Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Marcel J. de Groot"'
Autor:
Mark D. Andrews, Kevin N. Dack, Marcel J. de Groot, Maja Lambert, Carl J. Sennbro, Mogens Larsen, Martin Stahlhut
Publikováno v:
Journal of Medicinal Chemistry. 65:8828-8842
Interleukin 17A (IL-17A) is an interleukin cytokine whose dysregulation is implicated in autoimmune disorders such as psoriasis, and monoclonal antibodies against the IL-17A pathway are now well-established and very effective treatments. This article
Publikováno v:
The Medicinal Chemist's Guide to Solving ADMET Challenges ISBN: 9781788012270
The cytochrome P450s (CYPs) comprise a superfamily of haem-containing proteins that are predominantly expressed in the liver and catalyse the metabolism of a broad range of exogenous and endogenous molecules. The inhibition of P450-mediated drug meta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e81b638250ca72080247fe0db5c7e915
https://doi.org/10.1039/9781788016414-00220
https://doi.org/10.1039/9781788016414-00220
Publikováno v:
MedChemComm. 7:813-819
Herein, we describe the discovery of a novel binding pocket for CYP 2C9 inhibitors. Trifluoromethanesulfonamide compounds 1 and 2, identified within a Pfizer progesterone receptor antagonist program, were found to strongly inhibit the drug metabolizi
Autor:
Bruce M. Bechle, Stephen Martin Denton, Sebastien Galan, David James Rawson, Marcel J. de Groot, Brian E. Marron, Matthew S Johnson, Jo Hannam, Shoko Nakagawa, Dave Batchelor, Nigel Alan Swain, Steven M Reister, David Ellis, Mark L. Chapman, David Printzenhoff, Sarah J Ransley, Beaudoin Serge, David S. Millan, Christopher W. West, Kenneth John Butcher, R. Ian Storer, Stephen M Gaulier, Stupple Paul Anthony, Andrew Pike, Alan Daniel Brown, Christopher John Markworth, Bruce Brown, Zhixin Lin, Sasaki Kosuke, Paul A. Bradley, Ian Gurrell, Richard P. Butt, Mel Glossop, Ben S. Greener
Publikováno v:
Journal of medicinal chemistry. 60(16)
A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cyto
Autor:
Marcel J. de Groot, Karen Maubach, Neil Victor Harris, Kenneth Lyle Clark, Andrea Taylor, Peter Lockey, Christopher Higgs, Amanda J. Woodrooffe, R.A. Coleman, Richard Jon Davis, Jon Sutton, David E. Clark
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2212-2221
In this Letter, we present the results of a hit-finding and lead optimization programme against the EP4 receptor (EP4R). In a short time period, we were able to discover five structurally diverse series of hit compounds using a combination of virtual
Autor:
Richard Lonsdale, Jeremy N. Harvey, Adrian J. Mulholland, Kerensa T Houghton, Christine M. Bathelt, Jolanta Żurek, Marcel J. de Groot, Nicolas Foloppe
Publikováno v:
Journal of the American Chemical Society
Cytochrome P450 enzymes (P450s) are important in drug metabolism and have been linked to adverse drug reactions. P450s display broad substrate reactivity, and prediction of metabolites is complex. QM/MM studies of P450 reactivity have provided insigh
Publikováno v:
Channels. 5:201-204
The transient receptor potential channel TRPV1 is a polymodal nociceptor. It is primarily expressed in dorsal root ganglia and peripheral sensory nerve endings, and to a much lesser extent, in the central nervous system. It has also been implicated i
Autor:
Marcel J. de Groot, Steve England
Publikováno v:
British Journal of Pharmacology. 158:1413-1425
Voltage-gated sodium channels are key to the initiation and propagation of action potentials in electrically excitable cells. Molecular characterization has shown there to be nine functional members of the family, with a high degree of sequence homol
Publikováno v:
Drug Discovery Today. 14:964-972
Owing to the polymorphic nature of CYP2D6, clinically significant issues can arise when drugs rely on that enzyme either for clearance, or metabolism to an active metabolite. Available screening methods to determine if the compound is likely to cause
Autor:
Marcel J. De Groot, David H. Singleton, Nora K. Wallace, Jill Steidl-Nichols, Matt Deacon, David O. Nettleton, Christine Williams, Helen Boyd, David Price, James G. Boyd, Matthew D. Troutman
Publikováno v:
Journal of Medicinal Chemistry. 50:2931-2941
Novel fluorescent derivatives of dofetilide (1) have been synthesized. Analogues that feature a fluorescent probe attached through an aliphatic spacer to the central tertiary nitrogen of 1 have high affinity for the hERG channel, and affinity is depe