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Items: 20


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.


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.


Expression, purification, and characterization of multiple, multifunctional human glucocorticoid receptor proteins.

Simmons CA, Bledsoe RK, Guex N, Pearce KH.

Protein Expr Purif. 2008 Nov;62(1):29-35. doi: 10.1016/j.pep.2008.07.008. Epub 2008 Jul 30.


X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain.

Biggadike K, Bledsoe RK, Hassell AM, Kirk BE, McLay IM, Shewchuk LM, Stewart EL.

J Med Chem. 2008 Jun 26;51(12):3349-52. doi: 10.1021/jm800279t. Epub 2008 Jun 4.


Crystallization of protein-ligand complexes.

Hassell AM, An G, Bledsoe RK, Bynum JM, Carter HL 3rd, Deng SJ, Gampe RT, Grisard TE, Madauss KP, Nolte RT, Rocque WJ, Wang L, Weaver KL, Williams SP, Wisely GB, Xu R, Shewchuk LM.

Acta Crystallogr D Biol Crystallogr. 2007 Jan;63(Pt 1):72-9. Epub 2006 Dec 13. Review.


A ligand-mediated hydrogen bond network required for the activation of the mineralocorticoid receptor.

Bledsoe RK, Madauss KP, Holt JA, Apolito CJ, Lambert MH, Pearce KH, Stanley TB, Stewart EL, Trump RP, Willson TM, Williams SP.

J Biol Chem. 2005 Sep 2;280(35):31283-93. Epub 2005 Jun 20.


Structure and function of the glucocorticoid receptor ligand binding domain.

Bledsoe RK, Stewart EL, Pearce KH.

Vitam Horm. 2004;68:49-91. Review.


Structure-based design of potent retinoid X receptor alpha agonists.

Haffner CD, Lenhard JM, Miller AB, McDougald DL, Dwornik K, Ittoop OR, Gampe RT Jr, Xu HE, Blanchard S, Montana VG, Consler TG, Bledsoe RK, Ayscue A, Croom D.

J Med Chem. 2004 Apr 8;47(8):2010-29.


X-ray crystal structure of the liver X receptor beta ligand binding domain: regulation by a histidine-tryptophan switch.

Williams S, Bledsoe RK, Collins JL, Boggs S, Lambert MH, Miller AB, Moore J, McKee DD, Moore L, Nichols J, Parks D, Watson M, Wisely B, Willson TM.

J Biol Chem. 2003 Jul 18;278(29):27138-43. Epub 2003 May 7.


Crystal structure of the glucocorticoid receptor ligand binding domain reveals a novel mode of receptor dimerization and coactivator recognition.

Bledsoe RK, Montana VG, Stanley TB, Delves CJ, Apolito CJ, McKee DD, Consler TG, Parks DJ, Stewart EL, Willson TM, Lambert MH, Moore JT, Pearce KH, Xu HE.

Cell. 2002 Jul 12;110(1):93-105.


Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662.

Leesnitzer LM, Parks DJ, Bledsoe RK, Cobb JE, Collins JL, Consler TG, Davis RG, Hull-Ryde EA, Lenhard JM, Patel L, Plunket KD, Shenk JL, Stimmel JB, Therapontos C, Willson TM, Blanchard SG.

Biochemistry. 2002 May 28;41(21):6640-50.


Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha.

Spencer TA, Li D, Russel JS, Collins JL, Bledsoe RK, Consler TG, Moore LB, Galardi CM, McKee DD, Moore JT, Watson MA, Parks DJ, Lambert MH, Willson TM.

J Med Chem. 2001 Mar 15;44(6):886-97.


Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors.

Gampe RT Jr, Montana VG, Lambert MH, Miller AB, Bledsoe RK, Milburn MV, Kliewer SA, Willson TM, Xu HE.

Mol Cell. 2000 Mar;5(3):545-55.


Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands.

Moore LB, Parks DJ, Jones SA, Bledsoe RK, Consler TG, Stimmel JB, Goodwin B, Liddle C, Blanchard SG, Willson TM, Collins JL, Kliewer SA.

J Biol Chem. 2000 May 19;275(20):15122-7.


Production of monoclonal antibodies using recombinant baculovirus displaying gp64-fusion proteins.

Lindley KM, Su JL, Hodges PK, Wisely GB, Bledsoe RK, Condreay JP, Winegar DA, Hutchins JT, Kost TA.

J Immunol Methods. 2000 Feb 3;234(1-2):123-35.


Bile acids: natural ligands for an orphan nuclear receptor.

Parks DJ, Blanchard SG, Bledsoe RK, Chandra G, Consler TG, Kliewer SA, Stimmel JB, Willson TM, Zavacki AM, Moore DD, Lehmann JM.

Science. 1999 May 21;284(5418):1365-8.


Overexpression and characterization of the human mitochondrial and cytosolic branched-chain aminotransferases.

Davoodi J, Drown PM, Bledsoe RK, Wallin R, Reinhart GD, Hutson SM.

J Biol Chem. 1998 Feb 27;273(9):4982-9.


Cloning of the rat and human mitochondrial branched chain aminotransferases (BCATm).

Bledsoe RK, Dawson PA, Hutson SM.

Biochim Biophys Acta. 1997 Apr 25;1339(1):9-13.


Cloning and expression of the mammalian cytosolic branched chain aminotransferase isoenzyme.

Hutson SM, Bledsoe RK, Hall TR, Dawson PA.

J Biol Chem. 1995 Dec 22;270(51):30344-52.

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