Výsledky vyhledávání - "Thomas G. Consler"

Correlation betweenin VitroPeptide Binding Profiles and Cellular Activities for Estrogen Receptor-Modulating Compounds

Autor: Marie A. Iannone, John G. Gray, Su Jun Deng, Kenneth H. Pearce, Dana E. Vanderwall, Thomas G. Consler, Catherine A. Simmons, Jean Shearin, Sue H. Kadwell, Daniel L. Svoboda

Publikováno v: Molecular Endocrinology. 18:1064-1081

Numerous biochemical and structural studies have shown that the conformation of the estrogen receptor alpha (ERalpha) can be influenced by ligand binding. In turn, the conformational state of ERalpha affects the ability of the receptor to interact wi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20d2b59f816aa91dfe529419bc58c3d2
https://doi.org/10.1210/me.2003-0432

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A New Series of Estrogen Receptor Modulators That Display Selectivity for Estrogen Receptor β

Autor: Dana R Hohman, Lisa A. Orband-Miller, Susan L. Weaver, Eugene L. Stewart, Shawn P. Williams, John T. Moore, Thomas G. Consler, Paul Kenneth Spearing, Ning Go, Philip Stewart Turnbull, Millard H. Lambert, Ron L. Hale, Linda B. Moore, Stacey A. Jones, Amy T. Lu, Brad R. Henke, G. Bruce Wisely, Jean Shearin, R. Graham Robinett

Publikováno v: Journal of Medicinal Chemistry. 45:5492-5505

A series of 1,3,5-triazine-based estrogen receptor (ER) modulators that are modestly selective for the ERbeta subtype are reported. Compound 1, which displayed modest potency and selectivity for ERbeta vs ERalpha, was identified via high-throughput s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38cfec455bd262565ce05f02a5f0f141
https://doi.org/10.1021/jm020291h

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Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Reveals a Novel Mode of Receptor Dimerization and Coactivator Recognition

Autor: Thomas G. Consler, Kenneth H. Pearce, Chris J. Delves, Thomas B. Stanley, John T. Moore, Randy K. Bledsoe, Millard H. Lambert, Eugene L. Stewart, Valerie G. Montana, Derek J. Parks, David D. McKee, Christopher J. Apolito, H. Eric Xu, Timothy M. Willson

Publikováno v: Cell. 110:93-105

Transcriptional regulation by the glucocorticoid receptor (GR) is mediated by hormone binding, receptor dimerization, and coactivator recruitment. Here, we report the crystal structure of the human GR ligand binding domain (LBD) bound to dexamethason

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcf8f401a1be5048b1f1a377acb71026
https://doi.org/10.1016/s0092-8674(02)00817-6

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Functional Consequences of Cysteine Modification in the Ligand Binding Sites of Peroxisome Proliferator Activated Receptors by GW9662

Autor: Roderick G. Davis, Emily A. Hull-Ryde, Jon L. Collins, Jennifer L. Shenk, James M. Lenhard, Thomas G. Consler, Julie B. Stimmel, Timothy M. Willson, Lisa M. Leesnitzer, Steven G. Blanchard, Jeff E. Cobb, Christina Therapontos, Lisa G. Patel, Derek J. Parks, Kelli D. Plunket, Randy K. Bledsoe

Publikováno v: Biochemistry. 41:6640-6650

In the course of a high throughput screen to search for ligands of peroxisome proliferator activated receptor-gamma (PPARgamma), we identified GW9662 using a competition binding assay against the human ligand binding domain. GW9662 had nanomolar IC(5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd661a5d5f790806a3e2d39e9d4b42d1
https://doi.org/10.1021/bi0159581

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Solution Studies of Recombinant Human Stromal-Cell-Derived Factor-1

Autor: William D. Holmes, Thomas G. Consler, Warren J. Rocque, Walter S. Dallas, Derril H. Willard

Publikováno v: Protein Expression and Purification. 21:367-377

Stromal-cell-derived factor-1 (SDF-1alpha) is an 8-kDa chemokine that is constitutively expressed in bone-marrow-derived stromal cells and has been identified as a ligand for the CXCR4 receptor. We produced the chemokine recombinantly as methionine-S

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7a881498680eb62d32ea36de3bb9fdc
https://doi.org/10.1006/prep.2001.1402

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Pharmacophore Analysis of the Nuclear Oxysterol Receptor LXRα

Autor: Timothy M. Willson, Michael A. Watson, Randy K. Bledsoe, Jonathon S. Russel, Thomas A. Spencer, Jon L. Collins, Dansu Li, John T. Moore, Derek J. Parks, Linda B. Moore, Thomas G. Consler, Cristin M. Galardi, Millard H. Lambert, David D. McKee

Publikováno v: Journal of Medicinal Chemistry. 44:886-897

A cell-free assay was developed for the orphan nuclear receptor LXRalpha that measures the ligand-dependent recruitment of a peptide from the steroid receptor coactivator 1 (SRC1) to the nuclear receptor. Using this ligand-sensing assay (LiSA), the s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::062c6bd9d9a67bcd5efe125c72b9f14f
https://doi.org/10.1021/jm0004749

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Multiplexed molecular interactions of nuclear receptors using fluorescent microspheres

Autor: Derek J. Parks, Thomas G. Consler, John G. Gray, Marie A. Iannone, Kenneth H. Pearce, Julie B. Stimmel

Publikováno v: Cytometry. 44:326-337

Background We describe a novel microsphere-based system to identify and characterize multiplexed interactions of nuclear receptors with peptides that represent the LXXLL binding region of coactivator proteins. Methods In this system, individual micro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e5357180af1710a9e87c0fd9c0532b16
https://doi.org/10.1002/1097-0320(20010801)44:4<326::aid-cyto1124>3.0.co

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Expression, Purification, and Characterization of the Human Receptor Activator of NF-κB Ligand (RANKL) Extracellular Domain

Autor: Earnest Horne, Janet H. Parham, Christine R. Hoffman, Byron Ellis, Jane Bynum, Sue H. Kadwell, Kevin Blackburn, Wen-Ji Chen, Thomas G. Consler, Derril H. Willard, Marie A. Iannone, George Barrett

Publikováno v: Protein Expression and Purification. 20:48-57

Receptor activator of NF-kappaB ligand (RANKL) is a type II transmembrane protein found on osteoblasts which functions as a major determinant of osteoclast differentiation and activation. RANKL mediates bone homeostasis through binding to the cognate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b033efb85a5d4fe85c3bb554e0b48ab
https://doi.org/10.1006/prep.2000.1278

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Bile Acids: Natural Ligands for an Orphan Nuclear Receptor

Autor: Thomas G. Consler, Jürgen M. Lehmann, Derek J. Parks, Timothy M. Willson, David D. Moore, Gyan Chandra, Steven G. Blanchard, Randy K. Bledsoe, Steven A. Kliewer, Julie B. Stimmel, Ann Marie Zavacki

Publikováno v: Science. 284:1365-1368

Bile acids regulate the transcription of genes that control cholesterol homeostasis through molecular mechanisms that are poorly understood. Physiological concentrations of free and conjugated chenodeoxycholic acid, lithocholic acid, and deoxycholic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e44bca35714252140671c2455cc740c0
https://doi.org/10.1126/science.284.5418.1365

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Product Release Is the Major Contributor tok cat for the Hepatitis C Virus Helicase-catalyzed Strand Separation of Short Duplex DNA

Autor: Thomas G. Consler, David J.T. Porter, Frank Preugschat, Mary H. Hanlon, Derril H. Willard, Jeanne E. Wilson, Steven A. Short

Publikováno v: Journal of Biological Chemistry. 273:18906-18914

Hepatitis C virus (HCV) helicase catalyzes the ATP-dependent strand separation of duplex RNA and DNA containing a 3' single-stranded tail. Equilibrium and velocity sedimentation centrifugation experiments demonstrated that the enzyme was monomeric in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::064272f9d19478176ca6a2b87ee7f17d
https://doi.org/10.1074/jbc.273.30.18906

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