From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151
Olivier Mirguet
1
,
Yann Lamotte
2
,
Frédéric Donche
2
,
Jérôme Toum
2
,
Françoise Gellibert
2
,
Anne Bouillot
2
,
Romain Gosmini
2
,
Van Loc Nguyen
2
,
Delphine Delannée
2
,
Jonathan T Seal
2
,
Florence Blandel
2
,
Anne-Bénédicte Boullay
2
,
Eric Boursier
2
,
Sandrine Martin
2
,
Jean Marie Brusq
2
,
Gael Krysa
2
,
Alizon Riou
2
,
Rémi Tellier
2
,
Agnès Costaz
2
,
Pascal Huet
2
,
Yann Dudit
2
,
L Trottet
2
,
Jorge Kirilovsky
2
,
Edwige Nicodeme
2
1
Lipid Metabolism Discovery Performance Unit, GlaxoSmithKline, Les Ulis Cedex, France.
|
2
Lipid Metabolism Discovery Performance Unit, GlaxoSmithKline, 25 avenue du Québec, 91951 Les Ulis Cedex, France
|
Publication type: Journal Article
Publication date: 2012-04-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
22386529
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatic cell line HepG2.
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109
Total citations:
109
Citations from 2025:
3
(2.75%)
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GOST
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Mirguet O. et al. From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151 // Bioorganic and Medicinal Chemistry Letters. 2012. Vol. 22. No. 8. pp. 2963-2967.
GOST all authors (up to 50)
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Mirguet O., Lamotte Y., Donche F., Toum J., Gellibert F., Bouillot A., Gosmini R., Nguyen V. L., Delannée D., Seal J. T., Blandel F., Boullay A., Boursier E., Martin S., Brusq J. M., Krysa G., Riou A., Tellier R., Costaz A., Huet P., Dudit Y., Trottet L., Kirilovsky J., Nicodeme E. From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151 // Bioorganic and Medicinal Chemistry Letters. 2012. Vol. 22. No. 8. pp. 2963-2967.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.bmcl.2012.01.125
UR - https://doi.org/10.1016/j.bmcl.2012.01.125
TI - From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Mirguet, Olivier
AU - Lamotte, Yann
AU - Donche, Frédéric
AU - Toum, Jérôme
AU - Gellibert, Françoise
AU - Bouillot, Anne
AU - Gosmini, Romain
AU - Nguyen, Van Loc
AU - Delannée, Delphine
AU - Seal, Jonathan T
AU - Blandel, Florence
AU - Boullay, Anne-Bénédicte
AU - Boursier, Eric
AU - Martin, Sandrine
AU - Brusq, Jean Marie
AU - Krysa, Gael
AU - Riou, Alizon
AU - Tellier, Rémi
AU - Costaz, Agnès
AU - Huet, Pascal
AU - Dudit, Yann
AU - Trottet, L
AU - Kirilovsky, Jorge
AU - Nicodeme, Edwige
PY - 2012
DA - 2012/04/01
PB - Elsevier
SP - 2963-2967
IS - 8
VL - 22
PMID - 22386529
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (up to 50 authors)
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@article{2012_Mirguet,
author = {Olivier Mirguet and Yann Lamotte and Frédéric Donche and Jérôme Toum and Françoise Gellibert and Anne Bouillot and Romain Gosmini and Van Loc Nguyen and Delphine Delannée and Jonathan T Seal and Florence Blandel and Anne-Bénédicte Boullay and Eric Boursier and Sandrine Martin and Jean Marie Brusq and Gael Krysa and Alizon Riou and Rémi Tellier and Agnès Costaz and Pascal Huet and Yann Dudit and L Trottet and Jorge Kirilovsky and Edwige Nicodeme},
title = {From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2012},
volume = {22},
publisher = {Elsevier},
month = {apr},
url = {https://doi.org/10.1016/j.bmcl.2012.01.125},
number = {8},
pages = {2963--2967},
doi = {10.1016/j.bmcl.2012.01.125}
}
Cite this
MLA
Copy
Mirguet, Olivier, et al. “From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151.” Bioorganic and Medicinal Chemistry Letters, vol. 22, no. 8, Apr. 2012, pp. 2963-2967. https://doi.org/10.1016/j.bmcl.2012.01.125.