期刊
JOURNAL OF PEPTIDE RESEARCH
卷 63, 期 3, 页码 297-302出版社
WILEY
DOI: 10.1111/j.1399-3011.2004.00152.x
关键词
cystathionine; disulfide; estrogen receptor; helical peptides
Cystine, lanthionine, and cystathionine containing cyclic peptides incorporating the signature nuclear receptor (NR) box (LXXLL) motif have been synthesized and the abilities of these peptides to inhibit estrogen receptor (ER)-coactivator interactions have been determined. We found that helicity of these peptides directly correlated with their bioactivity. Cystathionine proved to be a redox-stable, isosteric replacement for the cystine disulfide. Cystathionine containing peptide 3 showed higher helical character and a lower inhibition constant (Ki, 7 nM) when compared with its cystine counterpart.
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