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

doi:10.1021/acs.orglett.5b00944

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 journal › Article › peer-review

28 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 language	English
Pages (from-to)	2270-2273
Number of pages	4
Journal	Organic Letters
Volume	17
Issue number	9
DOIs	https://doi.org/10.1021/acs.orglett.5b00944
State	Published - May 1 2015

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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.",

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AU - Moeller, Kevin D.

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AB - 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.

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Toward the selective inhibition of G proteins: Total synthesis of a simplified YM-254890 analog

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