α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH)
Тип публикации: Journal Article
Дата публикации: 2017-01-27
scimago Q1
wos Q1
БС1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
28085281
Drug Discovery
Molecular Medicine
Краткое описание
Given the putative role of PHGDH in cancer, development of inhibitors is required to explore its function. In this context, we established and validated a straightforward enzymatic assay suitable for high-throughput screening and we identified inhibitors with similar chemical scaffolds. Through a convergent pharmacophore approach, we synthesized α-ketothioamides that exhibit interesting in vitro PHGDH inhibition and encouraging cellular results. These novel probes may be used to understand the emerging biology of this metabolic target.
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ГОСТ |
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MLA
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ГОСТ
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Ravez S. et al. α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH) // Journal of Medicinal Chemistry. 2017. Vol. 60. No. 4. pp. 1591-1597.
ГОСТ со всеми авторами (до 50)
Скопировать
Ravez S., Corbet C., Spillier Q., Dutu A., Robin A. D., Mullarky E., Cantley L. C., O'Neil B., Frederick R. α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH) // Journal of Medicinal Chemistry. 2017. Vol. 60. No. 4. pp. 1591-1597.
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RIS
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TY - JOUR
DO - 10.1021/acs.jmedchem.6b01166
UR - https://doi.org/10.1021/acs.jmedchem.6b01166
TI - α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH)
T2 - Journal of Medicinal Chemistry
AU - Ravez, Séverine
AU - Corbet, Cyril
AU - Spillier, Quentin
AU - Dutu, Alice
AU - Robin, Anita D
AU - Mullarky, Edouard
AU - Cantley, L C
AU - O'Neil, Barry
AU - Frederick, Raphaël
PY - 2017
DA - 2017/01/27
PB - American Chemical Society (ACS)
SP - 1591-1597
IS - 4
VL - 60
PMID - 28085281
SN - 0022-2623
SN - 1520-4804
ER -
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BibTex (до 50 авторов)
Скопировать
@article{2017_Ravez,
author = {Séverine Ravez and Cyril Corbet and Quentin Spillier and Alice Dutu and Anita D Robin and Edouard Mullarky and L C Cantley and Barry O'Neil and Raphaël Frederick},
title = {α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH)},
journal = {Journal of Medicinal Chemistry},
year = {2017},
volume = {60},
publisher = {American Chemical Society (ACS)},
month = {jan},
url = {https://doi.org/10.1021/acs.jmedchem.6b01166},
number = {4},
pages = {1591--1597},
doi = {10.1021/acs.jmedchem.6b01166}
}
Цитировать
MLA
Скопировать
Ravez, Séverine, et al. “α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).” Journal of Medicinal Chemistry, vol. 60, no. 4, Jan. 2017, pp. 1591-1597. https://doi.org/10.1021/acs.jmedchem.6b01166.