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Merck

Targeting K+ channels for cancer therapy.

Journal of experimental therapeutics & oncology (2004-10-27)
Matteo Conti
摘要

A number of experimental evidences in cellular biology and pharmacology demonstrate that K+ channels are involved in the regulatory mechanisms of neoplastic cell proliferation and survival. Among the various types of K+ channels known so far, those that express an inwardly rectifying current (mainly the types named Kir, EAG and HERG) appear of peculiar importance in favoring cancer progression in vivo. In fact, besides helping to maintain a constantly depolarized value of the resting potential required for deregulated tumor growth, they can confer selective advantages to cancer cells in an hypoxic microenvironment, such as that of tumor masses. Inhibitors and modulators of K+ channels have been demonstrated to have the ability to impair cancer cell proliferation in vitro and to counteract cancer progression in vivo. A process of rigorous scientific verification at a pre-clinical level of the anticancer potential of K+ channels inhibitors and modulators have never been rationally performed thus far, but would appear opportune in the light of the data here discussed.