6C57

Crystal structure of mutant human geranylgeranyl pyrophosphate synthase (Y246D) in complex with bisphosphonate inhibitor FV0109

6C57 の概要

• エントリーDOI: 10.2210/pdb6c57/pdb
• 分子名称: Geranylgeranyl pyrophosphate synthase, {[(2-{3-[(4-fluorobenzene-1-carbonyl)amino]phenyl}thieno[2,3-d]pyrimidin-4-yl)amino]methylene}bis(phosphonic acid) (3 entities in total)
• 機能のキーワード: isoprenoid pathway, isopentenyl transferase, transferase inhibitor, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 75391.36

構造登録者

Park, J.,Bin, X.,Vincent, F.,Tsantrizos, Y.S.,Berghuis, A.M. (登録日: 2018-01-15, 公開日: 2018-09-05, 最終更新日: 2023-10-04)

• 主引用文献: Lacbay, C.M.,Waller, D.D.,Park, J.,Gomez Palou, M.,Vincent, F.,Huang, X.F.,Ta, V.,Berghuis, A.M.,Sebag, M.,Tsantrizos, Y.S.; Unraveling the Prenylation-Cancer Paradox in Multiple Myeloma with Novel Geranylgeranyl Pyrophosphate Synthase (GGPPS) Inhibitors.; J. Med. Chem., 61:6904-6917, 2018; PubMed: 30016091; DOI: 10.1021/acs.jmedchem.8b00886

実験手法

X-RAY DIFFRACTION (3.5 Å)