Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Heidi Figler"'
Autor:
James Horne, Patrick M. Sexton, Bernard L. Flynn, Peter J. Scammells, Heidi Figler, Celine Valant, Gemma N. Ferguson, Arthur Christopoulos, Joel Linden, David K. Chalmers
Publikováno v:
Journal of Medicinal Chemistry. 51:6165-6172
A pharmacophore-based screen identified 32 compounds including ethyl 5-amino-3-(4- tert-butylphenyl)-4-oxo-3,4-dihydrothieno[3,4- d]pyridazine-1-carboxylate ( 8) as a new allosteric modulator of the adenosine A1 receptor (A1AR). On the basis of this
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52be8bf9686eafbfee3d3886210eed44
https://doi.org/10.1021/jm800557d
https://doi.org/10.1021/jm800557d
Autor:
Joel Linden, Lixin Wang, Heidi Figler, Robert A. Figler, Andrew T. Gewirtz, Didier Merlin, Vasantha L. Kolachala, Simon M. Mwangi, Matam Vijay-Kumar, Shanthi Srinivasan, S Sitaraman, Brittani K. Ruble
Publikováno v:
British Journal of Pharmacology. 155:127-137
Background and purpose: The adenosine 2B (A2B) receptor is the predominant adenosine receptor expressed in the colon. Acting through the A2B receptor, adenosine mediates chloride secretion, as well as fibronectin and interleukin (IL)-6 synthesis and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1e6990f5fd624ab623ee251c8ad622dd
https://doi.org/10.1038/bjp.2008.227
https://doi.org/10.1038/bjp.2008.227
Autor:
Jaymes Beech, Joel Linden, Heidi Figler, Lana Saleh, Julie Frentzel, Ivan R. Corrêa, Christopher J. Noren, Brenda Baker, Melissa A. Marshall, Kimberly A. Kelly, Caroline Ramspacher, Siva Sai Krishna Dasa
High-throughput screening of combinatorial chemical libraries is a powerful approach for identifying targeted molecules. The display of combinatorial peptide libraries on the surface of bacteriophages offers a rapid, economical way to screen billions
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00ccd043a81d7578137f022021581643
https://europepmc.org/articles/PMC6252250/
https://europepmc.org/articles/PMC6252250/
Autor:
Heidi Figler, Ray A. Olsson, Timothy L. Macdonald, Molly Zigler, Lauren J. Murphree, Mahendra D. Chordia, Joel Linden
Publikováno v:
Journal of Medicinal Chemistry. 48:5131-5139
Allosteric enhancers (AEs) of the A(1) adenosine receptor (A(1)AR) have potential as drugs for treating neurological, cardiovascular, and renal diseases. This report describes the synthesis and evaluation of a series of 6-aryl-8H-indeno[1,2-d]thiazol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b4920cca7a7495efb4a8c0a1395ba6b
https://doi.org/10.1021/jm049132j
https://doi.org/10.1021/jm049132j
Publikováno v:
Molecular Pharmacology. 64:1557-1564
Endogenous ligands of G protein-coupled receptors bind to orthosteric sites that are topologically distinct from allosteric sites. Certain aminothiophenes such as (2-amino-4,5-dimethyl-3-thienyl)-[3-(trifluromethyl)-phenyl]-methanone (PD81,723) and 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b4c4e5d14b57b5c339927f774367388a
https://doi.org/10.1124/mol.64.6.1557
https://doi.org/10.1124/mol.64.6.1557
The second extracellular loop of the adenosine A1 receptor mediates activity of allosteric enhancers
Autor:
Dylan P. Kennedy, Mark Yeager, Susan A. Leonhardt, Robert A. Figler, Melissa A. Marshall, Michael D. Purdy, Heidi Figler, Fiona M. McRobb, Mahendra D. Chordia, Ruben Abagyan, Joel Linden
Publikováno v:
Molecular pharmacology, vol 85, iss 2
Allosteric enhancers of the adenosine A1 receptor amplify signaling by orthosteric agonists. Allosteric enhancers are appealing drug candidates because their activity requires that the orthosteric site be occupied by an agonist, thereby conferring sp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e9fa6d9fa561bd4c0821e062c9ca5b8
https://escholarship.org/uc/item/32n7m128
https://escholarship.org/uc/item/32n7m128
Autor:
C. Elisabet Tranberg, Andrea Zickgraf, Brian N. Giunta, Henning Luetjens, Heidi Figler, Lauren J. Murphree, Ruediger Falke, Holger Fleischer, Joel Linden, Peter J. Scammells, Ray. A. Olsson
Publikováno v:
Journal of Medicinal Chemistry. 45:382-389
2-Amino-3-benzoylthiophenes are allosteric enhancers (AE) of agonist activity at the A(1) adenosine receptor. The present report describes syntheses and assays of the AE activity at the human A(1)AR (hA(1)AR) of a panel of compounds consisting of nin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2759dccfd5e78f669a7d3d243aeda08
https://doi.org/10.1021/jm010081p
https://doi.org/10.1021/jm010081p
Autor:
John M. ARMSTRONG, Jiang Fan CHEN, Michael A. SCHWARZSCHILD, Sergey APASOV, Patrick T. SMITH, Charles CALDWELL, Pearl CHEN, Heidi FIGLER, Gail SULLIVAN, Steven FINK, Joel LINDEN, Michail SITKOVSKY
Publikováno v:
Biochemical Journal. 354:123-130
Agonist binding to extracellular A2A adenosine receptors (A2ARs) inhibits the activation of virtually all tested functions of T-cells and can induce apoptosis in thymocytes. The evaluation of levels of expression of these immunosuppressive receptors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a09005883846bb243ae42f2796a3df25
https://doi.org/10.1042/bj3540123
https://doi.org/10.1042/bj3540123
Autor:
Heidi Figler, Steven E. Bottle, Shane M. Devine, Joel Linden, Colin W. Pouton, Kate V McIntosh, Paul J. White, Alison Gregg, Peter J. Scammells, Vijay Urmaliya
Publikováno v:
Bioorganicmedicinal chemistry. 18(9)
A number of N(6)-substituted adenosine-5'-N-methylcarboxamides were synthesised and their pharmacology, in terms of their receptor affinity, selectivity and cardioprotective effects, were explored. The first series of compounds, 4a-4f and 5a-5f, show
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9883deaed1b1c15c73d46b2ecb26d3f7
https://pubmed.ncbi.nlm.nih.gov/20385496
https://pubmed.ncbi.nlm.nih.gov/20385496
Autor:
Robert A. Figler, Joel Linden, Heidi Figler, James C. Garrison, William E. McIntire, Dora Bigler-Wang
Publikováno v:
The FASEB Journal. 23
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::039a189d814e917f20ab316e5672e7f7
https://doi.org/10.1096/fasebj.23.1_supplement.583.1
https://doi.org/10.1096/fasebj.23.1_supplement.583.1