Arrestin regulation of small GTPases

Abstract

The regulation of small GTPases by arrestins is a relatively new way by which arrestin can exert influence over cell signalling cascades, hence, molecular interactions and specific binding partners are still being discovered. A pathway showcasing the regulation of GTPase activity by β-arrestin was first elucidated in 2001. Since this original study, growing evidence has emerged for arrestin modulation of GTPase activity through direct interactions and also via the scaffolding of GTPase regulatory proteins. Given the importance of small GTPases in a variety of essential cellular functions, pharmacological manipulation of this pathway may represent an area with therapeutic potential, particularly with respect to cancer pathology and cardiac hypertrophy. The regulation of small GTPases by arrestins is a relatively new way by which arrestin can exert influence over cell signalling cascades, hence, molecular interactions and specific binding partners are still being discovered. A pathway showcasing the regulation of GTPase activity by β-arrestin was first elucidated in 2001. Since this original study, growing evidence has emerged for arrestin modulation of GTPase activity through direct interactions and also via the scaffolding of GTPase regulatory proteins. Given the importance of small GTPases in a variety of essential cellular functions, pharmacological manipulation of this pathway may represent an area with therapeutic potential, particularly with respect to cancer pathology and cardiac hypertrophy. © 2014 Springer-Verlag Berlin Heidelberg.