Drug intelligence / Profile preview

bafilomycin

Development stage
Preclinical
Lead developer
Streptomyces griseus (natural product origin)
Modality
RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
In Vitro (research Use)
01

Overview

Bafilomycin refers to a family of toxic macrolide antibiotics produced by various Streptomyces species. The most widely studied member is bafilomycin A1. Bafilomycins are potent and specific inhibitors of vacuolar-type H+-ATPase (V-ATPase), an enzyme complex responsible for acidifying intracellular compartments such as lysosomes and endosomes. By inhibiting V-ATPase, bafilomycins prevent the acidification required for lysosomal proteases to function, thereby blocking autophagic flux at the stage of autophagosome-lysosome fusion and subsequent degradation. This mechanism makes them valuable research tools in studies of autophagy and endosomal trafficking. Bafilomycins also exhibit anti-tumor, anti-parasitic, immunosuppressant, antifungal activity and have been shown to impair mitochondrial function as potassium ionophores[1][2][5][8].

Other names
bafilomycinbafilomycinsbafilomycin A1
02

Targets

ATP1A3 (Na+/K+-ATPase alpha-3)ATP6V0C (ATPase H+ transporting V0 subunit c)

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