Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Kim L. Matthews"'
Autor:
Nicola L. Brice, Mark Carlton, David H. Margolin, Martin Bexon, Kim L. Matthews, Lee A. Dawson, Aaron L. Ellenbogen, C. Warren Olanow, Jordan Dubow, Karl Kieburtz
Publikováno v:
EClinicalMedicine, Vol 77, Iss , Pp 102882- (2024)
Summary: Background: CVN424 is a GPR6 inverse agonist that provides selective pharmacological control of the indirect striatopallidal pathway. We assessed the safety and efficacy of CVN424 as an adjunctive treatment to levodopa for reducing OFF-time
Externí odkaz:
https://doaj.org/article/03ffbbb6c9d240da9bd6c36037040312
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 381(1)
CVN424 is a novel small molecule and first-in-class candidate therapeutic to selectively modulate GPR6, an orphan G-protein coupled receptor. Expression of GPR6 is largely confined to the subset of striatal projection neurons that give rise to the in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b715384157c158490578340a3b61b97
https://pubmed.ncbi.nlm.nih.gov/35110393
https://pubmed.ncbi.nlm.nih.gov/35110393
Autor:
Sarah L. Martin, Dawn Yates, Grant Wishart, Ignacio Munoz-Sanjuan, Wesley Blackaby, Ovadia Lazari, Roger Cachope, Amanda Van de Poël, Leticia Toledo-Sherman, Esmieu William R K, Ivan Angulo-Herrera, Celia Dominguez, Rebecca E. Jarvis, Helen C. Cox, Amy Barnard, Graham Jones, Marcus Peacock, Sung-Wook Jang, Perla Breccia, Jennifer R. Bate, Cole Clissold, Philip Leonard, Maria Eznarriaga, Marieke Lamers, Mark Rose, George McAllister, Kim L. Matthews, Huw D. Vater
Publikováno v:
Journal of medicinal chemistry. 64(8)
Our group has recently shown that brain-penetrant ataxia telangiectasia-mutated (ATM) kinase inhibitors may have potential as novel therapeutics for the treatment of Huntington's disease (HD). However, the previously described pyranone-thioxanthenes
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f36cf11e03a84484aef8a9c43f147a9d
https://pubmed.ncbi.nlm.nih.gov/33783225
https://pubmed.ncbi.nlm.nih.gov/33783225
Autor:
Elizabeth Anne Saville-Stones, Alexander H. Borchers, David Allcock, Wesley Blackaby, Gillian Creighton-Gutteridge, Andrew J. Stott, Ignacio Munoz-Sanjuan, Julie Vann, Rebecca E. Jarvis, Dawn Yates, Celia Dominguez, Amanda Van de Poël, Vahri Beaumont, Michel Maillard, Scott Pollack, Rachel Williams, Christopher A. Luckhurst, Huw D. Vater, Omar Aziz, Alan Findlay Haughan, George McAllister, Kim L. Matthews, Perla Breccia
Publikováno v:
ACS Med Chem Lett
[Image: see text] Using an iterative structure–activity relationship driven approach, we identified a CNS-penetrant 5-(trifluoromethyl)-1,2,4-oxadiazole (TFMO, 12) with a pharmacokinetic profile suitable for probing class IIa histone deacetylase (H
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c008b16bb33ecffe8334e99c8e43a03d
https://pubmed.ncbi.nlm.nih.gov/33738065
https://pubmed.ncbi.nlm.nih.gov/33738065
Autor:
Marieke Lamers, Grant Wishart, Karen Barnes, Graham D. Smith, Ivan Angulo-Herrera, Sarah L. Martin, Rebecca E. Jarvis, Wesley Blackaby, Philip Leonard, Ovadia Lazari, Leticia Toledo-Sherman, David F. Fischer, Maria Eznarriaga, Simon J. Dowler, George McAllister, Rhea van de Bospoort, Dawn Yates, Annelieke Strijbosch, Helen C. Cox, Jennifer R. Bate, Esmieu William R K, Amanda Van de Poël, Roger Cachope, Sung-Wook Jang, Perla Breccia, Celia Dominguez, Mark Rose, Kim L. Matthews, Huw D. Vater, Stephen D. Penrose, Ignacio Munoz-Sanjuan
Publikováno v:
Journal of medicinal chemistry. 62(6)
Genetic and pharmacological evidence indicates that the reduction of ataxia telangiectasia-mutated (ATM) kinase activity can ameliorate mutant huntingtin (mHTT) toxicity in cellular and animal models of Huntington's disease (HD), suggesting that sele
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a89407c2d2edecea9555cc23f334e43
https://pubmed.ncbi.nlm.nih.gov/30840447
https://pubmed.ncbi.nlm.nih.gov/30840447
Autor:
Christopher A. Luckhurst, Omar Aziz, Vahri Beaumont, Roland W. Bürli, Perla Breccia, Michel C. Maillard, Alan F. Haughan, Marieke Lamers, Phil Leonard, Kim L. Matthews, Gilles Raphy, Andrew J. Stott, Ignacio Munoz-Sanjuan, Beth Thomas, Michael Wall, Grant Wishart, Dawn Yates, Celia Dominguez
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(1)
We have identified a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor 22, with500-fold selectivity over class I HDACs (1,2,3) and ∼150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform. Dose escalati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afc52289ed1bc17170b0a3a38854cb42
https://pubmed.ncbi.nlm.nih.gov/30463802
https://pubmed.ncbi.nlm.nih.gov/30463802
Autor:
Marieke Lamers, Jiffry Ismail, Kevin F. McGee, John Wityak, Gwen Wang, Jonathan Bard, Leticia Toledo-Sherman, Michele Luche, Mei Bai, Michael Conlon, W. Brent Clayton, Michael A. Lynch, Celia Dominguez, James C. Haber, Dawn Yates, Ryan Newell, Pat Wheelan, Ren Hua Song, Susan Deupree, Tania Mead, Macarena Irigoyen, Ignacio Munoz-Sanjuan, Douglas B. Kitchen, Emily Freeman, Kim L. Matthews, Jeff Webster, Bryan Cordell Duffy, IokTeng D. Kuok, Peter C. Michels, Alex S. Kiselyov, Steve Clifton, Lynette Ongeri, David D. Manning, Maria Beconi, Kathy Lyons, Yuri L. Khmelnitsky, Philip Leonard, Claire Wilson, Monica Hultman
Publikováno v:
Journal of Medicinal Chemistry. 58:2967-2987
Through medicinal chemistry lead optimization studies focused on calculated properties and guided by X-ray crystallography and computational modeling, potent pan-JNK inhibitors were identified that showed submicromolar activity in a cellular assay. U
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9dc502c0699e7153c7e8c0b037ee2fc1
https://doi.org/10.1021/jm5013598
https://doi.org/10.1021/jm5013598
Autor:
Dawn Yates, Michael Prime, Dirk Winkler, Kathryn Lyons, Maria Beconi, Leticia Toledo-Sherman, Daryl Simon Walter, Ignacio Munoz-Sanjuan, Steve Clifton, Celia Dominguez, Tania Mead, Catherine M. O'Connell, Kim L. Matthews
Publikováno v:
Drug Metabolism and Disposition. 40:2297-2306
Understanding whether regulation of tryptophan metabolites can ameliorate neurodegeneration is of high interest to investigators. A recent publication describes 3,4-dimethoxy-N-(4-(3-nitrophenyl)-5-(piperidin-1-ylmethyl)thiazol-2-yl)benzenesulfonamid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb46eb8292b21042ac77f7109f8e9241
https://doi.org/10.1124/dmd.112.046532
https://doi.org/10.1124/dmd.112.046532
Autor:
Celia Dominguez, Marieke Lamers, Samantha J. Hughes, Rebecca E. Jarvis, Grant Wishart, Helen L. Birch, Roland Bürli, Omar Aziz, Scott Pollack, Dawn Yates, Perla Breccia, Christopher A. Luckhurst, Philip Leonard, Andrew J. Stott, George McAllister, Kim L. Matthews, Elizabeth Anne Saville-Stones
Potent and selective class IIa HDAC tetrasubstituted cyclopropane hydroxamic acid inhibitors were identified with high oral bioavailability that exhibited good brain and muscle exposure. Compound 14 displayed suitable properties for assessment of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2917976f54e5700b574a852afba864e3
https://europepmc.org/articles/PMC4716601/
https://europepmc.org/articles/PMC4716601/
Autor:
Alison I. Muir, Izzy Boyfield, Kalindi Vaidya, Barry Sidney Orlek, Etienne Fleury, David G. Evans, Jackie S. Scott, Hindy Mok, Victoria J. Bolton, Ward John Gerard, Geoffrey Stemp, Tom D. Heightman, Kim L. Matthews, Kirk Lawless, Gareth J. Sanger, Fiona McKay, Alexander J. Stevens, Emma M. Jarvie, James Matthew Bailey, Susan Marie Westaway, Mervyn Thompson, Jonathan B. Basilla
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6452-6458
Optimisation of a series of benzazepine sulfonamide hit compounds identified from high throughput screening led to the discovery of a new series of tractable, potent motilin receptor agonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2f11cdd038a55294786dd33de3ee625
https://doi.org/10.1016/j.bmcl.2009.09.027
https://doi.org/10.1016/j.bmcl.2009.09.027