Zobrazeno 1 - 10
of 54
pro vyhledávání: '"J. Willem M. Nissink"'
Autor:
Thomas G. Hayhow, Beth Williamson, Mandy Lawson, Natalie Cureton, Erin L. Braybrooke, Andrew Campbell, Rodrigo J. Carbajo, Azadeh Cheraghchi-Bashi, Elisabetta Chiarparin, Coura R. Diène, Charlene Fallan, David I. Fisher, Frederick W. Goldberg, Lorna Hopcroft, Philip Hopcroft, Anne Jackson, Jason G. Kettle, Teresa Klinowska, Ulrike Künzel, Gillian Lamont, Hilary J. Lewis, Gareth Maglennon, Scott Martin, Pablo Morentin Gutierrez, Christopher J. Morrow, Myria Nikolaou, J. Willem M. Nissink, Patrick O’Shea, Radoslaw Polanski, Markus Schade, James S. Scott, Aaron Smith, Judith Weber, Joanne Wilson, Bin Yang, Claire Crafter
Publikováno v:
Communications Biology, Vol 7, Iss 1, Pp 1-17 (2024)
Abstract Targeting the estrogen receptor alpha (ERα) pathway is validated in the clinic as an effective means to treat ER+ breast cancers. Here we present the development of a VHL-targeting and orally bioavailable proteolysis-targeting chimera (PROT
Externí odkaz:
https://doaj.org/article/ec006f9560824ea494be6041bb1eeb60
Autor:
João Morado, Paul N. Mortenson, J. Willem M. Nissink, Jonathan W. Essex, Chris-Kriton Skylaris
Publikováno v:
Journal of Chemical Information and Modeling. 63:2810-2827
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d81d1bf17c4fa8245227450c823575ba
https://doi.org/10.1021/acs.jcim.2c01510
https://doi.org/10.1021/acs.jcim.2c01510
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b2ec7d4c4fb73ee3f4aed9c21a77b1bf
https://doi.org/10.1021/acs.jmedchem.2c01964
https://doi.org/10.1021/acs.jmedchem.2c01964
Autor:
J. Willem M. Nissink, Rongxuan Dou, Gabriele Fumagalli, Andrew Peter Thomas, Rodrigo J. Carbajo, Jonathan Tart, David R. Spring
Publikováno v:
Journal of Medicinal Chemistry. 64:17287-17303
RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identif
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9212a0ac1a748d6ed575d7720ac913c
https://doi.org/10.1021/acs.jmedchem.1c01334
https://doi.org/10.1021/acs.jmedchem.1c01334
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ae4c719e098004f12a5992670f8e8abc
https://doi.org/10.1021/acs.jmedchem.1c00920
https://doi.org/10.1021/acs.jmedchem.1c00920
Autor:
J. Willem M. Nissink, Jonathan B. Baell, Francis S. Willard, Ina Rothenaigner, Jonathan Z. Sexton, Douglas S. Auld, Jayme L. Dahlin, John Strelow, Michael A. Walters, Bruce K. Hua, Steve Haney, Lori Ferrins, Jarrod Walsh, Bridget K. Wagner, Jonathan A. Lee, Kamyar Hadian
Publikováno v:
Cell Chem. Bio. 28, 356-370 (2021)
Cell Chem Biol
Cell Chem Biol
Compounds that exhibit assay interference or undesirable mechanisms of bioactivity (“nuisance compounds”) are routinely encountered in cellular assays, including phenotypic and high-content screening assays. Much is known regarding compound-depen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f70a37970ff95ac15de8c8aee188c39
https://doi.org/10.1016/j.chembiol.2021.01.021
https://doi.org/10.1016/j.chembiol.2021.01.021
Autor:
J Willem M Nissink, Michal Bista, Jason Breed, Nikki Carter, Kevin Embrey, Jonathan Read, Jon J Winter-Holt
Publikováno v:
PLoS ONE, Vol 11, Iss 3, p e0151154 (2016)
MTH1 (NUDT1) is an oncologic target involved in the prevention of DNA damage. We investigate the way MTH1 recognises its substrates and present substrate-bound structures of MTH1 for 8-oxo-dGTP and 8-oxo-rATP as examples of novel strong and weak bind
Externí odkaz:
https://doaj.org/article/9fb8b358bc4f48ecb81ceedb4cb0f8a9
Autor:
William McCoull, Jon Winter-Holt, Marianne Schimpl, Elizabeth Underwood, Ross Overman, Juli Warwicker, Philip B. Rawlins, J. Willem M. Nissink, Alexander Pflug, Caroline Truman
Publikováno v:
Biochemical Journal
The activation loop (A-loop) plays a key role in regulating the catalytic activity of protein kinases. Phosphorylation in this region enhances the phosphoryl transfer rate of the kinase domain and increases its affinity for ATP. Furthermore, the A-lo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8d4c6e582a9e63dc834895d8a9b2dea
https://doi.org/10.1042/bcj20200735
https://doi.org/10.1042/bcj20200735
Autor:
João Morado, Marcel L. Verdonk, Jonathan W. Essex, Richard A. Ward, J. Willem M. Nissink, Chris-Kriton Skylaris, Paul N. Mortenson
Publikováno v:
Journal of chemical theory and computation. 17(11)
Conformational analysis is of paramount importance in drug design: it is crucial to determine pharmacological properties, understand molecular recognition processes, and characterize the conformations of ligands when unbound. Molecular Mechanics (MM)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ded4494aa32bbd7597ac3b73d780dc5
https://pubmed.ncbi.nlm.nih.gov/34644088
https://pubmed.ncbi.nlm.nih.gov/34644088
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::5ae60041f0f2dfe86225bfbc9ef0aea3
https://pubmed.ncbi.nlm.nih.gov/34478292
https://pubmed.ncbi.nlm.nih.gov/34478292