The SK3/K(Ca)2.3 potassium channel is a new cellular target for edelfosine.

ABSTRACT:

Background and purpose

The 1-O-octadecyl-2-O-methyl-sn-glycero-3-phosphocholine (edelfosine) is an ether-linked phospholipid with promising anti-cancer properties but some side effects that preclude its full clinical therapeutic exploitation. We hypothesized that this lipid could interact with plasma membrane ion channels and modulate their function.

Experimental approach

Using cell migration-proliferation assays, patch clamp, spectrofluorimetry and ¹²⁵I-Apamin binding experiments, we studied the effects of edelfosine on the migration of breast cancer MDA-MB-435s cells, mediated by the small conductance Ca²(+) -activated K(+) channel, SK3/K(Ca)2.3.

Key results

Edelfosine (1 µM) caused plasma membrane depolarization by substantially inhibiting activity of SK3/K(Ca)2.3

SUBMITTER: Potier M 

PROVIDER: S-EPMC3031066 | biostudies-literature | 2011 Jan

REPOSITORIES: biostudies-literature