Protein kinase C regulates the internalization and function of the human organic anion transporting polypeptide 1A2.

ABSTRACT:

Background and purpose

The human organic anion transporting polypeptide 1A2 (OATP1A2) is expressed in cells from several regions of the human body, including the kidney, cholangiocytes and the blood-brain barrier, and mediates the cellular flux of various anionic substances, including drugs in clinical use. Several related mammalian transporters have been shown to be subject to post-translational regulation, including kinase-induced internalization. In the present study the role of protein kinase C (PKC) in the regulation of OATP1A2 was investigated in an in vitro cell model.

Experimental approach

COS-7 cells in which OATP1A2 was overexpressed were treated with the PKC-specific activator (phorbol 12-myristate 13-acetate; PMA) and the PKC-specific inhibitor (Go6976). The impa

SUBMITTER: Zhou F 

PROVIDER: S-EPMC3058169 | biostudies-literature | 2011 Mar

REPOSITORIES: biostudies-literature