Autor: |
Shreder KR; ActivX Biosciences, Inc., 11025 North Torrey Pines Road, La Jolla, California 92037, USA. kevins@activx.com, Wong MS, Nomanbhoy T, Leventhal PS, Fuller SR |
Jazyk: |
angličtina |
Zdroj: |
Organic letters [Org Lett] 2004 Oct 14; Vol. 6 (21), pp. 3715-8. |
DOI: |
10.1021/ol048656a |
Abstrakt: |
[structure: see text] The synthesis of a photoaffinity probe for EGFR is described. O-Alkylation of 4-(meta-azidoanilino)-6-methoxy-7-hydroxy-quinazoline with a protected tetraethyleneglycol linker followed by the attachment of tetramethylrhodamine yielded the fluorescent probe AX7593. Photoaffinity labeling of EGFR by AX7593 (K(b) = 280 nM) was shown to have an efficiency of 34% and to be competitive with the EGFR inhibitors PP2 and AG1478. |
Databáze: |
MEDLINE |
Externí odkaz: |
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