Inhibition of cancer metabolism: a patent landscape

被引:4
|
作者
Katt, William P. [1 ]
Cerione, Richard A. [1 ,2 ]
机构
[1] Cornell Univ, Dept Mol Med, Ithaca, NY 14853 USA
[2] Cornell Univ, Dept Chem & Chem Biol, Ithaca, NY 14853 USA
关键词
cancer; drug discovery; glutaminase; glutaminolysis; glycolysis; isocitrate dehydrogenase; metabolism; patents; TCA cycle; PROGNOSTIC-SIGNIFICANCE; ALLOSTERIC INHIBITORS; GLUTAMINASE C; EXPRESSION; LAT1; TRANSPORTERS; MUTATIONS; ASCT2;
D O I
10.4155/ppa-2019-0012
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. Global solutions to a central problem. Researchers across the globe have patented efforts to target enzymes involved in cancer cell metabolism. Pins on the map represent individual research efforts, and are color coded to pathways or proteins. Several interesting small-molecule inhibitors revealed by these efforts are shown. [GRAPHICS]
引用
收藏
页码:117 / 138
页数:22
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