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Design and synthesis of a protein:Farnesyltransferase inhibitor based on sugar amino acids

✍ Scribed by Herman S Overkleeft; Steven H.L Verhelst; Elsbet Pieterman; Nico J Meeuwenoord; Mark Overhand; Louis H Cohen; Gijs A van der Marel; Jacques H van Boom

Book ID: 104261480
Publisher: Elsevier Science
Year: 1999
Tongue: French
Weight: 268 KB
Volume: 40
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(99)00697-8

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✦ Synopsis

The synthesis of four partially deoxygenated gluconic amino acids from fully acetylated D-glucal is described. Replacement of the central AA dipeptide in the CAAX tetrapeptide corresponding to the C-terminus of K-Ras p21 by one of these sugar amino acid building blocks led to a novel protein:farnesyl transferase inhibitor.

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