Old tricks and new trends to address tumors: a medicinal chemist’s perspective

IF 2.1 4区 综合性期刊 Q2 MULTIDISCIPLINARY SCIENCES Rendiconti Lincei-Scienze Fisiche E Naturali Pub Date : 2023-07-13 DOI:10.4081/scienze.2022.826
P. Seneci
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Abstract

Major efforts in the past decades have provided novel small molecule drugs and biologicals and innovative mechanisms against tumors, but the quest for safer, bioavailable and more effective active principles is still ongoing. This contribution focuses on innovative approaches to fulfill therapeutic goals in oncology; namely, the inhibition of the stabilizing interaction between the RNA-binding protein HuR and mRNAs of multiple oncogenes, and the unleashing of a strong immune reaction against cancer cells by antagonizing the PD-1 – PD-L1 interaction on the surface of cancer cells. “Classical” drug-like, bioavailable small molecules were either rationally designed from a naturally occurring template (tanshinones converted to aza-tanshinones – HuR), or from a synthetic peptidomimetic inhibitor (biphenyloxy aryls converted to disubstituted triazines – PD-L1); after their synthesis and activity profiling, early leads were identified to be further structurally optimized in the near future.
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治疗肿瘤的老方法和新趋势:一个药物化学家的观点
在过去的几十年里,主要的努力已经提供了新的小分子药物和生物制剂以及抗肿瘤的创新机制,但对更安全、生物可利用性和更有效的活性原理的追求仍在进行中。该贡献侧重于实现肿瘤学治疗目标的创新方法;即抑制rna结合蛋白HuR与多种癌基因mrna之间的稳定相互作用,通过拮抗癌细胞表面的PD-1 - PD-L1相互作用,对癌细胞产生强烈的免疫反应。“经典”类药物,生物可利用的小分子要么从自然存在的模板(丹参酮转化为aza-丹参酮- HuR)合理设计,要么从合成的拟肽抑制剂(联苯氧基芳基转化为二取代三嗪- PD-L1)设计;在对其进行合成和活性分析后,确定了早期先导物,并在不久的将来进行进一步的结构优化。
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来源期刊
Rendiconti Lincei-Scienze Fisiche E Naturali
Rendiconti Lincei-Scienze Fisiche E Naturali MULTIDISCIPLINARY SCIENCES-
CiteScore
4.10
自引率
10.00%
发文量
70
审稿时长
>12 weeks
期刊介绍: Rendiconti is the interdisciplinary scientific journal of the Accademia dei Lincei, the Italian National Academy, situated in Rome, which publishes original articles in the fi elds of geosciences, envi ronmental sciences, and biological and biomedi cal sciences. Particular interest is accorded to papers dealing with modern trends in the natural sciences, with interdisciplinary relationships and with the roots and historical development of these disciplines.
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