4DC2

Structure of PKC in Complex with a Substrate Peptide from Par-3

4DC2 の概要

• エントリーDOI: 10.2210/pdb4dc2/pdb
• 分子名称: Protein kinase C iota type, Partitioning defective 3 homolog, ADENINE, ... (4 entities in total)
• 機能のキーワード: kinase, substrate, cell polarity, par-3, atypical pkc, transferase-transferase substrate complex, transferase/transferase substrate
• 由来する生物種: Mus musculus (mouse); 詳細
• 細胞内の位置: Cytoplasm (By similarity): Q62074; Endomembrane system: Q9Z340
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 49039.89

構造登録者

Shang, Y.,Wang, C.,Yu, J.,Zhang, M. (登録日: 2012-01-17, 公開日: 2012-07-11, 最終更新日: 2024-11-20)

主引用文献

Wang, C.,Shang, Y.,Yu, J.,Zhang, M.
Substrate recognition mechanism of atypical protein kinase Cs revealed by the structure of PKC iota in complex with a substrate peptide from Par-3
Structure, 20:791-801, 2012

PubMed Abstract: Protein kinase C (PKC) play critical roles in many cellular functions including differentiation, proliferation, growth, and survival. However, the molecular bases governing PKC's substrate recognitions remain poorly understood. Here we determined the structure of PKCι in complex with a peptide from Par-3 at 2.4 Å. PKCι in the complex adopts catalytically competent, closed conformation without phosphorylation of Thr402 in the activation loop. The Par-3 peptide binds to an elongated groove formed by the N- and C-lobes of the kinase domain. The PKCι/Par-3 complex structure, together with extensive biochemical studies, reveals a set of substrate recognition sites common to all PKC isozymes as well as a hydrophobic pocket unique to aPKC. A consensus aPKC's substrate recognition sequence pattern can be readily identified based on the complex structure. Finally, we demonstrate that the pseudosubstrate sequence of PKCι resembles its substrate sequence, directly binds to and inhibits the activity of the kinase.

PubMed: 22579248
DOI: 10.1016/j.str.2012.02.022

実験手法

X-RAY DIFFRACTION (2.4 Å)