Solid-phase synthesis of Biotin-S-Farnesyl-L-Cysteine, a surrogate substrate for isoprenylcysteine Carboxylmethyltransferase (ICMT).

Autor: Stevenson GI; Eskitis Institute for Drug Discovery, Griffith University, Brisbane, Queensland 4111, Australia. Electronic address: g.stevenson@griffith.edu.au., Yong S, Fechner GA, Neve J, Lock A, Avery VM
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Oct 15; Vol. 23 (20), pp. 5671-3. Date of Electronic Publication: 2013 Aug 12.
DOI: 10.1016/j.bmcl.2013.08.022
Abstrakt: Inhibition of isoprenylcysteine Carboxylmethyltransferase (ICMT) is of particular interest as a potential target for the development of cancer chemotherapeutic agents. Screening for inhibitors of ICMT utilises a scintillation proximity assay (SPA) in which Biotin-S-Farnesyl-L-Cysteine (BFC) acts as a surrogate substrate. A solid-phase synthesis protocol for the preparation of BFC using 2-chlorotrityl chloride resin as a solid support has been developed to provide sufficient supply of BFC for high throughput screening (HTS) and subsequent chemistry campaigns to target inhibitors of ICMT. The BFC prepared by this method can be produced quickly on large scale and is stable when stored at -20 °C as a solid, in solution, or on the resin.
(Copyright © 2013 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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