Synthetic CREB targeting phosphopeptide sequences inhibit CREB
ubiquitination in a phosphorylation-dependent manner.
(A) Baseline level of CREB ubiquitination is detectable
in T84 cells (Lane 1). Lane 2 represents normoxic CREB in the presence
of the double-phosphorylated CREB-targeting phosphopeptide. Lane 3
represents hypoxic CREB in the absence of peptide treatment, and lanes
4–8 (left to right) represent CREB from hypoxia-treated cells in the
presence of the HIV-tat peptide alone, HIV-tat with scrambled peptide,
HIV-tat with the unphosphorylated CREB-targeting peptide, HIV-tat with
the single-phosphorylated CREB-targeting peptide, and HIV-tat with the
double-phosphorylated CREB-targeting peptide, respectively. Data are
representative of two experiments. (B) The CREB
targeting sequence is a substrate for PP1 dephosphorylation.
(Left) Coincubation of the phosphorylated form of the
CREB-targeting sequence (2P) with purified PP1 results in the
liberation of free phosphate when compared with the unphosphorylated
control (Ctl; No P; n = 6, P <
0.05). A threonine phosphopeptide (Ctl PP) served as a positive
control. (Right) The phosphatase inhibitors okadaic acid
(4 μM) and calyculin A (400 nM) abolished PP1-mediated
dephosphorylation of the phosphorylated targeting sequence of CREB
(n = 6, P < 0.05).
(C) Hypoxia decreases phosphopeptide dephosphorylation.
Coincubation of the double-phosphorylated CREB-targeting sequence (2P)
with normoxic T84 (Upper) but not hypoxic
(Lower) lysates results in peptide dephosphorylation as
measured by HPLC (representative tracings of two experiments). Abs.,
absorbance.