2R5T

Crystal Structure of Inactive Serum and Glucocorticoid- Regulated Kinase 1 in Complex with AMP-PNP

2R5T の概要

• エントリーDOI: 10.2210/pdb2r5t/pdb
• 分子名称: Serine/threonine-protein kinase Sgk1, MAGNESIUM ION, SULFATE ION, ... (5 entities in total)
• 機能のキーワード: agc protein kinase, apoptosis, atp-binding, cytoplasm, endoplasmic reticulum, nucleotide-binding, nucleus, phosphorylation, serine/threonine-protein kinase, transferase, ubl conjugation
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 42929.88

構造登録者

Zhao, B.,Lehr, R.,Smallwood, A.M.,Ho, T.F.,Maley, K.,Randall, T.,Head, M.S.,Koretke, K.K.,Schnackenberg, C.G. (登録日: 2007-09-04, 公開日: 2008-09-09, 最終更新日: 2024-02-21)

主引用文献

Zhao, B.,Lehr, R.,Smallwood, A.M.,Ho, T.F.,Maley, K.,Randall, T.,Head, M.S.,Koretke, K.K.,Schnackenberg, C.G.
Crystal structure of the kinase domain of serum and glucocorticoid-regulated kinase 1 in complex with AMP PNP.
Protein Sci., 16:2761-2769, 2007

PubMed Abstract: Serum and glucocorticoid-regulated kinase 1 (SGK1) is a serine/threonine protein kinase of the AGC family which participates in the control of epithelial ion transport and is implicated in proliferation and apoptosis. We report here the 1.9 A crystal structure of the catalytic domain of inactive human SGK1 in complex with AMP-PNP. SGK1 exists as a dimer formed by two intermolecular disulfide bonds between Cys258 in the activation loop and Cys193. Although most of the SGK1 structure closely resembles the common protein kinase fold, the structure around the active site is unique when compared to most protein kinases. The alphaC helix is not present in this inactive form of SGK1 crystal structure; instead, the segment corresponding to the C helix forms a beta-strand that is stabilized by the N-terminal segment of the activation loop through a short antiparallel beta-sheet. Since the differences from other kinases occur around the ATP binding site, this structure can provide valuable insight into the design of selective and highly potent ATP-competitive inhibitors of SGK1 kinase.

PubMed: 17965184
DOI: 10.1110/ps.073161707

実験手法

X-RAY DIFFRACTION (1.9 Å)