Vacuolar H+-ATPases: Intra- and intermolecular interactions

Mode of Cell Death Induction by Pharmacological Vacuolar H+-ATPase (V-ATPase) Inhibition

“…1S) (3,6). In fact, nanomolar concentrations of archazolid clearly induced apoptosis via caspase activation and the intrinsic pathway induction, phosphorylation of the stress-sensing proteins AMPK and eIF2␣, and inhibition of mTOR.…”

Inhibitors of V-ATPase Proton Transport Reveal Uncoupling Functions of Tether Linking Cytosolic and Membrane Domains of V0 Subunit a (Vph1p)

“…Column 1 contained the negative control (1% DMSO), column 2 contained the positive control (67 M disulfiram), and columns 23 and 24 were the wash wells containing 2-fold diluted SC medium plus 0.1% BSA. This left 320 wells (columns [3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22] to which test compounds were added. The SC medium (2-fold diluted) was distributed into columns 1 and 3-22 (10 l/well).…”

“…In this context, V-ATPase inhibitors are important research tools for studies requiring sudden inhibition of V-ATPases. The most commonly used V-ATPase inhibitors, bafilomycin A and concanamycin A, have been fundamental to the understanding of V-ATPase catalysis, regulation, and cellular functions (12)(13)(14)(15). Bafilomycin A and concanamycin A are now indispensable research tools for the study of important processes in which V-ATPases are involved, including autophagy (16,17) and membrane fusion (18) under normal physiology and pathophysiology.…”

Selective upregulation of TNFα expression in classically-activated human monocyte-derived macrophages (M1) through pharmacological interference with V-ATPase

“…The vacuolar-type H(+)-ATPases (V-ATPases) are ATP-dependent proton translocating macromolecular complexes that acidify lysosomes, endosomes, Golgi apparatus, and certain secretory granules in all eukaryotes [3,4]. V-ATPases participate in physiological processes such as cellular pH homeostasis, receptor-mediated endocytosis, virus and toxin entry, intracellular trafficking as well as protein degradation and processing [3].…”