Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor
Тип публикации: Journal Article
Дата публикации: 2021-12-10
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 1.726
CiteScore: 11.1
Impact factor: 7.3
ISSN: 00222623, 15204804
PubMed ID:
34889605
Drug Discovery
Molecular Medicine
Краткое описание
KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of KRASG12D presents a significant challenge due to the requirement of inhibitors to bind KRASG12D with high enough affinity to obviate the need for covalent interactions with the mutant KRAS protein. Here, we report the discovery and characterization of the first noncovalent, potent, and selective KRASG12D inhibitor, MRTX1133, which was discovered through an extensive structure-based activity improvement and shown to be efficacious in a KRASG12D mutant xenograft mouse tumor model.
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
|
|
|
bioRxiv
60 публикаций, 8.68%
|
|
|
Journal of Medicinal Chemistry
28 публикаций, 4.05%
|
|
|
Cancers
17 публикаций, 2.46%
|
|
|
European Journal of Medicinal Chemistry
14 публикаций, 2.03%
|
|
|
International Journal of Molecular Sciences
12 публикаций, 1.74%
|
|
|
ACS Medicinal Chemistry Letters
10 публикаций, 1.45%
|
|
|
Frontiers in Oncology
9 публикаций, 1.3%
|
|
|
Journal of the American Chemical Society
9 публикаций, 1.3%
|
|
|
Nature Communications
9 публикаций, 1.3%
|
|
|
Journal of Chemical Information and Modeling
7 публикаций, 1.01%
|
|
|
Scientific Reports
7 публикаций, 1.01%
|
|
|
Journal of Biological Chemistry
7 публикаций, 1.01%
|
|
|
Signal Transduction and Targeted Therapy
7 публикаций, 1.01%
|
|
|
Cancer Discovery
6 публикаций, 0.87%
|
|
|
Biomedicines
6 публикаций, 0.87%
|
|
|
Nature Chemical Biology
6 публикаций, 0.87%
|
|
|
Bioorganic Chemistry
6 публикаций, 0.87%
|
|
|
Cancer Research
6 публикаций, 0.87%
|
|
|
Proceedings of the National Academy of Sciences of the United States of America
6 публикаций, 0.87%
|
|
|
Cancer Cell
6 публикаций, 0.87%
|
|
|
Cells
5 публикаций, 0.72%
|
|
|
Future Medicinal Chemistry
5 публикаций, 0.72%
|
|
|
Trends in Cancer
5 публикаций, 0.72%
|
|
|
Critical Reviews in Oncology/Hematology
5 публикаций, 0.72%
|
|
|
Cancer Letters
5 публикаций, 0.72%
|
|
|
Molecular Oncology
5 публикаций, 0.72%
|
|
|
Methods in Molecular Biology
5 публикаций, 0.72%
|
|
|
Computational and Structural Biotechnology Journal
5 публикаций, 0.72%
|
|
|
Nature Cancer
4 публикации, 0.58%
|
|
|
10
20
30
40
50
60
|
Издатели
|
20
40
60
80
100
120
140
160
|
|
|
Elsevier
153 публикации, 22.14%
|
|
|
Springer Nature
113 публикаций, 16.35%
|
|
|
American Chemical Society (ACS)
83 публикации, 12.01%
|
|
|
openRxiv
61 публикация, 8.83%
|
|
|
MDPI
58 публикаций, 8.39%
|
|
|
Wiley
50 публикаций, 7.24%
|
|
|
Taylor & Francis
23 публикации, 3.33%
|
|
|
Frontiers Media S.A.
23 публикации, 3.33%
|
|
|
American Association for Cancer Research (AACR)
21 публикация, 3.04%
|
|
|
Royal Society of Chemistry (RSC)
10 публикаций, 1.45%
|
|
|
American Association for the Advancement of Science (AAAS)
9 публикаций, 1.3%
|
|
|
Proceedings of the National Academy of Sciences (PNAS)
6 публикаций, 0.87%
|
|
|
SAGE
5 публикаций, 0.72%
|
|
|
De Gruyter Brill
5 публикаций, 0.72%
|
|
|
American Society of Clinical Oncology (ASCO)
5 публикаций, 0.72%
|
|
|
AME Publishing Company
5 публикаций, 0.72%
|
|
|
Ovid Technologies (Wolters Kluwer Health)
5 публикаций, 0.72%
|
|
|
Rockefeller University Press
4 публикации, 0.58%
|
|
|
Georg Thieme Verlag KG
4 публикации, 0.58%
|
|
|
Cold Spring Harbor Laboratory
4 публикации, 0.58%
|
|
|
American Society for Clinical Investigation
4 публикации, 0.58%
|
|
|
Baishideng Publishing Group
3 публикации, 0.43%
|
|
|
BMJ
3 публикации, 0.43%
|
|
|
Spandidos Publications
3 публикации, 0.43%
|
|
|
The Company of Biologists
2 публикации, 0.29%
|
|
|
F1000 Research
2 публикации, 0.29%
|
|
|
Massachusetts Medical Society
2 публикации, 0.29%
|
|
|
American Society for Biochemistry and Molecular Biology
2 публикации, 0.29%
|
|
|
Public Library of Science (PLoS)
2 публикации, 0.29%
|
|
|
20
40
60
80
100
120
140
160
|
- 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
694
Всего цитирований:
694
Цитирований c 2025:
330
(47.76%)
Цитировать
ГОСТ |
RIS |
BibTex |
MLA
Цитировать
ГОСТ
Скопировать
Wang X. et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor // Journal of Medicinal Chemistry. 2021. Vol. 65. No. 4. pp. 3123-3133.
ГОСТ со всеми авторами (до 50)
Скопировать
Wang X., Allen S., Blake J. F., Bowcut V., Briere D. M., Calinisan A., Dahlke J. R., Fell J. B., Fischer J. P., Gunn R. J., Hallin J., Laguer J., Lawson J. D., Medwid J., Newhouse B., Nguyen P., Oleary J. M., Olson P., Pajk S., Rahbaek L., Rodriguez M., Smith C. R., Tang T. P., Thomas N. C., Vanderpool D., Vigers G. P., Christensen J. G., Marx M. A. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor // Journal of Medicinal Chemistry. 2021. Vol. 65. No. 4. pp. 3123-3133.
Цитировать
RIS
Скопировать
TY - JOUR
DO - 10.1021/acs.jmedchem.1c01688
UR - https://doi.org/10.1021/acs.jmedchem.1c01688
TI - Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor
T2 - Journal of Medicinal Chemistry
AU - Wang, Xiaolun
AU - Allen, Shelley
AU - Blake, James F.
AU - Bowcut, Vickie
AU - Briere, David M
AU - Calinisan, Andrew
AU - Dahlke, Joshua R
AU - Fell, Jay B
AU - Fischer, John P.
AU - Gunn, Robin J
AU - Hallin, Jill
AU - Laguer, Jade
AU - Lawson, J. David
AU - Medwid, James
AU - Newhouse, Brad
AU - Nguyen, Phong
AU - Oleary, Jacob M
AU - Olson, Peter
AU - Pajk, Spencer
AU - Rahbaek, Lisa
AU - Rodriguez, Mareli
AU - Smith, Christopher R.
AU - Tang, Tony P
AU - Thomas, Nicole C
AU - Vanderpool, Darin
AU - Vigers, Guy P
AU - Christensen, James G.
AU - Marx, Matthew A
PY - 2021
DA - 2021/12/10
PB - American Chemical Society (ACS)
SP - 3123-3133
IS - 4
VL - 65
PMID - 34889605
SN - 0022-2623
SN - 1520-4804
ER -
Цитировать
BibTex (до 50 авторов)
Скопировать
@article{2021_Wang,
author = {Xiaolun Wang and Shelley Allen and James F. Blake and Vickie Bowcut and David M Briere and Andrew Calinisan and Joshua R Dahlke and Jay B Fell and John P. Fischer and Robin J Gunn and Jill Hallin and Jade Laguer and J. David Lawson and James Medwid and Brad Newhouse and Phong Nguyen and Jacob M Oleary and Peter Olson and Spencer Pajk and Lisa Rahbaek and Mareli Rodriguez and Christopher R. Smith and Tony P Tang and Nicole C Thomas and Darin Vanderpool and Guy P Vigers and James G. Christensen and Matthew A Marx},
title = {Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor},
journal = {Journal of Medicinal Chemistry},
year = {2021},
volume = {65},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/acs.jmedchem.1c01688},
number = {4},
pages = {3123--3133},
doi = {10.1021/acs.jmedchem.1c01688}
}
Цитировать
MLA
Скопировать
Wang, Xiaolun, et al. “Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor.” Journal of Medicinal Chemistry, vol. 65, no. 4, Dec. 2021, pp. 3123-3133. https://doi.org/10.1021/acs.jmedchem.1c01688.
Ошибка в публикации?