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Items: 19


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.


Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.

Collins JL, Fivush AM, Watson MA, Galardi CM, Lewis MC, Moore LB, Parks DJ, Wilson JG, Tippin TK, Binz JG, Plunket KD, Morgan DG, Beaudet EJ, Whitney KD, Kliewer SA, Willson TM.

J Med Chem. 2002 May 9;45(10):1963-6.


Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha.

Xu HE, Stanley TB, Montana VG, Lambert MH, Shearer BG, Cobb JE, McKee DD, Galardi CM, Plunket KD, Nolte RT, Parks DJ, Moore JT, Kliewer SA, Willson TM, Stimmel JB.

Nature. 2002 Feb 14;415(6873):813-7.


Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.

Liu KG, Lambert MH, Ayscue AH, Henke BR, Leesnitzer LM, Oliver WR Jr, Plunket KD, Xu HE, Sternbach DD, Willson TM.

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3111-3.


Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.

Xu HE, Lambert MH, Montana VG, Plunket KD, Moore LB, Collins JL, Oplinger JA, Kliewer SA, Gampe RT Jr, McKee DD, Moore JT, Willson TM.

Proc Natl Acad Sci U S A. 2001 Nov 20;98(24):13919-24. Epub 2001 Nov 6.


A unique PPARgamma ligand with potent insulin-sensitizing yet weak adipogenic activity.

Rocchi S, Picard F, Vamecq J, Gelman L, Potier N, Zeyer D, Dubuquoy L, Bac P, Champy MF, Plunket KD, Leesnitzer LM, Blanchard SG, Desreumaux P, Moras D, Renaud JP, Auwerx J.

Mol Cell. 2001 Oct;8(4):737-47.


Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis.

Liu KG, Lambert MH, Leesnitzer LM, Oliver W Jr, Ott RJ, Plunket KD, Stuart LW, Brown PJ, Willson TM, Sternbach DD.

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2959-62.


Effects of fenofibrate on lipid parameters in obese rhesus monkeys.

Winegar DA, Brown PJ, Wilkison WO, Lewis MC, Ott RJ, Tong WQ, Brown HR, Lehmann JM, Kliewer SA, Plunket KD, Way JM, Bodkin NL, Hansen BC.

J Lipid Res. 2001 Oct;42(10):1543-51.


Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta.

Liu KG, Smith JS, Ayscue AH, Henke BR, Lambert MH, Leesnitzer LM, Plunket KD, Willson TM, Sternbach DD.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2385-8.


A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport.

Oliver WR Jr, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM.

Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5306-11. Epub 2001 Apr 17.


A synthetic triterpenoid, 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO), is a ligand for the peroxisome proliferator-activated receptor gamma.

Wang Y, Porter WW, Suh N, Honda T, Gribble GW, Leesnitzer LM, Plunket KD, Mangelsdorf DJ, Blanchard SG, Willson TM, Sporn MB.

Mol Endocrinol. 2000 Oct;14(10):1550-6.


Identification of a chemical tool for the orphan nuclear receptor FXR.

Maloney PR, Parks DJ, Haffner CD, Fivush AM, Chandra G, Plunket KD, Creech KL, Moore LB, Wilson JG, Lewis MC, Jones SA, Willson TM.

J Med Chem. 2000 Aug 10;43(16):2971-4. No abstract available.


Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.

Henke BR, Adkison KK, Blanchard SG, Leesnitzer LM, Mook RA Jr, Plunket KD, Ray JA, Roberson C, Unwalla R, Willson TM.

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3329-34.


A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.

Brown PJ, Winegar DA, Plunket KD, Moore LB, Lewis MC, Wilson JG, Sundseth SS, Koble CS, Wu Z, Chapman JM, Lehmann JM, Kliewer SA, Willson TM.

J Med Chem. 1999 Sep 23;42(19):3785-8. No abstract available.


A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat.

Brown KK, Henke BR, Blanchard SG, Cobb JE, Mook R, Kaldor I, Kliewer SA, Lehmann JM, Lenhard JM, Harrington WW, Novak PJ, Faison W, Binz JG, Hashim MA, Oliver WO, Brown HR, Parks DJ, Plunket KD, Tong WQ, Menius JA, Adkison K, Noble SA, Willson TM.

Diabetes. 1999 Jul;48(7):1415-24.


A peroxisome proliferator-activated receptor gamma ligand inhibits adipocyte differentiation.

Oberfield JL, Collins JL, Holmes CP, Goreham DM, Cooper JP, Cobb JE, Lenhard JM, Hull-Ryde EA, Mohr CP, Blanchard SG, Parks DJ, Moore LB, Lehmann JM, Plunket K, Miller AB, Milburn MV, Kliewer SA, Willson TM.

Proc Natl Acad Sci U S A. 1999 May 25;96(11):6102-6.


N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.

Cobb JE, Blanchard SG, Boswell EG, Brown KK, Charifson PS, Cooper JP, Collins JL, Dezube M, Henke BR, Hull-Ryde EA, Lake DH, Lenhard JM, Oliver W Jr, Oplinger J, Pentti M, Parks DJ, Plunket KD, Tong WQ.

J Med Chem. 1998 Dec 3;41(25):5055-69.


N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.

Henke BR, Blanchard SG, Brackeen MF, Brown KK, Cobb JE, Collins JL, Harrington WW Jr, Hashim MA, Hull-Ryde EA, Kaldor I, Kliewer SA, Lake DH, Leesnitzer LM, Lehmann JM, Lenhard JM, Orband-Miller LA, Miller JF, Mook RA Jr, Noble SA, Oliver W Jr, Parks DJ, Plunket KD, Szewczyk JR, Willson TM.

J Med Chem. 1998 Dec 3;41(25):5020-36.


Effects of troglitazone and metformin on glucose and lipid metabolism: alterations of two distinct molecular pathways.

Lenhard JM, Kliewer SA, Paulik MA, Plunket KD, Lehmann JM, Weiel JE.

Biochem Pharmacol. 1997 Oct 1;54(7):801-8.


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