COTI-2是一种新颖的小分子，在体外和体内对多种人类癌细胞系均具有活性。,Oncotarget

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COTI-2是一种新颖的小分子，在体外和体内对多种人类癌细胞系均具有活性。
Oncotarget Pub Date : 2016-05-07 , DOI: 10.18632/oncotarget.9133
Kowthar Y Salim ₁ , Saman Maleki Vareki ₂ , Wayne R Danter ₁ , James Koropatnick _{2,

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Affiliation

鉴定具有高功效和低毒性的新型抗癌化合物对于药物开发至关重要。高通量筛选和其他此类策略通常需要大量资源。因此，计算机电子计算机辅助药物设计已经获得了快速的接受和普及。我们采用了我们专有的计算平台（CHEMSAS®），该平台结合了传统和现代药理学原理，统计模型，药物化学和机器学习技术的独特组合，以发现和优化可靶向多种癌症的新型化合物。COTI-2是使用CHEMSAS鉴定的一种小分子候选抗癌药。这项研究描述了COTI-2的体外和体内评价。我们的数据表明，COTI-2对多种人类癌细胞系均有效，无论其起源或基因组成如何。大多数处理过的癌细胞系对纳摩尔浓度的COTI-2敏感。与传统的化学疗法或靶向治疗药物相比，COTI-2在体外和体内均表现出优异的抗肿瘤细胞活性。尽管具有强大的抗肿瘤功效，但COTI-2在体内仍是安全且耐受性良好的。尽管COTI-2的作用机理仍在研究中，但初步结果表明它不是传统的激酶或Hsp90抑制剂。在体外和体内，COTI-2均具有优异的抗肿瘤细胞活性。尽管具有强大的抗肿瘤功效，但COTI-2在体内仍是安全且耐受性良好的。尽管COTI-2的作用机理仍在研究中，但初步结果表明它不是传统的激酶或Hsp90抑制剂。在体外和体内，COTI-2均具有优异的抗肿瘤细胞活性。尽管具有强大的抗肿瘤功效，但COTI-2在体内仍是安全且耐受性良好的。尽管COTI-2的作用机理仍在研究中，但初步结果表明它不是传统的激酶或Hsp90抑制剂。

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COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo.

Identification of novel anti-cancer compounds with high efficacy and low toxicity is critical in drug development. High-throughput screening and other such strategies are generally resource-intensive. Therefore, in silico computer-aided drug design has gained rapid acceptance and popularity. We employed our proprietary computational platform (CHEMSAS®), which uses a unique combination of traditional and modern pharmacology principles, statistical modeling, medicinal chemistry, and machine-learning technologies to discover and optimize novel compounds that could target various cancers. COTI-2 is a small molecule candidate anti-cancer drug identified using CHEMSAS. This study describes the in vitro and in vivo evaluation of COTI-2. Our data demonstrate that COTI-2 is effective against a diverse group of human cancer cell lines regardless of their tissue of origin or genetic makeup. Most treated cancer cell lines were sensitive to COTI-2 at nanomolar concentrations. When compared to traditional chemotherapy or targeted-therapy agents, COTI-2 showed superior activity against tumor cells, in vitro and in vivo. Despite its potent anti-tumor efficacy, COTI-2 was safe and well-tolerated in vivo. Although the mechanism of action of COTI-2 is still under investigation, preliminary results indicate that it is not a traditional kinase or an Hsp90 inhibitor.

更新日期：2019-11-01

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