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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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Publication details

The article was received on 24 Apr 2018, accepted on 06 Jun 2018 and first published on 07 Jun 2018


Article type: Communication
DOI: 10.1039/C8CC03311K
Citation: Chem. Commun., 2018, Advance Article
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    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, Advance Article , DOI: 10.1039/C8CC03311K

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