1RJB

Crystal Structure of FLT3

1RJB の概要

• エントリーDOI: 10.2210/pdb1rjb/pdb
• 分子名称: FL cytokine receptor (2 entities in total)
• 機能のキーワード: kinase, autoinhibition, juxtamembrane domain, transferase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Membrane; Single-pass type I membrane protein: P36888
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 39799.32

構造登録者

Griffith, J.,Black, J.,Faerman, C.,Swenson, L.,Wynn, M.,Lu, F.,Lippke, J.,Saxena, K. (登録日: 2003-11-19, 公開日: 2004-02-03, 最終更新日: 2024-02-14)

主引用文献

Griffith, J.,Black, J.,Faerman, C.,Swenson, L.,Wynn, M.,Lu, F.,Lippke, J.,Saxena, K.
The structural basis for autoinhibition of FLT3 by the juxtamembrane domain.
Mol.Cell, 13:169-178, 2004

PubMed Abstract: FLT3 is a type III receptor tyrosine kinase that is thought to play a key role in hematopoiesis. Certain classes of FLT3 mutations cause constitutively activated forms of the receptor that are found in significant numbers of patients with acute myelogenous leukemia (AML). The mutations occur either in the activation loop, for example, as point mutations of Asp835 or as internal tandem duplication (ITD) sequences in the juxtamembrane (JM) domain. To further understand the nature of FLT3 autoinhibition and regulation, we have determined the crystal structure of the autoinhibited form of FLT3. This structure shows the autoinhibitory conformation of a complete JM domain in this class of receptor tyrosine kinases. The detailed inhibitory mechanism of the JM domain is revealed, which is likely utilized by other members of type III receptor tyrosine kinases.

PubMed: 14759363
DOI: 10.1016/S1097-2765(03)00505-7

実験手法

X-RAY DIFFRACTION (2.1 Å)