Highly Efficient Mono-Functionalization of Knob-in-Hole Antibodies with Strain-Promoted Click Chemistry | Zendy

Jorick J. Bruins | Zendy; Criss van de Wouw | Zendy; Koen Wagner | Zendy; Lina Bartels | Zendy; Bauke Albada | Zendy; Floris L. van Delft | Zendy

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Highly Efficient Mono-Functionalization of Knob-in-Hole Antibodies with Strain-Promoted Click Chemistry

Author(s) -

Jorick J. Bruins,

Criss van de Wouw,

Koen Wagner,

Lina Bartels,

Bauke Albada,

Floris L. van Delft

Publication year - 2019

Publication title -

acs omega

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.779

H-Index - 40

ISSN - 2470-1343

DOI - 10.1021/acsomega.9b01727

Subject(s) - surface modification , sortase , click chemistry , sortase a , chemistry , monoclonal antibody , combinatorial chemistry , trastuzumab , antibody , stereochemistry , biochemistry , biology , bacterial protein , genetics , cancer , breast cancer , immunology , gene

Knob-in-hole antibodies can be utilized to introduce a single tag for chemo-enzymatic functionalization. By either introducing a single C-terminal sortase tag (sortase-tag expressed protein ligation) or tyrosine tag (G 4 Y), mono-functionalization of the monoclonal antibody trastuzumab was achieved rapidly and in high yields. This method was applied to selectively and efficiently introduce a single fluorescent tag, cytokine or single-chain variable fragment, as well as produce clean homo dimers of trastuzumab.

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