Delineating functionally important regions and residues in the cathepsin B propeptide for inhibitory activity
Delineating functionally important regions and residues in the cathepsin B propeptide for inhibitory activity
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DOI:
10.1016/0014-5793(96)00847-2
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发表时间:
1996-09-09
期刊:
影响因子:
3.5
通讯作者:
Storer, AC
中科院分区:
文献类型:
--
作者:
Chen, YM;Plouffe, C;Storer, AC
Synthetic peptides derived from the proregion of rat cathepsin B were used to identify functionally important regions and residues for cathepsin B inhibition. Successive 5 amino acid deletions of a 56 amino acid propeptide from both the N- and C-termini has allowed the identification of two regions important for inhibitory activity: the NTTWQ (residues 21p-25p) and CGTVL (42p-46p) regions, Alanine scanning of residues within these two regions indicates that Trp-24p and Cys-42p contribute strongly to inhibition, their replacement by Ala resulting in 160- and 140-fold increases in K-i, respectively.