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Solution-phase synthesis of ICG-001, a β-turn peptidomimetic molecule inhibitor of β-catenin–Tcf-mediated transcription |
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| Authors: | Alessandro Piergentili Fabio Del Bello Francesco Gentili Mario Giannella Wilma Quaglia Cristian Vesprini Russell J. Thomas Graeme M. Robertson |
| Affiliation: | aDipartimento di Scienze Chimiche, Università di Camerino, Via S. Agostino, 1, 62032 Camerino, Italy bSiena Biotech S.p.A., Via Fiorentina, 1, 53100 Siena, Italy |
| Abstract: | The solution-phase synthesis of the β-turn peptidomimetic ICG-001, a selective inhibitor of Wnt/β-catenin signalling, which has been found to be important for both initiation and progression of cancers of different tissues and has been exploited as an extremely useful chemogenomic tool, was developed. This route is particularly suitable for the multigram scale preparation of ICG-001. |
| Keywords: | Wnt pathway Solution-phase synthesis Inhibitor Peptidomimetic ICG-001 |
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