Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer
Тип публикации: Journal Article
Дата публикации: 2020-04-06
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 1.726
CiteScore: 11.1
Impact factor: 7.3
ISSN: 00222623, 15204804
PubMed ID:
32250617
Drug Discovery
Molecular Medicine
Краткое описание
Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target's resurgence. As previously reported, the tetrahydropyridopyrimidines were identified as irreversible covalent inhibitors of KRASG12C that bind in the switch-II pocket of KRAS and make a covalent bond to cysteine 12. Using structure-based drug design in conjunction with a focused in vitro absorption, distribution, metabolism and excretion screening approach, analogues were synthesized to increase the potency and reduce metabolic liabilities of this series. The discovery of the clinical development candidate MRTX849 as a potent, selective covalent inhibitor of KRASG12C is described.
Найдено
Ничего не найдено, попробуйте изменить настройки фильтра.
Для доступа к списку цитирований публикации необходимо авторизоваться.
Для доступа к списку профилей, цитирующих публикацию, необходимо авторизоваться.
Топ-30
Журналы
|
10
20
30
40
50
60
|
|
|
Journal of Medicinal Chemistry
60 публикаций, 10.47%
|
|
|
bioRxiv
33 публикации, 5.76%
|
|
|
European Journal of Medicinal Chemistry
27 публикаций, 4.71%
|
|
|
Cancers
12 публикаций, 2.09%
|
|
|
Organic Process Research and Development
11 публикаций, 1.92%
|
|
|
Journal of the American Chemical Society
11 публикаций, 1.92%
|
|
|
Nature Communications
9 публикаций, 1.57%
|
|
|
Bioorganic Chemistry
9 публикаций, 1.57%
|
|
|
Bioorganic and Medicinal Chemistry
8 публикаций, 1.4%
|
|
|
International Journal of Molecular Sciences
7 публикаций, 1.22%
|
|
|
Nature Chemical Biology
7 публикаций, 1.22%
|
|
|
eLife
6 публикаций, 1.05%
|
|
|
Scientific Reports
6 публикаций, 1.05%
|
|
|
Journal of Chemical Information and Modeling
5 публикаций, 0.87%
|
|
|
Pharmaceuticals
5 публикаций, 0.87%
|
|
|
Medicinal Research Reviews
5 публикаций, 0.87%
|
|
|
ACS Chemical Biology
5 публикаций, 0.87%
|
|
|
RSC Medicinal Chemistry
5 публикаций, 0.87%
|
|
|
RSC Chemical Biology
5 публикаций, 0.87%
|
|
|
Annual Reports in Medicinal Chemistry
5 публикаций, 0.87%
|
|
|
Results in Chemistry
5 публикаций, 0.87%
|
|
|
Frontiers in Oncology
4 публикации, 0.7%
|
|
|
Cancer and Metastasis Reviews
4 публикации, 0.7%
|
|
|
Signal Transduction and Targeted Therapy
4 публикации, 0.7%
|
|
|
Drug Discovery Today
4 публикации, 0.7%
|
|
|
Journal of Biological Chemistry
4 публикации, 0.7%
|
|
|
Angewandte Chemie
4 публикации, 0.7%
|
|
|
Cancer Discovery
4 публикации, 0.7%
|
|
|
ACS Medicinal Chemistry Letters
4 публикации, 0.7%
|
|
|
10
20
30
40
50
60
|
Издатели
|
20
40
60
80
100
120
140
|
|
|
Elsevier
123 публикации, 21.47%
|
|
|
American Chemical Society (ACS)
122 публикации, 21.29%
|
|
|
Springer Nature
89 публикаций, 15.53%
|
|
|
MDPI
36 публикаций, 6.28%
|
|
|
openRxiv
34 публикации, 5.93%
|
|
|
Wiley
33 публикации, 5.76%
|
|
|
Taylor & Francis
26 публикаций, 4.54%
|
|
|
Royal Society of Chemistry (RSC)
23 публикации, 4.01%
|
|
|
American Association for Cancer Research (AACR)
14 публикаций, 2.44%
|
|
|
Frontiers Media S.A.
13 публикаций, 2.27%
|
|
|
eLife Sciences Publications
6 публикаций, 1.05%
|
|
|
American Association for the Advancement of Science (AAAS)
6 публикаций, 1.05%
|
|
|
Bentham Science Publishers Ltd.
5 публикаций, 0.87%
|
|
|
Ovid Technologies (Wolters Kluwer Health)
4 публикации, 0.7%
|
|
|
SAGE
4 публикации, 0.7%
|
|
|
Portland Press
3 публикации, 0.52%
|
|
|
Massachusetts Medical Society
3 публикации, 0.52%
|
|
|
BMJ
3 публикации, 0.52%
|
|
|
Proceedings of the National Academy of Sciences (PNAS)
2 публикации, 0.35%
|
|
|
American Society of Clinical Oncology (ASCO)
2 публикации, 0.35%
|
|
|
Annual Reviews
2 публикации, 0.35%
|
|
|
American Society for Biochemistry and Molecular Biology
1 публикация, 0.17%
|
|
|
Georg Thieme Verlag KG
1 публикация, 0.17%
|
|
|
Impact Journals
1 публикация, 0.17%
|
|
|
AME Publishing Company
1 публикация, 0.17%
|
|
|
Eco-Vector LLC
1 публикация, 0.17%
|
|
|
Beilstein-Institut
1 публикация, 0.17%
|
|
|
The Society of Synthetic Organic Chemistry, Japan
1 публикация, 0.17%
|
|
|
PeerJ
1 публикация, 0.17%
|
|
|
20
40
60
80
100
120
140
|
- 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
574
Всего цитирований:
574
Цитирований c 2025:
191
(33.33%)
Цитировать
ГОСТ |
RIS |
BibTex |
MLA
Цитировать
ГОСТ
Скопировать
Fell J. B. et al. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer // Journal of Medicinal Chemistry. 2020. Vol. 63. No. 13. pp. 6679-6693.
ГОСТ со всеми авторами (до 50)
Скопировать
Fell J. B., Fischer J. P., Baer B. R., Blake J. F., Bouhana K., Briere D. M., Brown K. D., Burgess L. E., Burns A. C., Burkard M. R., Chiang H., Chicarelli M. J., Cook A. W., Gaudino J. J., Hallin J., Hanson L., Hartley D. P., Hicken E. J., Hingorani G. P., Hinklin R. J., Mejia M. J., Olson P., Otten J. N., Rhodes S. P., Rodriguez M. E., Savechenkov P., Smith D. J., Sudhakar N., Sullivan F. X., Tang T. P., Vigers G. P., Wollenberg L., Christensen J. G., Marx M. A. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer // Journal of Medicinal Chemistry. 2020. Vol. 63. No. 13. pp. 6679-6693.
Цитировать
RIS
Скопировать
TY - JOUR
DO - 10.1021/acs.jmedchem.9b02052
UR - https://doi.org/10.1021/acs.jmedchem.9b02052
TI - Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer
T2 - Journal of Medicinal Chemistry
AU - Fell, Jay B
AU - Fischer, John P.
AU - Baer, Brian R
AU - Blake, James F.
AU - Bouhana, Karyn
AU - Briere, David M
AU - Brown, Karin D
AU - Burgess, Laurence E
AU - Burns, Aaron C
AU - Burkard, Michael R
AU - Chiang, Harrah
AU - Chicarelli, Mark J
AU - Cook, Adam W.
AU - Gaudino, John J.
AU - Hallin, Jill
AU - Hanson, Lauren
AU - Hartley, Dylan P.
AU - Hicken, Erik J
AU - Hingorani, Gary P.
AU - Hinklin, Ronald J
AU - Mejia, Macedonio J
AU - Olson, Peter
AU - Otten, Jennifer N
AU - Rhodes, Susan P
AU - Rodriguez, Martha E
AU - Savechenkov, Pavel
AU - Smith, Darin J.
AU - Sudhakar, Niranjan
AU - Sullivan, Francis X.
AU - Tang, Tony P
AU - Vigers, Guy P.A.
AU - Wollenberg, Lance
AU - Christensen, James G.
AU - Marx, Matthew A.
PY - 2020
DA - 2020/04/06
PB - American Chemical Society (ACS)
SP - 6679-6693
IS - 13
VL - 63
PMID - 32250617
SN - 0022-2623
SN - 1520-4804
ER -
Цитировать
BibTex (до 50 авторов)
Скопировать
@article{2020_Fell,
author = {Jay B Fell and John P. Fischer and Brian R Baer and James F. Blake and Karyn Bouhana and David M Briere and Karin D Brown and Laurence E Burgess and Aaron C Burns and Michael R Burkard and Harrah Chiang and Mark J Chicarelli and Adam W. Cook and John J. Gaudino and Jill Hallin and Lauren Hanson and Dylan P. Hartley and Erik J Hicken and Gary P. Hingorani and Ronald J Hinklin and Macedonio J Mejia and Peter Olson and Jennifer N Otten and Susan P Rhodes and Martha E Rodriguez and Pavel Savechenkov and Darin J. Smith and Niranjan Sudhakar and Francis X. Sullivan and Tony P Tang and Guy P.A. Vigers and Lance Wollenberg and James G. Christensen and Matthew A. Marx},
title = {Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer},
journal = {Journal of Medicinal Chemistry},
year = {2020},
volume = {63},
publisher = {American Chemical Society (ACS)},
month = {apr},
url = {https://doi.org/10.1021/acs.jmedchem.9b02052},
number = {13},
pages = {6679--6693},
doi = {10.1021/acs.jmedchem.9b02052}
}
Цитировать
MLA
Скопировать
Fell, Jay B., et al. “Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.” Journal of Medicinal Chemistry, vol. 63, no. 13, Apr. 2020, pp. 6679-6693. https://doi.org/10.1021/acs.jmedchem.9b02052.
Ошибка в публикации?