Výsledky vyhledávání - "Marie-Therese Schaeffer"

Discovery, design and synthesis of a selective S1P3 receptor allosteric agonist

Autor: Timothy P. Spicer, Marie-Therese Schaeffer, Peter Hodder, Hugh Rosen, Xuemei Peng, Peter Chase, Steven D. Brown, Ramulu Poddutoori, Mariangela Urbano, Miguel Guerrero, Edward Roberts

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:6346-6349

Potent and selective S1P3 receptor (S1P3-R) agonists may represent important proof-of-principle tools used to clarify the receptor biological function and assess the therapeutic potential of the S1P3-R in cardiovascular, inflammatory and pulmonary di

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d98640b804031031179087d831a133c
https://doi.org/10.1016/j.bmcl.2013.09.075

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Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7)

Autor: Mariangela Urbano, Olivier Civelli, Subash Velaparthi, Hugh Rosen, Marie-Therese Schaeffer, Steven D. Brown, Zhiwei Wang, Peter Hodder, Miguel Guerrero, Edward Roberts, S. Adrian Saldanha, Peter Chase, Jian Zhao

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:7135-7141

Novel small molecule antagonists of NPBWR1 (GPR7) are herein reported. A high-throughput screening (HTS) of the Molecular Libraries-Small Molecule Repository library identified 5-chloro-4-(4-methoxyphenoxy)-2-(p-tolyl)pyridazin-3(2H)-one as a NPBWR1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef79ca019a4a4668683808e2cd7efee3
https://doi.org/10.1016/j.bmcl.2012.09.074

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Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonists

Autor: Mariangela Urbano, Hugh Rosen, Melissa Crisp, Miguel Guerrero, Peter Hodder, Edward Roberts, Jian Zhao, Peter Chase, Marie-Therese Schaeffer, Steven D. Brown

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:537-542

High affinity and selective small molecule agonists of the S1P4 receptor (S1P4-R) may have significant therapeutic utility in diverse disease areas including autoimmune diseases, viral infections and thrombocytopenia. A high-throughput screening (HTS

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e2c58669ef114fa9d90fdb3047c633fb
https://doi.org/10.1016/j.bmcl.2011.10.096

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SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P4) receptor

Autor: Jian Zhao, Mariangela Urbano, Miguel Guerrero, Hugh Rosen, Subash Velaparthi, Edward Roberts, Marie-Therese Schaeffer, Steven J. Brown

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:5470-5474

Recent evidence suggests an innovative application of chemical modulators targeting the S1P4 receptor as novel mechanism-based drugs for the treatment of influenza virus infection. Modulation of the S1P4 receptor may also represent an alternative the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bd5f83e05ec04a5d2050b04bf69a18fa
https://doi.org/10.1016/j.bmcl.2011.06.132

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Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation

Autor: Junying Wang, Jing Chen Xiao, D. Sloan Stribling, Marie-Therese Schaeffer, Alison M. Strack, Lauren P. Shearman, Cathy C. R.-R. Huang, D. Euan MacIntyre, Thomas F. Walsh, Christina B. Madsen-Duggan, Chun-Pyn Shen, John S. Debenham, Jeffrey J. Hale, Tung M. Fong, Julie Lao, Xinchun Tong

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:2591-2594

The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9a2f9d84b2ab0be0bec0ac56bc26960
https://doi.org/10.1016/j.bmcl.2009.03.005

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Ligand-Binding Pocket Shape Differences between Sphingosine 1-Phosphate (S1P) Receptors S1P1 and S1P3 Determine Efficiency of Chemical Probe Identification by Ultrahigh-Throughput Screening

Autor: Timothy P. Spicer, Peter Hodder, Pedro J. Gonzalez-Cabrera, Steven J. Brown, Peter Chase, Jacqueline Chapman, Hugh Rosen, Marie Therese Schaeffer, Euijung Jo, Stephan C. Schürer

Publikováno v: ACS Chemical Biology. 3:486-498

We have studied the sphingosine 1-phosphate (S1P) receptor system to better understand why certain molecular targets within a closely related family are much more tractable when identifying compelling chemical leads. Five medically important G-protei

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8acacf88dd44090b4ed557cea1cef717
https://doi.org/10.1021/cb800051m

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Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:681-685

Synthesis, SAR, and binding affinities are described for a new class of 1,8-naphthyridinone CB1 receptor specific inverse agonists. Food intake, knockout mouse, and pharmacokinetic evaluation of 14 indicate that this compound is an effective orally a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37afeaeaf562672568ac44a526b40c47
https://doi.org/10.1016/j.bmcl.2005.10.028

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Molecular Basis of the Pharmacological Difference between Rat and Human Bombesin Receptor Subtype-3 (BRS-3)

Autor: Xiao-Ming Guan, Lex H.T. Van der Ploeg, Marie-Therese Schaeffer, Jie Liu, Tung M. Fong, Zhege J. Lao, Michael M. Jiang, Jiaping Zhang

Publikováno v: Biochemistry. 41:8954-8960

We cloned the gene and cDNA for rat bombesin receptor subtype-3 (BRS-3) and characterized its mRNA expression pattern and pharmacological properties. Despite the high degree of sequence similarity (80% identical), rat and human BRS-3 differ markedly

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::654e154f447cbb1d1874215a228fd5c8
https://doi.org/10.1021/bi0202777

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Actions of a picomolar short-acting S1P1 agonist in S1P1-eGFP knock-in mice

Autor: Pedro J. Gonzalez-Cabrera, Fiona Scott, Bryan Clemons, Marie-Therese Schaeffer, Gor Sarkisyan, Hugh Rosen, Liming Huang, Nhan Nguyen, Stuart M. Cahalan, Adam Richard Yeager

Publikováno v: Nature chemical biology

Sphingosine 1-phosphate receptor 1 (S1P(1)) is critical for lymphocyte recirculation and is a clinical target for treatment of multiple sclerosis. By generating a short-duration S1P(1) agonist and mice in which fluorescently tagged S1P(1) replaces wi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33e6c21ed8eeaf8e5a06cd75b9edd518
http://europepmc.org/articles/PMC3430385

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Use of Bioluminescent Aequorin for the Pharmacological Characterization of 5ht Receptors

Autor: Marie-Therese Schaeffer, Jian Liu, L. H. T. Van Der Ploeg, Doris F. Cully, T. M. Fong, M. Chou

Publikováno v: Journal of Receptors and Signal Transduction. 19:927-938

A convenient functional assay for 5HT2a and 5HT2c receptors is reported utilizing the bioluminescent aequorin to detect intracellular calcium changes. Using this assay, the pharmacological properties of many 5HT ligands can be determined in a 96-well

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3fea0f2a0680bc4554064ed87a594281
https://doi.org/10.3109/10799899909038432

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