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The EZMTT cell proliferation assay provides precise measurement for drug combinations and better correlation between in vitro and in vivo efficacy.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-03-20 , DOI: 10.1016/j.bmcl.2020.127134
Jingjing Rui 1 , Ning Xu 1 , JianBing Yin 2 , Yan Yu 1 , Ruisong Bai 1 , Weike Su 1 , Benfang Ruan 1
Affiliation  

The rate of drug-induced proliferation (DIP) has been proposed as an unbiased alternative drug effect metric. However, current assays are not easy and precise enough to track minor changes in cell growth. Here, we report the optimized EZMTT based detection method which can continuously measure time-dependent growth after drug treatment and reliably detect partial drug resistance for cancer cells. Importantly, tracking time-dependent growth after drug treatment demonstrated that a KGA allosteric inhibitor alone failed to completely inhibit cancer cell growth, but a drug combination was able to provide complete inhibition in cell-based assays that translated well in in vivo animal experiments. In conclusion, this simple EZMTT method provided precise measurement of loss of susceptibility after drug treatment and has great potential to be developed for drug efficacy and drug combination studies to solve the unmet medical need.

中文翻译:

EZMTT细胞增殖测定法可精确测量药物组合,并在体内外功效之间建立更好的关联。

已经提出了药物诱导的增殖率(DIP)作为无偏见的替代药物作用度量。但是,当前的检测方法不够容易且不够精确,无法跟踪细胞生长的微小变化。在这里,我们报告了基于EZMTT的优化检测方法,该方法可以连续测量药物治疗后的时间依赖性生长并可靠地检测癌细胞的部分耐药性。重要的是,跟踪药物治疗后的时间依赖性生长证明,单独使用KGA变构抑制剂不能完全抑制癌细胞的生长,但是在体内动物实验中翻译良好的基于​​细胞的测定中,药物组合能够提供完全的抑制作用。结论,
更新日期:2020-04-20
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