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Items: 25

1.

Identification of a pharmacological inhibitor of Epac1 that protects the heart against acute and chronic models of cardiac stress.

Laudette M, Coluccia A, Sainte-Marie Y, Solari A, Fazal L, Sicard P, Silvestri R, Mialet-Perez J, Pons S, Ghaleh B, Blondeau JP, Lezoualc'h F.

Cardiovasc Res. 2019 Oct 1;115(12):1766-1777. doi: 10.1093/cvr/cvz076.

PMID:
30873562
2.

Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.

Heightman TD, Berdini V, Braithwaite H, Buck IM, Cassidy M, Castro J, Courtin A, Day JEH, East C, Fazal L, Graham B, Griffiths-Jones CM, Lyons JF, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Reader M, Rees DC, Rich SJ, Richardson C, Saini H, Thompson NT, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW.

J Med Chem. 2018 Jun 14;61(11):4978-4992. doi: 10.1021/acs.jmedchem.8b00421. Epub 2018 May 31.

PMID:
29775310
3.

Beneficial effects of exercise training in heart failure are lost in male diabetic rats.

Boudia D, Domergue V, Mateo P, Fazal L, Prud'homme M, Prigent H, Delcayre C, Cohen-Solal A, Garnier A, Ventura-Clapier R, Samuel JL.

J Appl Physiol (1985). 2017 Dec 1;123(6):1579-1591. doi: 10.1152/japplphysiol.00117.2017. Epub 2017 Sep 7.

4.

Imbalanced Angiogenesis in Peripartum Cardiomyopathy - Diagnostic Value of Placenta Growth Factor.

Mebazaa A, Seronde MF, Gayat E, Tibazarwa K, Anumba DOC, Akrout N, Sadoune M, Sarb J, Arrigo M, Motiejunaite J, Laribi S, Legrand M, Deschamps L, Fazal L, Bouadma L, Collet C, Manivet P, Solal AC, Launay JM, Samuel JL, Sliwa K.

Circ J. 2017 Oct 25;81(11):1654-1661. doi: 10.1253/circj.CJ-16-1193. Epub 2017 May 27.

5.

Multifunctional Mitochondrial Epac1 Controls Myocardial Cell Death.

Fazal L, Laudette M, Paula-Gomes S, Pons S, Conte C, Tortosa F, Sicard P, Sainte-Marie Y, Bisserier M, Lairez O, Lucas A, Roy J, Ghaleh B, Fauconnier J, Mialet-Perez J, Lezoualc'h F.

Circ Res. 2017 Feb 17;120(4):645-657. doi: 10.1161/CIRCRESAHA.116.309859. Epub 2017 Jan 17.

PMID:
28096195
6.

Loss of Notch3 Signaling in Vascular Smooth Muscle Cells Promotes Severe Heart Failure Upon Hypertension.

Ragot H, Monfort A, Baudet M, Azibani F, Fazal L, Merval R, Polidano E, Cohen-Solal A, Delcayre C, Vodovar N, Chatziantoniou C, Samuel JL.

Hypertension. 2016 Aug;68(2):392-400. doi: 10.1161/HYPERTENSIONAHA.116.07694. Epub 2016 Jun 13.

PMID:
27296994
7.

Cyclic AMP Sensor EPAC Proteins and Their Role in Cardiovascular Function and Disease.

Lezoualc'h F, Fazal L, Laudette M, Conte C.

Circ Res. 2016 Mar 4;118(5):881-97. doi: 10.1161/CIRCRESAHA.115.306529. Review.

PMID:
26941424
8.

Inhibition of Galectin-3 Pathway Prevents Isoproterenol-Induced Left Ventricular Dysfunction and Fibrosis in Mice.

Vergaro G, Prud'homme M, Fazal L, Merval R, Passino C, Emdin M, Samuel JL, Cohen Solal A, Delcayre C.

Hypertension. 2016 Mar;67(3):606-12. doi: 10.1161/HYPERTENSIONAHA.115.06161. Epub 2016 Jan 18.

PMID:
26781273
9.

Tissue kallikrein is required for the cardioprotective effect of cyclosporin A in myocardial ischemia in the mouse.

Youcef G, Belaidi E, Waeckel L, Fazal L, Clemessy M, Vincent MP, Zadigue G, Richer C, Alhenc-Gelas F, Ovize M, Pizard A.

Biochem Pharmacol. 2015 Mar 1;94(1):22-9. doi: 10.1016/j.bcp.2015.01.007. Epub 2015 Jan 23.

PMID:
25623731
10.

Carabin protects against cardiac hypertrophy by blocking calcineurin, Ras, and Ca2+/calmodulin-dependent protein kinase II signaling.

Bisserier M, Berthouze-Duquesnes M, Breckler M, Tortosa F, Fazal L, de Régibus A, Laurent AC, Varin A, Lucas A, Branchereau M, Marck P, Schickel JN, Deloménie C, Cazorla O, Soulas-Sprauel P, Crozatier B, Morel E, Heymes C, Lezoualc'h F.

Circulation. 2015 Jan 27;131(4):390-400; discussion 400. doi: 10.1161/CIRCULATIONAHA.114.010686. Epub 2014 Nov 4.

PMID:
25369805
11.

Akt-mediated cardioprotective effects of aldosterone in type 2 diabetic mice.

Fazal L, Azibani F, Bihry N, Coutance G, Polidano E, Merval R, Vodovar N, Launay JM, Delcayre C, Samuel JL.

FASEB J. 2014 Jun;28(6):2430-40. doi: 10.1096/fj.13-239822. Epub 2014 Feb 20.

PMID:
24558200
12.

Effects of biological sex on the pathophysiology of the heart.

Fazal L, Azibani F, Vodovar N, Cohen Solal A, Delcayre C, Samuel JL.

Br J Pharmacol. 2014 Feb;171(3):555-66. doi: 10.1111/bph.12279. Review.

13.

Aldosterone mediates cardiac fibrosis in the setting of hypertension.

Azibani F, Fazal L, Chatziantoniou C, Samuel JL, Delcayre C.

Curr Hypertens Rep. 2013 Aug;15(4):395-400. doi: 10.1007/s11906-013-0354-3. Review.

PMID:
23686824
14.

[Hypertension-induced fibrosis: a balance story].

Azibani F, Fazal L, Chatziantoniou C, Samuel JL, Delcayre C.

Ann Cardiol Angeiol (Paris). 2012 Jun;61(3):150-5. doi: 10.1016/j.ancard.2012.05.004. Epub 2012 May 25. French.

PMID:
22681982
15.

Aldosterone inhibits the fetal program and increases hypertrophy in the heart of hypertensive mice.

Azibani F, Devaux Y, Coutance G, Schlossarek S, Polidano E, Fazal L, Merval R, Carrier L, Solal AC, Chatziantoniou C, Launay JM, Samuel JL, Delcayre C.

PLoS One. 2012;7(5):e38197. doi: 10.1371/journal.pone.0038197. Epub 2012 May 30.

16.

Aldosterone inhibits antifibrotic factors in mouse hypertensive heart.

Azibani F, Benard L, Schlossarek S, Merval R, Tournoux F, Fazal L, Polidano E, Launay JM, Carrier L, Chatziantoniou C, Samuel JL, Delcayre C.

Hypertension. 2012 Jun;59(6):1179-87. doi: 10.1161/HYPERTENSIONAHA.111.190512. Epub 2012 Apr 30.

PMID:
22547442
17.

The heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer.

Graham B, Curry J, Smyth T, Fazal L, Feltell R, Harada I, Coyle J, Williams B, Reule M, Angove H, Cross DM, Lyons J, Wallis NG, Thompson NT.

Cancer Sci. 2012 Mar;103(3):522-7. doi: 10.1111/j.1349-7006.2011.02191.x. Epub 2012 Feb 9.

18.

Dengue fever treatment with Carica papaya leaves extracts.

Ahmad N, Fazal H, Ayaz M, Abbasi BH, Mohammad I, Fazal L.

Asian Pac J Trop Biomed. 2011 Aug;1(4):330-3. doi: 10.1016/S2221-1691(11)60055-5.

19.

Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.

Squires M, Ward G, Saxty G, Berdini V, Cleasby A, King P, Angibaud P, Perera T, Fazal L, Ross D, Jones CG, Madin A, Benning RK, Vickerstaffe E, O'Brien A, Frederickson M, Reader M, Hamlett C, Batey MA, Rich S, Carr M, Miller D, Feltell R, Thiru A, Bethell S, Devine LA, Graham BL, Pike A, Cosme J, Lewis EJ, Freyne E, Lyons J, Irving J, Murray C, Newell DR, Thompson NT.

Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15.

20.

Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.

Woodhead AJ, Angove H, Carr MG, Chessari G, Congreve M, Coyle JE, Cosme J, Graham B, Day PJ, Downham R, Fazal L, Feltell R, Figueroa E, Frederickson M, Lewis J, McMenamin R, Murray CW, O'Brien MA, Parra L, Patel S, Phillips T, Rees DC, Rich S, Smith DM, Trewartha G, Vinkovic M, Williams B, Woolford AJ.

J Med Chem. 2010 Aug 26;53(16):5956-69. doi: 10.1021/jm100060b.

PMID:
20662534
21.

AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.

Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD.

Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27.

22.

Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).

McHardy T, Caldwell JJ, Cheung KM, Hunter LJ, Taylor K, Rowlands M, Ruddle R, Henley A, de Haven Brandon A, Valenti M, Davies TG, Fazal L, Seavers L, Raynaud FI, Eccles SA, Aherne GW, Garrett MD, Collins I.

J Med Chem. 2010 Mar 11;53(5):2239-49. doi: 10.1021/jm901788j.

23.

Aurora B kinase inhibition in mitosis: strategies for optimising the use of aurora kinase inhibitors such as AT9283.

Curry J, Angove H, Fazal L, Lyons J, Reule M, Thompson N, Wallis N.

Cell Cycle. 2009 Jun 15;8(12):1921-9. Epub 2009 Jun 15.

PMID:
19440047
24.

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.

Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL, Heathcote M, Maman S, Matthews JE, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Rees DC, Reule M, Tisi D, Williams G, Vinković M, Wyatt PG.

J Med Chem. 2009 Jan 22;52(2):379-88. doi: 10.1021/jm800984v.

PMID:
19143567
25.

N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.

Bamborough P, Angell RM, Bhamra I, Brown D, Bull J, Christopher JA, Cooper AW, Fazal LH, Giordano I, Hind L, Patel VK, Ranshaw LE, Sims MJ, Skone PA, Smith KJ, Vickerstaff E, Washington M.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8. Epub 2007 Apr 13.

PMID:
17600705

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