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Gustav Julius Wørmer

A Cyclopropene Electrophile that Targets Glutathione S-Transferase Omega-1 in Cells

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A Cyclopropene Electrophile that Targets Glutathione S-Transferase Omega-1 in Cells. / Wormer, Gustav J.; Hansen, Bente K.; Palmfeldt, Johan; Poulsen, Thomas B.

I: Angewandte Chemie International Edition, Bind 58, Nr. 34, 07.2019, s. 11918-11922.

Publikation: Bidrag til tidsskrift/Konferencebidrag i tidsskrift /Bidrag til avisTidsskriftartikelForskningpeer review

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@article{0a9fd05615ae426f8c689d562c8df1b8,
title = "A Cyclopropene Electrophile that Targets Glutathione S-Transferase Omega-1 in Cells",
abstract = "Cyclopropenes are an important new addition to the portfolio of functional groups that can be used for bioorthogonal couplings. The inert nature of these highly strained compounds in complex biological systems is almost counterintuitive given their established electrophilic properties in organic synthesis. Here we provide the first demonstration of a cyclopropene that is capable of direct conjugation to protein targets in cells and show that this compound preferentially alkylates the active site cysteine of glutathione S-transferase omega-1 (GSTO1).",
keywords = "chemical proteomics, bioorthogonal chemistry, cyclopropene, electrophiles, GSTO1 inhibition, DISCOVERY, REVEALS, POTENT, ANALOG",
author = "Wormer, {Gustav J.} and Hansen, {Bente K.} and Johan Palmfeldt and Poulsen, {Thomas B.}",
year = "2019",
month = jul,
doi = "10.1002/anie.201907520",
language = "English",
volume = "58",
pages = "11918--11922",
journal = "Angewandte Chemie International Edition",
issn = "1433-7851",
publisher = "Wiley - VCH Verlag GmbH & CO. KGaA",
number = "34",

}

RIS

TY - JOUR

T1 - A Cyclopropene Electrophile that Targets Glutathione S-Transferase Omega-1 in Cells

AU - Wormer, Gustav J.

AU - Hansen, Bente K.

AU - Palmfeldt, Johan

AU - Poulsen, Thomas B.

PY - 2019/7

Y1 - 2019/7

N2 - Cyclopropenes are an important new addition to the portfolio of functional groups that can be used for bioorthogonal couplings. The inert nature of these highly strained compounds in complex biological systems is almost counterintuitive given their established electrophilic properties in organic synthesis. Here we provide the first demonstration of a cyclopropene that is capable of direct conjugation to protein targets in cells and show that this compound preferentially alkylates the active site cysteine of glutathione S-transferase omega-1 (GSTO1).

AB - Cyclopropenes are an important new addition to the portfolio of functional groups that can be used for bioorthogonal couplings. The inert nature of these highly strained compounds in complex biological systems is almost counterintuitive given their established electrophilic properties in organic synthesis. Here we provide the first demonstration of a cyclopropene that is capable of direct conjugation to protein targets in cells and show that this compound preferentially alkylates the active site cysteine of glutathione S-transferase omega-1 (GSTO1).

KW - chemical proteomics

KW - bioorthogonal chemistry

KW - cyclopropene

KW - electrophiles

KW - GSTO1 inhibition

KW - DISCOVERY

KW - REVEALS

KW - POTENT

KW - ANALOG

U2 - 10.1002/anie.201907520

DO - 10.1002/anie.201907520

M3 - Journal article

C2 - 31291041

VL - 58

SP - 11918

EP - 11922

JO - Angewandte Chemie International Edition

JF - Angewandte Chemie International Edition

SN - 1433-7851

IS - 34

ER -