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AcGlcAs:一种新的P53向,具有强大的细胞摄取和癌细胞选择性

Ying Liang¹, Quanlin An², Huaxin Song¹

¹Shanghai Institute of Hematology, State Key Laboratory of Medical Genomics, National Research Center for Translational Medicine (Shanghai), Ruijin Hospital affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China.

Journal of medicinal chemistry

|December 9, 2023

概括

一种新型的,AcGlcAs,增强细胞吸收,并针对PML/RARα和突变p53. 这种新化合物在治疗p53突变癌症方面表现有前途,具有更好的选择性和生物可用性.

科学领域:

在瘤学瘤学.
药用化学医学化学
药理学药理学是指药理学的学科.

背景情况:

三氧化物 (ATO) 通过向PML/RARα,有效对抗急性血清性白血病.
ATO还与p53相互作用,p53是各种癌症中经常发生突变的蛋白质,但在细胞吸收和癌症选择性方面面临挑战.
针对突变的p53具有重要的治疗潜力,用于广泛的癌症.

研究的目的:

开发一种具有增强细胞吸收和改善PML/RARα和突变p53.3的基化合物的新型化合物.
评估新型的癌细胞选择性和临床前疗效.

主要方法:

素的结构-活性关系分析.
通过将与硫和四乙-β-d-硫糖结合,合理设计和合成一种新型 (AcGlcAs).
通过醇介导途径对细胞吸收的评估.
在55个癌细胞系中针对PML/RARα和突变p53的体外评估.
在p53突变异种移植瘤的小鼠中进行临床前研究.

主要成果:

与ATO相比,AcGlcAs的细胞吸收量显著增加 (高达127倍).
AcGlcAs对PML/RARα和突变p53.3都具有强大的向性.
该化合物对癌症细胞系比正常细胞系表现出偏好的细胞毒性.
在p53突变异种移植瘤的小鼠中,AcGlcAs显著改善了生存率.
AcGlcAs显示出良好的血稳定性和口服生物可用性.

结论:

AcGlcAs是一种有前途的新衍生物,具有增强的细胞吸收和强大的PML/RARα和突变p53.3的双重向.
它的选择性杀死癌细胞和有利的临床前资料表明,AcGlcAs是治疗p53-突变癌症的潜在临床候选人.

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