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leads to reversal of angiotensin II-stimulated b -arrestin ubiquitination from
a sustained to a transient pattern, with a corresponding reversal of AT 1a R- b -
arrestin binding from stable endosome-localized complexes to transiently
associated complexes seen only at the plasma membrane. Quite unexpectedly,
however, the same b -arrestin mutant is stably ubiquitinated and associated
tightly with two other activated class B receptors, the V 2 R and neurokinin 1
receptor. Furthermore, V 2 R-stimulated b -arrestin ubiquitination is impaired
in a quintuple lysine mutant b -arrestin2 in which five lysines at positions 18,
107, 108, 207, and 296 are altered to ariginines. 56 These provocative findings
suggest that different 7TMRs are capable of inducing sustained b -arrestin
ubiquitination at distinct sites on b -arrestin2. Whether the susceptibility of
target lysines in b -arrestin is a result of distinct conformational changes or
whether it reflects the activity of distinct E3 ubiquitin ligases that bind and
modify different domains in b -arrestin remains an important topic for future
studies.
Unlike stable ubiquitination that is targeted to specific lysines in
b -arrestin2, transient ubiquitination appears to be a random modification
because it is eliminated only when all the lysines in b -arrestin2 are mutated
to arginines ( b -arrestin2-0K). 51 Although b -arrestin2-0K is capable of
equivalent protein-protein interactions with the b 2 AR as the non-
ubiquitinated wild-type protein in vitro , in a cellular context it shows impair-
ment in binding because unlike the wild type, it cannot be ubiquitinated at
proper site(s). In fact, the recruitment of b -arrestin2-0K-GFP to either
b 2 AR or V 2 R is very transient and detected only when GRKs are over-
expressed to augment receptor phosphorylation or when activated receptor
complexes are forcibly retained at the plasma membrane by blocking inter-
nalization. 51 Accordingly, ubiquitination of b -arrestin2 is not required for its
initial recruitment to the cell-surface 7TMR, but it is required for
prolonging and stabilizing the b -arrestin-receptor interaction.
2.3. Functional effects
Apart from stabilizing receptor interaction as discussed above, ubiquitination
of b -arrestin has been shown to promote both its endocytic and scaffolding
functions. While earlier studies had indicated a dependence of b 2 AR inter-
nalization on b -arrestin ubiquitination status, later studies carried out with
two modified b -arrestins, namely, b -arrestin2-0K that lacks ubiquitin
acceptor sites and b -arrestin2-Ub which remains stably ubiquitinated have
provided important
insights. 51
b -Arrestin2-0K does not promote
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