Výsledky vyhledávání - "James W. Apriletti"

Differential effects of TR ligands on hormone dissociation rates: Evidence for multiple ligand entry/exit pathways

Autor: Phuong Nguyen, Paul Webb, James W. Apriletti, Marie Togashi, Ngoc Ha Nguyen, Igor Polikarpov, John D. Baxter, Thomas S. Scanlan, Suzana Telles da Cunha Lima

Publikováno v: Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP

Some nuclear receptor (NR) ligands promote dissociation of radiolabeled bound hormone from the buried ligand binding cavity (LBC) more rapidly than excess unlabeled hormone itself. This result was interpreted to mean that challenger ligands bind allo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1b8a045b6095ce11ef918966c87dd18
https://doi.org/10.1016/j.jsbmb.2009.08.003

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Human Thyroid Receptor Forms Tetramers in Solution, Which Dissociate Into Dimers Upon Ligand Binding

Autor: Luiz Alberto Simeoni, Sandra Martha Gomes Dias, Francisco de Assis Rocha Neves, Ana Carolina Migliorini Figueira, Maria A.M. Santos, Igor Polikarpov, James W. Apriletti, Paul Webb, Ralff C. J. Ribeiro, John D. Baxter

Publikováno v: Cell Biochemistry and Biophysics. 44:453-462

Thyroid hormone nuclear receptors (TRs) bind to DNA and activate transcription as heterodimers with the retinoid X receptor (RXR) or as homodimers or monomers. RXR also binds to DNA and activates transcription as homodimers but can, in addition, self

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c5fc07a79f2f75840fd85870aee3bfd
https://doi.org/10.1385/cbb:44:3:453

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Structural Determinants of Selective Thyromimetics

Autor: James W. Apriletti, Hikari A. I. Yoshihara, John D. Baxter, Thomas S. Scanlan

Publikováno v: Journal of Medicinal Chemistry. 46:3152-3161

The thyromimetic GC-1 shows a preference for binding the beta form of the thyroid hormone receptor (TR). GC-1 was designed as an analogue of the thyromimetic DIMIT, which has a lower affinity for TR and is not selective. GC-1 has a methylene group li

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd3c7cd525e05d8d5a86bf5a86d56c00
https://doi.org/10.1021/jm0301181

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Two Resistance to Thyroid Hormone Mutants with Impaired Hormone Binding

Autor: Ben Sandler, John D. Baxter, Robert J. Fletterick, James W. Apriletti, Hoa Nguyen, Brian L. West, B. Russell Huber, Suzana T. Cunha Lima

Publikováno v: Molecular Endocrinology. 17:643-652

Resistance to hormones is commonly due to mutations in genes encoding receptors. Resistance to thyroid hormone is due mostly to mutations of the beta-form of the human (h) thyroid hormone receptor (hTRbeta). We determined x-ray crystal structures of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f885b69bb9cb1385d541db352fa350c4
https://doi.org/10.1210/me.2002-0095

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Corepressor SMRT Functions as a Coactivator for Thyroid Hormone Receptor T3Rα from a Negative Hormone Response Element

Autor: Hege Berghagen, James W. Apriletti, Kristin Krogsrud, Erlend Ragnhildstveit, Gunnar Thuestad, Fahri Saatcioglu

Publikováno v: Journal of Biological Chemistry. 277:49517-49522

Nuclear receptors are ligand-modulated transcription factors that transduce the presence of lipophilic ligands into changes in gene expression. Nuclear receptor activity is regulated by ligand-induced interactions with coactivator or corepressor mole

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7da2547fda0ef610d61747442b4ffaeb
https://doi.org/10.1074/jbc.m209546200

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Rational Design and Synthesis of a Novel Thyroid Hormone Antagonist That Blocks Coactivator Recruitment

Autor: James W. Apriletti, Ngoc Ha Nguyen, Paul Webb, Suzana T. Cunha Lima, Thomas S. Scanlan, John D. Baxter

Publikováno v: Journal of Medicinal Chemistry. 45:3310-3320

Recent efforts have focused on the design and synthesis of thyroid hormone (T(3)) antagonists as potential therapeutic agents and chemical probes to understand hormone-signaling pathways. We previously reported the development of novel first-generati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee07e7cf813211f912970edd404996d0
https://doi.org/10.1021/jm0201013

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Structure-Based Design and Synthesis of a Thyroid Hormone Receptor (TR) Antagonist

Autor: Weijun Feng, Brian L. West, Paul Webb, Karin Mellstrom, James W. Apriletti, Thomas S. Scanlan, Ralff C. J. Ribeiro, John D. Baxter, Peter J. Kushner, Patrick Goede, Robert J. Fletterick, Richard L. Wagner, Stefan Nilsson

Publikováno v: Endocrinology. 143:517-524

Antagonists have been developed for several nuclear receptors but not for others, including TRs. TR antagonists may have significant clinical utility for treating hormone excess states and other conditions. A structure derived "extension hypothesis"

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e48757ee20e97ea7e2935e7bf8e6749
https://doi.org/10.1210/endo.143.2.8617

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Synthesis and biological activity of novel thyroid hormone analogues: 5′-aryl substituted GC-1 derivatives

Autor: Grazia Chiellini, Ngoc Ha Nguyen, James W. Apriletti, Thomas S. Scanlan, John D. Baxter

Publikováno v: Bioorganic & Medicinal Chemistry. 10:333-346

Compounds that selectively modulate thyroid hormone action by functioning as isoform-selective agonists or antagonists of the thyroid hormone receptors (TRs) might be useful for medical therapy. We have synthesized a high affinity TRbeta-selective ag

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75ebe172df8c61521ec204575f154acf
https://doi.org/10.1016/s0968-0896(01)00284-x

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Hormone Selectivity in Thyroid Hormone Receptors

Autor: B. Russell Huber, Suzana T. Cunha Lima, Andrew K. Shiau, Alexander E. Kelly, Robert J. Fletterick, Richard L. Wagner, Brian L. West, James W. Apriletti, Thomas S. Scanlan, John D. Baxter

Publikováno v: Molecular Endocrinology. 15:398-410

Separate genes encode thyroid hormone receptor subtypes TRalpha (NR1A1) and TRbeta (NR1A2). Products from each of these contribute to hormone action, but the subtypes differ in tissue distribution and physiological response. Compounds that discrimina

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76f71bb11f38a70a08812d0ae8bca0d0
https://doi.org/10.1210/mend.15.3.0608

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Selective modulation of thyroid hormone receptor action

Autor: J. David Furlow, James W. Apriletti, Thomas S. Scanlan, Brian L. West, Robert J. Fletterick, Russ Huber, John D. Baxter, Wolfgang H. Dillmann, Paul Webb

Publikováno v: The Journal of Steroid Biochemistry and Molecular Biology. 76:31-42

Thyroid hormones have some actions that might be useful therapeutically, but others that are deleterious. Potential therapeutically useful actions include those to induce weight loss and lower plasma cholesterol levels. Potential deleterious actions

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a99beb819f2b2c7625c425c55ae286a0
https://doi.org/10.1016/s0960-0760(01)00052-8

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