α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH)
Séverine Ravez
1
,
Cyril Corbet
2
,
Quentin Spillier
1, 2
,
Alice Dutu
1
,
Anita D Robin
3
,
Edouard Mullarky
3
,
L C Cantley
3
,
Barry O'Neil
2
,
Raphaël Frederick
1
Publication type: Journal Article
Publication date: 2017-01-27
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
28085281
Drug Discovery
Molecular Medicine
Abstract
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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Metrics
62
Total citations:
62
Citations from 2024:
18
(29.03%)
Cite this
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RIS |
BibTex |
MLA
Cite this
GOST
Copy
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.
GOST all authors (up to 50)
Copy
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.
Cite this
RIS
Copy
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 -
Cite this
BibTex (up to 50 authors)
Copy
@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}
}
Cite this
MLA
Copy
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.