Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy,Journal of Medicinal Chemistry

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Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2016-12-22 00:00:00 , DOI: 10.1021/acs.jmedchem.6b01167
Séverine Ravez ₁ , Quentin Spillier _{1,

2} , Romain Marteau ₁ , Olivier Feron ₂ , Raphaël Frédérick ₁

Affiliation

Recent advances in the understanding of the relationship between cancer and metabolism have highlighted the relevance of the serine synthetic pathway (SSP), which consists of three successive enzymatic reactions. Enzymes of the SSP, such as phosphoglycerate dehydrogenase (PHGDH) and phosphoserine aminotransferase 1 (PSAT-1), were recently highlighted because they are amplified in a significant subset of human tumors, and their suppression by RNAi caused a decrease in cancer cell survival and growth. Currently, the discovery of drugs that inhibit these enzymes is still in its infancy, and the identification of suitable inhibitors could serve to understand the emerging biology of these metabolic enzymes. In this review, we present the SSP as a significant and novel emerging area for medicinal chemistry and we provide an overview of one of the key enzymes of the pathway, PHGDH.

中文翻译：

丝氨酸合成途径抑制剂对癌症治疗的发展中的挑战和机遇。

在理解癌症与代谢之间的关系方面的最新进展突显了丝氨酸合成途径（SSP）的相关性，该途径由三个连续的酶促反应组成。最近重点介绍了SSP的酶，例如磷酸甘油酸脱氢酶（PHGDH）和磷酸丝氨酸氨基转移酶1（PSAT-1），因为它们在人类肿瘤的重要子集中被扩增，并且被RNAi抑制会导致癌细胞存活率降低和生长。目前，抑制这些酶的药物的发现还处于起步阶段，合适的抑制剂的鉴定可以用来了解这些代谢酶的新兴生物学。在这篇评论中，

更新日期：2016-12-22

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