Výsledky vyhledávání - "Joshua G. McCoy"

A novel class of ion displacement ligands as antagonists of the αIIbβ3 receptor that limit conformational reorganization of the receptor

Autor: Robert Blue, Christopher A. LeClair, Marta Filizola, Craig J. Thomas, Mariana Babayeva, Won-Seok Choi, Mark A. Nedelman, Amanda Weil Harrington, Sarasija Naini, Elisabetta Volpi, Jian-kang Jiang, Min Shen, Joseph Fernandez, Andrea Negri, Wenwei Huang, Jihong Li, George A. David, Joshua G. McCoy, Barry S. Coller

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:1148-1153

A collection of αIIbβ3 integrin receptor antagonists possessing a unique MIDAS metal ion displacement mechanism of action is presented. Insight into these agents’ structure-activity relationships, binding modality, and pharmacokinetic and pharmac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bf46f8bf19a934abc340a37e8f64cb0
https://doi.org/10.1016/j.bmcl.2013.12.122

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A New Small-Molecule Antagonist Inhibits Graves' Disease Antibody Activation of the TSH Receptor

Autor: Marvin C. Gershengorn, Joshua G. McCoy, Elena Eliseeva, Susanne Neumann, Cesidio Giuliani, Wenwei Huang, F. Monaco, Giorgio Napolitano

Publikováno v: The Journal of Clinical Endocrinology & Metabolism. 96:548-554

Context: Graves' disease (GD) is caused by persistent, unregulated stimulation of thyrocytes by thyroid-stimulating antibodies (TSAbs) that activate the TSH receptor (TSHR). We previously reported the first small-molecule antagonist of human TSHR and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4055797d68c9e7719e118ca772d978e9
https://doi.org/10.1210/jc.2010-1935

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Structure-Guided Design of a High-Affinity Platelet Integrin αIIbβ3 Receptor Antagonist That Disrupts Mg2+ Binding to the MIDAS

Autor: Wenwei Huang, Mark Rasmussen, Richard H. Aster, Jihong Li, Marta Filizola, Craig J. Thomas, Jianghai Zhu, Jieqing Zhu, Andrea Negri, Barry S. Coller, Won-Seok Choi, Timothy A. Springer, Joshua G. McCoy, Daniel W. Bougie, Sarasija Naini, Min Shen

An integrin found on platelets, α(IIb)β(3) mediates platelet aggregation, and α(IIb)β(3) antagonists are effective antithrombotic agents in the clinic. Ligands bind to integrins in part by coordinating a magnesium ion (Mg(2+)) located in the β s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28684dd3ea4e1c8072807713e63e2899
https://europepmc.org/articles/PMC3390238/

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Selective Modulation of Gq/Gs pathways by Naphtho Pyrano Pyrimidines as antagonists of the Neuropeptide S Receptor

Autor: Joshua G. McCoy, Ke Liu, Wei Zheng, Christopher P. Austin, Juan J. Marugan, Noel Southall, Wenwei Huang, Markus Heilig

Publikováno v: ACS chemical neuroscience. 1(8)

Antagonists of the neuropeptide S receptor have been postulated as promising therapeutics in the treatment of respiratory, sleep, anxiety, and addictive disorders. Here, we present the SAR of a new series of orthosteric antagonists. Neuropeptide S re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0014bb907c64011f07d0d28546eca2fd
https://pubmed.ncbi.nlm.nih.gov/21116448

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Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening

Autor: Anne-Marie L. Hogan, Douglas S. Auld, Donna M. Huryn, James Inglese, Kurt R. Brunden, Jennifer Wichterman, Alex Crowe, John Q. Trojanowski, Christopher P. Austin, Wenwei Huang, Carlo Ballatore, Virginia M.-Y. Lee, Amos B. Smith, Ruili Huang, Ronald L. Johnson, Joshua G. McCoy

Publikováno v: Biochemistry. 48(32)

Inclusions comprised of fibrils of the microtubule- (MT-) associated protein tau are found in the brains of those with Alzheimer's disease (AD) and other neurodegenerative tauopathies. The pathology that is observed in these diseases is believed to r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7051915a3714dfa7ba189711d99c9bc
https://pubmed.ncbi.nlm.nih.gov/19580328

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Structure-Guided Design of A Novel High Affinity Integrin αIIbβ3 Receptor Antagonist (RUC-2) That Displaces Mg2+ From the β3 MIDAS

Autor: Won-Seok Choi, Sarasija Naini, Jianghai Zhu, Joshua G. McCoy, Marta Filizola, Jihong Li, Timothy A. Springer, Andrea Negri, Min Shen, Jieqing Zhu, Barry S. Coller, Wenwei Huang, Craig J. Thomas

Publikováno v: Blood. 118:3255-3255

Abstract 3255 The platelet αIIbβ3 integrin receptor plays a central role in hemostasis and thrombosis. Small molecule inhibitors of αIIbβ3 based on the RGD cell recognition sequence block ligand binding by interacting with αIIb D224 via their po

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ae5262a19367fb0997d9a0ad7c773bb0
https://doi.org/10.1182/blood.v118.21.3255.3255

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The synthesis and evaluation of dihydroquinazolin-4-ones and quinazolin-4-ones as thyroid stimulating hormone receptor agonists

Autor: Noel Southall, Susanne Neumann, Wenwei Huang, Joshua G. McCoy, Craig J. Thomas, Paul Shin, James Inglese, Steve Titus, Wei Zheng, Elena Eliseeva, Erika Englund, William Leister, Christopher P. Austin, Marvin C. Gershengorn

Publikováno v: MedChemComm. 2:1016

We herein describe the rapid synthesis of a diverse set of dihydroquinazolin-4-ones and quinazolin-4-ones, their biological evaluation as thyroid stimulating hormone receptor (TSHR) agonists, and SAR analysis. Among the compounds screened, 8b was 60-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2e734e77a72c963835b053d8acb9edb
https://doi.org/10.1039/c1md00145k

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