Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Sarah A. Nickolls"'
Publikováno v:
PLoS ONE, Vol 8, Iss 12, p e83691 (2013)
Agonists at the µ-opioid receptor are known to produce potent analgesic responses in the clinical setting, therefore, an increased understanding of the molecular interactions of ligands at this receptor could lead to improved analgesics. As historic
Externí odkaz:
https://doaj.org/article/e33a888ffa244cbeb048b16be12c30c5
Autor:
Cathleen Hsu, Robert M. Owen, Evan D. Morris, Gang Feng, Guido van Amerongen, Andy N. Mead, Sarah A. Nickolls, David S. Reynolds, Lishuang Cao, Juha Kammonen, Clara Stead, Ruolun Qiu, Donal Gorman, Richard P. Butt, Adam R. Brown, Joop M. A. van Gerven, Rachel Gurrell, Christine Anne Louise Watson, Mark Whitlock, Laigao Chen, Rebecca L. Fish, Andrew Pike, Pinky Dua
Publikováno v:
British Journal of Pharmacology. 175:708-725
Background and purpose Benzodiazepines, non-selective positive allosteric modulators (PAMs) of GABAA receptors, have significant side effects that limit their clinical utility. As many of these side effects are mediated by the α1 subunit, there has
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::da051882a6b4724d68b80dbf86c2760e
https://doi.org/10.1111/bph.14119
https://doi.org/10.1111/bph.14119
Residues W320 and Y328 within the binding site of the μ-opioid receptor influence opiate ligand bias
Autor:
Rubben Torella, Monique Hooley, J. Daniel Hothersall, Sarah A. Nickolls, Alastair J. H. Brown, Gordon McMurray, Sian Humphreys
Publikováno v:
Neuropharmacology. 118:46-58
The development of G protein-biased agonists for the μ-opioid receptor (MOR) offers a clear drug discovery rationale for improved analgesia and reduced side-effects of opiate pharmacotherapy. However, our understanding of the molecular mechanisms go
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d3b0dcc0b296770be7b290c048ce1c6
Autor:
Robert M, Owen, David, Blakemore, Lishuang, Cao, Neil, Flanagan, Rebecca, Fish, Karl R, Gibson, Rachel, Gurrell, Chan Woo, Huh, Juha, Kammonen, Elisabeth, Mortimer-Cassen, Sarah A, Nickolls, Kiyoyuki, Omoto, Dafydd, Owen, Andy, Pike, David C, Pryde, David S, Reynolds, Rosemarie, Roeloffs, Colin, Rose, Clara, Stead, Mifune, Takeuchi, Joseph S, Warmus, Christine, Watson
Publikováno v:
Journal of medicinal chemistry. 62(12)
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::1b852c98ab428508fb3c4d5969e61528
https://pubmed.ncbi.nlm.nih.gov/30964988
https://pubmed.ncbi.nlm.nih.gov/30964988
Autor:
Colin R. Rose, Elisabeth Mortimer-Cassen, Juha Kammonen, Rebecca L. Fish, David C. Pryde, Lishuang Cao, Sarah A. Nickolls, Neil J. Flanagan, Karl Richard Gibson, Joseph S. Warmus, Christine Anne Louise Watson, Chan Woo Huh, David J. Reynolds, Rachel Gurrell, Kiyoyuki Omoto, Andrew Pike, Clara Stead, David C. Blakemore, Rosemarie Roeloffs, Dafydd R. Owen, Mifune Takeuchi, Robert M. Owen
Publikováno v:
Journal of Medicinal Chemistry.
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described. From a set of initial hits multiple subseries were des
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::69244f4f78fe59a3b806c142bdaa534b
https://doi.org/10.1021/acs.jmedchem.9b00322
https://doi.org/10.1021/acs.jmedchem.9b00322
Autor:
Sarah Elizabeth Skerratt, Xiaohe Tong, Lei Zhao, Rita Ferreira, Joe Warmus, Sarah A. Nickolls, Sian Humphreys, Csilla C. Jorgensen
Publikováno v:
MedChemComm. 7:1564-1571
Iron is essential to life and is actively absorbed by enterocytes and secreted into plasma by the iron exporter ferroportin (SLC40A1). Dysregulation of iron homeostasis is a key component of many diseases such as hemochromatosis and beta-thalassemia.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::62781111e627aa7e2e4155be1c3e167b
https://doi.org/10.1039/c6md00260a
https://doi.org/10.1039/c6md00260a
Publikováno v:
The FASEB Journal. 29:1446-1455
Cannabinoids are reported to have actions through peroxisome proliferator-activated receptors (PPARs), which led us to investigate PPAR agonists for activity at the cannabinoid receptors. Radio-ligand binding and functional assays were conducted usin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d68b6dbee1ea570e62ec6f697c45a30e
https://doi.org/10.1096/fj.14-263053
https://doi.org/10.1096/fj.14-263053
Autor:
Gareth T. Young, Sarah J Nickolls, David C. Pryde, Cathryn Adams, Juha Kammonen, Clara Stead, Darren Cawkill, Adam R. Brown
Publikováno v:
Journal of biomolecular screening. 21(10)
Glycine receptor 3 (GlyRα3) is a ligand-gated ion channel of the cys-loop family that plays a key role in mediating inhibitory neurotransmission and regulation of pain signaling in the dorsal horn. Potentiation of GlyRα3 function is therefore of in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c78532857654f04af9f4a8a1deeaf00
https://pubmed.ncbi.nlm.nih.gov/27412533
https://pubmed.ncbi.nlm.nih.gov/27412533
Publikováno v:
SLAS Discovery. 16:706-716
The correct interpretation of data is fundamental to the study of G-protein-coupled receptor pharmacology. Often, new assay technologies are assimilated into the drug discovery environment without full consideration of the data generated. In this stu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31d53511c607a3c44cf6f108657832f5
https://doi.org/10.1177/1087057111406548
https://doi.org/10.1177/1087057111406548
Publikováno v:
European Journal of Pharmacology. 615:33-39
Melanocortin MC 3 and MC 4 receptor agonists have pharmaceutical benefit in the regulation of energy homeostasis. These agonists are defined by two parameters, their potency and their efficacy. However, these parameters are dependent upon the system
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a76753f17ac10cb6a6f38726ba9d8440
https://doi.org/10.1016/j.ejphar.2009.04.065
https://doi.org/10.1016/j.ejphar.2009.04.065