Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Perla Breccia"'
Autor:
Natsuko Macabuag, William Esmieu, Perla Breccia, Rebecca Jarvis, Wesley Blackaby, Ovadia Lazari, Liudvikas Urbonas, Maria Eznarriaga, Rachel Williams, Annelieke Strijbosch, Rhea Van de Bospoort, Kim Matthews, Cole Clissold, Tammy Ladduwahetty, Huw Vater, Patrick Heaphy, Douglas G. Stafford, Hong-Jun Wang, John E. Mangette, George McAllister, Vahri Beaumont, Thomas F. Vogt, Hilary A. Wilkinson, Elizabeth M. Doherty, Celia Dominguez
Publikováno v:
Journal of medicinal chemistry. 65(18)
Huntington's disease (HD) is a lethal autosomal dominant neurodegenerative disorder resulting from a CAG repeat expansion in the huntingtin (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf9b7293f23145d9276a05495bc08822
https://pubmed.ncbi.nlm.nih.gov/36098485
https://pubmed.ncbi.nlm.nih.gov/36098485
Autor:
Daniel Todd, Marta Stebbeds, Emma Thatcher, Amy Barnard, Jeremy Anton, Arnold Sienerth, Mijke Visser, Philip Mitchell, Perla Breccia, David Smith, George McAllister, Tasir Haque, Longbin Liu, Celia Dominguez, Ignacio Munoz-Sanjuan
Publikováno v:
I: Experimental therapeutics – preclinical.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0e4521dee279338bd3e3376a4e41e41c
https://doi.org/10.1136/jnnp-2022-ehdn.235
https://doi.org/10.1136/jnnp-2022-ehdn.235
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:
Celia Dominguez, Rebecca E. Jarvis, Stephen D. Penrose, Perla Breccia, Alan Findlay Haughan, Andrew J. Stott, Roland Bürli
Publikováno v:
Organic Letters. 17:1401-1404
Synthesis of (S)-2-methyl-3-fluorophenyl cyclopentanone methyl ester (1S)-1 has been achieved by both inter- and intramolecular alkylation reactions on multigram scale, using chiral pool reagents. The intramolecular variant is a novel example of a ch
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8474ef1a1e4dde479275df9d082b1f8e
https://doi.org/10.1021/acs.orglett.5b00207
https://doi.org/10.1021/acs.orglett.5b00207
Autor:
Giovanni Auricchio, Alessandra Topai, Angelo Martino, Vittorio Colizzi, Ilaria Cerbara, Francesca Angeli, Perla Breccia, Fabrizio Poccia
Publikováno v:
Journal of Medicinal Chemistry. 52:3716-3722
The Vgamma9 Vdelta2 T cells mediate rapid, innate-like immune responses to pathogens and are important in several key immunoregulatory pathways, including those involved in infections and tumor development. Vgamma9 Vdelta2 T cells respond to low mole
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c93ad6bb2e633821284954454f214e4a
https://doi.org/10.1021/jm900054u
https://doi.org/10.1021/jm900054u
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:
Loïc René, Ruth Pérez-Fernández, Pilar Prados, Michiel Luc Maria Van Gool, Michèle Reboud-Ravaux, Bernard Badet, Masayuki Takahashi, Javier de Mendoza, Perla Breccia, Nicole Boggetto
Publikováno v:
Journal of Medicinal Chemistry. 46:5196-5207
Original inhibitors of HIV-1 protease based on a chiral bicyclic guanidinium scaffold linked to short peptidic mimics of the terminal protease sequences and to a lipophilic group were designed. These inhibitors prevent dimerization of the native prot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c38d810154441325d3b6ca83cb954ed
https://doi.org/10.1021/jm030871u
https://doi.org/10.1021/jm030871u