Faculty of Biology and Biotechnology, Higher School of Economics, Moscow, Russia.
Dokl Biochem Biophys. 2023 Dec;513(1):324-327. doi: 10.1134/S1607672923700503. Epub 2023 Sep 29.
Gemcitabine monophosphate (dFdCMP), one of the intracellular forms of phosphorylated gemcitabine, determines its antitumor activity. A pharmaco-molecular model for determining relative gemcitabine monophosphate level based on the assessment of the activity of ENT1 and ENT2 channels as well as dCK and CDA enzymes in tumor tissue was developed. Relative gemcitabine monophosphate level is a more relevant predictive factor of gemcitabine resistance of bladder cancer as compared with the expression of individual markers related to dFdCMP formation.
单磷酸吉西他滨(dFdCMP)是吉西他滨的一种细胞内磷酸化形式,决定了其抗肿瘤活性。开发了一种基于肿瘤组织中 ENT1 和 ENT2 通道以及 dCK 和 CDA 酶活性评估来确定相对单磷酸吉西他滨水平的药物分子模型。与与 dFdCMP 形成相关的单个标志物的表达相比,相对单磷酸吉西他滨水平是膀胱癌对吉西他滨耐药性的更相关的预测因子。