title: Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog.
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.
authors: †Department of Chemistry, Washington University, St. Louis, Missouri 63130, United States.
authors: Derek T
authors: DT
authors: Rensing
authors: †Department of Chemistry, Washington University, St. Louis, Missouri 63130, United States.
authors: Sakshi
authors: S
authors: Uppal
authors: ‡Department of Cell Biology and Physiology, Washington University School of Medicine, St. Louis, Missouri 63110, United States.
authors: Kendall J
authors: KJ
authors: Blumer
authors: †Department of Chemistry, Washington University, St. Louis, Missouri 63130, United States.
authors: Kevin D
authors: KD
authors: Moeller
mesh_terms: D018360:Crystallography, X-Ray; D019204:GTP-Binding Proteins / Q000819:agonists* / Q000737:chemistry; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry; D015398:Signal Transduction
chemical_list: D010456:Peptides, Cyclic; C475455:YM-254890; D019204:GTP-Binding Proteins