Date published: 2025-11-26

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Sar1B Inhibitors

Sar1B inhibitors are chemical entities that can diminish the functional activity of Sar1B, a protein involved in COPII vesicle-mediated transport from the ER to the Golgi. These inhibitors cover categories like protein transport inhibitors (Brefeldin A, Monensin), PI3K inhibitors (Wortmannin, LY294002), retrograde transport inhibitor (Retro-2), dynamin inhibitor (Dynasore), clathrin-mediated endocytosis inhibitor (Pitstop 2), exocytosis inhibitor (Exo1), and protein kinase inhibitors (H89, Go6983, Genistein, Staurosporine). By inhibiting these specific cellular processes and signaling molecules, the inhibitors can influence Sar1B's function without directly blocking its activity.

Brefeldin A and Monensin disrupt protein transport, a process that Sar1B is directly involved in. By inhibiting protein transport, these compounds can disrupt the normal functioning of Sar1B. Similarly, Wortmannin and LY294002 are inhibitors of PI3K, an enzyme that produces PI3P, a phosphoinositide that Sar1B interacts with to recruit proteins to the membrane for vesicle formation. Inhibiting PI3K can therefore result in a reduction of Sar1B-dependent vesicle formation and transport. Retro-2, Dynasore, Pitstop 2, and Exo1 interfere with either retrograde transport, endocytosis, or exocytosis, all vital components of the overall vesicle transport system. By disrupting these processes, these compounds can indirectly affect the function of Sar1B

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