Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Máire A. Convery"'
Autor:
Giovanna Bergamini, Stefano Livia, Kenneth David Down, Marcus Bantscheff, Nick Barton, Friedrich B M Reinhard, Paola Grandi, Daniel Thomas, David N. Mallett, Paul Martin Gore, Sophie M. Bertrand, Z.A. Henley, Edith M. Hessel, James E. Rowedder, Mark Price, J. Nicole Hamblin, Birgit Dümpelfeld, Augustin Amour, Steve Keeling, Christina Rau, Máire A. Convery, Chris D. Edwards, Jonathan A. Taylor, Paul Rowland, Aoife C. Maxwell
Publikováno v:
Journal of Medicinal Chemistry. 63:638-655
Optimization of a lead series of PI3Kδ inhibitors based on a dihydroisobenzofuran core led to the identification of potent, orally bioavailable compound 19. Selectivity profiling of compound 19 showed similar potency for class III PI3K, Vps34, and P
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee509ec4ce8051c7f53718e7e95b2637
https://doi.org/10.1021/acs.jmedchem.9b01585
https://doi.org/10.1021/acs.jmedchem.9b01585
Autor:
Sebastien Andre Campos, Sorif Uddin, Daniel Thomas, Paul Rowland, Birgit Duempelfeld, Douglas W. Thomson, Andrew Sharpe, James E. Rowedder, Kenneth David Down, Máire A. Convery, Augustin Amour, Michael Daniel Goldsmith, Grant A. McGonagle, David N. Mallett, Edith M. Hessel, Jana Krause, Kevin James Doyle, J. Nicole Hamblin, Srividya Sriskantharajah, Edward P. Cannons, Vipulkumar Kantibhai Patel, Chris D. Edwards, Cole Clissold, Nick Barton, Anderson Niall Andrew, John J. Coward
Publikováno v:
Journal of medicinal chemistry. 64(18)
Optimization of a previously reported lead series of PI3Kδ inhibitors with a novel binding mode led to the identification of a clinical candidate compound 31 (GSK251). Removal of an embedded Ames-positive heteroaromatic amine by reversing a sulfonam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acd30d2dabfe0764f96af2bbb1bd2724
https://pubmed.ncbi.nlm.nih.gov/34510892
https://pubmed.ncbi.nlm.nih.gov/34510892
Autor:
Simon Peace, Gianpaolo Bravi, Máire A. Convery, Hannah Davies, Graham G. A. Inglis, Joanna M. Redmond, Sandeep Pal, Heather Hobbs, Declan Summers, Ian B. Campbell
Publikováno v:
Journal of Medicinal Chemistry. 62:6972-6984
4-(Pyrimidin-4-yl)morpholines are privileged pharmacophores for PI3K and PIKKs inhibition by virtue of the morpholine oxygen, both forming the key hydrogen bonding interaction and conveying selectivity over the broader kinome. Key to the morpholine u
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2748d65fb9fe5910b1e6ccf3827644ab
https://doi.org/10.1021/acs.jmedchem.9b00348
https://doi.org/10.1021/acs.jmedchem.9b00348
Autor:
Pamela A. Haile, Linda N. Casillas, Bartholomew J. Votta, Gren Z. Wang, Adam K. Charnley, Xiaoyang Dong, Michael J. Bury, Joseph J. Romano, John F. Mehlmann, Bryan W. King, Karl F. Erhard, Charles R. Hanning, David B. Lipshutz, Biva M. Desai, Carol A. Capriotti, Michelle C. Schaeffer, Scott B. Berger, Mukesh K. Mahajan, Michael A. Reilly, Rakesh Nagilla, Elizabeth J. Rivera, Helen H. Sun, John K. Kenna, Allison M. Beal, Michael T. Ouellette, Mike Kelly, Gillian Stemp, Máire A. Convery, Anna Vossenkämper, Thomas T. MacDonald, Peter J. Gough, John Bertin, Robert W. Marquis
Publikováno v:
Journal of Medicinal Chemistry. 62:6482-6494
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::eaccf9e5808f38c133e85649c11ad3f1
https://doi.org/10.1021/acs.jmedchem.9b00575
https://doi.org/10.1021/acs.jmedchem.9b00575
Autor:
Máire A. Convery, Daniel Thomas, Chris D. Edwards, Craig Jamieson, James E. Rowedder, Ian Robert Baldwin, David N. Mallett, Chun-wa Chung, Charlotte J. Hardy, Nick Barton, Jonathan A. Spencer, Paul Rowland
Publikováno v:
ACS Med Chem Lett
[Image: see text] A macrocyclization approach has been explored on a series of benzoxazine phosphoinositide 3-kinase δ inhibitors, resulting in compounds with improved potency, permeability, and in vivo clearance while maintaining good solubility. T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9dbc1735d34e567458cec0c9c2f06956
https://pubmed.ncbi.nlm.nih.gov/32676144
https://pubmed.ncbi.nlm.nih.gov/32676144
Autor:
Peter C. Ray, Margaret Huggett, Robert H. Bates, Paco De Dios Anton, Daniel A. Fletcher, Chun-wa Chung, Alfonso Mendoza-Losana, Simon Green, Jingkun Zeng, Fabio Zuccotto, David Barros, Lourdes Encinas, Paul G. Wyatt, Claire J. MacKenzie, Raquel Fernandez-Menendez, Máire A. Convery, Federica Prati
Publikováno v:
Chemmedchem
'ChemMedChem ', vol: 13, pages: 672-677 (2018)
'ChemMedChem ', vol: 13, pages: 672-677 (2018)
Our findings reported herein provide support for the benefits of including functional group complexity (FGC) within fragments when screening against protein targets such as Mycobacterium tuberculosis InhA. We show that InhA fragment actives with FGC
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb7bb532b4852aa902492b02c72ca407
http://europepmc.org/articles/PMC5915743
http://europepmc.org/articles/PMC5915743
Autor:
Angela Bridges, Sandrine Jayne, Jennifer Schofield, Ana Sousa Manso, Duncan S. Holmes, Xi-Ping Zhang, Larissa Lezina, Michael T. McCabe, Mark James Bamford, Anastasia Wyce, David Jonathan Hirst, Máire A. Convery, Tom Slocombe, Andrew C. Pearce, Don O. Somers, Simon D. Wagner, Paul Scott-Stevens, Ann Louise Walker, Jonathan P. Hutchinson, Constantinos Demetriou, Cassie Messenger, Melissa C. Musso, Sian Evans, Ruth C. Barber, Joanne Morley, Thomas Gobbetti
Publikováno v:
The Journal of Biological Chemistry
B-cell lymphoma 6 (BCL6) is a zinc finger transcriptional repressor possessing a BTB–POZ (BR-C, ttk, and bab for BTB; pox virus and zinc finger for POZ) domain, which is required for homodimerization and association with corepressors. BCL6 has mult
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74c7e6fdf77eb69b9270c5b0a66260fc
https://doi.org/10.1016/j.jbc.2021.100928
https://doi.org/10.1016/j.jbc.2021.100928
Autor:
Arthur Shu, Yiqian Lian, Huijie Li, Curt Dale Haffner, Terry Vincent Hughes, Ami S. Lakdawala, Julie A. Cox, Pamela A. Haile, Constantine Kreatsoulas, Beth Anne Knapp-Reed, Lisa M. Shewchuk, David B. Lipshutz, John F. Mehlmann, Michael T. Ouellette, Christopher J Aquino, Mark Elban, Nicole Cathleen Goodwin, Huiqiang Zhou, Adam Kenneth Charnley, Bartholomew J. Votta, Robert W. Marquis, Joseph J. Romano, Linda N. Casillas, Peter J. Gough, Máire A. Convery, John Bertin
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we report the discovery of pyrazolocarboxamides as novel, potent, and kinase selective inhibitors of receptor interacting protein 2 kinase (RIP2). Fragment based screening and design principles led to the identification of th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdf5d01bc977b3b388a3da2de569f9a2
https://pubmed.ncbi.nlm.nih.gov/31749904
https://pubmed.ncbi.nlm.nih.gov/31749904
Autor:
Paul Rowland, Anthony William James Cooper, Kenneth David Down, Nick Barton, James E. Rowedder, Máire A. Convery, Natalie Wellaway, J. Nicole Hamblin, Jonathan A. Taylor, Simon Peace, Graham G. A. Inglis
Publikováno v:
Journal of medicinal chemistry. 61(24)
A deconstruction of previously reported phosphoinositide 3-kinase δ (PI3Kδ) inhibitors and subsequent regrowth led to the identification of a privileged fragment for PI3Kδ, which was exploited to deliver a potent, efficient, and selective lead ser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95aea5a963251f6352a1e3b6f72ebca0
https://pubmed.ncbi.nlm.nih.gov/30532965
https://pubmed.ncbi.nlm.nih.gov/30532965
Autor:
Catherine E. Peishoff, Donald O. Somers, Heather A. Carlson, Aqeel Ahmed, Michael Kranz, Kelly L. Damm-Ganamet, Richard D. Smith, Jeanne A. Stuckey, James B. Dunbar, Guanglei Cui, Millard H. Lambert, Patricia A. Elkins, Máire A. Convery
Publikováno v:
Journal of Chemical Information and Modeling. 56:1063-1077
The 2014 CSAR Benchmark Exercise was the last community-wide exercise that was conducted by the group at the University of Michigan, Ann Arbor. For this event, GlaxoSmithKline (GSK) donated unpublished crystal structures and affinity data from in-hou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::425d373351999c72a51aef450c547183
https://doi.org/10.1021/acs.jcim.5b00523
https://doi.org/10.1021/acs.jcim.5b00523