Drug intelligence / Profile preview

golgicide A

Development stage
Unknown
Modality
Small Molecules
01

Overview

Golgicide A is a potent, highly specific, and reversible small-molecule inhibitor of Golgi brefeldin A-resistant guanine nucleotide exchange factor 1 (GBF1), a cis-Golgi ArfGEF. It binds within the interfacial cleft formed between ADP-ribosylation factor 1 (Arf1) and the GBF1 Sec7 domain, preventing Arf1 activation and subsequent coatomer protein complex I (COPI) recruitment to Golgi membranes. This disruption leads to the rapid disassembly and dispersal of the Golgi apparatus and trans-Golgi network (TGN). Golgicide A is widely used as a research tool to study Golgi assembly, secretory pathways, retrograde transport of bacterial toxins (such as Shiga toxin), and viral replication (such as Hepatitis C virus and enteroviruses).

Other names
6,8-Difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline6,8-difluoro-3a,4,5,9b-tetrahydro-4-(3-pyridinyl)-3H-cyclopenta[c]quinolineGolgicide A
02

Targets

ARF1 (ADP-ribosylation factor 1)GBF1 (Golgi-specific brefeldin A-resistance guanine nucleotide exchange factor 1)

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