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Items: 8

1.

Inhibition of IL-23 mediated inflammation with a novel small molecule inverse agonist of RORgt.

Gauld S, Jacquet S, Gauvin D, Wallace C, Wang Y, McCarthy R, Goess C, Leys L, Huang S, Su Z, Edelmayer R, Wetter J, Salte K, McGaraughty S, Argiriadi M, Honore P, Luccarini JM, Bressac D, Desino K, Breinlinger E, Cusack K, Potin D, Kort M, Masson P.

J Pharmacol Exp Ther. 2019 Aug 2. pii: jpet.119.258046. doi: 10.1124/jpet.119.258046. [Epub ahead of print]

2.

Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists.

Amaudrut J, Argiriadi MA, Barth M, Breinlinger EC, Bressac D, Broqua P, Calderwood DJ, Chatar M, Cusack KP, Gauld SB, Jacquet S, Kamath RV, Kort ME, Lepais V, Luccarini JM, Masson P, Montalbetti C, Mounier L, Potin D, Poupardin O, Rouaud S, Spitzer L, Wallace CD.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1799-1806. doi: 10.1016/j.bmcl.2019.05.015. Epub 2019 May 9.

PMID:
31101472
3.

Optimized protein kinase Cθ (PKCθ) inhibitors reveal only modest anti-inflammatory efficacy in a rodent model of arthritis.

George DM, Breinlinger EC, Argiriadi MA, Zhang Y, Wang J, Bansal-Pakala P, Duignan DB, Honore P, Lang Q, Mittelstadt S, Rundell L, Schwartz A, Sun J, Edmunds JJ.

J Med Chem. 2015 Jan 8;58(1):333-46. doi: 10.1021/jm5013006. Epub 2014 Oct 9.

PMID:
25254961
4.

Discovery of selective and orally bioavailable protein kinase Cθ (PKCθ) inhibitors from a fragment hit.

George DM, Breinlinger EC, Friedman M, Zhang Y, Wang J, Argiriadi M, Bansal-Pakala P, Barth M, Duignan DB, Honore P, Lang Q, Mittelstadt S, Potin D, Rundell L, Edmunds JJ.

J Med Chem. 2015 Jan 8;58(1):222-36. doi: 10.1021/jm500669m. Epub 2014 Jul 7.

PMID:
25000588
5.

Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase.

Cogan DA, Aungst R, Breinlinger EC, Fadra T, Goldberg DR, Hao MH, Kroe R, Moss N, Pargellis C, Qian KC, Swinamer AD.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3251-5. doi: 10.1016/j.bmcl.2008.04.043. Epub 2008 Apr 25.

PMID:
18462940
6.

Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3.

Hayes ME, Breinlinger EC, Wallace GA, Grongsaard P, Miao W, McPherson MJ, Stoffel RH, Green DW, Roth GP.

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2414-9. doi: 10.1016/j.bmcl.2008.02.049. Epub 2008 Feb 26.

PMID:
18337097
7.

Controlled multi-stage recognition of guests using orthogonal electro- and photochemical inputs.

Goodman A, Breinlinger E, Ober M, Rotello VM.

J Am Chem Soc. 2001 Jun 27;123(25):6213-4. No abstract available.

PMID:
11414870
8.

Model systems for flavoenzyme activity. Control of flavin recognition via specific electrostatic interactions.

Goodman AJ, Breinlinger EC, McIntosh CM, Grimaldi LN, Rotello VM.

Org Lett. 2001 May 17;3(10):1531-4.

PMID:
11388859

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