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

Research output: Contribution to journalArticlepeer-review

22 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)2270-2273
Number of pages4
JournalOrganic Letters
Volume17
Issue number9
DOIs
StatePublished - May 1 2015

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