Issue 3, 2012
From the journal:

Organic & Biomolecular Chemistry

Click-enabled heterotrifunctional template for sequential bioconjugations†

David M. Beal,‡*a   Victoria E. Albrow,a   George Burslem,a   Louisa Hitchen,a   Carla Fernandes,a   Cris Lapthorn,a   Lee R. Roberts,a   Matthew D. Selbya  and  Lyn H. Jones§a  

* Corresponding authors

a Chemical Biology Group, Worldwide Medicinal Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent, UK
E-mail: dmb38@kent.ac.uk
Tel: +44 (0) 1304 824209

Abstract

A heterotrifunctional template was developed that utilizes thiol–maleimide and click chemistries (both copper-free and copper-mediated) to effect sequential biomolecule conjugations in a one-pot process. The breadth of compatible substrates was illustrated through highly efficient conjugations of protein, peptide, sugar, lipid, fluoroalkane, biotin and fluorophore molecules. This template should be useful for the creation of chemically-enhanced/enabled biotherapeutics, especially through the expression of discontinuous (and heterogeneous) epitopes.

Graphical abstract: Click-enabled heterotrifunctional template for sequential bioconjugations

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Article information

DOI
https://doi.org/10.1039/C1OB06398G
Article type
Paper
Submitted
16 Aug 2011
Accepted
10 Oct 2011
First published
10 Oct 2011

Org. Biomol. Chem., 2012,10, 548-554

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Click-enabled heterotrifunctional template for sequential bioconjugations

D. M. Beal, V. E. Albrow, G. Burslem, L. Hitchen, C. Fernandes, C. Lapthorn, L. R. Roberts, M. D. Selby and L. H. Jones, Org. Biomol. Chem., 2012, 10, 548 DOI: 10.1039/C1OB06398G

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