Solid-phase synthesis of Biotin-S-Farnesyl-L-Cysteine, a surrogate substrate for isoprenylcysteine Carboxylmethyltransferase (ICMT).
Bioorg Med Chem Lett
; 23(20): 5671-3, 2013 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-23988355
ABSTRACT
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.
Palavras-chave
Biotin-S-Farnesyl-l-Cysteine (BFC); DMF; HBTU; HOBt; Isoprenylcysteine Carboxylmethyltransferase (ICMT); N,N-dimethylformamide; O-benzotriazole-N,N,N', N'-tetramethyluronium hexafluoro-phosphate; Prenylation; S-adenosyl-l-homocysteine; S-adenosyl-l-methionine; S:N; SAH; SAM; hydroxy-benzotriazole; signal to noise
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Proteínas Metiltransferases
/
Biotina
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Cisteína
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article