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LG186: an inhibitor of GBF1 function that causes Golgi disassembly in human and canine cells
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Boal, Frederic, Guetzoyan, Lucie, Sessions, Richard B., Zeghouf, Mahel, Spooner, Robert A. , Lord, Mike, Cherfils, Jacqueline, Clarkson, Guy J., Roberts, L. M. (Lynne M.) and Stephens, David J. (2010) LG186: an inhibitor of GBF1 function that causes Golgi disassembly in human and canine cells. Traffic, Vol.11 (No.12). pp. 1537-1551. doi:10.1111/j.1600-0854.2010.01122.x ISSN 1398-9219.
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Official URL: http://dx.doi.org/10.1111/j.1600-0854.2010.01122.x
Abstract
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. Brefeldin A (BFA) is relatively non-selective inhibiting at least three targets in human cells, Golgi brefeldin A resistance factor 1 (GBF1), brefeldin A inhibited guanine nucleotide exchange factor 1 (BIG1) and brefeldin A inhibited guanine nucleotide exchange factor 2 (BIG2). Here, we show that the previously described compound Exo2 acts through inhibition of Arf-GEF function, but causes other phenotypic changes that are not GBF1 related. We describe the engineering of Exo2 to produce LG186, a more selective, reversible inhibitor of Arf-GEF function. Using multiple-cell-based assays and GBF1 mutants, our data are most consistent with LG186 acting by selective inhibition of GBF1. Unlike other Arf-GEF and reported GBF1 inhibitors including BFA, Exo2 and Golgicide A, LG186 induces disassembly of the Golgi stack in both human and canine cells.
| Item Type: | Journal Article | ||||
|---|---|---|---|---|---|
| Subjects: | Q Science > QH Natural history > QH301 Biology | ||||
| Divisions: | Faculty of Science, Engineering and Medicine > Science > Life Sciences (2010- ) > Biological Sciences ( -2010) Faculty of Science, Engineering and Medicine > Science > Chemistry |
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| Journal or Publication Title: | Traffic | ||||
| Publisher: | Wiley-Blackwell Publishing Ltd. | ||||
| ISSN: | 1398-9219 | ||||
| Official Date: | December 2010 | ||||
| Dates: |
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| Volume: | Vol.11 | ||||
| Number: | No.12 | ||||
| Number of Pages: | 15 | ||||
| Page Range: | pp. 1537-1551 | ||||
| DOI: | 10.1111/j.1600-0854.2010.01122.x | ||||
| Status: | Peer Reviewed | ||||
| Publication Status: | Published | ||||
| Access rights to Published version: | Restricted or Subscription Access | ||||
| Funder: | Biotechnology and Biological Sciences Research Council (Great Britain) (BBSRC), Medical Research Council (Great Britain) (MRC), Assocation pour la Recherche contre le Cancer, ANR Physique-Chimie du Vivant |
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