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Issue 53, 2018
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Single-site labeling of lysine in proteins through a metal-free multicomponent approach

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Abstract

We report a chemoselective and site-selective approach that distinguishes one Lys from its multiple copies, N-terminus, and other competitors. The phospha-Mannich protocol works with multiple proteins and installs probes without structural and functional perturbations. It delivers an antibody–drug conjugate with selective anti-proliferative activity towards HER2 expressing SKBR3 breast cancer cells.

Graphical abstract: Single-site labeling of lysine in proteins through a metal-free multicomponent approach

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Article information


Submitted
24 Apr 2018
Accepted
06 Jun 2018
First published
07 Jun 2018

Chem. Commun., 2018,54, 7302-7305
Article type
Communication

Single-site labeling of lysine in proteins through a metal-free multicomponent approach

M. Chilamari, N. Kalra, S. Shukla and V. Rai, Chem. Commun., 2018, 54, 7302
DOI: 10.1039/C8CC03311K

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