Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Erika A. Currier"'
Autor:
Ethan S. Burstein, Roger Olsson, Erika A. Currier, Sine Mandrup Bertozzi, Jacob Jensen, Jian Nong Ma, Magnus Gustafsson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5918-5921
1-(Benzothiazol-2-yl)-1-(4-chlorophenyl)ethanol (1) was identified as a positive allosteric modulator (PAM) of the CaSR in a functional cell-based assay. This compound belongs to a class of compounds that is structurally distinct from other known pos
Autor:
Roger Olsson, Erika A. Currier, Jian Nong Ma, Fredrik Lehmann, Ethan S. Burstein, Kristina Luthman, Uli Hacksell
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:4844-4854
A series of novel isochromanone based urotensin II receptor agonists have been synthesized and evaluated for their activity using a functional cell based assay (R-SAT). Several potent and efficacious derivatives were identified with 3-(3,4-dichloroph
Autor:
Steven R. Ohrmund, Carsten B. Andersen, Roger Olsson, Andria L. Del Tredici, Erika A. Currier, Norman Nash, Birgitte W. Lund, Fabrice Piu, Luke C. Fairbain
Publikováno v:
Molecular Pharmacology. 73:900-908
Steroidogenic factor SF-1, a constitutively active nuclear hormone receptor, is essential to the development of adrenal and gonadal glands and acts as a shaping factor of sexual determination and differentiation. Its effects are exerted primarily thr
Autor:
Jacques T. Weissman, Fabrice Piu, Mark R. Brann, Andria L. Del Tredici, Jian-Nong Ma, Norman Nash, Ethan S. Burstein, Tracy Spalding, Hans H. Schiffer, Erika A. Currier, David M. Weiner
Publikováno v:
Current Pharmaceutical Design. 12:1717-1729
Chemical genomics is a drug discovery strategy that relies heavily on high-throughput screening (HTS) and therefore benefits from functional assay platforms that allow HTS against all relevant genomic targets. Receptor Selection and Amplification Tec
Autor:
Kristina Luthman, Roger Olsson, Erika A. Currier, Uli Hacksell, Vladimir Sherbukhin, Fredrik Lehmann, Anna Pettersen
Publikováno v:
Journal of Medicinal Chemistry. 49:2232-2240
Six different series of nonpeptidic urotensin II receptor agonists have been synthesized and evaluated for their agonistic activity in a cell-based assay (R-SAT). The compounds are ring-opened analogues of the isochromanone-based agonist AC-7954 with
Autor:
Birgitte W. Lund, Fabrice Piu, Glenn Croston, Mark R. Brann, Natalie K Gauthier, Roger Olsson, Erika A. Currier, Uli Hacksell
Publikováno v:
Biochemical Pharmacology. 71:156-162
Drugs targeting retinoid receptors have been developed to treat a variety of therapeutic indications, but their success has been limited in part due to lack of selectivity. A novel functional cell-based assay R-SATtrade mark was employed to screen a
Autor:
Ethan S. Burstein, Tracy A. Spalding, Michele Feddock, Erika A. Currier, Anthony Essex, Mark R. Brann, Jian-Nong Ma, Norman Nash
Publikováno v:
Biochemical Pharmacology. 67:1279-1284
Many naturally occurring peptides exhibit a high degree of promiscuity across G-protein coupled receptor subtypes. The degree to which this phenomenon occurs, and its physiological significance is not well characterized. In addition, many ‘orphan
Autor:
Mark R. Brann, Ethan S. Burstein, Daniel L. Severance, Uli Hacksell, Jian Nong Ma, Brian F. O'Dowd, Nina Mohell, Linda Thunberg, Roger Olsson, David M. Weiner, Erika A. Currier, Norman Nash, Stig Allenmark, Glenn Croston
Publikováno v:
Journal of Medicinal Chemistry. 45:4950-4953
A functional cell-based screen identified 3-(4-chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one hydrochloride (AC-7954, 1) as a nonpeptidic agonist of the urotensin-II receptor. Racemic 1 had an EC50 of 300 nM at the human UII receptor and wa
Autor:
Terri L. Messier, Mark R. Brann, Donghui Li, Ethan S. Burstein, Niels Skjaerbaek, Erika A. Currier, Uli Hacksell, Tracy A. Spalding, Carol Trotter
Publikováno v:
Molecular Pharmacology. 61:1297-1302
Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. Most drugs bind to these sites and mimic or block the action of the native ligands. Using a high-throughput functional screen, we identified a
Autor:
Anne Eeg, Natalie K Gauthier, Vladimir Sherbukhin, Birgitte W. Lund, Fabrice Piu, Uli Hacksell, Mark R. Brann, Roger Olsson, Erika A. Currier
Publikováno v:
Journal of Medicinal Chemistry. 48:7517-7519
4'-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARbeta2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophili