Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7
Тип публикации: Journal Article
Дата публикации: 2017-11-07
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 5.495
CiteScore: 27.6
Impact factor: 16.9
ISSN: 14337851, 15213773
PubMed ID:
28976073
General Chemistry
Catalysis
Краткое описание
Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell-permeable inhibitors or suitable tool compounds for these enzymes. We describe the discovery of a new class of inhibitor that is highly potent towards the histone lysine demethylases KDM2A/7A. A modular synthetic approach was used to explore the chemical space and accelerate the investigation of key structure-activity relationships, leading to the development of a small molecule with around 75-fold selectivity towards KDM2A/7A versus other KDMs, as well as cellular activity at low micromolar concentrations.
Найдено
Ничего не найдено, попробуйте изменить настройки фильтра.
Для доступа к списку цитирований публикации необходимо авторизоваться.
Топ-30
Журналы
|
1
2
|
|
|
Epigenomes
2 публикации, 5.13%
|
|
|
Journal of Organic Chemistry
2 публикации, 5.13%
|
|
|
Genes
1 публикация, 2.56%
|
|
|
Frontiers in Cell and Developmental Biology
1 публикация, 2.56%
|
|
|
Pharmaceutics
1 публикация, 2.56%
|
|
|
Nature Communications
1 публикация, 2.56%
|
|
|
Scientific Reports
1 публикация, 2.56%
|
|
|
Journal of Drug Delivery Science and Technology
1 публикация, 2.56%
|
|
|
Drug Discovery Today
1 публикация, 2.56%
|
|
|
European Journal of Medicinal Chemistry
1 публикация, 2.56%
|
|
|
Journal of Molecular Biology
1 публикация, 2.56%
|
|
|
Journal of Biological Chemistry
1 публикация, 2.56%
|
|
|
Computational and Structural Biotechnology Journal
1 публикация, 2.56%
|
|
|
FEBS Journal
1 публикация, 2.56%
|
|
|
RSC Chemical Biology
1 публикация, 2.56%
|
|
|
Chemical Science
1 публикация, 2.56%
|
|
|
Synlett
1 публикация, 2.56%
|
|
|
Advances in Protein Chemistry and Structural Biology
1 публикация, 2.56%
|
|
|
Topics in Medicinal Chemistry
1 публикация, 2.56%
|
|
|
Molecular and Cellular Proteomics
1 публикация, 2.56%
|
|
|
Progress in Molecular Biology and Translational Science
1 публикация, 2.56%
|
|
|
Medicinal Research Reviews
1 публикация, 2.56%
|
|
|
Experimental and Therapeutic Medicine
1 публикация, 2.56%
|
|
|
Biochemical Pharmacology
1 публикация, 2.56%
|
|
|
Biochimica et Biophysica Acta - Gene Regulatory Mechanisms
1 публикация, 2.56%
|
|
|
Green Chemistry
1 публикация, 2.56%
|
|
|
Signal Transduction and Targeted Therapy
1 публикация, 2.56%
|
|
|
Cellular and Molecular Life Sciences
1 публикация, 2.56%
|
|
|
Molecules and Cells
1 публикация, 2.56%
|
|
|
1
2
|
Издатели
|
2
4
6
8
10
12
|
|
|
Elsevier
12 публикаций, 30.77%
|
|
|
Springer Nature
6 публикаций, 15.38%
|
|
|
MDPI
4 публикации, 10.26%
|
|
|
Royal Society of Chemistry (RSC)
4 публикации, 10.26%
|
|
|
Wiley
3 публикации, 7.69%
|
|
|
American Society for Biochemistry and Molecular Biology
2 публикации, 5.13%
|
|
|
American Chemical Society (ACS)
2 публикации, 5.13%
|
|
|
Taylor & Francis
2 публикации, 5.13%
|
|
|
Frontiers Media S.A.
1 публикация, 2.56%
|
|
|
Georg Thieme Verlag KG
1 публикация, 2.56%
|
|
|
Spandidos Publications
1 публикация, 2.56%
|
|
|
Autonomous Non-profit Organization Editorial Board of the journal Uspekhi Khimii
1 публикация, 2.56%
|
|
|
2
4
6
8
10
12
|
- Мы не учитываем публикации, у которых нет DOI.
- Статистика публикаций обновляется еженедельно.
Вы ученый?
Создайте профиль, чтобы получать персональные рекомендации коллег, конференций и новых статей.
Войти с ORCID
Метрики
39
Всего цитирований:
39
Цитирований c 2025:
7
(17.95%)
Цитировать
ГОСТ |
RIS |
BibTex |
MLA
Цитировать
ГОСТ
Скопировать
Gerken P. A. et al. Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7 // Angewandte Chemie - International Edition. 2017. Vol. 56. No. 49. pp. 15555-15559.
ГОСТ со всеми авторами (до 50)
Скопировать
Gerken P. A., Wolstenhulme J. R., Tumber A., Hatch S. B., Zhang Y., Müller S., Chandler S. A., Mair B., Li F., Nijman S. M., Konietzny R., Szommer T., Yapp C., Fedorov O., Benesch J. L., Vedadi M., Kessler B., Kawamura A., Brennan P. E., Smith M. H. Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7 // Angewandte Chemie - International Edition. 2017. Vol. 56. No. 49. pp. 15555-15559.
Цитировать
RIS
Скопировать
TY - JOUR
DO - 10.1002/anie.201706788
UR - https://doi.org/10.1002/anie.201706788
TI - Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7
T2 - Angewandte Chemie - International Edition
AU - Gerken, Philip A
AU - Wolstenhulme, Jamie R
AU - Tumber, Anthony
AU - Hatch, Stephanie B
AU - Zhang, Yijia
AU - Müller, Susanne
AU - Chandler, Shane A
AU - Mair, Barbara
AU - Li, Fengling
AU - Nijman, Sebastian M.B.
AU - Konietzny, Rebecca
AU - Szommer, Tamas
AU - Yapp, Clarence
AU - Fedorov, Oleg
AU - Benesch, Justin L.P.
AU - Vedadi, Masoud
AU - Kessler, B.
AU - Kawamura, Akane
AU - Brennan, Paul E.
AU - Smith, Martin H.
PY - 2017
DA - 2017/11/07
PB - Wiley
SP - 15555-15559
IS - 49
VL - 56
PMID - 28976073
SN - 1433-7851
SN - 1521-3773
ER -
Цитировать
BibTex (до 50 авторов)
Скопировать
@article{2017_Gerken,
author = {Philip A Gerken and Jamie R Wolstenhulme and Anthony Tumber and Stephanie B Hatch and Yijia Zhang and Susanne Müller and Shane A Chandler and Barbara Mair and Fengling Li and Sebastian M.B. Nijman and Rebecca Konietzny and Tamas Szommer and Clarence Yapp and Oleg Fedorov and Justin L.P. Benesch and Masoud Vedadi and B. Kessler and Akane Kawamura and Paul E. Brennan and Martin H. Smith},
title = {Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7},
journal = {Angewandte Chemie - International Edition},
year = {2017},
volume = {56},
publisher = {Wiley},
month = {nov},
url = {https://doi.org/10.1002/anie.201706788},
number = {49},
pages = {15555--15559},
doi = {10.1002/anie.201706788}
}
Цитировать
MLA
Скопировать
Gerken, Philip A., et al. “Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7.” Angewandte Chemie - International Edition, vol. 56, no. 49, Nov. 2017, pp. 15555-15559. https://doi.org/10.1002/anie.201706788.
Ошибка в публикации?