3P9G

Crystal structure of the TSG101 UEV domain in complex with FA459 peptide

3P9G の概要

• エントリーDOI: 10.2210/pdb3p9g/pdb
• 関連するPDBエントリー: 3OBQ 3P9H
• 分子名称: Tumor susceptibility gene 101 protein, Gag polyprotein (3 entities in total)
• 機能のキーワード: protein transport, ubiquitin
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Cytoplasm: Q99816; Matrix protein p17: Virion (By similarity): Q9YP46
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 17585.30

構造登録者

Hurley, J.H.,Im, Y.J. (登録日: 2010-10-17, 公開日: 2011-06-29, 最終更新日: 2023-12-06)

主引用文献

Kim, S.E.,Liu, F.,Im, Y.J.,Stephen, A.G.,Fivash, M.J.,Waheed, A.A.,Freed, E.O.,Fisher, R.J.,Hurley, J.H.,Burke, T.R.
Elucidation of New Binding Interactions with the Tumor Susceptibility Gene 101 (Tsg101) Protein Using Modified HIV-1 Gag-p6 Derived Peptide Ligands.
ACS Med Chem Lett, 2:337-341, 2011

PubMed Abstract: Targeting protein-protein interactions is gaining greater recognition as an attractive approach to therapeutic development. An example of this may be found with the human cellular protein encoded by the tumor susceptibility gene 101 (Tsg101), where interaction with the p6 C-terminal domain of the nascent viral Gag protein is required for HIV-1 particle budding and release. This association of Gag with Tsg101 is highly dependent on a "Pro-Thr-Ala-Pro" ("PTAP") peptide sequence within the p6 protein. Although p6-derived peptides offer potential starting points for developing Tsg101-binding inhibitors, the affinities of canonical peptides are outside the useful range (K(d) values greater than 50 μM). Reported herein are crystal structures of Tsg101 in complex with two structurally-modified PTAP-derived peptides. This data define new regions of ligand interaction not previously identified with canonical peptide sequences. This information could be highly useful in the design of Tsg101-binding antagonists.

PubMed: 21643473
DOI: 10.1021/ml1002579

実験手法

X-RAY DIFFRACTION (1.8 Å)