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Lipidated Stapled Peptides Targeting the Acyl Binding Protein UNC119.

ABSTRACT: The acyl-binding UNC119 proteins mediate the activation and transport of various N-myristoylated proteins. In particular, UNC119a plays a crucial role in the completion of cytokinesis. Herein, we report the use of a lipidated peptide originating from the UNC119 binding partner Gnat1 as the basis for the design of lipidated, stabilized ?-helical peptides that target UNC119a. By using the hydrocarbon peptide-stapling approach, cell-permeable binders of UNC119a were generated that induced the accumulation of cytokinetic and binucleated cells; this suggests UNC119a as a potential target for the inhibition of cytokinesis.

SUBMITTER: Cromm PM

PROVIDER: S-EPMC6973269 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Lipidated Stapled Peptides Targeting the Acyl Binding Protein UNC119.

Cromm Philipp M PM Adihou Hélène H Kapoor Shobhna S Vazquez-Chantada Mercedes M Davey Paul P Longmire David D Hennes Elisabeth E Hofer Walter W Küchler Philipp P Chiarparin Elisabetta E Waldmann Herbert H Grossmann Tom N TN

Chembiochem : a European journal of chemical biology 20191119 24

The acyl-binding UNC119 proteins mediate the activation and transport of various N-myristoylated proteins. In particular, UNC119a plays a crucial role in the completion of cytokinesis. Herein, we report the use of a lipidated peptide originating from the UNC119 binding partner Gnat1 as the basis for the design of lipidated, stabilized α-helical peptides that target UNC119a. By using the hydrocarbon peptide-stapling approach, cell-permeable binders of UNC119a were generated that induced the accum ...[more]

PMID: 31680402

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