Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Nichola L, Davies"'
Autor:
Jason G. Kettle, Sharan K. Bagal, Sue Bickerton, Michael S. Bodnarchuk, Scott Boyd, Jason Breed, Rodrigo J. Carbajo, Doyle J. Cassar, Atanu Chakraborty, Sabina Cosulich, Iain Cumming, Michael Davies, Nichola L. Davies, Andrew Eatherton, Laura Evans, Lyman Feron, Shaun Fillery, Emma S. Gleave, Frederick W. Goldberg, Lyndsey Hanson, Stephanie Harlfinger, Martin Howard, Rachel Howells, Anne Jackson, Paul Kemmitt, Gillian Lamont, Scott Lamont, Hilary J. Lewis, Libin Liu, Michael J. Niedbala, Christopher Phillips, Radek Polanski, Piotr Raubo, Graeme Robb, David M. Robinson, Sarah Ross, Matthew G. Sanders, Michael Tonge, Rebecca Whiteley, Stephen Wilkinson, Junsheng Yang, Wenman Zhang
Publikováno v:
Journal of Medicinal Chemistry. 65:6940-6952
Autor:
Edward J. Hennessy, Marianne Schimpl, Emma Rivers, Paul D. Smith, Elizabeth Hardaker, Ann T. Doherty, Nichola L. Davies, Jon Travers, Qianxiu Zhu, Beth Williamson, Graham Smith, Lorraine Mooney, Helen Musgrove, Kristin Goldberg, Muireann Coen, Anne-Laure Lainé, Xiefeng Jiang, Philip Hopcroft, Yuting Zheng, Robert I Troup, George Hodgson, Nicola Lindsay, Lindsay McMurray, Olga Collingwood, Stephen D. Wilkinson, Sharon Tentarelli, Guang He, Philip B. Rawlins, Roshini Markandu, Jon Winter-Holt, Josephine Walton, Ankur Karmokar, J. Willem M. Nissink, Yumeng Mao, Dejian Yang, Alexander Pflug, Gary Fairley, Scott Boyd, Cheng Wang, Anne Jackson, Martin R. Brown, William McCoull, Neville McLean, Venkatesh Pilla Reddy
Publikováno v:
Journal of Medicinal Chemistry. 64:13524-13539
Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncology therapeutics by restoring the innate immune response in the tumor microenvironment. Highly selective dual Mer/Axl kinase inhib
Autor:
Jason G, Kettle, Sharan K, Bagal, Sue, Bickerton, Michael S, Bodnarchuk, Scott, Boyd, Jason, Breed, Rodrigo J, Carbajo, Doyle J, Cassar, Atanu, Chakraborty, Sabina, Cosulich, Iain, Cumming, Michael, Davies, Nichola L, Davies, Andrew, Eatherton, Laura, Evans, Lyman, Feron, Shaun, Fillery, Emma S, Gleave, Frederick W, Goldberg, Lyndsey, Hanson, Stephanie, Harlfinger, Martin, Howard, Rachel, Howells, Anne, Jackson, Paul, Kemmitt, Gillian, Lamont, Scott, Lamont, Hilary J, Lewis, Libin, Liu, Michael J, Niedbala, Christopher, Phillips, Radek, Polanski, Piotr, Raubo, Graeme, Robb, David M, Robinson, Sarah, Ross, Matthew G, Sanders, Michael, Tonge, Rebecca, Whiteley, Stephen, Wilkinson, Junsheng, Yang, Wenman, Zhang
Publikováno v:
Journal of medicinal chemistry. 65(9)
KRAS is an archetypal high-value intractable oncology drug target. The glycine to cysteine mutation at codon 12 represents an Achilles heel that has now rendered this important GTPase druggable. Herein, we report our structure-based drug design appro
Autor:
Jon J. Winter-Holt, Catherine Bardelle, Elisabetta Chiarparin, Ian L. Dale, Paul R. J. Davey, Nichola L. Davies, Christopher Denz, Shaun M. Fillery, Carine M. Guérot, Fujin Han, Samantha J. Hughes, Meghana Kulkarni, Zhaoqun Liu, Alexander Milbradt, Thomas A. Moss, Huijun Niu, Joe Patel, Alfred A. Rabow, Marianne Schimpl, Junjie Shi, Dongqing Sun, Dejian Yang, Sylvie Guichard
Publikováno v:
Journal of medicinal chemistry. 65(4)
ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncology target. While several small molecule inhibitors have been described in the literature, their cellular activity
Autor:
Iain A. Cumming, Sébastien L. Degorce, Anna Aagaard, Erin L. Braybrooke, Nichola L. Davies, Coura R. Diène, Andrew J. Eatherton, Hannah R. Felstead, Sam D. Groombridge, Eva M. Lenz, Yunxia Li, Youfeng Nai, Stuart Pearson, Graeme R. Robb, James S. Scott, Oliver R. Steward, Chengyan Wu, Yafeng Xue, Lanping Zhang, Yanxiu Zhang
Publikováno v:
Bioorganicmedicinal chemistry. 63
In this article, we report the discovery of a series of pyrimidopyridones as inhibitors of IRAK4 kinase. From a previously disclosed 5-azaquinazoline series, we found that switching the pyridine ring for an N-substituted pyridone gave a novel hinge b
Autor:
William, McCoull, Scott, Boyd, Martin R, Brown, Muireann, Coen, Olga, Collingwood, Nichola L, Davies, Ann, Doherty, Gary, Fairley, Kristin, Goldberg, Elizabeth, Hardaker, Guang, He, Edward J, Hennessy, Philip, Hopcroft, George, Hodgson, Anne, Jackson, Xiefeng, Jiang, Ankur, Karmokar, Anne-Laure, Lainé, Nicola, Lindsay, Yumeng, Mao, Roshini, Markandu, Lindsay, McMurray, Neville, McLean, Lorraine, Mooney, Helen, Musgrove, J Willem M, Nissink, Alexander, Pflug, Venkatesh Pilla, Reddy, Philip B, Rawlins, Emma, Rivers, Marianne, Schimpl, Graham F, Smith, Sharon, Tentarelli, Jon, Travers, Robert I, Troup, Josephine, Walton, Cheng, Wang, Stephen, Wilkinson, Beth, Williamson, Jon, Winter-Holt, Dejian, Yang, Yuting, Zheng, Qianxiu, Zhu, Paul D, Smith
Publikováno v:
Journal of medicinal chemistry. 64(18)
Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncology therapeutics by restoring the innate immune response in the tumor microenvironment. Highly selective dual Mer/Axl kinase inhib
Publikováno v:
Magnetic Resonance, Vol 2, Pp 489-498 (2021)
Knowledge of free ligand conformational preferences (energy minima) and conformational dynamics (rotational energy barriers) of small molecules in solution can guide drug design hypotheses and help rank ideas to bias syntheses towards more active com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82cfc6ec4c727018b769eba7caac0251
https://mr.copernicus.org/articles/2/489/2021/
https://mr.copernicus.org/articles/2/489/2021/
Autor:
Elisabetta Chiarparin, Amber Balazs, Martin J. Packer, Jeffrey W. Johannes, Nichola L. Davies, William McCoull, Graeme R. Robb, Piotr Raubo, Yu Dong, Alexander Hird, Rodrigo J. Carbajo, Michelle Lamb
Publikováno v:
Journal of Medicinal Chemistry. 62:9418-9437
The three-dimensional conformations adopted by a free ligand in solution impact bioactivity and physicochemical properties. Solution 1D NMR spectra inherently contain information on ligand conformational flexibility and three-dimensional shape, as we
Autor:
Amber Y. S. Balazs, Nichola L. Davies, David Longmire, Martin J. Packer, Elisabetta Chiarparin
Knowledge of free ligand conformational preferences (energy minima) and conformational dynamics (rotational energy barriers) of small molecules in solution can guide drug design hypotheses and help rank ideas to bias syntheses towards more active com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::657411fa1462ccc4f0f639b1b2b6fd85
https://mr.copernicus.org/preprints/mr-2021-27/
https://mr.copernicus.org/preprints/mr-2021-27/
Autor:
Camila de-Almeida, Keith R. Mulholland, Kang Zhao, Barlaam Bernard Christophe, Gilles Ouvry, Gareth Hughes, Martin Pass, Elaine Cadogan, Zhenhua Wang, Andrew D. Campbell, Nidal Al-Huniti, Natalie Stratton, Sébastien L. Degorce, Joanne Wilson, Myriam Didelot, Philip A. MacFaul, Stephen T. Durant, Richard Ducray, Baochang Zhai, Kurt Gordon Pike, Lorraine A. Hassall, Jane L. Holmes, Thomas M. McGuire, Nichola L. Davies, Allan Dishington, Yingxue Chen, Nicola Colclough, Graeme R. Robb
Publikováno v:
Journal of Medicinal Chemistry. 61:3823-3841
ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse xenograft models. However, the properties of 7 result in a relatively high predicted clinically