Timothy Willson

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Norris John David; Joseph James David; Sherk Andrea Barreto; Juzumiene Dalia; Turnbull Philip Stewart; Rafferty Stephen William; Cui Huaxia; Anderson Erin; Fan Daju; Dye Delita Arnelle; Deng Xiang; Kazmin Dmitri; Chang Ching-Yi; Willson Timothy Mark; McDonnell Donald Patrick
Differential presentation of protein interaction surfaces on the androgen receptor defines the pharmacological actions of bound ligands.
Chao Esther Y; Caravella Justin A; Watson Mike A; Campobasso Nino; Ghisletti Serena; Billin Andrew N; Galardi Cristin; Wang Ping; Laffitte Bryan A; Iannone Marie A; Goodwin Bryan J; Nichols Jason A; Parks Derek J; Stewart Eugene; Wiethe Robert W; Williams Shawn P; Smallwood Angela; Pearce Kenneth H; Glass Christopher K; Willson Timothy M; Zuercher William J; Collins Jon L
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
Shearer Barry G; Patel Hari S; Billin Andrew N; Way James M; Winegar Deborah A; Lambert Millard H; Xu Robert X; Leesnitzer Lisa M; Merrihew Raymond V; Huet Stephane; Willson Timothy M
Discovery of a novel class of PPARdelta partial agonists.

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2009: Norris John David; Joseph James David; Sherk Andrea Barreto; Juzumiene Dalia; Turnbull Philip Stewart; Rafferty Stephen William; Cui Huaxia; Anderson Erin; Fan Daju; Dye Delita Arnelle; Deng Xiang; Kazmin Dmitri; Chang Ching-Yi; Willson Timothy Mark; McDonnell Donald Patrick
Differential presentation of protein interaction surfaces on the androgen receptor defines the pharmacological actions of bound ligands.
Chemistry & biology 2009;16(4):452-60.
2008: Chao Esther Y; Caravella Justin A; Watson Mike A; Campobasso Nino; Ghisletti Serena; Billin Andrew N; Galardi Cristin; Wang Ping; Laffitte Bryan A; Iannone Marie A; Goodwin Bryan J; Nichols Jason A; Parks Derek J; Stewart Eugene; Wiethe Robert W; Williams Shawn P; Smallwood Angela; Pearce Kenneth H; Glass Christopher K; Willson Timothy M; Zuercher William J; Collins Jon L
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
Journal of medicinal chemistry 2008;51(18):5758-65.
2008: Shearer Barry G; Patel Hari S; Billin Andrew N; Way James M; Winegar Deborah A; Lambert Millard H; Xu Robert X; Leesnitzer Lisa M; Merrihew Raymond V; Huet Stephane; Willson Timothy M
Discovery of a novel class of PPARdelta partial agonists.
Bioorganic & medicinal chemistry letters 2008;18(18):5018-22.
2008: Wang Hongwei; Li Hao; Moore Linda B; Johnson Michael D L; Maglich Jodi M; Goodwin Bryan; Ittoop Olivia R R; Wisely Bruce; Creech Katrina; Parks Derek J; Collins Jon L; Willson Timothy M; Kalpana Ganjam V; Venkatesh Madhukumar; Xie Wen; Cho Sool Y; Roboz John; Redinbo Matthew; Moore John T; Mani Sridhar
The phytoestrogen coumestrol is a naturally occurring antagonist of the human pregnane X receptor.
Molecular endocrinology (Baltimore, Md.) 2008;22(4):838-57.
2008: Shearer Barry G; Steger David J; Way James M; Stanley Thomas B; Lobe David C; Grillot Didier A; Iannone Marie A; Lazar Mitchell A; Willson Timothy M; Billin Andrew N
Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist.
Molecular endocrinology (Baltimore, Md.) 2008;22(2):523-9.
2008: Girroir Elizabeth E; Hollingshead Holly E; Billin Andrew N; Willson Timothy M; Robertson Gavin P; Sharma Arun K; Amin Shantu; Gonzalez Frank J; Peters Jeffrey M
Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) ligands inhibit growth of UACC903 and MCF7 human cancer cell lines.
Toxicology 2008;243(1-2):236-43.
2008: Hollingshead Holly E; Borland Michael G; Billin Andrew N; Willson Timothy M; Gonzalez Frank J; Peters Jeffrey M
Ligand activation of peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) and inhibition of cyclooxygenase 2 (COX2) attenuate colon carcinogenesis through independent signaling mechanisms.
Carcinogenesis 2008;29(1):169-76.
2007: Hyatt Stephen M; Lockamy Elizabeth L; Stein Rebecca A; McDonnell Donald P; Miller Aaron B; Orband-Miller Lisa A; Willson Timothy M; Zuercher William J
On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.
Journal of medicinal chemistry 2007;50(26):6722-4.
2007: Hollingshead Holly E; Killins Renee L; Borland Michael G; Girroir Elizabeth E; Billin Andrew N; Willson Timothy M; Sharma Arun K; Amin Shantu; Gonzalez Frank J; Peters Jeffrey M
Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) ligands do not potentiate growth of human cancer cell lines.
Carcinogenesis 2007;28(12):2641-9.
2007: Hollingshead Holly E; Morimura Keiichirou; Adachi Masahiro; Kennett Mary J; Billin Andrew N; Willson Timothy M; Gonzalez Frank J; Peters Jeffrey M
PPARbeta/delta protects against experimental colitis through a ligand-independent mechanism.
Digestive diseases and sciences 2007;52(11):2912-9.
2007: Trump Ryan P; Cobb Jeffrey E; Shearer Barry G; Lambert Millard H; Nolte Robert T; Willson Timothy M; Buckholz Richard G; Zhao Sumin M; Leesnitzer Lisa M; Iannone Marie A; Pearce Kenneth H; Billin Andrew N; Hoekstra William J
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Bioorganic & medicinal chemistry letters 2007;17(14):3916-20.
2007: Burdick Andrew D; Bility Moses T; Girroir Elizabeth E; Billin Andrew N; Willson Timothy M; Gonzalez Frank J; Peters Jeffrey M
Ligand activation of peroxisome proliferator-activated receptor-beta/delta(PPARbeta/delta) inhibits cell growth of human N/TERT-1 keratinocytes.
Cellular signalling 2007;19(6):1163-71.
2007: Xue Yu; Chao Esther; Zuercher William J; Willson Timothy M; Collins Jon L; Redinbo Matthew R
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
Bioorganic & medicinal chemistry 2007;15(5):2156-66.
2007: Sprecher Dennis L; Massien Christine; Pearce Greg; Billin Andrew N; Perlstein Itay; Willson Timothy M; Hassall David G; Ancellin Nicolas; Patterson Scott D; Lobe David C; Johnson Tony G
Triglyceride:high-density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator activated receptor delta agonist.
Arteriosclerosis, thrombosis, and vascular biology 2007;27(2):359-65.
2007: Ghisletti Serena; Huang Wendy; Ogawa Sumito; Pascual Gabriel; Lin Mu-En; Willson Timothy M; Rosenfeld Michael G; Glass Christopher K
Parallel SUMOylation-dependent pathways mediate gene- and signal-specific transrepression by LXRs and PPARgamma.
Molecular cell 2007;25(1):57-70.
2007: Trump Ryan P; Blanc Jean-Baptiste E; Stewart Eugene L; Brown Peter J; Caivano Matilde; Gray David W; Hoekstra William J; Willson Timothy M; Han Bajin; Turnbull Philip
Design and synthesis of an array of selective androgen receptor modulators.
Journal of combinatorial chemistry 2007;9(1):107-14.
2006: Wang Liping; Zuercher William J; Consler Thomas G; Lambert Millard H; Miller Aaron B; Orband-Miller Lisa A; McKee David D; Willson Timothy M; Nolte Robert T
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.
The Journal of biological chemistry 2006;281(49):37773-81.
2006: Whitby Richard J; Dixon Sally; Maloney Patrick R; Delerive Philippe; Goodwin Bryan J; Parks Derek J; Willson Timothy M
Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.
Journal of medicinal chemistry 2006;49(23):6652-5.
2006: Marin Holly E; Peraza Marjorie A; Billin Andrew N; Willson Timothy M; Ward Jerrold M; Kennett Mary J; Gonzalez Frank J; Peters Jeffrey M
Ligand activation of peroxisome proliferator-activated receptor beta inhibits colon carcinogenesis.
Cancer research 2006;66(8):4394-401.
2006: Chao Esther Y H; Collins Jon L; Gaillard Stéphanie; Miller Aaron B; Wang Liping; Orband-Miller Lisa A; Nolte Robert T; McDonnell Donald P; Willson Timothy M; Zuercher William J
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Bioorganic & medicinal chemistry letters 2006;16(4):821-4.
2006: Zhang Yanqiao; Lee Florence Ying; Barrera Gabriel; Lee Hans; Vales Charisse; Gonzalez Frank J; Willson Timothy M; Edwards Peter A
Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice.
Proceedings of the National Academy of Sciences of the United States of America 2006;103(4):1006-11.
2006: Kim D J; Bility M T; Billin A N; Willson T M; Gonzalez F J; Peters J M
PPARbeta/delta selectively induces differentiation and inhibits cell proliferation.
Cell death and differentiation 2006;13(1):53-60.
2005: Pascual Gabriel; Fong Amy L; Ogawa Sumito; Gamliel Amir; Li Andrew C; Perissi Valentina; Rose David W; Willson Timothy M; Rosenfeld Michael G; Glass Christopher K
A SUMOylation-dependent pathway mediates transrepression of inflammatory response genes by PPAR-gamma.
Nature 2005;437(7059):759-63.
2005: Bledsoe Randy K; Madauss Kevin P; Holt Jason A; Apolito Christopher J; Lambert Millard H; Pearce Kenneth H; Stanley Thomas B; Stewart Eugene L; Trump Ryan P; Willson Timothy M; Williams Shawn P
A ligand-mediated hydrogen bond network required for the activation of the mineralocorticoid receptor.
The Journal of biological chemistry 2005;280(35):31283-93.
2005: Jaye Michael C; Krawiec John A; Campobasso Nino; Smallwood Angela; Qiu Chunyan; Lu Quinn; Kerrigan John J; De Los Frailes Alvaro Maite; Laffitte Bryan; Liu Wu-Schyong; Marino Joseph P; Meyer Craig R; Nichols Jason A; Parks Derek J; Perez Paloma; Sarov-Blat Lea; Seepersaud Sheila D; Steplewski Klaudia M; Thompson Scott K; Wang Ping; Watson Mike A; Webb Christine L; Haigh David; Caravella Justin A; Macphee Colin H; Willson Timothy M; Collins Jon L
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
Journal of medicinal chemistry 2005;48(17):5419-22.
2005: Wu Ya-Ling; Yang Xiaojing; Ren Zhong; McDonnell Donald P; Norris John D; Willson Timothy M; Greene Geoffrey L
Structural basis for an unexpected mode of SERM-mediated ER antagonism.
Molecular cell 2005;18(4):413-24.
2005: Zuercher William J; Gaillard Stéphanie; Orband-Miller Lisa A; Chao Esther Y H; Shearer Barry G; Jones David G; Miller Aaron B; Collins Jon L; McDonnell Donald P; Willson Timothy M
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.
Journal of medicinal chemistry 2005;48(9):3107-9.
2005: Fiorucci Stefano; Clerici Carlo; Antonelli Elisabetta; Orlandi Stefano; Goodwin Bryan; Sadeghpour Bahman M; Sabatino Giuseppe; Russo Giuseppe; Castellani Danilo; Willson Timothy M; Pruzanski Mark; Pellicciari Roberto; Morelli Antonio
Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis.
The Journal of pharmacology and experimental therapeutics 2005;313(2):604-12.
2005: Hoekstra William J; Patel Hari S; Liang Xi; Blanc Jean-Baptiste E; Heyer Dennis O; Willson Timothy M; Iannone Marie A; Kadwell Sue H; Miller Lisa A; Pearce Kenneth H; Simmons Catherine A; Shearin Jean
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.
Journal of medicinal chemistry 2005;48(6):2243-7.
2005: Krylova Irina N; Sablin Elena P; Moore Jamie; Xu Robert X; Waitt Gregory M; MacKay J Andrew; Juzumiene Dalia; Bynum Jane M; Madauss Kevin; Montana Valerie; Lebedeva Lioudmila; Suzawa Miyuki; Williams Jon D; Williams Shawn P; Guy Rodney K; Thornton Joseph W; Fletterick Robert J; Willson Timothy M; Ingraham Holly A
Structural analyses reveal phosphatidyl inositols as ligands for the NR5 orphan receptors SF-1 and LRH-1.
Cell 2005;120(3):343-55.
2004: Xu Robert X; Lambert Millard H; Wisely Bruce B; Warren Erin N; Weinert Emily E; Waitt Gregory M; Williams Jon D; Collins Jon L; Moore Linda B; Willson Timothy M; Moore John T
A structural basis for constitutive activity in the human CAR/RXRalpha heterodimer.
Molecular cell 2004;16(6):919-28.
2004: Li Andrew C; Binder Christoph J; Gutierrez Alejandra; Brown Kathleen K; Plotkin Christine R; Pattison Jennifer W; Valledor Annabel F; Davis Roger A; Willson Timothy M; Witztum Joseph L; Palinski Wulf; Glass Christopher K
Differential inhibition of macrophage foam-cell formation and atherosclerosis in mice by PPARalpha, beta/delta, and gamma.
The Journal of clinical investigation 2004;114(11):1564-76.
2004: Stewart Eugene L; Brown Peter J; Bentley James A; Willson Timothy M
Selection, application, and validation of a set of molecular descriptors for nuclear receptor ligands.
Combinatorial chemistry & high throughput screening 2004;7(5):407-12.
2004: Pellicciari Roberto; Costantino Gabriele; Camaioni Emidio; Sadeghpour Bahman M; Entrena Antonio; Willson Timothy M; Fiorucci Stefano; Clerici Carlo; Gioiello Antimo
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.
Journal of medicinal chemistry 2004;47(18):4559-69.
2004: Schmuth Matthias; Elias Peter M; Hanley Karen; Lau Peggy; Moser A; Willson Timothy M; Bikle Daniel D; Feingold Kenneth R
The effect of LXR activators on AP-1 proteins in keratinocytes.
The Journal of investigative dermatology 2004;123(1):41-8.
2004: Maglich Jodi M; Watson Joe; McMillen Patrick J; Goodwin Bryan; Willson Timothy M; Moore John T
The nuclear receptor CAR is a regulator of thyroid hormone metabolism during caloric restriction.
The Journal of biological chemistry 2004;279(19):19832-8.
2004: Schmuth Matthias; Haqq Christopher M; Cairns William J; Holder Julie C; Dorsam Sheri; Chang Sandra; Lau Peggy; Fowler Ashley J; Chuang Gary; Moser Arthur H; Brown Barbara E; Mao-Qiang Man; Uchida Yoshikazu; Schoonjans Kristina; Auwerx Johan; Chambon P; Willson Timothy M; Elias Peter M; Feingold Kenneth R
Peroxisome proliferator-activated receptor (PPAR)-beta/delta stimulates differentiation and lipid accumulation in keratinocytes.
The Journal of investigative dermatology 2004;122(4):971-83.
2003: Place Andrew E; Suh Nanjoo; Williams Charlotte R; Risingsong Renee; Honda Tadashi; Honda Yukiko; Gribble Gordon W; Leesnitzer Lisa M; Stimmel Julie B; Willson Timothy M; Rosen Evan; Sporn Michael B
The novel synthetic triterpenoid, CDDO-imidazolide, inhibits inflammatory response and tumor growth in vivo.
Clinical cancer research : an official journal of the American Association for Cancer Research 2003;9(7):2798-806.
2003: Maglich Jodi M; Caravella Justin A; Lambert Millard H; Willson Timothy M; Moore John T; Ramamurthy Lakshman
The first completed genome sequence from a teleost fish (Fugu rubripes) adds significant diversity to the nuclear receptor superfamily.
Nucleic acids research 2003;31(14):4051-8.
2003: Williams Shawn; Bledsoe Randy K; Collins Jon L; Boggs Sharon; Lambert Millard H; Miller Ann B; Moore John; McKee David D; Moore Linda; Nichols Jason; Parks Derek; Watson Mike; Wisely Bruce; Willson Timothy M
X-ray crystal structure of the liver X receptor beta ligand binding domain: regulation by a histidine-tryptophan switch.
The Journal of biological chemistry 2003;278(29):27138-43.
2003: Baker Keith D; Shewchuk Lisa M; Kozlova Tatiana; Makishima Makoto; Hassell Annie; Wisely Bruce; Caravella Justin A; Lambert Millard H; Reinking Jeffrey L; Krause Henry; Thummel Carl S; Willson Timothy M; Mangelsdorf David J
The Drosophila orphan nuclear receptor DHR38 mediates an atypical ecdysteroid signaling pathway.
Cell 2003;113(6):731-42.
2003: Sznaidman Marcos L; Haffner Curt D; Maloney Patrick R; Fivush Adam; Chao Esther; Goreham Donna; Sierra Michael L; LeGrumelec Christelle; Xu H Eric; Montana Valerie G; Lambert Millard H; Willson Timothy M; Oliver William R; Sternbach Daniel D
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Bioorganic & medicinal chemistry letters 2003;13(9):1517-21.
2003: Anisfeld Andrew M; Kast-Woelbern Heidi R; Meyer Marie E; Jones Stacey A; Zhang Yanqiao; Williams Kevin J; Willson Timothy; Edwards Peter A
Syndecan-1 expression is regulated in an isoform-specific manner by the farnesoid-X receptor.
The Journal of biological chemistry 2003;278(22):20420-8.
2003: Maglich Jodi M; Parks Derek J; Moore Linda B; Collins Jon L; Goodwin Bryan; Billin Andrew N; Stoltz Catherine A; Kliewer Steven A; Lambert Millard H; Willson Timothy M; Moore John T
Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes.
The Journal of biological chemistry 2003;278(19):17277-83.
2003: Fowler Ashley J; Sheu Mary Y; Schmuth Matthias; Kao Jack; Fluhr Joachim W; Rhein Linda; Collins Jon L; Willson Timothy M; Mangelsdorf David J; Elias Peter M; Feingold Kenneth R
Liver X receptor activators display anti-inflammatory activity in irritant and allergic contact dermatitis models: liver-X-receptor-specific inhibition of inflammation and primary cytokine production.
The Journal of investigative dermatology 2003;120(2):246-55.
2002: Kliewer Steven A; Goodwin Bryan; Willson Timothy M
The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism.
Endocrine reviews 2002;23(5):687-702.
2002: Wisely G Bruce; Miller Ann B; Davis Roderick G; Thornquest Alan D; Johnson Robert; Spitzer Tim; Sefler Andrea; Shearer Barry; Moore John T; Miller Aaron B; Willson Timothy M; Williams Shawn P
Hepatocyte nuclear factor 4 is a transcription factor that constitutively binds fatty acids.
Structure (London, England : 1993) 2002;10(9):1225-34.
2002: Pellicciari Roberto; Fiorucci Stefano; Camaioni Emidio; Clerici Carlo; Costantino Gabriele; Maloney Patrick R; Morelli Antonio; Parks Derek J; Willson Timothy M
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
Journal of medicinal chemistry 2002;45(17):3569-72.
2002: Bledsoe Randy K; Montana Valerie G; Stanley Thomas B; Delves Chris J; Apolito Christopher J; McKee David D; Consler Thomas G; Parks Derek J; Stewart Eugene L; Willson Timothy M; Lambert Millard H; Moore John T; Pearce Kenneth H; Xu H Eric
Crystal structure of the glucocorticoid receptor ligand binding domain reveals a novel mode of receptor dimerization and coactivator recognition.
Cell 2002;110(1):93-105.
2002: Willson Timothy M; Moore John T
Genomics versus orphan nuclear receptors--a half-time report.
Molecular endocrinology (Baltimore, Md.) 2002;16(6):1135-44.
2002: Joseph Sean B; McKilligin Elaine; Pei Liming; Watson Michael A; Collins Alan R; Laffitte Bryan A; Chen Mingyi; Noh Grace; Goodman Joanne; Hagger Graham N; Tran Jonathan; Tippin Tim K; Wang Xuping; Lusis Aldons J; Hsueh Willa A; Law Ronald E; Collins Jon L; Willson Timothy M; Tontonoz Peter
Synthetic LXR ligand inhibits the development of atherosclerosis in mice.
Proceedings of the National Academy of Sciences of the United States of America 2002;99(11):7604-9.
2002: Leesnitzer Lisa M; Parks Derek J; Bledsoe Randy K; Cobb Jeff E; Collins Jon L; Consler Thomas G; Davis Roderick G; Hull-Ryde Emily A; Lenhard James M; Patel Lisa; Plunket Kelli D; Shenk Jennifer L; Stimmel Julie B; Therapontos Christina; Willson Timothy M; Blanchard Steven G
Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662.
Biochemistry 2002;41(21):6640-50.
2002: Collins Jon L; Fivush Adam M; Watson Michael A; Galardi Cristin M; Lewis Michael C; Moore Linda B; Parks Derek J; Wilson Joan G; Tippin Tim K; Binz Jane G; Plunket Kelli D; Morgan Daniel G; Beaudet Elizabeth J; Whitney Karl D; Kliewer Steven A; Willson Timothy M
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
Journal of medicinal chemistry 2002;45(10):1963-6.
2002: Moore Linda B; Maglich Jodi M; McKee David D; Wisely Bruce; Willson Timothy M; Kliewer Steven A; Lambert Millard H; Moore John T
Pregnane X receptor (PXR), constitutive androstane receptor (CAR), and benzoate X receptor (BXR) define three pharmacologically distinct classes of nuclear receptors.
Molecular endocrinology (Baltimore, Md.) 2002;16(5):977-86.
2002: Kliewer Steven A; Willson Timothy M
Regulation of xenobiotic and bile acid metabolism by the nuclear pregnane X receptor.
Journal of lipid research 2002;43(3):359-64.
2002: Xu H Eric; Stanley Thomas B; Montana Valerie G; Lambert Millard H; Shearer Barry G; Cobb Jeffery E; McKee David D; Galardi Cristin M; Plunket Kelli D; Nolte Robert T; Parks Derek J; Moore John T; Kliewer Steven A; Willson Timothy M; Stimmel Julie B
Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha.
Nature 2002;415(6873):813-7.
2002: Kast Heidi R; Goodwin Bryan; Tarr Paul T; Jones Stacey A; Anisfeld Andrew M; Stoltz Catherine M; Tontonoz Peter; Kliewer Steve; Willson Timothy M; Edwards Peter A
Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor.
The Journal of biological chemistry 2002;277(4):2908-15.
2002: Moore John T; Goodwin Bryan; Willson Timothy M; Kliewer Steven A
Nuclear receptor regulation of genes involved in bile acid metabolism.
Critical reviews in eukaryotic gene expression 2002;12(2):119-35.
2001: Liu K G; Lambert M H; Ayscue A H; Henke B R; Leesnitzer L M; Oliver W R; Plunket K D; Xu H E; Sternbach D D; Willson T M
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Bioorganic & medicinal chemistry letters 2001;11(24):3111-3.
2001: Xu H E; Lambert M H; Montana V G; Plunket K D; Moore L B; Collins J L; Oplinger J A; Kliewer S A; Gampe R T; McKee D D; Moore J T; Willson T M
Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proceedings of the National Academy of Sciences of the United States of America 2001;98(24):13919-24.
2001: Liu K G; Lambert M H; Leesnitzer L M; Oliver W; Ott R J; Plunket K D; Stuart L W; Brown P J; Willson T M; Sternbach D D
Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis.
Bioorganic & medicinal chemistry letters 2001;11(22):2959-62.
2001: Willson T M; Jones S A; Moore J T; Kliewer S A
Chemical genomics: functional analysis of orphan nuclear receptors in the regulation of bile acid metabolism.
Medicinal research reviews 2001;21(6):513-22.
2001: Whitney K D; Watson M A; Goodwin B; Galardi C M; Maglich J M; Wilson J G; Willson T M; Collins J L; Kliewer S A
Liver X receptor (LXR) regulation of the LXRalpha gene in human macrophages.
The Journal of biological chemistry 2001;276(47):43509-15.
2001: Kast H R; Nguyen C M; Sinal C J; Jones S A; Laffitte B A; Reue K; Gonzalez F J; Willson T M; Edwards P A
Farnesoid X-activated receptor induces apolipoprotein C-II transcription: a molecular mechanism linking plasma triglyceride levels to bile acids.
Molecular endocrinology (Baltimore, Md.) 2001;15(10):1720-8.
2001: Liu K G; Smith J S; Ayscue A H; Henke B R; Lambert M H; Leesnitzer L M; Plunket K D; Willson T M; Sternbach D D
Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta.
Bioorganic & medicinal chemistry letters 2001;11(17):2385-8.
2001: Way J M; Görgün C Z; Tong Q; Uysal K T; Brown K K; Harrington W W; Oliver W R; Willson T M; Kliewer S A; Hotamisligil G S
Adipose tissue resistin expression is severely suppressed in obesity and stimulated by peroxisome proliferator-activated receptor gamma agonists.
The Journal of biological chemistry 2001;276(28):25651-3.
2001: Watkins R E; Wisely G B; Moore L B; Collins J L; Lambert M H; Williams S P; Willson T M; Kliewer S A; Redinbo M R
The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity.
Science (New York, N.Y.) 2001;292(5525):2329-33.
2001: Brown P J; Stuart L W; Hurley K P; Lewis M C; Winegar D A; Wilson J G; Wilkison W O; Ittoop O R; Willson T M
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Bioorganic & medicinal chemistry letters 2001;11(9):1225-7.
2001: Oliver W R; Shenk J L; Snaith M R; Russell C S; Plunket K D; Bodkin N L; Lewis M C; Winegar D A; Sznaidman M L; Lambert M H; Xu H E; Sternbach D D; Kliewer S A; Hansen B C; Willson T M
A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport.
Proceedings of the National Academy of Sciences of the United States of America 2001;98(9):5306-11.
2001: Connor C E; Norris J D; Broadwater G; Willson T M; Gottardis M M; Dewhirst M W; McDonnell D P
Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor.
Cancer research 2001;61(7):2917-22.
2001: Spencer T A; Li D; Russel J S; Collins J L; Bledsoe R K; Consler T G; Moore L B; Galardi C M; McKee D D; Moore J T; Watson M A; Parks D J; Lambert M H; Willson T M
Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha.
Journal of medicinal chemistry 2001;44(6):886-97.
2001: Staudinger J L; Goodwin B; Jones S A; Hawkins-Brown D; MacKenzie K I; LaTour A; Liu Y; Klaassen C D; Brown K K; Reinhard J; Willson T M; Koller B H; Kliewer S A
The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity.
Proceedings of the National Academy of Sciences of the United States of America 2001;98(6):3369-74.
2001: Way J M; Harrington W W; Brown K K; Gottschalk W K; Sundseth S S; Mansfield T A; Ramachandran R K; Willson T M; Kliewer S A
Comprehensive messenger ribonucleic acid profiling reveals that peroxisome proliferator-activated receptor gamma activation has coordinate effects on gene expression in multiple insulin-sensitive tissues.
Endocrinology 2001;142(3):1269-77.
2001: Maglich J M; Sluder A; Guan X; Shi Y; McKee D D; Carrick K; Kamdar K; Willson T M; Moore J T
Comparison of complete nuclear receptor sets from the human, Caenorhabditis elegans and Drosophila genomes.
Genome biology 2001;2(8):RESEARCH0029.
2000: Wang Y; Porter W W; Suh N; Honda T; Gribble G W; Leesnitzer L M; Plunket K D; Mangelsdorf D J; Blanchard S G; Willson T M; Sporn M B
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.
Molecular endocrinology (Baltimore, Md.) 2000;14(10):1550-6.
2000: Goodwin B; Jones S A; Price R R; Watson M A; McKee D D; Moore L B; Galardi C; Wilson J G; Lewis M C; Roth M E; Maloney P R; Willson T M; Kliewer S A
A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis.
Molecular cell 2000;6(3):517-26.
2000: Maloney P R; Parks D J; Haffner C D; Fivush A M; Chandra G; Plunket K D; Creech K L; Moore L B; Wilson J G; Lewis M C; Jones S A; Willson T M
Identification of a chemical tool for the orphan nuclear receptor FXR.
Journal of medicinal chemistry 2000;43(16):2971-4.
2000: Li A C; Brown K K; Silvestre M J; Willson T M; Palinski W; Glass C K
Peroxisome proliferator-activated receptor gamma ligands inhibit development of atherosclerosis in LDL receptor-deficient mice.
The Journal of clinical investigation 2000;106(4):523-31.
2000: Moore L B; Goodwin B; Jones S A; Wisely G B; Serabjit-Singh C J; Willson T M; Collins J L; Kliewer S A
St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor.
Proceedings of the National Academy of Sciences of the United States of America 2000;97(13):7500-2.
2000: Moore L B; Parks D J; Jones S A; Bledsoe R K; Consler T G; Stimmel J B; Goodwin B; Liddle C; Blanchard S G; Willson T M; Collins J L; Kliewer S A
Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands.
The Journal of biological chemistry 2000;275(20):15122-7.
2000: Spencer T A; Li D; Russel J S; Tomkinson N C; Willson T M
Further studies on the synthesis of 24(S),25-epoxycholesterol. A new, efficient preparation of desmosterol.
The Journal of organic chemistry 2000;65(7):1919-23.
2000: Gampe R T; Montana V G; Lambert M H; Miller A B; Bledsoe R K; Milburn M V; Kliewer S A; Willson T M; Xu H E
Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors.
Molecular cell 2000;5(3):545-55.
2000: Willson T M; Brown P J; Sternbach D D; Henke B R
The PPARs: from orphan receptors to drug discovery.
Journal of medicinal chemistry 2000;43(4):527-50.
2000: Jones S A; Moore L B; Shenk J L; Wisely G B; Hamilton G A; McKee D D; Tomkinson N C; LeCluyse E L; Lambert M H; Willson T M; Kliewer S A; Moore J T
The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution.
Molecular endocrinology (Baltimore, Md.) 2000;14(1):27-39.
1999: Henke B R; Adkison K K; Blanchard S G; Leesnitzer L M; Mook R A; Plunket K D; Ray J A; Roberson C; Unwalla R; Willson T M
Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.
Bioorganic & medicinal chemistry letters 1999;9(23):3329-34.
1999: Suh N; Wang Y; Williams C R; Risingsong R; Gilmer T; Willson T M; Sporn M B
A new ligand for the peroxisome proliferator-activated receptor-gamma (PPAR-gamma), GW7845, inhibits rat mammary carcinogenesis.
Cancer research 1999;59(22):5671-3.
1999: Fuqua S A; Schiff R; Parra I; Friedrichs W E; Su J L; McKee D D; Slentz-Kesler K; Moore L B; Willson T M; Moore J T
Expression of wild-type estrogen receptor beta and variant isoforms in human breast cancer.
Cancer research 1999;59(21):5425-8.
1999: Brown P J; Winegar D A; Plunket K D; Moore L B; Lewis M C; Wilson J G; Sundseth S S; Koble C S; Wu Z; Chapman J M; Lehmann J M; Kliewer S A; Willson T M
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.
Journal of medicinal chemistry 1999;42(19):3785-8.
1999: Huang J T; Welch J S; Ricote M; Binder C J; Willson T M; Kelly C; Witztum J L; Funk C D; Conrad D; Glass C K
Interleukin-4-dependent production of PPAR-gamma ligands in macrophages by 12/15-lipoxygenase.
Nature 1999;400(6742):378-82.
1999: Brown K K; Henke B R; Blanchard S G; Cobb J E; Mook R; Kaldor I; Kliewer S A; Lehmann J M; Lenhard J M; Harrington W W; Novak P J; Faison W; Binz J G; Hashim M A; Oliver W O; Brown H R; Parks D J; Plunket K D; Tong W Q; Menius J A; Adkison K; Noble S A; Willson T M
A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat.
Diabetes 1999;48(7):1415-24.
1999: Oberfield J L; Collins J L; Holmes C P; Goreham D M; Cooper J P; Cobb J E; Lenhard J M; Hull-Ryde E A; Mohr C P; Blanchard S G; Parks D J; Moore L B; Lehmann J M; Plunket K; Miller A B; Milburn M V; Kliewer S A; Willson T M
A peroxisome proliferator-activated receptor gamma ligand inhibits adipocyte differentiation.
Proceedings of the National Academy of Sciences of the United States of America 1999;96(11):6102-6.
1999: Parks D J; Blanchard S G; Bledsoe R K; Chandra G; Consler T G; Kliewer S A; Stimmel J B; Willson T M; Zavacki A M; Moore D D; Lehmann J M
Bile acids: natural ligands for an orphan nuclear receptor.
Science (New York, N.Y.) 1999;284(5418):1365-8.
1999: Kliewer S A; Lehmann J M; Willson T M
Orphan nuclear receptors: shifting endocrinology into reverse.
Science (New York, N.Y.) 1999;284(5415):757-60.
1999: Xu H E; Lambert M H; Montana V G; Parks D J; Blanchard S G; Brown P J; Sternbach D D; Lehmann J M; Wisely G B; Willson T M; Kliewer S A; Milburn M V
Molecular recognition of fatty acids by peroxisome proliferator-activated receptors.
Molecular cell 1999;3(3):397-403.
1999: Kliewer S A; Lehmann J M; Milburn M V; Willson T M
The PPARs and PXRs: nuclear xenobiotic receptors that define novel hormone signaling pathways.
Recent progress in hormone research 1999;54():345-67; discussion 367-8.
1998: Parks D J; Tomkinson N C; Villeneuve M S; Blanchard S G; Willson T M
Differential activity of rosiglitazone enantiomers at PPAR gamma.
Bioorganic & medicinal chemistry letters 1998;8(24):3657-8.
1998: Henke B R; Blanchard S G; Brackeen M F; Brown K K; Cobb J E; Collins J L; Harrington W W; Hashim M A; Hull-Ryde E A; Kaldor I; Kliewer S A; Lake D H; Leesnitzer L M; Lehmann J M; Lenhard J M; Orband-Miller L A; Miller J F; Mook R A; Noble S A; Oliver W; Parks D J; Plunket K D; Szewczyk J R; Willson T M
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
Journal of medicinal chemistry 1998;41(25):5020-36.
1998: Kliewer S A; Willson T M
The nuclear receptor PPARgamma - bigger than fat.
Current opinion in genetics & development 1998;8(5):576-81.
1998: Nolte R T; Wisely G B; Westin S; Cobb J E; Lambert M H; Kurokawa R; Rosenfeld M G; Willson T M; Glass C K; Milburn M V
Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma.
Nature 1998;395(6698):137-43.
1998: Lehmann J M; McKee D D; Watson M A; Willson T M; Moore J T; Kliewer S A
The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
The Journal of clinical investigation 1998;102(5):1016-23.
1998: Moore J T; McKee D D; Slentz-Kesler K; Moore L B; Jones S A; Horne E L; Su J L; Kliewer S A; Lehmann J M; Willson T M
Cloning and characterization of human estrogen receptor beta isoforms.
Biochemical and biophysical research communications 1998;247(1):75-8.
1998: Kliewer S A; Moore J T; Wade L; Staudinger J L; Watson M A; Jones S A; McKee D D; Oliver B B; Willson T M; Zetterström R H; Perlmann T; Lehmann J M
An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway.
Cell 1998;92(1):73-82.
1998: Ricote M; Li A C; Willson T M; Kelly C J; Glass C K
The peroxisome proliferator-activated receptor-gamma is a negative regulator of macrophage activation.
Nature 1998;391(6662):79-82.
1997: Brown P J; Smith-Oliver T A; Charifson P S; Tomkinson N C; Fivush A M; Sternbach D D; Wade L E; Orband-Miller L; Parks D J; Blanchard S G; Kliewer S A; Lehmann J M; Willson T M
Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library.
Chemistry & biology 1997;4(12):909-18.
1997: Willson T M; Norris J D; Wagner B L; Asplin I; Baer P; Brown H R; Jones S A; Henke B; Sauls H; Wolfe S; Morris D C; McDonnell D P
Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of estrogen receptor in bone.
Endocrinology 1997;138(9):3901-11.
1997: Henke B R; Aquino C J; Birkemo L S; Croom D K; Dougherty R W; Ervin G N; Grizzle M K; Hirst G C; James M K; Johnson M F; Queen K L; Sherrill R G; Sugg E E; Suh E M; Szewczyk J W; Unwalla R J; Yingling J; Willson T M
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
Journal of medicinal chemistry 1997;40(17):2706-25.
1997: Zavacki A M; Lehmann J M; Seol W; Willson T M; Kliewer S A; Moore D D
Activation of the orphan receptor RIP14 by retinoids.
Proceedings of the National Academy of Sciences of the United States of America 1997;94(15):7909-14.
1997: Kliewer S A; Sundseth S S; Jones S A; Brown P J; Wisely G B; Koble C S; Devchand P; Wahli W; Willson T M; Lenhard J M; Lehmann J M
Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma.
Proceedings of the National Academy of Sciences of the United States of America 1997;94(9):4318-23.
1997: Lehmann J M; Kliewer S A; Moore L B; Smith-Oliver T A; Oliver B B; Su J L; Sundseth S S; Winegar D A; Blanchard D E; Spencer T A; Willson T M
Activation of the nuclear receptor LXR by oxysterols defines a new hormone response pathway.
The Journal of biological chemistry 1997;272(6):3137-40.
1996: Willson T M; Lehmann J M; Kliewer S A
Discovery of ligands for the nuclear peroxisome proliferator-activated receptors.
Annals of the New York Academy of Sciences 1996;804():276-83.
1996: Hirst G C; Aquino C; Birkemo L; Croom D K; Dezube M; Dougherty R W; Ervin G N; Grizzle M K; Henke B; James M K; Johnson M F; Momtahen T; Queen K L; Sherrill R G; Szewczyk J; Willson T M; Sugg E E
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
Journal of medicinal chemistry 1996;39(26):5236-45.
1996: Willson T M; Henke B R; Momtahen T M; Myers P L; Sugg E E; Unwalla R J; Croom D K; Dougherty R W; Grizzle M K; Johnson M F; Queen K L; Rimele T J; Yingling J D; James M K
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
Journal of medicinal chemistry 1996;39(15):3030-4.
1996: Henke B R; Willson T M; Sugg E E; Croom D K; Dougherty R W; Queen K L; Birkemo L S; Ervin G N; Grizzle M K; Johnson M F; James M K
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
Journal of medicinal chemistry 1996;39(14):2655-8.
1996: Willson T M; Cobb J E; Cowan D J; Wiethe R W; Correa I D; Prakash S R; Beck K D; Moore L B; Kliewer S A; Lehmann J M
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
Journal of medicinal chemistry 1996;39(3):665-8.
1995: Kliewer S A; Lenhard J M; Willson T M; Patel I; Morris D C; Lehmann J M
A prostaglandin J2 metabolite binds peroxisome proliferator-activated receptor gamma and promotes adipocyte differentiation.
Cell 1995;83(5):813-9.
1995: Lehmann J M; Moore L B; Smith-Oliver T A; Wilkison W O; Willson T M; Kliewer S A
An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma).
The Journal of biological chemistry 1995;270(22):12953-6.
1994: Willson T M; Henke B R; Momtahen T M; Charifson P S; Batchelor K W; Lubahn D B; Moore L B; Oliver B B; Sauls H R; Triantafillou J A
3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats.
Journal of medicinal chemistry 1994;37(11):1550-2.

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