Discovery and evaluation of nNa_v1.5 sodium channel blockers with potent cell invasion inhibitory activity in breast cancer cells.

ABSTRACT: Voltage-gated sodium channels (VGSC) are a well-established drug target for anti-epileptic, anti-arrhythmic and pain medications due to their presence and the important roles that they play in excitable cells. Recently, their presence has been recognized in non-excitable cells such as cancer cells and their overexpression has been shown to be associated with metastatic behavior in a variety of human cancers. The neonatal isoform of the VGSC subtype, Na_v1.5 (nNa_v1.5) is overexpressed in the highly aggressive human breast cancer cell line, MDA-MB-231. The activity of nNa_v1.5 is known to promote the breast cancer cell invasion in vitro and metastasis in vivo, and its expression in primary mammary tumors has been associated with metastasis and patient death. Me

SUBMITTER: Dutta S 

PROVIDER: S-EPMC5935567 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature