Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog.

Derek T Rensing, Sakshi Uppal, Kendall J Blumer, Kevin D Moeller

Organic letters 2015 May 1

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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.

Citation

Derek T Rensing, Sakshi Uppal, Kendall J Blumer, Kevin D Moeller. Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog. Organic letters. 2015 May 1;17(9):2270-3