Zobrazeno 1 - 10
of 120
pro vyhledávání: '"Tom D. Heightman"'
Autor:
Emiliano Tamanini, Shin Miyamura, Ildiko M. Buck, Benjamin D. Cons, Lee Dawson, Charlotte East, Takashi Futamura, Shintaro Goto, Charlotte Griffiths-Jones, Tetsuya Hashimoto, Tom D. Heightman, Shunpei Ishikawa, Hideki Ito, Yosuke Kaneko, Tatsuya Kawato, Kazumi Kondo, Naoki Kurihara, James M. McCarthy, Yukiko Mori, Tsuyoshi Nagase, Yuichiro Nakaishi, Judith Reeks, Akimasa Sato, Patrick Schöpf, Kuninori Tai, Taichi Tamai, Dominic Tisi, Alison J.-A. Woolford
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1591-1597
Fragment-based ligand discovery was successfully applied to histone deacetylase HDAC2. In addition to the anticipated hydroxamic acid- and benzamide-based fragment screening hits, a low affinity (∼1 mM) α-amino-amide zinc binding fragment was iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a51f121f3406b6de752dce46b777833
https://doi.org/10.1021/acsmedchemlett.2c00272
https://doi.org/10.1021/acsmedchemlett.2c00272
Publikováno v:
ACS Central Science, Vol 2, Iss 12, Pp 927-934 (2016)
Externí odkaz:
https://doaj.org/article/d20016a3986646cdb7ded20fc04088a2
Autor:
Nicola G. Wallis, Alison J.-A. Woolford, Nicola E. Wilsher, Neil T. Thompson, Lukas Stanczuk, Alpesh D. Shah, Caroline J. Richardson, Sharna J. Rich, David C. Rees, Michael Reader, Marc O'Reilly, David Norton, Christopher W. Murray, Sandra Muench, Vanessa Martins, John F. Lyons, Justyna Kucia-Tran, Christopher J. Hindley, Tom D. Heightman, Roberta Ferraldeschi, Charlotte East, Aurélie Courtin, Juan Castro, Jessica L. Brothwood, Luke Bevan, Valerio Berdini, Joanne M. Munck
Supplementary tables 1-6 summarise the kinase panel screen data (1) mouse PK parameters (2) and further details of the anti-tumour activity (5) conferred by ASTX029, plus details of cell lines used in this study (3 and 4) and further details of the e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::45c83a97aa3dd2ed35fbdc9ef36e9bb5
https://doi.org/10.1158/1535-7163.22521489.v1
https://doi.org/10.1158/1535-7163.22521489.v1
Autor:
Nicola G. Wallis, Alison J.-A. Woolford, Nicola E. Wilsher, Neil T. Thompson, Lukas Stanczuk, Alpesh D. Shah, Caroline J. Richardson, Sharna J. Rich, David C. Rees, Michael Reader, Marc O'Reilly, David Norton, Christopher W. Murray, Sandra Muench, Vanessa Martins, John F. Lyons, Justyna Kucia-Tran, Christopher J. Hindley, Tom D. Heightman, Roberta Ferraldeschi, Charlotte East, Aurélie Courtin, Juan Castro, Jessica L. Brothwood, Luke Bevan, Valerio Berdini, Joanne M. Munck
Supplementary figures 1-7 show the effects of AST029 on ERK signalling in RAS-mutant cell lines (1) and tumour xenograft tissue (3), ASTX029 plasma PK linearity (2), ASTX029 activity in a cell line panel showing MAPK mutation status (4) the effects o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::185aef78c19fca4a606a8b2c178f1341
https://doi.org/10.1158/1535-7163.22521498.v1
https://doi.org/10.1158/1535-7163.22521498.v1
Autor:
Caroline Richardson, Zining Wu, Henriëtte M. G. Willems, William E. Wixted, Alison Jo-Anne Woolford, Charlotte Mary Griffiths-Jones, Yolanda Sanchez, David Norton, Jeffrey K. Kerns, T.G. Davies, William G. Bonnette, Sharna J. Rich, James F. Callahan, Hong Nie, Lawrence Wolfe, Maria Grazia Carr, Marcel L. Verdonk, William L. Rumsey, Tom D. Heightman
Publikováno v:
Journal of Medicinal Chemistry. 64:15949-15972
The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this pathway as therapeutics for diseases involving chronic oxidative stress. The protein KEAP1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba196f8cf42319174247f8aba6d5c760
https://doi.org/10.1021/acs.jmedchem.1c01351
https://doi.org/10.1021/acs.jmedchem.1c01351
Autor:
Jeffrey W. Johannes, Fiona Pachl, Amber Balazs, Tieguang Yao, C. Larner, Lisa McWilliams, Marianne Schimpl, Scott W. Martin, Kevin J. Embrey, Tom D. Heightman, Paul Hemsley, Jonathan P. Orme, Derek Barratt, Giuditta Illuzzi, Andrew Madin, Paolo Di Fruscia, Avipsa Ghosh, Martin J. Packer, Scott D. Edmondson, Elisabetta Leo, Xiaolan Zheng, Matthew D. Chuba, Xiaohui Pei, Mark J. O'Connor, Verity Talbot, Ke Zhang, Stephen Fawell, Elizabeth Underwood, Anna Staniszewska, Lina Liu, Lin Xue, Sonja J. Gill, Anders Gunnarsson, Andrew Pike, Susan E. Critchlow, Jeffrey G. Varnes, Andrew X. Zhang, Sébastien L. Degorce, J. Lane, Sudhir M. Hande, Hongyao She, Sabina Cosulich, Michal Bista
Publikováno v:
Journal of Medicinal Chemistry. 64:14498-14512
Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA mutation. However, some have failed in combination with first-line chemotherapies, usually
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6d5da59f02fe0bf1798c2492422c31c3
https://doi.org/10.1021/acs.jmedchem.1c01012
https://doi.org/10.1021/acs.jmedchem.1c01012
Autor:
Neil T. Thompson, Nicola G. Wallis, Michael Reader, Christopher J. Hindley, Juan Castro, John Lyons, David C. Rees, Nicola E. Wilsher, Caroline Richardson, Tom D. Heightman, Lukas Stanczuk, Alpesh Shah, Sharna J. Rich, Charlotte East, Valerio Berdini, Marc O'Reilly, Justyna Kucia-Tran, Jessica L. Brothwood, Joanne M. Munck, Alison Jo-Anne Woolford, Sandra Muench, Christopher William Murray, David Norton, Luke Bevan, Aurélie Courtin, Roberta Ferraldeschi, Vanessa Martins
Publikováno v:
Molecular Cancer Therapeutics. 20:1757-1768
The MAPK signaling pathway is commonly upregulated in human cancers. As the primary downstream effector of the MAPK pathway, ERK is an attractive therapeutic target for the treatment of MAPK-activated cancers and for overcoming resistance to upstream
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6856599564530823950e091fd6e69a67
https://doi.org/10.1158/1535-7163.mct-20-0909
https://doi.org/10.1158/1535-7163.mct-20-0909
Autor:
Christopher William Murray, David C. Rees, Richard J. Hall, Jeffrey D. St. Denis, Tom D. Heightman
Publikováno v:
RSC Medicinal Chemistry
This Review describes the increasing demand for organic synthesis to facilitate fragment-based drug discovery (FBDD), focusing on polar, unprotected fragments. In FBDD, X-ray crystal structures are used to design target molecules for synthesis with n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18f66aee7eaec74f4b73592ae0e30c31
http://europepmc.org/articles/PMC8130625
http://europepmc.org/articles/PMC8130625
Autor:
Michael Reader, Aurélie Courtin, Steven Howard, Nicola G. Wallis, Jonathan Shannon, Hugh Walton, Christopher William Murray, Joseph E. Coyle, Joanne M. Munck, Alison Jo-Anne Woolford, Torren M. Peakman, David C. Rees, James Edward Harvey Day, Charlotte Mary Griffiths-Jones, Marc O'Reilly, Alpesh Shah, David Norton, Valerio Berdini, Lynsey Fazal, Maria Grazia Carr, Charlotte East, Tom D. Heightman, Nicola E. Wilsher, Ildiko Maria Buck, Luke Bevan, Stuart Thomas Onions, Michael Cooke, Justyna Kucia-Tran, Sandra Muench, Nick Palmer, Sharna J. Rich, Vanessa Martins, David Cousin, Puja Pathuri, John P. Watts
Publikováno v:
Journal of medicinal chemistry. 64(16)
Aberrant activation of the mitogen-activated protein kinase pathway frequently drives tumor growth, and the ERK1/2 kinases are positioned at a key node in this pathway, making them important targets for therapeutic intervention. Recently, a number of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62d0e8543148c5c72af0eca510047c9f
https://pubmed.ncbi.nlm.nih.gov/34387469
https://pubmed.ncbi.nlm.nih.gov/34387469
Publikováno v:
Chemical Science. 10:2264-2271
In fragment-based drug discovery (FBDD), a weakly binding fragment hit is elaborated into a potent ligand by bespoke functionalization along specific directions (growth vectors) from the fragment core in order to complement the 3D structure of the ta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::12ab8b78a1fc587ba05e2d9ffb9dddcd
https://doi.org/10.1039/c8sc04789h
https://doi.org/10.1039/c8sc04789h