S, Ryan T. Synaptic vesicle recycling at CNS snapses without AP-2. J Neurosci. 2009;29:3865-74 pubmed publisher
    ..These results demonstrate that in the absence of AP-2, SV proteins still become endocytosed, and synaptic vesicle recycling remains operational. ..
  15. Laniosz V, Dabydeen S, Havens M, Meneses P. Human papillomavirus type 16 infection of human keratinocytes requires clathrin and caveolin-1 and is brefeldin a sensitive. J Virol. 2009;83:8221-32 pubmed publisher
  16. Schotman H, Karhinen L, Rabouille C. dGRASP-mediated noncanonical integrin secretion is required for Drosophila epithelial remodeling. Dev Cell. 2008;14:171-82 pubmed publisher
    ..We speculate that this mechanism might be used during development as a means of targeting a specific subset of transmembrane proteins to the plasma membrane. ..
  17. Ortiz Zapater E, Soriano Ortega E, Marcote M, Ortiz Masia D, Aniento F. Trafficking of the human transferrin receptor in plant cells: effects of tyrphostin A23 and brefeldin A. Plant J. 2006;48:757-70 pubmed
    ..In contrast, treatment with brefeldin A, which inhibits recycling from endosomes back to the plasma membrane in plant cells, leads to the accumulation ..
  18. Madison S, Nebenführ A. Live-cell imaging of dual-labeled Golgi stacks in tobacco BY-2 cells reveals similar behaviors for different cisternae during movement and brefeldin A treatment. Mol Plant. 2011;4:896-908 pubmed publisher tobacco BY-2 cells to distinguish sub-compartments of the Golgi during monensin treatments, movement, and brefeldin A (BFA)-induced disassembly...
  19. Hummel E, Schmickl R, Hinz G, Hillmer S, Robinson D. Brefeldin A action and recovery in Chlamydomonas are rapid and involve fusion and fission of Golgi cisternae. Plant Biol (Stuttg). 2007;9:489-501 pubmed
    ..These structures then divide by vertical fission to produce Golgi stacks of normal size and morphology roughly 60 min after drug wash-out...
  20. Richter S, Geldner N, Schrader J, Wolters H, Stierhof Y, Rios G, et al. Functional diversification of closely related ARF-GEFs in protein secretion and recycling. Nature. 2007;448:488-92 pubmed
  21. Langhans M, Hawes C, Hillmer S, Hummel E, Robinson D. Golgi regeneration after brefeldin A treatment in BY-2 cells entails stack enlargement and cisternal growth followed by division. Plant Physiol. 2007;145:527-38 pubmed
    b>Brefeldin A (BFA) treatment stops secretion and leads to the resorption of much of the Golgi apparatus into the endoplasmic reticulum...
  22. Halter D, Neumann S, van Dijk S, Wolthoorn J, De Mazière A, Vieira O, et al. Pre- and post-Golgi translocation of glucosylceramide in glycosphingolipid synthesis. J Cell Biol. 2007;179:101-15 pubmed
    ..FAPP2 knockdown strongly reduces GM3 synthesis. Overall, we show that newly synthesized GlcCer enters two pathways: one toward the noncytosolic surface of a post-Golgi membrane and one via the ER toward the Golgi lumen LacCer synthase. ..
  23. Larsson D, Wickström M, Hassan S, Oberg K, Granberg D. The cytotoxic agents NSC-95397, brefeldin A, bortezomib and sanguinarine induce apoptosis in neuroendocrine tumors in vitro. Anticancer Res. 2010;30:149-56 pubmed
    The aim of this study was to investigate the apoptosis resulting from NSC 95397, brefeldin A, bortezomib and sanguinarine in neuroendocrine tumor cell lines...
  24. Robinson D, Jiang L, Schumacher K. The endosomal system of plants: charting new and familiar territories. Plant Physiol. 2008;147:1482-92 pubmed publisher
  25. Pantazopoulou A, Peñalva M. Characterization of Aspergillus nidulans RabC/Rab6. Traffic. 2011;12:386-406 pubmed publisher
    ..rabC? mutants, showing markedly impaired apical extension, have conspicuously fragmented, brefeldin A-insensitive early and late GEs, indicating that the Golgi network organization requires RabC...
  26. Anders N, Jurgens G. Large ARF guanine nucleotide exchange factors in membrane trafficking. Cell Mol Life Sci. 2008;65:3433-45 pubmed publisher
    ..This review summarizes recent findings on the function of large ARF-GEFs, and the use of the inhibitor Brefeldin A as a potent tool in understanding membrane trafficking...
  27. Vogel F, Hofius D, Sonnewald U. Intracellular trafficking of Potato leafroll virus movement protein in transgenic Arabidopsis. Traffic. 2007;8:1205-14 pubmed
    ..Interestingly, inhibition of the 26S proteasome led to aggregation of MP17 in aggresome-like structures. Formation of these structures could be inhibited by colchicine, as was shown for aggresomes in mammalian cells. ..
  28. Fernández Ulibarri I, Vilella M, Lázaro Diéguez F, Sarri E, Martínez S, Jimenez N, et al. Diacylglycerol is required for the formation of COPI vesicles in the Golgi-to-ER transport pathway. Mol Biol Cell. 2007;18:3250-63 pubmed
    ..Our findings implicate diacylglycerol in the retrograde transport of proteins from Golgi to the ER and suggest that it plays a critical role at a late stage of COPI vesicle formation. ..
  29. Lam S, Cai Y, Tse Y, Wang J, Law A, Pimpl P, et al. BFA-induced compartments from the Golgi apparatus and trans-Golgi network/early endosome are distinct in plant cells. Plant J. 2009;60:865-81 pubmed publisher
    b>Brefeldin A (BFA) is a useful tool for studying protein trafficking and identifying organelles in the plant secretory and endocytic pathways...
  30. Islam A, Shen X, Hiroi T, Moss J, Vaughan M, Levine S. The brefeldin A-inhibited guanine nucleotide-exchange protein, BIG2, regulates the constitutive release of TNFR1 exosome-like vesicles. J Biol Chem. 2007;282:9591-9 pubmed
    ..We investigated whether the brefeldin A (BFA)-inhibited guanine nucleotide-exchange proteins, BIG1 and/or BIG2, are required for TNFR1 release from ..
  31. Patterson G, Hirschberg K, Polishchuk R, Gerlich D, Phair R, Lippincott Schwartz J. Transport through the Golgi apparatus by rapid partitioning within a two-phase membrane system. Cell. 2008;133:1055-67 pubmed publisher
    ..Simulation and experimental testing of this rapid partitioning model reproduced all the key characteristics of the Golgi apparatus, including polarized lipid and protein gradients, exponential cargo export kinetics, and cargo waves. ..
  32. Matto M, Sklan E, David N, Melamed Book N, Casanova J, Glenn J, et al. Role for ADP ribosylation factor 1 in the regulation of hepatitis C virus replication. J Virol. 2011;85:946-56 pubmed publisher
    ..Huh7.5 cells, in which HCV replicates and produces infectious viral particles, were exposed to brefeldin A or golgicide A, pharmacological inhibitors of Arf1 activation...
  33. Schoberer J, Runions J, Steinkellner H, Strasser R, Hawes C, Osterrieder A. Sequential depletion and acquisition of proteins during Golgi stack disassembly and reformation. Traffic. 2010;11:1429-44 pubmed publisher
    ..apparatus in tobacco leaf epidermal cells in response to the induced expression of the GTP-locked Sar1p or Brefeldin A (BFA), and reassembly on BFA washout...
  34. Kleine Vehn J, Dhonukshe P, Swarup R, Bennett M, Friml J. Subcellular trafficking of the Arabidopsis auxin influx carrier AUX1 uses a novel pathway distinct from PIN1. Plant Cell. 2006;18:3171-81 pubmed actin-dependent constitutive trafficking, which is not sensitive to the vesicle trafficking inhibitor brefeldin A. AUX1 subcellular dynamics are not influenced by the auxin influx inhibitor NOA but are blocked by the auxin ..
  35. Wann A, Ingram K, Coleman P, McHale N, Levick J. Mechanosensitive hyaluronan secretion: stimulus-response curves and role of transcription-translation-translocation in rabbit joints. Exp Physiol. 2009;94:350-61 pubmed publisher
    ..the transcription-translation inhibitors actinomycin D and puromycin and by the Golgi translocation inhibitor brefeldin A. There is thus a graded coupling between HA secretion and cyclic joint movement that depends partly on new ..
  36. Gonzales E, van der Zee M, Dictus W, van den Biggelaar J. Brefeldin A or monensin inhibits the 3D organizer in gastropod, polyplacophoran, and scaphopod molluscs. Dev Genes Evol. 2007;217:105-18 pubmed
    ..To elucidate 3D function in a standardized fashion, we used monensin and brefeldin A (BFA) to rapidly and reversibly interfere with protein processing and secretion, thereby inhibiting the ..
  37. Tagami Y, Watanabe Y. Effects of brefeldin A on the localization of Tobamovirus movement protein and cell-to-cell movement of the virus. Virology. 2007;361:133-40 pubmed
    ..Treatment with brefeldin A (BFA), which disrupts ER-to-Golgi transport, inhibited the formation of irregularly shaped and filamentous ..
  38. Casanova J. Regulation of Arf activation: the Sec7 family of guanine nucleotide exchange factors. Traffic. 2007;8:1476-85 pubmed
    ..Here we review recent progress in our understanding of the structure, localization and biology of the different classes of Arf GEFs. ..
  39. Langhans M, Robinson D. 1-Butanol targets the Golgi apparatus in tobacco BY-2 cells, but in a different way to Brefeldin A. J Exp Bot. 2007;58:3439-47 pubmed
    ..Since the fungal lactone Brefeldin A (BFA) also prevents COPI-vesicle production by the Golgi apparatus, the sequential and simultaneous application ..
  40. Citterio C, Vichi A, Pacheco Rodriguez G, Aponte A, Moss J, Vaughan M. Unfolded protein response and cell death after depletion of brefeldin A-inhibited guanine nucleotide-exchange protein GBF1. Proc Natl Acad Sci U S A. 2008;105:2877-82 pubmed publisher
    ..Three mammalian GEFs are inhibited by brefeldin A (BFA)...
  41. Vicetti Miguel R, Maryak S, Cherpes T. Brefeldin A, but not monensin, enables flow cytometric detection of interleukin-4 within peripheral T cells responding to ex vivo stimulation with Chlamydia trachomatis. J Immunol Methods. 2012;384:191-5 pubmed publisher
    ..trachomatis genital tract infection were used to compare the ability of brefeldin A (BFA) and monensin (MN) to concurrently trap interferon-? (IFN-?), tumor necrosis factor (TNF), interleukin (IL)..
  42. Amenós M, Corrales I, Poschenrieder C, Illes P, Baluska F, Barceló J. Different effects of aluminum on the actin cytoskeleton and brefeldin A-sensitive vesicle recycling in root apex cells of two maize varieties differing in root elongation rate and aluminum tolerance. Plant Cell Physiol. 2009;50:528-40 pubmed publisher
    ..Visualization of boron-cross-linked rhamnogalacturonan II (RGII)-containing brefeldin A (BFA) compartments revealed that Al inhibited the formation of these compartments, especially in variety 16x36...
  43. Moon J, Kim S, Shin S, Park J. Regulation of brefeldin A-induced ER stress and apoptosis by mitochondrial NADP?-dependent isocitrate dehydrogenase. Biochem Biophys Res Commun. 2012;417:760-4 pubmed publisher
    b>Brefeldin A (BFA), an endoplasmic reticulum (ER)-Golgi transport inhibitor, has been shown to cause accumulation of proteins in the ER, ER stress, and ultimately apoptosis...
  44. Saint Jore Dupas C, Nebenführ A, Boulaflous A, Follet Gueye M, Plasson C, Hawes C, et al. Plant N-glycan processing enzymes employ different targeting mechanisms for their spatial arrangement along the secretory pathway. Plant Cell. 2006;18:3182-200 pubmed
    ..We conclude that the localization of N-glycan processing enzymes corresponds to an assembly line in the early secretory pathway and depends on both TMD length and signals in the cytoplasmic tail. ..
  45. Micaroni M, Perinetti G, Berrie C, Mironov A, Mironov A. The SPCA1 Ca2+ pump and intracellular membrane trafficking. Traffic. 2010;11:1315-33 pubmed publisher
    ..and delays retrograde redistribution of the GA glycosylation enzymes into the endoplasmic reticulum caused by brefeldin A; however, exit of these enzymes from the endoplasmic reticulum is not affected...
  46. Manolea F, Chun J, Chen D, Clarke I, Summerfeldt N, Dacks J, et al. Arf3 is activated uniquely at the trans-Golgi network by brefeldin A-inhibited guanine nucleotide exchange factors. Mol Biol Cell. 2010;21:1836-49 pubmed publisher
    ..These results suggest that Arf3 plays a unique function at the TGN that likely involves recruitment by a specific receptor. ..
  47. Kwok S, Daskal I. Brefeldin A activates CHOP promoter at the AARE, ERSE and AP-1 elements. Mol Cell Biochem. 2008;319:203-8 pubmed publisher
    b>Brefeldin A induces apoptosis in PC-3 and MCF-7 cells at a concentration of 30 ng/ml. RT-PCR analyses showed up-regulation of CHOP/GADD153 and splicing of XBP-1 mRNA in brefeldin A-treated cells...
  48. Canals M, Lopez Gimenez J, Milligan G. Cell surface delivery and structural re-organization by pharmacological chaperones of an oligomerization-defective alpha(1b)-adrenoceptor mutant demonstrates membrane targeting of GPCR oligomers. Biochem J. 2009;417:161-72 pubmed publisher
  49. Belov G, Feng Q, Nikovics K, Jackson C, Ehrenfeld E. A critical role of a cellular membrane traffic protein in poliovirus RNA replication. PLoS Pathog. 2008;4:e1000216 pubmed publisher
    ..Virus replication is inhibited by brefeldin A (BFA), implicating some components(s) of the cellular secretory pathway in virus growth...
  50. Chun J, Shapovalova Z, Dejgaard S, Presley J, Melancon P. Characterization of class I and II ADP-ribosylation factors (Arfs) in live cells: GDP-bound class II Arfs associate with the ER-Golgi intermediate compartment independently of GBF1. Mol Biol Cell. 2008;19:3488-500 pubmed publisher
    ..Live cell imaging detected Arfs on peripheral puncta that also contained Golgi-specific brefeldin A (BFA) resistance factor (GBF) 1 and the ERGIC marker p58...
  51. Wang L, Wang Z, Zhang X, FitzHarris G, Baltz J, Sun Q, et al. Brefeldin A disrupts asymmetric spindle positioning in mouse oocytes. Dev Biol. 2008;313:155-66 pubmed
    ..We show here that treating denuded mouse oocytes with brefeldin A, an inhibitor of Golgi-based membrane fusion, abolished the asymmetric positioning of the metaphase I spindle ..
  52. Robinson D, Langhans M, Saint Jore Dupas C, Hawes C. BFA effects are tissue and not just plant specific. Trends Plant Sci. 2008;13:405-8 pubmed publisher
    b>Brefeldin A (BFA) is one of the most popular drugs used by researchers for studies on secretion and endocytosis because it interferes with specific vesicle coat proteins via action on a guanine nucleotide exchange factor...
  53. Genoves A, Navarro J, Pallas V. The Intra- and intercellular movement of Melon necrotic spot virus (MNSV) depends on an active secretory pathway. Mol Plant Microbe Interact. 2010;23:263-72 pubmed publisher
    ..Hence, the secretory pathway inhibitor, Brefeldin A (BFA), and the overexpression of the GTPase-defective mutant of Sar1p, Sar1[H74L], fully retained the p7B ..