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

8 Citations (Scopus)

27 Downloads (Pure)

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

Access to Document

10.1021/acs.bioconjchem.0c00282

Accepted_ManuscriptAccepted author manuscript, 301 KB

Cite this

@article{56cb3b2e04474fc08379107aec2f6a87,

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",

year = "2020",

month = jul,

day = "15",

doi = "10.1021/acs.bioconjchem.0c00282",

language = "English",

volume = "31",

pages = "1745–1749",

journal = "Bioconjugate Chemistry",

issn = "1043-1802",

publisher = "American Chemical Society",

number = "7",

}

TY - JOUR

T1 - A peptide-duocarmycin conjugate targeting the Thomsen-Friedenreich antigen has potent and selective antitumour activity

AU - Cartwright, Oliver Charles

AU - Beekman, Andrew Michael

AU - Cominetti, Marco M. D.

AU - Russell, David A.

AU - Searcey, Mark

PY - 2020/7/15

Y1 - 2020/7/15

N2 - 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.

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.

UR - http://www.scopus.com/inward/record.url?scp=85088176869&partnerID=8YFLogxK

U2 - 10.1021/acs.bioconjchem.0c00282

DO - 10.1021/acs.bioconjchem.0c00282

M3 - Article

C2 - 32515945

SN - 1043-1802

VL - 31

SP - 1745

EP - 1749

JO - Bioconjugate Chemistry

JF - Bioconjugate Chemistry

IS - 7

ER -

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

Abstract

Access to Document

Other files and links

Andrew Beekman

Mark Searcey

Cite this

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

Abstract

Access to Document

Other files and links

Profiles

Andrew Beekman

Mark Searcey

Cite this