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Papers authored by Willson TM

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Open access chemical and clinical probes to support drug discovery.

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Edwards AM, Bountra C, Kerr DJ, and Willson TM

Nature chemical biology 5(7):436-40, 2009 Jul - Who cited this? | PubMed ID: 19536100 | Fulltext

Differential presentation of protein interaction surfaces on the androgen receptor defines the pharmacological actions of bound ligands.

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Norris JD, Joseph JD, Sherk AB, Juzumiene D, Turnbull PS, Rafferty SW, Cui H, Anderson E, Fan D, Dye DA, Deng X, Kazmin D, Chang CY, Willson TM, and McDonnell DP

Chemistry & biology 16(4):452-60, 2009 Apr 24 - Who cited this? | PubMed ID: 19389631 | Fulltext

Chemical approaches to nuclear receptors in metabolism.

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Margolis RN, Moore DD, Willson TM, and Guy RK

Science signaling 2(82):mr5, 2009 - Who cited this? | PubMed ID: 19654413 | Fulltext

The P300 acetylase is critical for ligand-activated farnesoid X receptor (FXR) induction of SHP.

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Fang S, Tsang S, Jones R, Ponugoti B, Yoon H, Wu SY, Chiang CM, Willson TM, and Kemper JK

The Journal of biological chemistry, 2008 Oct 8 - Who cited this? | PubMed ID: 18842595 | Fulltext

Selective Partial Agonism of Liver X Receptor {alpha} Is Related to Differential Corepressor Recruitment.

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Phelan CA, Weaver JM, Steger DJ, Joshi S, Maslany JT, Collins JL, Zuercher WJ, Willson TM, Walker M, Jaye M, and Lazar MA

Molecular endocrinology (Baltimore, Md.) 22(10):2241-9, 2008 Oct - Who cited this? | PubMed ID: 18669643 | Fulltext

Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.

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Chao EY, Caravella JA, Watson MA, Campobasso N, Ghisletti S, Billin AN, Galardi C, Wang P, Laffitte BA, Iannone MA, Goodwin BJ, Nichols JA, Parks DJ, Stewart E, Wiethe RW, Williams SP,

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Journal of medicinal chemistry 51(18):5758, 2008 Sep 25 - Who cited this? | PubMed ID: 18800767 | Fulltext

Liver X receptor agonists increase airway reactivity in a model of asthma via increasing airway smooth muscle growth.

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Birrell MA, De Alba J, Catley MC, Hardaker E, Wong S, Collins M, Clarke DL, Farrow SN, Willson TM, Collins JL, and Belvisi MG

Journal of immunology (Baltimore, Md. : 1950) 181(6):4265, 2008 Sep 15 - Who cited this? | PubMed ID: 18768884 | Fulltext

Discovery of a novel class of PPARdelta partial agonists.

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Shearer BG, Patel HS, Billin AN, Way JM, Winegar DA, Lambert MH, Xu RX, Leesnitzer LM, Merrihew RV, Huet S, and Willson TM

Bioorganic & medicinal chemistry letters 18(18):5018-22, 2008 Sep 15 - Who cited this? | PubMed ID: 18722772 | Fulltext

ApoE promotes the proteolytic degradation of Abeta.

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Jiang Q, Lee CY, Mandrekar S, Wilkinson B, Cramer P, Zelcer N, Mann K, Lamb B, Willson TM, Collins JL, Richardson JC, Smith JD, Comery TA, Riddell D, Holtzman DM, Tontonoz P,

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Neuron 58(5):681, 2008 Jun 12 - Who cited this? | PubMed ID: 18549781 | Fulltext

The phytoestrogen coumestrol is a naturally occurring antagonist of the human pregnane X receptor.

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Wang H, Li H, Moore LB, Johnson MD, Maglich JM, Goodwin B, Ittoop OR, Wisely B, Creech K, Parks DJ, Collins JL, Willson TM, Kalpana GV, Venkatesh M, Xie W, Cho SY,

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Molecular endocrinology (Baltimore, Md.) 22(4):838, 2008 Apr - Who cited this? | PubMed ID: 18096694 | Fulltext

Identification and Characterization of a Selective Peroxisome Proliferator-Activated Receptor {beta}/{delta} (NR1C2) Antagonist.

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Shearer BG, Steger DJ, Way JM, Stanley TB, Lobe DC, Grillot DA, Iannone MA, Lazar MA, Willson TM, and Billin AN

Molecular endocrinology (Baltimore, Md.) 22(2):523-9, 2008 Feb - Who cited this? | PubMed ID: 17975020 | Fulltext

Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) ligands inhibit growth of UACC903 and MCF7 human cancer cell lines.

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Girroir EE, Hollingshead HE, Billin AN, Willson TM, Robertson GP, Sharma AK, Amin S, Gonzalez FJ, and Peters JM

Toxicology 243(1-2):236-43, 2008 Jan 14 - Who cited this? | PubMed ID: 18054822 | Fulltext

Ligand activation of peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) and inhibition of cyclooxygenase 2 (COX2) attenuate colon carcinogenesis through independent signaling mechanisms.

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Hollingshead HE, Borland MG, Billin AN, Willson TM, Gonzalez FJ, and Peters JM

Carcinogenesis 29(1):169-76, 2008 Jan - Who cited this? | PubMed ID: 17893232 | Fulltext

On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.

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Hyatt SM, Lockamy EL, Stein RA, McDonnell DP, Miller AB, Orband-Miller LA, Willson TM, and Zuercher WJ

Journal of medicinal chemistry 50(26):6722, 2007 Dec 27 - Who cited this? | PubMed ID: 18052088 | Fulltext

Peroxisome proliferator-activated receptor- /{delta} (PPAR /{delta}) ligands do not potentiate growth of human cancer cell lines.

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Hollingshead HE, Killins RL, Borland MG, Girroir EE, Billin AN, Willson TM, Sharma AK, Amin S, Gonzalez FJ, and Peters JM

Carcinogenesis 28(12):2641-9, 2007 Dec - Who cited this? | PubMed ID: 17693664 | Fulltext

Novel role for the liver X nuclear receptor in the suppression of lung inflammatory responses.

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Birrell MA, Catley MC, Hardaker E, Wong S, Willson TM, McCluskie K, Leonard T, Farrow SN, Collins JL, Haj-Yahia S, and Belvisi MG

The Journal of biological chemistry 282(44):31882, 2007 Nov 2 - Who cited this? | PubMed ID: 17766241 | Fulltext

PPARbeta/delta protects against experimental colitis through a ligand-independent mechanism.

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Hollingshead HE, Morimura K, Adachi M, Kennett MJ, Billin AN, Willson TM, Gonzalez FJ, and Peters JM

Digestive diseases and sciences 52(11):2912-9, 2007 Nov - Who cited this? | PubMed ID: 17404849 | Fulltext

Co-crystal structure guided array synthesis of PPARgamma inverse agonists.

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Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, and Hoekstra WJ

Bioorganic & medicinal chemistry letters 17(14):3916-20, 2007 Jul 15 - Who cited this? | PubMed ID: 17533125 | Fulltext

Ligand activation of peroxisome proliferator-activated receptor-beta/delta(PPARbeta/delta) inhibits cell growth of human N/TERT-1 keratinocytes.

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Burdick AD, Bility MT, Girroir EE, Billin AN, Willson TM, Gonzalez FJ, and Peters JM

Cellular signalling 19(6):1163-71, 2007 Jun - Who cited this? | PubMed ID: 17254750 | Fulltext

Sweet dreams for LXR.

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Lazar MA and Willson TM

Cell metabolism 5(3):159, 2007 Mar - Who cited this? | PubMed ID: 17339022 | Fulltext

Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.

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Xue Y, Chao E, Zuercher WJ, Willson TM, Collins JL, and Redinbo MR

Bioorganic & medicinal chemistry 15(5):2156-66, 2007 Mar 1 - Who cited this? | PubMed ID: 17215127 | Fulltext

Triglyceride:high-density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator activated receptor delta agonist.

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Sprecher DL, Massien C, Pearce G, Billin AN, Perlstein I, Willson TM, Hassall DG, Ancellin N, Patterson SD, Lobe DC, and Johnson TG

Arteriosclerosis, thrombosis, and vascular biology 27(2):359-65, 2007 Feb - Who cited this? | PubMed ID: 17110604 | Fulltext

Parallel SUMOylation-dependent pathways mediate gene- and signal-specific transrepression by LXRs and PPARgamma.

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Ghisletti S, Huang W, Ogawa S, Pascual G, Lin ME, Willson TM, Rosenfeld MG, and Glass CK

Molecular cell 25(1):57, 2007 Jan 12 - Who cited this? | PubMed ID: 17218271 | Fulltext

Peroxisome proliferator-activated receptor-delta, a regulator of oxidative capacity, fuel switching and cholesterol transport.

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Fürnsinn C, Willson TM, and Brunmair B

Diabetologia 50(1):8-17, 2007 Jan - Who cited this? | PubMed ID: 17119917 | Fulltext

Design and synthesis of an array of selective androgen receptor modulators.

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Trump RP, Blanc JB, Stewart EL, Brown PJ, Caivano M, Gray DW, Hoekstra WJ, Willson TM, Han B, and Turnbull P

Journal of combinatorial chemistry 9(1):107-14, 2007 - Who cited this? | PubMed ID: 17206838 | Fulltext

X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation.

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Wang L, Zuercher WJ, Consler TG, Lambert MH, Miller AB, Orband-Miller LA, McKee DD, Willson TM, and Nolte RT

The Journal of biological chemistry 281(49):37773, 2006 Dec 8 - Who cited this? | PubMed ID: 16990259 | Fulltext

Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.

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Whitby RJ, Dixon S, Maloney PR, Delerive P, Goodwin BJ, Parks DJ, and Willson TM

Journal of medicinal chemistry 49(23):6652-5, 2006 Nov 16 - Who cited this? | PubMed ID: 17154495 | Fulltext

Ligand activation of peroxisome proliferator-activated receptor beta inhibits colon carcinogenesis.

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Marin HE, Peraza MA, Billin AN, Willson TM, Ward JM, Kennett MJ, Gonzalez FJ, and Peters JM

Cancer research 66(8):4394, 2006 Apr 15 - Who cited this? | PubMed ID: 16618765 | Fulltext

Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.

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Chao EY, Collins JL, Gaillard S, Miller AB, Wang L, Orband-Miller LA, Nolte RT, McDonnell DP, Willson TM, and Zuercher WJ

Bioorganic & medicinal chemistry letters 16(4):821, 2006 Feb 15 - Who cited this? | PubMed ID: 16307879 | Fulltext

Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice.

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Zhang Y, Lee FY, Barrera G, Lee H, Vales C, Gonzalez FJ, Willson TM, and Edwards PA

Proceedings of the National Academy of Sciences of the United States of America 103(4):1006-11, 2006 Jan 24 - Who cited this? | PubMed ID: 16410358 | Fulltext

PPARbeta/delta selectively induces differentiation and inhibits cell proliferation.

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Kim DJ, Bility MT, Billin AN, Willson TM, Gonzalez FJ, and Peters JM

Cell death and differentiation 13(1):53, 2006 Jan - Who cited this? | PubMed ID: 16021179 | Fulltext

Protective effects of a peroxisome proliferator-activated receptor-beta/delta agonist in experimental autoimmune encephalomyelitis.

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Polak PE, Kalinin S, Dello Russo C, Gavrilyuk V, Sharp A, Peters JM, Richardson J, Willson TM, Weinberg G, and Feinstein DL

Journal of neuroimmunology 168(1-2):65-75, 2005 Nov - Who cited this? | PubMed ID: 16098614 | Fulltext

A SUMOylation-dependent pathway mediates transrepression of inflammatory response genes by PPAR-gamma.

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Pascual G, Fong AL, Ogawa S, Gamliel A, Li AC, Perissi V, Rose DW, Willson TM, Rosenfeld MG, and Glass CK

Nature 437(7059):759, 2005 Sep 29 - Who cited this? | PubMed ID: 16127449 | Fulltext

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

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

The Journal of biological chemistry 280(35):31283-93, 2005 Sep 2 - Who cited this? | PubMed ID: 15967794 | Fulltext

Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.

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Jaye MC, Krawiec JA, Campobasso N, Smallwood A, Qiu C, Lu Q, Kerrigan JJ, De Los Frailes Alvaro M, Laffitte B, Liu WS, Marino JP, Meyer CR, Nichols JA, Parks DJ, Perez P, Sarov-Blat L,

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Journal of medicinal chemistry 48(17):5419-22, 2005 Aug 25 - Who cited this? | PubMed ID: 16107141 | Fulltext

Structural basis for an unexpected mode of SERM-mediated ER antagonism.

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Wu YL, Yang X, Ren Z, McDonnell DP, Norris JD, Willson TM, and Greene GL

Molecular cell 18(4):413, 2005 May 13 - Who cited this? | PubMed ID: 15893725 | Fulltext

Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.

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Zuercher WJ, Gaillard S, Orband-Miller LA, Chao EY, Shearer BG, Jones DG, Miller AB, Collins JL, McDonnell DP, and Willson TM

Journal of medicinal chemistry 48(9):3107, 2005 May 5 - Who cited this? | PubMed ID: 15857113 | Fulltext

Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis.

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Fiorucci S, Clerici C, Antonelli E, Orlandi S, Goodwin B, Sadeghpour BM, Sabatino G, Russo G, Castellani D, Willson TM, Pruzanski M, Pellicciari R, and Morelli A

The Journal of pharmacology and experimental therapeutics 313(2):604-12, 2005 May - Who cited this? | PubMed ID: 15644430 | Fulltext

Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.

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Hoekstra WJ, Patel HS, Liang X, Blanc JB, Heyer DO, Willson TM, Iannone MA, Kadwell SH, Miller LA, Pearce KH, Simmons CA, and Shearin J

Journal of medicinal chemistry 48(6):2243-7, 2005 Mar 24 - Who cited this? | PubMed ID: 15771467 | Fulltext

Structural analyses reveal phosphatidyl inositols as ligands for the NR5 orphan receptors SF-1 and LRH-1.

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Krylova IN, Sablin EP, Moore J, Xu RX, Waitt GM, MacKay JA, Juzumiene D, Bynum JM, Madauss K, Montana V, Lebedeva L, Suzawa M, Williams JD, Williams SP, Guy RK, Thornton JW,

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Cell 120(3):343, 2005 Feb 11 - Who cited this? | PubMed ID: 15707893 | Fulltext

Isoxazolyl-serine-based agonists of peroxisome proliferator-activated receptor: design, synthesis, and effects on cardiomyocyte differentiation.

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Wei ZL, Petukhov PA, Bizik F, Teixeira JC, Mercola M, Volpe EA, Glazer RI, Willson TM, and Kozikowski AP

Journal of the American Chemical Society 126(51):16714-5, 2004 Dec 29 - Who cited this? | PubMed ID: 15612696 | Fulltext

A structural basis for constitutive activity in the human CAR/RXRalpha heterodimer.

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Xu RX, Lambert MH, Wisely BB, Warren EN, Weinert EE, Waitt GM, Williams JD, Collins JL, Moore LB, Willson TM, and Moore JT

Molecular cell 16(6):919-28, 2004 Dec 22 - Who cited this? | PubMed ID: 15610735 | Fulltext

Differential inhibition of macrophage foam-cell formation and atherosclerosis in mice by PPARalpha, beta/delta, and gamma.

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Li AC, Binder CJ, Gutierrez A, Brown KK, Plotkin CR, Pattison JW, Valledor AF, Davis RA, Willson TM, Witztum JL, Palinski W, and Glass CK

The Journal of clinical investigation 114(11):1564-76, 2004 Dec - Who cited this? | PubMed ID: 15578089 | Fulltext

Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.

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Pellicciari R, Costantino G, Camaioni E, Sadeghpour BM, Entrena A, Willson TM, Fiorucci S, Clerici C, and Gioiello A

Journal of medicinal chemistry 47(18):4559-69, 2004 Aug 26 - Who cited this? | PubMed ID: 15317466 | Fulltext

Selection, application, and validation of a set of molecular descriptors for nuclear receptor ligands.

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Stewart EL, Brown PJ, Bentley JA, and Willson TM

Combinatorial chemistry & high throughput screening 7(5):407-12, 2004 Aug - Who cited this? | PubMed ID: 15320707 | Fulltext

The effect of LXR activators on AP-1 proteins in keratinocytes.

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Schmuth M, Elias PM, Hanley K, Lau P, Moser A, Willson TM, Bikle DD, and Feingold KR

The Journal of investigative dermatology 123(1):41-8, 2004 Jul - Who cited this? | PubMed ID: 15191540 | Fulltext

Polyunsaturated fatty acids including docosahexaenoic and arachidonic acid bind to the retinoid X receptor alpha ligand-binding domain.

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Lengqvist J, Mata De Urquiza A, Bergman AC, Willson TM, Sjövall J, Perlmann T, and Griffiths WJ

Molecular & cellular proteomics : MCP 3(7):692-703, 2004 Jul - Who cited this? | PubMed ID: 15073272 | Fulltext

The nuclear receptor CAR is a regulator of thyroid hormone metabolism during caloric restriction.

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Maglich JM, Watson J, McMillen PJ, Goodwin B, Willson TM, and Moore JT

The Journal of biological chemistry 279(19):19832-8, 2004 May 7 - Who cited this? | PubMed ID: 15004031 | Fulltext

Peroxisome proliferator-activated receptor (PPAR)-beta/delta stimulates differentiation and lipid accumulation in keratinocytes.

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Schmuth M, Haqq CM, Cairns WJ, Holder JC, Dorsam S, Chang S, Lau P, Fowler AJ, Chuang G, Moser AH, Brown BE, Mao-Qiang M, Uchida Y, Schoonjans K, Auwerx J, Chambon P,

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The Journal of investigative dermatology 122(4):971, 2004 Apr - Who cited this? | PubMed ID: 15102088 | Fulltext

Tyrosine agonists reverse the molecular defects associated with dominant-negative mutations in human peroxisome proliferator-activated receptor gamma.

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Agostini M, Gurnell M, Savage DB, Wood EM, Smith AG, Rajanayagam O, Garnes KT, Levinson SH, Xu HE, Schwabe JW, Willson TM, O'Rahilly S, and Chatterjee VK

Endocrinology 145(4):1527, 2004 Apr - Who cited this? | PubMed ID: 14657011 | Fulltext

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