6QB9

Structure of an anti-Mcl1 scFv

6QB9 の概要

• エントリーDOI: 10.2210/pdb6qb9/pdb
• 関連するPDBエントリー: 6QB3 6QB4
• 分子名称: scFv55, L(+)-TARTARIC ACID (3 entities in total)
• 機能のキーワード: mcl1, scfv, azd5991, apoptosis
• 由来する生物種: Homo sapiens
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 53158.09

構造登録者

Hargreaves, D. (登録日: 2018-12-20, 公開日: 2019-11-06, 最終更新日: 2024-11-20)

主引用文献

Luptak, J.,Bista, M.,Fisher, D.,Flavell, L.,Gao, N.,Wickson, K.,Kazmirski, S.L.,Howard, T.,Rawlins, P.B.,Hargreaves, D.
Antibody fragments structurally enable a drug-discovery campaign on the cancer target Mcl-1.
Acta Crystallogr D Struct Biol, 75:1003-1014, 2019

PubMed Abstract: Apoptosis is a crucial process by which multicellular organisms control tissue growth, removal and inflammation. Disruption of the normal apoptotic function is often observed in cancer, where cell death is avoided by the overexpression of anti-apoptotic proteins of the Bcl-2 (B-cell lymphoma 2) family, including Mcl-1 (myeloid cell leukaemia 1). This makes Mcl-1 a potential target for drug therapy, through which normal apoptosis may be restored by inhibiting the protective function of Mcl-1. Here, the discovery and biophysical properties of an anti-Mcl-1 antibody fragment are described and the utility of both the scFv and Fab are demonstrated in generating an Mcl-1 crystal system amenable to iterative structure-guided drug design.

PubMed: 31692474
DOI: 10.1107/S2059798319014116

実験手法

X-RAY DIFFRACTION (1.85 Å)