发明名称 Site-specific chemoenzymatic protein modifications
摘要 The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.
申请公布号 US9359400(B2) 申请公布日期 2016.06.07
申请号 US201414329758 申请日期 2014.07.11
申请人 NOVARTIS AG 发明人 Usera Aimee;Robinson Zachary;Cobb Jennifer
分类号 C07K5/103;A61K49/00;A61K47/48;C07K5/083;C07K5/062;C07K1/13;C07D209/42;C07K7/02;C07K5/072;C07C271/22;C07C317/28;A61K38/06;A61K38/05;A61K38/07 主分类号 C07K5/103
代理机构 Brinks Gilson & Lione 代理人 Brinks Gilson & Lione ;Marshall Ryan L.
主权项 1. A compound of the formula R1-(Leu)x-Gln-(Gly)y-(A-W-B-R2) z wherein x is 0 or 1; y is 0 or 1; z is 0 or 1; R1 is selected from the group consisting of: wherein R4 is selected from —H, —N3, and W is selected from: C1-C6 linear or branches alkyl or polyethylene glycol having a molecular weight of between about 40 and about 80,000 amu; A is absent or selected from —O—, —NH—, and —S—; B is absent or selected from —O—, —C(O)—, —NH—, —C(O)NH—, —NHC(O)—, —NHC(O)O—, —OC(O)NH—, —OC(O)O—, —C═N(OH)—, —S(O2)—, —NHS(O2)—, —S(O2)NH—, —S(O)—, —NHS(O)—, —S(O)NH—; —C(O)O—, —OC(O)—, —S—, ═NH—O—, ═NH—NH— and ═NH—N(C1-C20alkyl)-; R2 is selected from the group consisting of: a fatty acid, linear or branched C1-C3 alkyl-N3, cyclooctynyl, polysaccharide, —CH(OCH3)2, each n is an integer independently selected from 0 to 6; and each Q is selected from H and —NO2.
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