Zobrazeno 1 - 10
of 94
pro vyhledávání: '"R J, Davey"'
Autor:
James S. Scott, Darren Stead, Bernard Barlaam, Jason Breed, Rodrigo J. Carbajo, Elisabetta Chiarparin, Natalie Cureton, Paul R. J. Davey, David I. Fisher, Eric T. Gangl, Tyler Grebe, Ryan D. Greenwood, Sudhir Hande, Holia Hatoum-Mokdad, Samantha J. Hughes, Thomas A. Hunt, Tony Johnson, Stefan L. Kavanagh, Teresa C. M. Klinowska, Carrie J. B. Larner, Mandy Lawson, Andrew S. Lister, David Longmire, Stacey Marden, Thomas M. McGuire, Caroline McMillan, Lindsay McMurray, Christopher J. Morrow, J. Willem M. Nissink, Thomas A. Moss, Daniel H. O’Donovan, Radoslaw Polanski, Stephen Stokes, Kumar Thakur, Dawn Trueman, Caroline Truman, Michael J. Tucker, Haixia Wang, Nicky Whalley, Dedong Wu, Ye Wu, Bin Yang, Wenzhan Yang
Publikováno v:
Journal of Medicinal Chemistry. 66:2918-2945
Autor:
Alan Gerber, Sven Hennig, Rosa Bellavita, Isabel Everard, Thirza van Ramshorst, Elisabetta Chiarparin, Nina Louisa Efrém, Nicholas M Pearce, Paul R. J. Davey, Tom N. Grossmann, Paolo Grieco, Mathias Wendt, Mercedes Vazquez-Chantada
Publikováno v:
Angewandte Chemie (International Ed. in English)
Angewandte Chemie-International Edition, 60(25), 13937-13944. Wiley
Wendt, M, Bellavita, R, Gerber, A, Efrém, N L, van Ramshorst, T, Pearce, N M, Davey, P R J, Everard, I, Vazquez-Chantada, M, Chiarparin, E, Grieco, P, Hennig, S & Grossmann, T N 2021, ' Bicyclic β-Sheet Mimetics that Target the Transcriptional Coactivator β-Catenin and Inhibit Wnt Signaling ', Angewandte Chemie-International Edition, vol. 60, no. 25, pp. 13937-13944 . https://doi.org/10.1002/anie.202102082
Angewandte Chemie-International Edition, 60(25), 13937-13944. John Wiley and Sons Ltd
Angewandte Chemie-International Edition, 60(25), 13937-13944. Wiley
Wendt, M, Bellavita, R, Gerber, A, Efrém, N L, van Ramshorst, T, Pearce, N M, Davey, P R J, Everard, I, Vazquez-Chantada, M, Chiarparin, E, Grieco, P, Hennig, S & Grossmann, T N 2021, ' Bicyclic β-Sheet Mimetics that Target the Transcriptional Coactivator β-Catenin and Inhibit Wnt Signaling ', Angewandte Chemie-International Edition, vol. 60, no. 25, pp. 13937-13944 . https://doi.org/10.1002/anie.202102082
Angewandte Chemie-International Edition, 60(25), 13937-13944. John Wiley and Sons Ltd
Protein complexes are defined by the three‐dimensional structure of participating binding partners. Knowledge about these structures can facilitate the design of peptidomimetics which have been applied for example, as inhibitors of protein–protei
Autor:
Craig F. Steven, Martin Lee, Gary S. Nichol, Paul R. J. Davey, Elisabetta Chiarparin, Valerie G. Brunton, Alison N. Hulme
Publikováno v:
Steven, C F, Lee, M, Nichol, G S, Davey, P R J, Chiarparin, E, Brunton, V G & Hulme, A N 2022, ' Design, Synthesis, and Analytical Evaluation of Fsp3-Inspired Raman Probes for Cellular Imaging ', European Journal of Organic Chemistry . https://doi.org/10.1002/ejoc.202200393
The fraction of sp 3 -hybdrised carbons (Fsp 3 ) in drug candidates and other biologically relevant compounds has been proposed to be an important physicochemical consideration within medicinal chemistry. Currently available small-molecule probes for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b628c744c874dbb66683f7f772cbcae
https://hdl.handle.net/20.500.11820/4bad3341-53a7-4468-8429-2af89587f01b
https://hdl.handle.net/20.500.11820/4bad3341-53a7-4468-8429-2af89587f01b
Autor:
Alice R Eddershaw, Karl Syson, Paul R. J. Davey, Gregory Hamm, Christopher D. Stubbs, Paul Clarkson, Elizabeth Underwood, Lucy V Edwardes
Publikováno v:
Biochemistry. 59:4775-4786
Protein arginine methyltransferases (PRMTs) are of great interest for the development of therapeutics due to their involvement in a number of malignancies, such as lung and colon cancer. PRMT5 catalyzes the formation of symmetrical dimethylarginine o
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:
Michael J. Tucker, Thomas A. Moss, James S. Scott, Barlaam Bernard Christophe, Paul R. J. Davey, Ryan Greenwood, Stephen Stokes, Gary Fairley, Radoslaw Polanski, Holia Hatoum-Mokdad, David Longmire, Eric Gangl, Bin Yang, Andrew Lister, Jeffrey G. Varnes
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition of fluorine on
Autor:
Stefan Geschwindner, Mercedes Vazquez-Chantada, Hacer Karatas, Carmen Carrillo García, Elisabetta Chiarparin, Dennis Schade, Malin Lemurell, Tom N. Grossmann, Paul R. J. Davey, Alleyn T. Plowright, Jeremy Kah Sheng Pang, Hélène Adihou, Boon Seng Soh, Stéphanie M. Guéret, Wanjin Hong, Carola M. Wassvik, Ranganath Gopalakrishnan, Eric Valeur, Tim Förster, Herbert Waldmann, Raphael Gasper, Ajaybabu V. Pobbati
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-10 (2020)
Adihou, H, Gopalakrishnan, R, Förster, T, Guéret, S M, Gasper, R, Geschwindner, S, Carrillo García, C, Karatas, H, Pobbati, A V, Vazquez-Chantada, M, Davey, P, Wassvik, C M, Pang, J K S, Soh, B S, Hong, W, Chiarparin, E, Schade, D, Plowright, A T, Valeur, E, Lemurell, M, Grossmann, T N & Waldmann, H 2020, ' A protein tertiary structure mimetic modulator of the Hippo signalling pathway ', Nature Communications, vol. 11, no. 1, 5425 . https://doi.org/10.1038/s41467-020-19224-8
Nature Communications, 11(1):5425. Nature Publishing Group
Nature Communications
Adihou, H, Gopalakrishnan, R, Förster, T, Guéret, S M, Gasper, R, Geschwindner, S, Carrillo García, C, Karatas, H, Pobbati, A V, Vazquez-Chantada, M, Davey, P, Wassvik, C M, Pang, J K S, Soh, B S, Hong, W, Chiarparin, E, Schade, D, Plowright, A T, Valeur, E, Lemurell, M, Grossmann, T N & Waldmann, H 2020, ' A protein tertiary structure mimetic modulator of the Hippo signalling pathway ', Nature Communications, vol. 11, no. 1, 5425 . https://doi.org/10.1038/s41467-020-19224-8
Nature Communications, 11(1):5425. Nature Publishing Group
Nature Communications
Transcription factors are key protein effectors in the regulation of gene transcription, and in many cases their activity is regulated via a complex network of protein–protein interactions (PPI). The chemical modulation of transcription factor acti
Autor:
Teresa Klinowska, J. Willem M. Nissink, Hoan K. Huynh, Jason Breed, Christopher J. Morrow, Paul R. J. Davey, Thomas A. Moss, Jeffrey G. Varnes, Rodrigo J. Carbajo, James S. Scott, Bin Yang, Radoslaw Polanski, Ryan Greenwood
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we report the use of metathesis to construct a novel tetracyclic core in a series of estrogen receptor degraders. This improved the chemical stability, as assessed using an NMR-MS based assay, and gave a molecule with excelle
Autor:
Scott G. Lamont, Robert D. M. Davies, Christopher J. Morrow, Thomas A. Moss, Andrew Lister, Eric Gangl, Rodrigo J. Carbajo, Paul R. J. Davey, Craig S. Donald, James S. Scott, Tony Johnson, Sébastien L. Degorce, Jon Curwen, Mandy Lawson, Sam D. Groombridge, David Buttar, Radoslaw Polanski, Ryan Greenwood, Andrew Bailey, Jennifer H. Pink
Publikováno v:
Journal of Medicinal Chemistry. 62:1593-1608
Herein, we report the identification and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen receptor degrader antagonists. Replacement of a phenol, present in our previously reported tetrahydroisoquinoline scaffold, w
Autor:
Haixia Wang, Stefan Kavanagh, Radoslaw Polanski, Eric Gangl, Michael J. Tucker, Jason Breed, Thomas Anthony Hunt, Paul R. J. Davey, Mandy Lawson, Darren Stead, Oona Delpuech, Ye Wu, J. Willem M. Nissink, Barlaam Bernard Christophe, Dedong Wu, Sudhir M. Hande, Amber Balazs, Dermot F. McGinnity, Wenzhan Yang, Thomas A. Moss, Bin Yang, Sladjana Gagrica, Kumar Thakur, Stacey Marden, Tyler Grebe, Daniel Hillebrand O'donovan, Teresa Klinowska, Samantha Jayne Hughes, Kara Herlihy, David I Fisher, Stephen Stokes, Holia Hatoum-Mokdad, Tony Johnson, James S. Scott, Elisabetta Chiarparin, Bo Peng, Sophie L. M. Janbon, Scott Throner, Ryan Greenwood, David Matthew Wilson, Andrew Lister, Stephen Fawell, Hoan Huynh, Jeffrey G. Varnes, Christopher J. Morrow, Rodrigo J. Carbajo
Publikováno v:
Journal of medicinal chemistry. 63(23)
Herein we report the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD) and antagonists for the treatment of ER+ breast cancer. Structure based design together with systematic investigation of each region