Exo1: a new chemical inhibitor of the exocytic pathway

Proc Natl Acad Sci U S A. 2003 May 27;100(11):6469-74. doi: 10.1073/pnas.0631766100. Epub 2003 May 8.

Abstract

A phenotypic screen was used to search for drug-like molecules that can interfere with specific steps in membrane traffic. 2-(4-Fluorobenzoylamino)-benzoic acid methyl ester (Exo1), identified in this screen, induces a rapid collapse of the Golgi to the endoplasmic reticulum, thus acutely inhibiting the traffic emanating from the endoplasmic reticulum. Like Brefeldin A (BFA), Exo1 induces the rapid release of ADP-ribosylation factor (ARF) 1 from Golgi membranes but has less effect on the organization of the trans-Golgi network. Our data indicate that Exo1 acts by a different mechanism from BFA. Unlike BFA, Exo1 does not induce the ADP-ribosylation of CtBP/Bars50 and does not interfere with the activity of guanine nucleotide exchange factors specific for Golgi-based ARFs. Thus, Exo1 allows the fatty acid exchange activity of Bars50 to be distinguished from ARF1 activity in the control of Golgi tubulation.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenosine Diphosphate Ribose / metabolism
  • Benzamides / chemistry
  • Benzamides / pharmacology*
  • Benzoates / chemistry
  • Benzoates / pharmacology*
  • Brefeldin A / pharmacology
  • Cell Line
  • Exocytosis*
  • Golgi Apparatus / metabolism
  • Guanine Nucleotide Exchange Factors / metabolism
  • Microscopy, Fluorescence
  • Phenotype

Substances

  • 2-(4-fluorobenzoylamino)benzoic acid methyl ester
  • Benzamides
  • Benzoates
  • Guanine Nucleotide Exchange Factors
  • Brefeldin A
  • Adenosine Diphosphate Ribose