A peptide-duocarmycin conjugate targeting the Thomsen-Friedenreich antigen has potent and selective antitumour activity

Oliver Charles Cartwright; Andrew Michael Beekman; Marco M. D. Cominetti; David A. Russell; Mark Searcey

doi:10.1021/acs.bioconjchem.0c00282

A peptide-duocarmycin conjugate targeting the Thomsen-Friedenreich antigen has potent and selective antitumour activity

Oliver Charles Cartwright, Andrew Michael Beekman, Marco M. D. Cominetti, David A. Russell, Mark Searcey

Norwich Institute for Healthy Aging

Research output: Contribution to journal › Article › peer-review

7 Citations (Scopus)

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Abstract

Solid phase synthesis allowed the rapid generation of a peptide-drug conjugate. A peptide targeting the Thomsen-Friedenreich antigen (TFα) was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The compound, containing a cathepsin B cleavable linker, was shown to be active and selective against TFα expressing tumour cell lines.

Original language	English
Pages (from-to)	1745–1749
Number of pages	5
Journal	Bioconjugate Chemistry
Volume	31
Issue number	7
Early online date	9 Jun 2020
DOIs	https://doi.org/10.1021/acs.bioconjchem.0c00282
Publication status	Published - 15 Jul 2020

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10.1021/acs.bioconjchem.0c00282

Accepted_ManuscriptAccepted author manuscript, 301 KB

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title = "A peptide-duocarmycin conjugate targeting the Thomsen-Friedenreich antigen has potent and selective antitumour activity",

abstract = "Solid phase synthesis allowed the rapid generation of a peptide-drug conjugate. A peptide targeting the Thomsen-Friedenreich antigen (TFα) was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The compound, containing a cathepsin B cleavable linker, was shown to be active and selective against TFα expressing tumour cell lines.",

author = "Cartwright, {Oliver Charles} and Beekman, {Andrew Michael} and Cominetti, {Marco M. D.} and Russell, {David A.} and Mark Searcey",

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AU - Cartwright, Oliver Charles

AU - Beekman, Andrew Michael

AU - Cominetti, Marco M. D.

AU - Russell, David A.

AU - Searcey, Mark

PY - 2020/7/15

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AB - Solid phase synthesis allowed the rapid generation of a peptide-drug conjugate. A peptide targeting the Thomsen-Friedenreich antigen (TFα) was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The compound, containing a cathepsin B cleavable linker, was shown to be active and selective against TFα expressing tumour cell lines.

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A peptide-duocarmycin conjugate targeting the Thomsen-Friedenreich antigen has potent and selective antitumour activity

Abstract

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Andrew Beekman

Mark Searcey

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A peptide-duocarmycin conjugate targeting the Thomsen-Friedenreich antigen has potent and selective antitumour activity

Abstract

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Andrew Beekman

Mark Searcey

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