4XBR

In cellulo Crystal Structure of PAK4 in complex with Inka

4XBR の概要

• エントリーDOI: 10.2210/pdb4xbr/pdb
• 関連するPDBエントリー: 4XBU
• 分子名称: Protein FAM212A,Serine/threonine-protein kinase PAK 4, ADENOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION (3 entities in total)
• 機能のキーワード: pak4, inka, crystallization, transferase, peptide
• 由来する生物種: Homo sapiens (Human); 詳細
• 細胞内の位置: Cytoplasm : O96013
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 41803.17

構造登録者

Baskaran, Y.,Ang, K.C.,Anekal, P.V.,Chan, W.L.,Grimes, J.M.,Manser, E.,Robinson, R.C. (登録日: 2014-12-17, 公開日: 2015-12-02, 最終更新日: 2024-11-13)

主引用文献

Baskaran, Y.,Ang, K.C.,Anekal, P.V.,Chan, W.L.,Grimes, J.M.,Manser, E.,Robinson, R.C.
An in cellulo-derived structure of PAK4 in complex with its inhibitor Inka1
Nat Commun, 6:8681-8681, 2015

PubMed Abstract: PAK4 is a metazoan-specific kinase acting downstream of Cdc42. Here we describe the structure of human PAK4 in complex with Inka1, a potent endogenous kinase inhibitor. Using single mammalian cells containing crystals 50 μm in length, we have determined the in cellulo crystal structure at 2.95 Å resolution, which reveals the details of how the PAK4 catalytic domain binds cellular ATP and the Inka1 inhibitor. The crystal lattice consists only of PAK4-PAK4 contacts, which form a hexagonal array with channels of 80 Å in diameter that run the length of the crystal. The crystal accommodates a variety of other proteins when fused to the kinase inhibitor. Inka1-GFP was used to monitor the process crystal formation in living cells. Similar derivatives of Inka1 will allow us to study the effects of PAK4 inhibition in cells and model organisms, to allow better validation of therapeutic agents targeting PAK4.

PubMed: 26607847
DOI: 10.1038/ncomms9681

実験手法

X-RAY DIFFRACTION (2.94 Å)