Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)
Nicola E.A Chessum
1
,
Swee Y. Sharp
1
,
John J. Caldwell
1
,
A Elisa Pasqua
1
,
Birgit Wilding
1
,
Giampiero Colombano
1
,
Ian M. Collins
1
,
Bugra Ozer
1
,
Meirion Richards
1
,
Martin Rowlands
1
,
Mark Stubbs
1
,
Rosemary Burke
1
,
P. Craig McAndrew
1
,
Paul Clarke
1
,
Paul Workman
1
,
Matthew D Cheeseman
1
,
K JONES
1
1
Cancer Research
UK Cancer Therapeutics Unit at The Institute of Cancer Research, London SW7 3RP, United Kingdom
|
Тип публикации: Journal Article
Дата публикации: 2018-01-05
scimago Q1
wos Q1
БС1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
29240418
Drug Discovery
Molecular Medicine
Краткое описание
Demonstrating intracellular protein target engagement is an essential step in the development and progression of new chemical probes and potential small molecule therapeutics. However, this can be particularly challenging for poorly studied and noncatalytic proteins, as robust proximal biomarkers are rarely known. To confirm that our recently discovered chemical probe 1 (CCT251236) binds the putative transcription factor regulator pirin in living cells, we developed a heterobifunctional protein degradation probe. Focusing on linker design and physicochemical properties, we generated a highly active probe 16 (CCT367766) in only three iterations, validating our efficient strategy for degradation probe design against nonvalidated protein targets.
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(11.37%)
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ГОСТ |
RIS |
BibTex |
MLA
Цитировать
ГОСТ
Скопировать
Chessum N. E. et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766) // Journal of Medicinal Chemistry. 2018. Vol. 61. No. 3. pp. 918-933.
ГОСТ со всеми авторами (до 50)
Скопировать
Chessum N. E., Sharp S. Y., Caldwell J. J., Pasqua A. E., Wilding B., Colombano G., Collins I. M., Ozer B., Richards M., Rowlands M., Stubbs M., Burke R., McAndrew P. C., Clarke P., Workman P., Cheeseman M. D., JONES K. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766) // Journal of Medicinal Chemistry. 2018. Vol. 61. No. 3. pp. 918-933.
Цитировать
RIS
Скопировать
TY - JOUR
DO - 10.1021/acs.jmedchem.7b01406
UR - https://doi.org/10.1021/acs.jmedchem.7b01406
TI - Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)
T2 - Journal of Medicinal Chemistry
AU - Chessum, Nicola E.A
AU - Sharp, Swee Y.
AU - Caldwell, John J.
AU - Pasqua, A Elisa
AU - Wilding, Birgit
AU - Colombano, Giampiero
AU - Collins, Ian M.
AU - Ozer, Bugra
AU - Richards, Meirion
AU - Rowlands, Martin
AU - Stubbs, Mark
AU - Burke, Rosemary
AU - McAndrew, P. Craig
AU - Clarke, Paul
AU - Workman, Paul
AU - Cheeseman, Matthew D
AU - JONES, K
PY - 2018
DA - 2018/01/05
PB - American Chemical Society (ACS)
SP - 918-933
IS - 3
VL - 61
PMID - 29240418
SN - 0022-2623
SN - 1520-4804
ER -
Цитировать
BibTex (до 50 авторов)
Скопировать
@article{2018_Chessum,
author = {Nicola E.A Chessum and Swee Y. Sharp and John J. Caldwell and A Elisa Pasqua and Birgit Wilding and Giampiero Colombano and Ian M. Collins and Bugra Ozer and Meirion Richards and Martin Rowlands and Mark Stubbs and Rosemary Burke and P. Craig McAndrew and Paul Clarke and Paul Workman and Matthew D Cheeseman and K JONES},
title = {Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)},
journal = {Journal of Medicinal Chemistry},
year = {2018},
volume = {61},
publisher = {American Chemical Society (ACS)},
month = {jan},
url = {https://doi.org/10.1021/acs.jmedchem.7b01406},
number = {3},
pages = {918--933},
doi = {10.1021/acs.jmedchem.7b01406}
}
Цитировать
MLA
Скопировать
Chessum, Nicola E.A, et al. “Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).” Journal of Medicinal Chemistry, vol. 61, no. 3, Jan. 2018, pp. 918-933. https://doi.org/10.1021/acs.jmedchem.7b01406.