Author: Brandon Alexander Holt; Gabriel A. Kwong
Title: Bacterial defiance as a form of prodrug failure Document date: 2019_2_21
ID: 9le4s67m_6
Snippet: To construct bacteria-activated prodrugs, we synthesized cationic (polyarginine) AMPs in charge complexation with anionic peptide locks (polyglutamic acid) by a linker peptide (RRS|RRV) specific for the ubiquitous bacterial protease OmpT 26 . Upon proteolytic cleavage of the linker, the hairpin prodrug is unlocked to release free AMP, creating a mechanism for auto-titration (Fig. 1B) . 10.....
Document: To construct bacteria-activated prodrugs, we synthesized cationic (polyarginine) AMPs in charge complexation with anionic peptide locks (polyglutamic acid) by a linker peptide (RRS|RRV) specific for the ubiquitous bacterial protease OmpT 26 . Upon proteolytic cleavage of the linker, the hairpin prodrug is unlocked to release free AMP, creating a mechanism for auto-titration (Fig. 1B) . 10
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