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Items: 26


The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.

Liddle J, Beaufils B, Binnie M, Bouillot A, Denis AA, Hann MM, Haslam CP, Holmes DS, Hutchinson JP, Kranz M, McBride A, Mirguet O, Mole DJ, Mowat CG, Pal S, Rowland P, Trottet L, Uings IJ, Walker AL, Webster SP.

Bioorg Med Chem Lett. 2017 May 1;27(9):2023-2028. doi: 10.1016/j.bmcl.2017.02.078. Epub 2017 Mar 9.


Increased levels of 3-hydroxykynurenine parallel disease severity in human acute pancreatitis.

Skouras C, Zheng X, Binnie M, Homer NZ, Murray TB, Robertson D, Briody L, Paterson F, Spence H, Derr L, Hayes AJ, Tsoumanis A, Lyster D, Parks RW, Garden OJ, Iredale JP, Uings IJ, Liddle J, Wright WL, Dukes G, Webster SP, Mole DJ.

Sci Rep. 2016 Sep 27;6:33951. doi: 10.1038/srep33951.


Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.

Mirguet O, Gosmini R, Toum J, Clément CA, Barnathan M, Brusq JM, Mordaunt JE, Grimes RM, Crowe M, Pineau O, Ajakane M, Daugan A, Jeffrey P, Cutler L, Haynes AC, Smithers NN, Chung CW, Bamborough P, Uings IJ, Lewis A, Witherington J, Parr N, Prinjha RK, Nicodème E.

J Med Chem. 2013 Oct 10;56(19):7501-15. doi: 10.1021/jm401088k. Epub 2013 Sep 25.


Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile.

Uings IJ, Needham D, Matthews J, Haase M, Austin R, Angell D, Leavens K, Holt J, Biggadike K, Farrow SN.

Br J Pharmacol. 2013 Jul;169(6):1389-403. doi: 10.1111/bph.12232.


Discovery and characterization of small molecule inhibitors of the BET family bromodomains.

Chung CW, Coste H, White JH, Mirguet O, Wilde J, Gosmini RL, Delves C, Magny SM, Woodward R, Hughes SA, Boursier EV, Flynn H, Bouillot AM, Bamborough P, Brusq JM, Gellibert FJ, Jones EJ, Riou AM, Homes P, Martin SL, Uings IJ, Toum J, Clement CA, Boullay AB, Grimley RL, Blandel FM, Prinjha RK, Lee K, Kirilovsky J, Nicodeme E.

J Med Chem. 2011 Jun 9;54(11):3827-38. doi: 10.1021/jm200108t. Epub 2011 May 13.


Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.

Diallo H, Angell DC, Barnett HA, Biggadike K, Coe DM, Cooper TW, Craven A, Gray JR, House D, Jack TI, Keeling SP, Macdonald SJ, McLay IM, Oliver S, Taylor SJ, Uings IJ, Wellaway N.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1126-33. doi: 10.1016/j.bmcl.2010.12.121. Epub 2010 Dec 31.


Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.

Yates CM, Brown PJ, Stewart EL, Patten C, Austin RJ, Holt JA, Maglich JM, Angell DC, Sasse RZ, Taylor SJ, Uings IJ, Trump RP.

J Med Chem. 2010 Jun 10;53(11):4531-44. doi: 10.1021/jm100447c.


Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.

Biggadike K, Bledsoe RK, Coe DM, Cooper TW, House D, Iannone MA, Macdonald SJ, Madauss KP, McLay IM, Shipley TJ, Taylor SJ, Tran TB, Uings IJ, Weller V, Williams SP.

Proc Natl Acad Sci U S A. 2009 Oct 27;106(43):18114-9. doi: 10.1073/pnas.0909125106. Epub 2009 Oct 12.


Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.

Barnett HA, Coe DM, Cooper TW, Jack TI, Jones HT, Macdonald SJ, McLay IM, Rayner N, Sasse RZ, Shipley TJ, Skone PA, Somers GI, Taylor S, Uings IJ, Woolven JM, Weingarten GG.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):158-62. doi: 10.1016/j.bmcl.2008.10.128. Epub 2008 Nov 5.


The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.

Madauss KP, Bledsoe RK, Mclay I, Stewart EL, Uings IJ, Weingarten G, Williams SP.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6097-9. doi: 10.1016/j.bmcl.2008.10.021. Epub 2008 Oct 8.


Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease.

Salter M, Biggadike K, Matthews JL, West MR, Haase MV, Farrow SN, Uings IJ, Gray DW.

Am J Physiol Lung Cell Mol Physiol. 2007 Sep;293(3):L660-7. Epub 2007 Jun 15.


Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.

Madauss KP, Deng SJ, Austin RJ, Lambert MH, McLay I, Pritchard J, Short SA, Stewart EL, Uings IJ, Williams SP.

J Med Chem. 2004 Jun 17;47(13):3381-7.


Functional analysis of the interleukin-5 receptor antagonist peptide, AF18748.

Rosas M, Uings IJ, van Aalst C, Lammers JW, Koenderman L, Coffer PJ.

Cytokine. 2004 Jun 21;26(6):247-54.


Mometasone furoate is a less specific glucocorticoid than fluticasone propionate.

Austin RJ, Maschera B, Walker A, Fairbairn L, Meldrum E, Farrow SN, Uings IJ.

Eur Respir J. 2002 Dec;20(6):1386-92.


Glucocorticoid-induced osteopenia in the mouse as assessed by histomorphometry, microcomputed tomography, and biochemical markers.

McLaughlin F, Mackintosh J, Hayes BP, McLaren A, Uings IJ, Salmon P, Humphreys J, Meldrum E, Farrow SN.

Bone. 2002 Jun;30(6):924-30.


Inhibition of nuclear factor-kappaB activation un-masks the ability of TNF-alpha to induce human eosinophil apoptosis.

Fujihara S, Ward C, Dransfield I, Hay RT, Uings IJ, Hayes B, Farrow SN, Haslett C, Rossi AG.

Eur J Immunol. 2002 Feb;32(2):457-66.


Modified peptide antagonists of interleukin 5 exhibit extended in vivo persistence but restricted species specificity.

Uings IJ, Balasubramanian P, McLoughlin PG, Yin Q, Dash L, Beresford A, Kearney S, Barrett RW, McKinnon M, England BP.

Cytokine. 2001 Jul 7;15(1):10-9.


Cytokine-specific transcriptional regulation through an IL-5Ralpha interacting protein.

Geijsen N, Uings IJ, Pals C, Armstrong J, McKinnon M, Raaijmakers JA, Lammers JW, Koenderman L, Coffer PJ.

Science. 2001 Aug 10;293(5532):1136-8.


Cell receptors and cell signalling.

Uings IJ, Farrow SN.

Mol Pathol. 2000 Dec;53(6):295-9. Review.


Indolocarbazoles: potent and selective inhibitors of platelet-derived growth factor receptor autophosphorylation.

Spacey GD, Uings IJ, Slater M, Hirst S, Bonser RW.

Biochem Pharmacol. 1998 Feb 1;55(3):261-71.


An interleukin 5 mutant distinguishes between two functional responses in human eosinophils.

McKinnon M, Page K, Uings IJ, Banks M, Fattah D, Proudfoot AE, Graber P, Arod C, Fish R, Wells TN, Solari R.

J Exp Med. 1997 Jul 7;186(1):121-9.


Construction and expression of a functional chimeric receptor from PDGFr-beta and c-erbB-2.

Uings IJ, Spacey GD, Bonser RW.

Biochem Soc Trans. 1995 May;23(2):186S. No abstract available.


Tyrosine phosphorylation is involved in receptor coupling to phospholipase D but not phospholipase C in the human neutrophil.

Uings IJ, Thompson NT, Randall RW, Spacey GD, Bonser RW, Hudson AT, Garland LG.

Biochem J. 1992 Feb 1;281 ( Pt 3):597-600. Erratum in: Biochem J 1992 May 1;283(Pt 3):919.

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