Zobrazeno 1 - 10
of 173
pro vyhledávání: '"Christian C, Felder"'
Autor:
Wessel A. C. Burger, Vi Pham, Ziva Vuckovic, Alexander S. Powers, Jesse I. Mobbs, Yianni Laloudakis, Alisa Glukhova, Denise Wootten, Andrew B. Tobin, Patrick M. Sexton, Steven M. Paul, Christian C. Felder, Radostin Danev, Ron O. Dror, Arthur Christopoulos, Celine Valant, David M. Thal
Publikováno v:
Nature Communications, Vol 14, Iss 1, Pp 1-11 (2023)
Abstract The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of high therapeutic interest due to its expression in regions of the brain involved in the regulation of psychosis, cognition, and addiction. The mAChR agonist,
Externí odkaz:
https://doaj.org/article/7484d1906038449ebf83ab0a1980953a
Autor:
Scott A. Hollingsworth, Brendan Kelly, Celine Valant, Jordan Arthur Michaelis, Olivia Mastromihalis, Geoff Thompson, A. J. Venkatakrishnan, Samuel Hertig, Peter J. Scammells, Patrick M. Sexton, Christian C. Felder, Arthur Christopoulos, Ron O. Dror
Publikováno v:
Nature Communications, Vol 10, Iss 1, Pp 1-9 (2019)
Allosteric GPCR modulators can achieve exquisite subtype selectivity, but the underlying mechanism is unclear. Using molecular dynamics simulations, the authors here identify a previously undetected dynamic pocket in muscarinic GPCRs that is critical
Externí odkaz:
https://doaj.org/article/a0e90ef319f249dd8f9b3fd6b23a0233
Publikováno v:
Trends in Pharmacological Sciences. 43:1098-1112
Modern interest in muscarinic acetylcholine receptor (mAChR) activators for schizophrenia began in the 1990s when xanomeline, an M
Autor:
Jurgen Wess, Celine Valant, Andrew B. Tobin, David Thal, Roy D. Schwarz, Neil M. Nathanson, Ernst Mutschler, Fred Mitchelson, Chris Langmead, Günter Lambrecht, Heinz J. Kilbinger, Rudolf Hammer, Christian C. Felder, Frederick Ehlert, Richard M. Eglen, Arthur Christopoulos, R.A. John Challiss, Noel J. Buckley, David A. Brown, Sophie Bradley, Nigel J. M. Birdsall
Publikováno v:
IUPHAR/BPS Guide to Pharmacology CITE. 2023
Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [53]) are activated by the endogenous agonist acetylcholine. All five (M1-M5) mAChRs are ubiquitously expressed in
Autor:
Ruth A. Ross, Roger G. Pertwee, Raphael Mechoulam, Ken Mackie, George Kunos, Allyn C. Howlett, Miles Herkenham, Peter Greasley, Christian C. Felder, Maurice R. Elphick, Vincenzo Di Marzo, William A. Devane, Ben F. Cravatt, Pierre Casellas, Guy Cabral, Heather Bradshaw, Tom I. Bonner, Francis Barth, Stephen P.H. Alexander, Mary Abood
Publikováno v:
IUPHAR/BPS Guide to Pharmacology CITE. 2023
Cannabinoid receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Cannabinoid Receptors [119]) are activated by endogenous ligands that include N-arachidonoylethanolamine (anandamide), N-homo-γ-linolenoylethanolamine, N-docosatetra-7,10
Autor:
Jack K. McDonald, Emma T. van der Westhuizen, Vi Pham, Geoff Thompson, Christian C. Felder, Steven M. Paul, David M. Thal, Arthur Christopoulos, Celine Valant
Publikováno v:
ACS Chemical Neuroscience. 13:1206-1218
Autor:
Alexander S. Powers, Vi Pham, Wessel A. C. Burger, Geoff Thompson, Yianni Laloudakis, Nicholas W. Barnes, Patrick M. Sexton, Steven M. Paul, Arthur Christopoulos, David M. Thal, Christian C. Felder, Celine Valant, Ron O. Dror
Publikováno v:
Nature Chemical Biology.
A drug’s selectivity for target receptors is essential to its therapeutic utility, but achieving selectivity between similar receptors is challenging. The serendipitous discovery of ligands that stimulate target receptors more strongly than closely
Publikováno v:
PLoS ONE, Vol 12, Iss 12, p e0188330 (2017)
Rodent genomic alignment sequences support a 2-exon model for muscarinic M4 receptor. Using this model a novel N-terminal extension was discovered in the human muscarinic acetylcholine M4 receptor. An open reading frame was discovered in the human, m
Externí odkaz:
https://doaj.org/article/1a80c16f89fc47e6acd5288c98a23616
Publikováno v:
The American journal of psychiatry. 179(9)
Schizophrenia remains a challenging disease to treat effectively with current antipsychotic medications due to their limited efficacy across the entire spectrum of core symptoms as well as their often burdensome side-effect profiles and poor tolerabi
Autor:
Alexander S. Powers, Vi Pham, Wessel A. C. Burger, Geoff Thompson, Yianni Laloudakis, Nicholas W. Barnes, Patrick M. Sexton, Steven M. Paul, Arthur Christopoulos, David M. Thal, Christian C. Felder, Celine Valant, Ron O. Dror
Publikováno v:
Nature Chemical Biology. 19:529-529