A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Cyrille S. Kounde; Maria M. Shchepinova; Charlie N. Saunders; Marcel Muelbaier; Mark D. Rackham; John D. Harling; Edward W. Tate

doi:10.1039/d0cc00523a

A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Cyrille S. Kounde, Maria M. Shchepinova, Charlie N. Saunders, Marcel Muelbaier, Mark D. Rackham, John D. Harling, Edward W. Tate

Department of Chemistry

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

113 Citations (SciVal)

Abstract

With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy.

Original language	English
Pages (from-to)	5532-5535
Number of pages	4
Journal	Chemical Communications
Volume	56
Issue number	41
DOIs	https://doi.org/10.1039/d0cc00523a
Publication status	Published - 21 May 2020

ASJC Scopus subject areas

Electronic, Optical and Magnetic Materials
Catalysis
Ceramics and Composites
General Chemistry
Surfaces, Coatings and Films
Metals and Alloys
Materials Chemistry

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10.1039/d0cc00523aLicence: CC BY-NC

Cite this

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abstract = "With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy.",

author = "Kounde, \{Cyrille S.\} and Shchepinova, \{Maria M.\} and Saunders, \{Charlie N.\} and Marcel Muelbaier and Rackham, \{Mark D.\} and Harling, \{John D.\} and Tate, \{Edward W.\}",

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AU - Kounde, Cyrille S.

AU - Shchepinova, Maria M.

AU - Saunders, Charlie N.

AU - Muelbaier, Marcel

AU - Rackham, Mark D.

AU - Harling, John D.

AU - Tate, Edward W.

PY - 2020/5/21

Y1 - 2020/5/21

N2 - With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy.

AB - With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy.

UR - https://www.scopus.com/pages/publications/85085264012

U2 - 10.1039/d0cc00523a

DO - 10.1039/d0cc00523a

M3 - Article

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AN - SCOPUS:85085264012

SN - 1359-7345

VL - 56

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EP - 5535

JO - Chemical Communications

JF - Chemical Communications

IS - 41

ER -

A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Abstract

ASJC Scopus subject areas

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