V-ATPase inhibitors and implication in cancer treatment

Summary Acidity is one of the main features of the tumors. The V-ATPase is the primary responsible for the control of tumor microenvironment by proton extrusion to the extracellular medium. The acid environment favors tissue damage, activation of destructive enzymes in the extracellular matrix, the...

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Bibliographic Details
Published in:Cancer treatment reviews 2009-12, Vol.35 (8), p.707-713
Main Authors: Pérez-Sayáns, Mario, Somoza-Martín, José Manuel, Barros-Angueira, Francisco, Rey, José Manuel Gándara, García-García, Abel
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
Archazolid
Bafilomycin
Bridged Bicyclo Compounds, Heterocyclic - pharmacology
Bridged Bicyclo Compounds, Heterocyclic - therapeutic use
Cell Survival
Chemoresistance
Concanamycin
Drug Resistance, Neoplasm
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Enzyme Inhibitors - therapeutic use
Hematology, Oncology and Palliative Medicine
Humans
Indolyls
Macrolides - pharmacology
Macrolides - therapeutic use
Salicylihalamide
Tumor cell growth
Tumor metastasis
V-ATPase inhibitors
V-ATPases
Vacuolar Proton-Translocating ATPases - antagonists & inhibitors
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Summary:Summary Acidity is one of the main features of the tumors. The V-ATPase is the primary responsible for the control of tumor microenvironment by proton extrusion to the extracellular medium. The acid environment favors tissue damage, activation of destructive enzymes in the extracellular matrix, the acquisition of metastatic cell phenotypes as well as increasing the destructive capacity. The application of specific inhibitors of V-ATPases, can decrease the acidity of tumor and may allow the reduction of tumor metastasis, acting on the survival of tumor cells and prevent the phenomena of chemoresistance. Among the most important inhibitors can be distinguished benzolactone enamides (salicylihalamide), lobatamide A and B, apicularen, indolyls, oximidine, macrolactone archazolid, lobatamide C, and cruentaren. The latest generation of inhibitors includes NiK12192, FR202126, and PPI SB 242784. The purpose of this paper is to describe the latest advances in the field of V-ATPase inhibitors, describe further developments related to the classic inhibitors, and discuss new potential applications of these drugs in cancer treatment.
ISSN:0305-7372
1532-1967
DOI:10.1016/j.ctrv.2009.08.003