7S2Y

SAMHD1 HD domain bound to CNDAC

7S2Y の概要

• エントリーDOI: 10.2210/pdb7s2y/pdb
• 分子名称: Deoxynucleoside triphosphate triphosphohydrolase SAMHD1, 4-amino-1-{2-cyano-2-deoxy-5-O-[(S)-hydroxy{[(S)-hydroxy(phosphonooxy)phosphoryl]oxy}phosphoryl]-beta-D-arabinofuranosyl}pyrimidin-2(1H)-one, 2'-DEOXYADENOSINE 5'-TRIPHOSPHATE, ... (6 entities in total)
• 機能のキーワード: samhd1, inhibitor, sapacitabine, hydrolase
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 259926.05

構造登録者

Digianantonio, K.M.,Xiong, Y. (登録日: 2021-09-04, 公開日: 2021-10-27, 最終更新日: 2023-10-18)

主引用文献

Rothenburger, T.,Thomas, D.,Schreiber, Y.,Wratil, P.R.,Pflantz, T.,Knecht, K.,Digianantonio, K.,Temple, J.,Schneider, C.,Baldauf, H.M.,McLaughlin, K.M.,Rothweiler, F.,Bilen, B.,Farmand, S.,Bojkova, D.,Costa, R.,Ferreiros, N.,Geisslinger, G.,Oellerich, T.,Xiong, Y.,Keppler, O.T.,Wass, M.N.,Michaelis, M.,Cinatl Jr., J.
Differences between intrinsic and acquired nucleoside analogue resistance in acute myeloid leukaemia cells.
J Exp Clin Cancer Res, 40:317-317, 2021

PubMed Abstract: SAMHD1 mediates resistance to anti-cancer nucleoside analogues, including cytarabine, decitabine, and nelarabine that are commonly used for the treatment of leukaemia, through cleavage of their triphosphorylated forms. Hence, SAMHD1 inhibitors are promising candidates for the sensitisation of leukaemia cells to nucleoside analogue-based therapy. Here, we investigated the effects of the cytosine analogue CNDAC, which has been proposed to be a SAMHD1 inhibitor, in the context of SAMHD1.

PubMed: 34641952
DOI: 10.1186/s13046-021-02093-4

実験手法

X-RAY DIFFRACTION (2.8 Å)