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题目:: Structure-based design, synthesis, and pharmacologic evaluation of peptide RGS4 inhibitors.
作者:: Jin(Y),Zhong(H),Omnaas(J R),Neubig(R R),Mosberg(H I)
状态:: 发布时间2004-03-10 , 更新时间 2007-11-14
期刊:: J Pept Res
摘要:: Regulators of G-protein signaling (RGS) proteins form a multifunctional signaling family. A key role of RGS proteins is binding to the G-protein Galpha-subunit and acting as GTPase-activating proteins (GAPs), thereby rapidly terminating G protein-coupled receptor (GPCR) signaling. Using the published RGS4-Gialpha1 X-ray structure we have designed and synthesized a series of cyclic peptides, modeled on the Gialpha Switch I region, that inhibit RGS4 GAP activity. These compounds should prove useful for elucidating RGS-mediated activity and serve as a starting point for the development of a novel class of therapeutic agent.
语言:: eng
DOI:

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