针对 G 蛋白的选择性抑制：简化版 YM-254890 类似物的全合成。
Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog.
机构信息
†Department of Chemistry, Washington University, St. Louis, Missouri 63130, United States.
‡Department of Cell Biology and Physiology, Washington University School of Medicine, St. Louis, Missouri 63110, United States.
出版信息
Org Lett. 2015 May 1;17(9):2270-3. doi: 10.1021/acs.orglett.5b00944. Epub 2015 Apr 15.
A simplified analog (WU-07047) of the selective Gαq/11 inhibitor YM-254890 has been synthesized, and an initial probe of its activity conducted. In the analog, the two peptide-based linkers in the cyclic YM-254890 have been replaced with hydrocarbon chains. This enables a convergent approach to the synthesis of the analog. Biochemical assays showed that while the simplified analog is not as potent as YM-254890, it does still inhibit Gq.
已经合成了选择性 Gαq/11 抑制剂 YM-254890 的简化类似物，并对其活性进行了初步研究。在类似物中，环状 YM-254890 中的两个基于肽的接头已被烃链取代。这使得类似物的合成可以采用收敛方法。生化测定表明，尽管简化类似物不如 YM-254890 有效，但它仍能抑制 Gq。
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