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Items: 5


Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.

Labeeuw O, Levoin N, Billot X, Danvy D, Calmels T, Krief S, Ligneau X, Berrebi-Bertrand I, Robert P, Lecomte JM, Schwartz JC, Capet M.

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5263-5266. doi: 10.1016/j.bmcl.2016.09.049. Epub 2016 Sep 19.


Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.

Levoin N, Labeeuw O, Billot X, Calmels T, Danvy D, Krief S, Berrebi-Bertrand I, Lecomte JM, Schwartz JC, Capet M.

Eur J Med Chem. 2017 Jan 5;125:565-572. doi: 10.1016/j.ejmech.2016.09.074. Epub 2016 Sep 24.


The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors.

Watson M, Roulston A, Bélec L, Billot X, Marcellus R, Bédard D, Bernier C, Branchaud S, Chan H, Dairi K, Gilbert K, Goulet D, Gratton MO, Isakau H, Jang A, Khadir A, Koch E, Lavoie M, Lawless M, Nguyen M, Paquette D, Turcotte E, Berger A, Mitchell M, Shore GC, Beauparlant P.

Mol Cell Biol. 2009 Nov;29(21):5872-88. doi: 10.1128/MCB.00112-09. Epub 2009 Aug 24.


Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.

Nguyen M, Marcellus RC, Roulston A, Watson M, Serfass L, Murthy Madiraju SR, Goulet D, Viallet J, Bélec L, Billot X, Acoca S, Purisima E, Wiegmans A, Cluse L, Johnstone RW, Beauparlant P, Shore GC.

Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. Epub 2007 Nov 26.


Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.

Billot X, Chateauneuf A, Chauret N, Denis D, Greig G, Mathieu MC, Metters KM, Slipetz DM, Young RN.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1129-32.


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