Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Miller Duncan Charles"'
Autor:
Lan Z. Wang, Miller Duncan Charles, Bernard T. Golding, Ian Hickson, Martin E.M. Noble, Celine Cano, Suzannah J. Harnor, Michael J. Waring, Harry J Shrives, Shaimaa Khalifa, Jane Totobenazara, Stephen J. Hobson, Elaine Willmore, Hannah L Stewart, Mathew P. Martin, Susan J. Tudhope, Huw D. Thomas, Islam Al-Khawaldeh, Claire E. Jennings, João V de Souza, Max J. Temple, Jane A. Endicott, Cinzia Bordoni, Honorine Lebraud, Agnieszka K. Bronowska, Ian R. Hardcastle, Amy B. Heptinstall, Stephen R. Wedge, Christine Basmadjian, Gregory G Aldred, Julie A. Tucker, Mohammed J Al Yasiri
Publikováno v:
Journal of Medicinal Chemistry. 64:10001-10018
NF-κB-inducing kinase (NIK) is a key enzyme in the noncanonical NF-κB pathway, of interest in the treatment of a variety of diseases including cancer. Validation of NIK as a drug target requires potent and selective inhibitors. The protein contains
Autor:
Benoit Carbain, Keisha Hearn, Ildiko Maria Buck, Burcu Anil, Sarah J. Cully, Gianni Chessari, Jane A. Endicott, John Lunec, Neil T. Thompson, Juan Castro, Roger J. Griffin, Rhian S. Holvey, Karen Haggerty, Charlotte H. Revill, Ruth H. Bawn, Stephen R. Wedge, Christiane Riedinger, Christopher N. Johnson, Bernard T. Golding, Lynsey Fazal, Ian R. Hardcastle, Mladen Vinkovic, Claire E. Jennings, Jong Sook Ahn, Bian Zhang, Pamela A. Williams, Celine Cano, Suzannah J. Harnor, Ben Cons, Stephen J. Hobson, E. Anscombe, Jeffrey D. St. Denis, Steven Howard, David R. Newell, Emiliano Tamanini, Nicola E. Wilsher, Miller Duncan Charles, Huw D. Thomas, Timothy J. Blackburn, Martin E.M. Noble, Judith Reeks, Yan Zhao, Luke Bevan
Publikováno v:
Journal of Medicinal Chemistry. 64:4071-4088
Inhibition of murine double minute 2 (MDM2)-p53 protein-protein interaction with small molecules has been shown to reactivate p53 and inhibit tumor growth. Here, we describe rational, structure-guided, design of novel isoindolinone-based MDM2 inhibit
Autor:
Kate McAdam, Cinzia Bordoni, Miller Duncan Charles, Daniel J. Brough, James H. Hunter, Pasquale A. Morese, Nikolay Sitnikov, Mélanie Uguen, Gemma Davison, J. Daniel Lopez-Fernandez, Paul Ratcliffe, Alexia Papaioannou, Michael J. Waring
Publikováno v:
The Medicinal Chemist's Guide to Solving ADMET Challenges ISBN: 9781788012270
Interaction with cardiac ion channels can potentially result in severe or even fatal cardiac side effects. The most prominent of cardiac channels, human ether-a-go-go-related gene (hERG), voltage-gated sodium channel 1.5 (NaV1.5) and voltage-gated ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6b724a3741ae0b28930cbef06ccb7441
https://doi.org/10.1039/9781788016414-00403
https://doi.org/10.1039/9781788016414-00403
Autor:
Ian R. Hardcastle, Celine Cano, Mathew P. Martin, Leanne E Knight, Michael J. Waring, Islam Al-Khawaldeh, J. Daniel Lopez-Fernandez, Miller Duncan Charles, Jane A. Endicott, Martin E.M. Noble, Shengying Lin, D.J. Wood, Conghao Gai
Publikováno v:
Journal of Medicinal Chemistry. 62:3741-3752
Identifying ligand binding sites on proteins is a critical step in target-based drug discovery. Current approaches to this require resource-intensive screening of large libraries of lead-like or fragment molecules. Here, we describe an efficient and
Autor:
Peter J. Bungay, Martin Corless, Sarah Elizabeth Skerratt, Joseph S. Warmus, Sharan K. Bagal, C. Elizabeth Payne, Miller Duncan Charles, Kemp Mark Ian, David R. Fenwick, Paul Blackwell, Yoshihisa Murata, Bruce Brown, Laia Malet Sanz, David Fengas, James Michael Crawforth, Victoria Gray, Wolfgang Klute, Alan Daniel Brown, David C. Blakemore, Edward B. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:230-239
The voltage gated sodium channel NaV1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole NaV1
Autor:
Simon J. Cook, Mathew P. Martin, Julie A. Tucker, Miller Duncan Charles, Timothy J. Blackburn, Stephanie M. Myers, Ai-Ching Wong, Nick C. Martin, Mercedes Arasta, Martin E.M. Noble, Huw D. Thomas, Ruth H. Bawn, Lan-Zhen Wang, Noel Edwards, Pamela A. Lochhead, Celine Cano, Suzannah J. Harnor, Tristan Reuillon, Laurent Rigoreau, Lauren Molyneux, Roger J. Griffin, David R. Newell, Bernard T. Golding, Tim Hammonds, Amy B. Heptinstall, P.J. Owen, Stephen R. Wedge, Ian R. Hardcastle, Leon Pang, Jane A. Endicott
Extracellular regulated kinase 5 (ERK5) signalling has been implicated in driving a number of cellular phenotypes including endothelial cell angiogenesis and tumour cell motility. Novel ERK5 inhibitors were identified using high throughput screening,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b20469b74ddfa9b4388aacc50467a77
https://eprints.whiterose.ac.uk/148098/1/ERK5LeadIDPaper_EurJMedChem_2019_04_29.docx
https://eprints.whiterose.ac.uk/148098/1/ERK5LeadIDPaper_EurJMedChem_2019_04_29.docx
Autor:
Bernard T. Golding, Alfie Brennan, Tristan Reuillon, Miller Duncan Charles, Celine Cano, Gary S. Beale, Annalisa Bertoli, Sari F. Alhasan, Helen L. Reeves, David R. Newell, Roger J. Griffin
Publikováno v:
Chemical Science
Two series of inhibitors of sulfatase 2, ARSA and ARSB were designed based on biphenyl and biphenyl ether scaffolds substituted with e.g. sulfamate and carboxylate groups.
Inhibitors of sulfatase-2 are putative anticancer agents, but the discove
Inhibitors of sulfatase-2 are putative anticancer agents, but the discove
Autor:
Alan Daniel Brown, Joseph S. Warmus, Matthew Corbett, Yoshihisa Murata, C. Elizabeth Payne, Kiyoyuki Omoto, Tanya L. Hay, Miller Duncan Charles, Sharan K. Bagal, Peter J. Bungay, David C. Blakemore, Edward B. Stevens, Kemp Mark Ian
Publikováno v:
MedChemComm. 7:1925-1931
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we describe the discovery and optimisation of a Nav1.8 inhibiting phenyl imidazole series that delivers chemical equi
Autor:
Thomas Ryckmans, James Edward John Mills, Mark E. Bunnage, Miller Duncan Charles, Alan Daniel Brown, C M Barker, Sarah Elizabeth Skerratt
Publikováno v:
Med. Chem. Commun.. 3:174-178
Given the large amounts of screening data now available, empirical methods derived from matched-molecular pairs are being used as a means for suggesting bioisosteric replacements to the medicinal chemist. The pairwise analysis of compounds has been e
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6108-6111
Optimisation of the potency of a bicyclic CRF antagonist whilst retaining metabolic stability is described. A core change and incorporation of metabolically stable lipophilic groups resulted in a further potency gain without increasing metabolic liab