PTPN5 + Fragment ERK2

PTPN5 + Fragment ERK2

PTPN5 + Fragment ERK2: Human striatal enriched protein tyrosine phosphatase (STEP) in complex with a fragment of the ERK2 activation loop
PDB Code: 2CJZ
PTPN5 is a member of the KIM (kinase interaction motif) domain containing phosphatases and the R7 family of receptor tyrosine phosphatases (PTP’s). In cells, PTPN5 counter balances the activity of MAP kinases in the cytosol and is therefore critical regulators of the cellular response to extracellular stimuli. It is a brain-specific phosphatase expressed preferentially in neurons of the striatum, hippocampus and cortex. Alternative splicing of PTPN5 produces a number of isoforms which are either membrane-associated (e.g. STEP61) or shorter cytosolic variants (STEP46). In addition, a recent study links PTPN5 to disease progression of Alzheimer’s disease suggesting this phosphatase as an interesting drug target.
The structure of PTPN5 is characterized by an atypical WPD-loop conformation. This catalytically important loop has been shown to switch between a closed and an open conformation upon substrate binding. In order to understand how this particular WPD loop conformation influences substrate binding we generated also an inactive mutant in which the active site cysteine (Cys472) has been mutated to a serine residue and co-crystallized this mutant with the a fragment of the ERK2 activation loop (DHTGFLpTEpYVATR), a specific PTPN5 substrate. The structure of the substrate complex was solved at 1.7 Å resolution and refined to an R-factor of 17.5% (R free 20.5%). However, only the phosphotyrosine was visible in the electron density suggesting that the flanking peptide residues are disordered. Despite the unstructured peptide sequence the well resolved phosphotyrosine residue gave still interesting insight in substrate recognition in the active site as well as in rearrangements in the PTPN5 structure in the presence of substrate.

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