Katt William P, Cerione Richard A
Department of Molecular Medicine, Cornell University, Ithaca, NY 14853-6401, USA.
Department of Chemistry & Chemical Biology, Cornell University, Ithaca, NY 14853-6401, USA.
Pharm Pat Anal. 2019 Jul;8(4):117-138. doi: 10.4155/ppa-2019-0012. Epub 2019 Aug 15.
Cancer metabolism is currently a hot topic. Since it was first realized that cancer cells rely upon an altered metabolic program to sustain their rapid proliferation, the enzymes that support those metabolic changes have appeared to be good targets for pharmacological intervention. Here, we discuss efforts pertaining to targets in cancer metabolism, focusing upon the tricarboxylic acid cycle and the mechanisms which feed nutrients into it. We describe a broad landscape of small-molecule inhibitors, targeting a dozen different proteins, each implicated in cancer progression. We hope that this will serve as a reference both to the areas being most highly examined today and, relatedly, the areas that are still ripe for novel intervention.
癌症代谢是当前的一个热门话题。自从人们首次认识到癌细胞依赖改变的代谢程序来维持其快速增殖以来，支持这些代谢变化的酶似乎成为了药物干预的良好靶点。在此，我们讨论与癌症代谢靶点相关的研究进展，重点关注三羧酸循环以及为其提供营养物质的机制。我们描述了一系列小分子抑制剂的概况，这些抑制剂靶向十几种不同的蛋白质，每种蛋白质都与癌症进展有关。我们希望这将既作为当今研究最为深入的领域的参考，也作为仍然适合进行新型干预的领域的参考。
