Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Pamela A. Lochhead"'
Autor:
Simon J. Cook, Pamela A. Lochhead
Publikováno v:
Frontiers in Cell and Developmental Biology, Vol 10 (2022)
The RAS-regulated RAF-MEK1/2-ERK1/2 signalling pathway is frequently de-regulated in human cancer. Melanoma in particular exhibits a high incidence of activating BRAFV600E/K and NRASQ61L/K mutations and such cells are addicted to the activity of thes
Externí odkaz:
https://doaj.org/article/3a13eac860ed4e48b91f9389ed52f702
Autor:
Pamela A. Lochhead, Julie A. Tucker, Natalie J. Tatum, Jinhua Wang, David Oxley, Andrew M. Kidger, Victoria P. Johnson, Megan A. Cassidy, Nathanael S. Gray, Martin E. M. Noble, Simon J. Cook
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-16 (2020)
Selective ERK5 inhibitors target ERK5 kinase activity, but they do not phenocopy the effects of ERK5 genetic depletion. Here, the authors demonstrate that the direct interaction of these inhibitors to ERK5 kinase domain induces conformational changes
Externí odkaz:
https://doaj.org/article/74f91df61c624308a4815d6adcffb1f9
Autor:
Sònia Najas, Juan Arranz, Pamela A. Lochhead, Anne L. Ashford, David Oxley, Jean M. Delabar, Simon J. Cook, María José Barallobre, Maria L. Arbonés
Publikováno v:
EBioMedicine, Vol 2, Iss 2, Pp 120-134 (2015)
Alterations in cerebral cortex connectivity lead to intellectual disability and in Down syndrome, this is associated with a deficit in cortical neurons that arises during prenatal development. However, the pathogenic mechanisms that cause this defici
Externí odkaz:
https://doaj.org/article/2e2616fe74d7438690f9863488a1d0a7
Publikováno v:
Biochemical Society Transactions
ERK5 is a protein kinase that also contains a nuclear localisation signal and a transcriptional transactivation domain. Inhibition of ERK5 has therapeutic potential in cancer and inflammation and this has prompted the development of ERK5 kinase inhib
Autor:
Natalie J. Tatum, Megan A Cassidy, Pamela A. Lochhead, David Oxley, Julie A. Tucker, Victoria P Johnson, Andrew M. Kidger, Simon J. Cook, Martin E.M. Noble, Nathanael S. Gray, Jinhua Wang
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-16 (2020)
Nature Communications
Nature Communications
The dual protein kinase-transcription factor, ERK5, is an emerging drug target in cancer and inflammation, and small-molecule ERK5 kinase inhibitors have been developed. However, selective ERK5 kinase inhibitors fail to recapitulate ERK5 genetic abla
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:
Lesley Gilmour, Jonathan Clark, Simon J. Cook, Lan-Zhen Wang, Pamela A. Lochhead, Matthew Squires, Rebecca Gilley, Stephen R. Wedge, Caroline Foxton, David R. Newell
Publikováno v:
Cell Cycle
ERK5, encoded by MAPK7, has been proposed to play a role in cell proliferation, thus attracting interest as a cancer therapeutic target. While oncogenic RAS or BRAF cause sustained activation of the MEK1/2-ERK1/2 pathway, ERK5 is directly activated b
Autor:
Kevin Hudson, Pamela A. Lochhead, Raffaella Gallo, Rachel Rowlinson, Mark Cockerill, Sylvie Guichard, Kathryn Balmanno, Richard A. Ward, Lisa M. Baak, Anne L. Ashford, Simon J. Cook, Tom Dunkley, Louise Goodwin
Publikováno v:
Cellular and Molecular Life Sciences
The dual-specificity tyrosine-phosphorylation-regulated kinase, DYRK1B, is expressed de novo during myogenesis, amplified or mutated in certain cancers and mutated in familial cases of metabolic syndrome. DYRK1B is activated by cis auto-phosphorylati
Autor:
Kathryn Balmanno, Pamela A. Lochhead, Jonathan Clark, David Oxley, Simon J. Cook, Rebecca Gilley
Publikováno v:
Cellular Signalling. 24:170-180
The pro-apoptotic BH3 only protein BIM(EL) is phosphorylated by ERK1/2 and this targets it for proteasome-dependent degradation. A recent study has shown that ERK5, an ERK1/2-related MAPK, is activated during mitosis and phosphorylates BIM(EL) to pro
Publikováno v:
Oncogene. 29:2591-2598
Cancer cells acquire characteristics of deregulated growth, survival and increased metastatic potential. Genetic mutations that provide a selective advantage by promoting these characteristics have been termed 'drivers,' whereas mutations that do not