Selective Lysine Modification Enabled by Intramolecular Acyl Transfer
作者:David Hymel、Fa Liu
DOI:10.1021/acs.orglett.0c00816
日期:2020.4.17
recombinant proteins are valuable for the discovery and development of biologic therapeutics. We report here a Lys modification strategy that engages a Cys residue to covalently tether the reagents to the target that facilitates a proximity-driven intramolecular O-to-N acyl-transfer process yielding desired Lys-acylated products. We utilized GLP-1 as a case study, followed by desulfurization of the Cys
4-substitued-3-[1 or 2 amino acid residue]-azetidin-2-one derivatives
申请人:Synphar Laboratories, Inc.
公开号:US05986108A1
公开(公告)日:1999-11-16
Disclosed herein are azetidin-2-one compounds which exhibit excellent cysteine proteinase inhibitory activity. The compounds are 4-substituted-3-1 or 2 amino acid residue}-azetidin-2-ones of forumula I ##STR1## wherein AAR is a 1 or 2 acid residue, and R.sub.1 and R.sub.2 are as defined herein. The compounds can be used in the treatment of various diseases such as muscular dystrophy, bone resorption disorders, myocardial infarction and cancer metastasis.