Zobrazeno 1 - 10
of 103
pro vyhledávání: '"Ian R. Hardcastle"'
Autor:
Gemma Davison, Mathew P. Martin, Shannon Turberville, Selma Dormen, Richard Heath, Amy B. Heptinstall, Marie Lawson, Duncan C. Miller, Yi Min Ng, James N. Sanderson, Ian Hope, Daniel J. Wood, Céline Cano, Jane A. Endicott, Ian R. Hardcastle, Martin E. M. Noble, Michael J. Waring
Publikováno v:
Journal of Medicinal Chemistry. 65:15416-15432
The development of ligands for biological targets is critically dependent on the identification of sites on proteins that bind molecules with high affinity. A set of compounds, called FragLites, can identify such sites, along with the interactions re
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:
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:
Kathy Boxall, Mangaleswaran Sivaprakasam, David P. Turner, Roger J. Griffin, Corine Mas-Droux, Benoit Carbain, Bernard T. Golding, Richard Bayliss, Ian R. Hardcastle, Mark W. Richards, Andrew M. Fry, Christopher R. Coxon, David R. Newell, Celine Cano, Suzannah J. Harnor, Christopher J. Matheson
Publikováno v:
RSC Medicinal Chemistry
Renewed interest in covalent inhibitors of enzymes implicated in disease states has afforded several agents targeted at protein kinases of relevance to cancers.
Renewed interest in covalent inhibitors of enzymes implicated in disease states has
Renewed interest in covalent inhibitors of enzymes implicated in disease states has
Autor:
Kelly Coffey, Timothy J Blackburn, Susan Cook, Bernard T Golding, Roger J Griffin, Ian R Hardcastle, Lorraine Hewitt, Kety Huberman, Hesta V McNeill, David R Newell, Celine Roche, Claudia A Ryan-Munden, Anna Watson, Craig N Robson
Publikováno v:
PLoS ONE, Vol 7, Iss 10, p e45539 (2012)
Tip60 (KAT5) is a histone acetyltransferase (HAT enzyme) involved in multiple cellular processes including transcriptional regulation, DNA damage repair and cell signalling. In prostate cancer, aggressive cases over-express Tip60 which functions as a
Externí odkaz:
https://doaj.org/article/ad0f8a29724847c78bbacae4be080277
Publikováno v:
Future Medicinal Chemistry. 10:1369-1388
Inhibition of CDKs is an attractive approach to cancer therapy due to their vital role in cell growth and transcription. Pan-CDK inhibitors have shown some clinical benefit, and trials are ongoing. Selective CDK4 and CDK6 inhibitors have been license
Autor:
Benoit Carbain, E. Anscombe, Jane A. Endicott, Christopher R. Coxon, Mathew P. Martin, Stephen R. Wedge, Christopher Wong, Svitlana Korolchuk, Mangaleswaran Sivaprakasam, Bernard T. Golding, Lisa K. Harlow, Celine Cano, Suzannah J. Harnor, Christopher J. Matheson, Lan Z. Wang, David M. Turner, Martin E.M. Noble, David R. Newell, Ian R. Hardcastle, Roger J. Griffin, Susan J. Tudhope
Publikováno v:
Journal of Medicinal Chemistry
Purines and related heterocycles substituted at C-2 with 4’-sulfamoylanilino and at C-6 with a variety of groups have been synthesized with the aim of achieving selectivity of binding to CDK2 over CDK1. 6-Substituents that favour competitive inhibi
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:
Duncan C, Miller, Mathew P, Martin, Santosh, Adhikari, Alfie, Brennan, Jane A, Endicott, Bernard T, Golding, Ian R, Hardcastle, Amy, Heptinstall, Stephen, Hobson, Claire, Jennings, Lauren, Molyneux, Yvonne, Ng, Stephen R, Wedge, Martin E M, Noble, Celine, Cano
Publikováno v:
Organic & Biomolecular Chemistry
Structure-guided expansion of a fragment hit for the ATAD2 bromodomain enabled improvement in ATAD2 inhibition and selectivity over BRD4.
ATAD2 is an ATPase that is overexpressed in a variety of cancers and associated with a poor patient prognos
ATAD2 is an ATPase that is overexpressed in a variety of cancers and associated with a poor patient prognos