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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights
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Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights

机译：单羧酸转运蛋白1和4抑制剂作为治疗实体瘤的潜在治疗方法：综述结构 - 活动关系见解

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摘要

Development of multidrug resistance (MDR) is one of the major causes leading to failure of cancer chemotherapy and radiotherapy. Monocarboxylate transporters (MCTs) MCT1 and MCT4, which are overexpressed in solid tumours, play a very important role in cancer cell survival and proliferation. These lactate transporters work complimentarily to drive lactate shuttle in tumour cells, which results in maintenance of H+ ion (pH) balance necessary for their survival. Inhibition of these transmembrane proteins has been demonstrated as a novel strategy to treat drug resistant solid cancers. Presently, only a few small molecule MCT1 inhibitors such as AZD3965 and AR-C155858 are known with clinical potential. Even lesser mention of MCT4 inhibitors, which include molecules having scaffolds such as pyrazole and indazole, is available in the literature. Current overview presents the status of recent developments undertaken in identification of efficacious MCT1 and/or MCT4 inhibitors as a potential anticancer therapy overcoming MDR. Further, detailed structure-activity relationships for different classes of compounds has been proposed to streamline the understandings learnt from ongoing research work. Through this review, we aim to highlight the importance of these excellent targets and facilitate future development of selective, potent and safe MCT1 and/or MCT4 inhibitors as promising chemotherapy for drug resistant cancer. (C) 2020 Elsevier Masson SAS. All rights reserved.
机译：多药耐药性的发展（MDR）是导致癌症化疗和放射疗法失败的主要原因之一。单羧酸转运蛋白（MCTS）MCT1和MCT4在实体肿瘤中过表达，在癌细胞存活和增殖中起着非常重要的作用。这些乳酸转运蛋白互动地在肿瘤细胞中推动乳酸乳酸梭，这导致维持其存活所必需的H +离子（pH）平衡。已经证明了对这些跨膜蛋白的抑制作用作为治疗耐药性固体癌的新策略。目前，只有少数小分子MCT1抑制剂，如AZD3965和Ar-C155858，具有临床电位。甚至提及MCT4抑制剂，包括具有支架如吡唑和吲唑类的分子，可在文献中获得。目前的概述提出了近期开发的状态，以鉴定有效的MCT1和/或MCT4抑制剂作为克服MDR的潜在抗癌治疗。此外，提出了对不同类别化合物的详细结构 - 活性关系，以简化从正在进行的研究工作中了解的理解。通过本综述，我们的目标是突出这些优异的目标的重要性，并促进选择性，有效和安全的MCT1和/或MCT4抑制剂的未来发展，作为耐药性癌症的有希望的化疗。 （c）2020 Elsevier Masson SAS。版权所有。

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