Výsledky vyhledávání - "Shane Rountree"

Akademický článek

USP7 inhibitors suppress tumour neoangiogenesis and promote synergy with immune checkpoint inhibitors by downregulating fibroblast VEGF

Autor: Anamarija Jurisic, Pei‐Ju Sung, Mark Wappett, Julien Daubriac, Ian T. Lobb, Wei‐Wei Kung, Nyree Crawford, Natalie Page, Eamon Cassidy, Stephanie Feutren‐Burton, J. S. Shane Rountree, Matthew D. Helm, Colin R. O'Dowd, Richard D. Kennedy, Gerald Gavory, Aaron N. Cranston, Daniel B. Longley, Xavier Jacq, Timothy Harrison

Publikováno v: Clinical and Translational Medicine, Vol 14, Iss 4, Pp n/a-n/a (2024)

Abstract Background Understanding how to modulate the microenvironment of tumors that are resistant to immune checkpoint inhibitors represents a major challenge in oncology.Here we investigate the ability of USP7 inhibitors to reprogram the tumor mic

Externí odkaz: https://doaj.org/article/c9655525645b43019fcffa228b383b32

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Akademický článek

Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical development

Autor: Natalie Page, Mark Wappett, Colin R. O’Dowd, Martin O’Rourke, Gerald Gavory, Lixin Zhang, J. S. Shane Rountree, Linda Jordan, Oliver Barker, Hayley Gibson, Caroline Boyd, Stephanie Feutren-Burton, Estelle McLean, Graham Trevitt, Timothy Harrison

Publikováno v: Scientific Reports, Vol 12, Iss 1, Pp 1-14 (2022)

Abstract The serine/threonine protein kinase AKT plays a pivotal role within the PI3K pathway in regulating cellular proliferation and apoptotic cellular functions, and AKT hyper-activation via gene amplification and/or mutation has been implicated i

Externí odkaz: https://doaj.org/article/268d8b675f8340a193869fbd593ec763

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Identification and Structure-Guided Development of Pyrimidinone Based USP7 Inhibitors

Autor: Eamon Cassidy, Peter Hewitt, Elias Arkoudis, Natalie Page, Gerald Gavory, Hugues Miel, J. S. Shane Rountree, Caroline Hughes, Ewa Odrzywol, Keeva McClelland, Matthew Helm, Colin O'Dowd, Scarlett Dvorkin, Tim Harrison, Linda Jordan, Oliver Barker, Stephanie Feutren-Burton, Ewelina Rozycka, Jakub T. Flasz

Publikováno v: O'Dowd, C R, Helm, M D, Rountree, J S S, Flasz, J T, Arkoudis, E, Miel, H, Hewitt, P R, Jordan, L, Barker, O, Hughes, C, Rozycka, E, Cassidy, E, McClelland, K, Odrzywol, E, Page, N, Fuetren-Burton, S, Dvorkin, S, Gavory, G & Harrison, T 2018, ' Identification and structure-guided development of pyrimidinone based USP7 inhibitors ', ACS Medicinal Chemistry Letters, vol. 9, no. 3, pp. 238-243 . https://doi.org/10.1021/acsmedchemlett.7b00512

[Image: see text] Ubiquitin specific protease 7 (USP7, HAUSP) has become an attractive target in drug discovery due to the role it plays in modulating Mdm2 levels and consequently p53. Increasing interest in USP7 is emerging due to its potential invo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92f42201b193e5dbba8db4243fe20048
https://pubmed.ncbi.nlm.nih.gov/29541367

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Abstract LB-049: Targeting the ubiquitin-proteasome system by small molecule inhibition of the DUBome

Autor: Ewelina Rozycka, Stephanie Burton, Natalie Page, Christina Bell, Steven Whitehead, Matthew Helm, Colin O'Dowd, Oliver Barker, Frank Burkamp, Steven Shepherd, Gerald Gavory, Eamon Cassidy, Shane Rountree, Tim Harrison, Peter Hewitt, Xavier Jacq, Mark Wappett

Publikováno v: Cancer Research. 79:LB-049

The current interest in protein homeostasis as a therapeutic strategy has highlighted the importance of protein ubiquitination as a post-translational modification. Protein degradation has been enabled by several approaches (e.g. small molecule degra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b335541ffa3408590a07af3c2fc2b81e
https://doi.org/10.1158/1538-7445.am2019-lb-049

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Efficient synthesis from d-lyxonolactone of 2-acetamido-1,4-imino-1,2,4-trideoxy-l-arabinitol LABNAc, a potent pyrrolidine inhibitor of hexosaminidases

Autor: Robert J. Nash, Kyoko Ikeda, Mark R. Wormald, J. S. Shane Rountree, George W. J. Fleet, Terry D. Butters, Raymond A. Dwek, Naoki Asano, Emma L. Evinson

Publikováno v: Tetrahedron Letters. 48:4287-4291

The synthesis from d-lyxonolactone of 2-acetamido-1,4-imino-1,2,4-trideoxy-l-arabinitol LABNAc proceeded in an overall yield of 25%; the enantiomer, 2-acetamido-1,4-imino-1,2,4-trideoxy-d-arabinitol DABNAc, was prepared from l-lyxonolactone. LABNAc a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::89510733bf5a247df41d00273582367e
https://doi.org/10.1016/j.tetlet.2007.04.041

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Abstract LB-319: Development and characterization of ADC999: A novel, potent orally available Wee1 inhibitor with robust antitumor efficacy in vivo

Autor: Gerald Gavory, Shane Rountree, Estelle McLean, Stephanie Burton, Andy Wilkinson, Adam Treder, Julien Daubriac, Steven Shepherd, Tim Harrison, Ewelina Rozycka, Mary McFarland, Beronia Gorges, Colin O'Dowd, Caroline Boyd, Frank Burkamp

Publikováno v: Cancer Research. 77:LB-319

Wee1 is a tyrosine kinase that phosphorylates cyclin-dependent kinase 1 (CDC2) to inactivate the CDC2/cyclinB complex. Wee1 is therefore a key regulator of the cell cycle, maintaining the G2 checkpoint arrest to allow for pre-mitotic repair upon geno

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::113cd1071e115359dfe798616e066b70
https://doi.org/10.1158/1538-7445.am2017-lb-319

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Abstract B17: Development of novel, potent orally available Wee1 inhibitors with robust antitumor efficacy in vivo

Autor: Stephanie Burton, Frank Burkamp, Colin O'Dowd, Andy Wilkinson, Beronia Gorges, Mary McFarland, Adam Treder, Dominic Janssen, Shane Rountree, Estelle McLean, Tim Harrison, Caroline Boyd, Gerald Gavory, Ewelina Rozycka, Steven Sheperd

Publikováno v: Molecular Cancer Research. 15:B17-B17

Wee1 is a tyrosine kinase that phosphorylates cyclin-dependent kinase 1 (CDC2) to inactive the CDC2/cyclinB complex. Wee1 is therefore a key regulator of the cell cycle, maintaining the G2 checkpoint arrest to allow for pre-mitotic repair upon genomi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::087c674f19c713d9453ae6868442b5c7
https://doi.org/10.1158/1557-3125.dnarepair16-b17

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Abstract LB-159: A novel, potent and selective inhibitor of Wee1 with robust antitumor activity in various cancer xenograph models

Autor: Gerald Gavory, Colin O’Dowd, Frank Burkamp, Shane Rountree, Ewelina Rozycka, Caroline Boyd, Beronia Gorges, Stephanie Burton, Andy Wilkinson, Steven Shepherd, Dominic Janssen, Mary McFarland, Tim Harrison

Publikováno v: Cancer Research. 76:LB-159

Wee1 is a tyrosine kinase that phosphorylates cyclin-dependent kinase 1 (CDK1/CDC2) to inactive the CDC2/cyclinB complex. Wee1 is therefore a key regulator of the cell cycle, maintaining the G2 checkpoint arrest to allow for premitotic repair in case

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3e303cdbec59be9f965c90ada485e97a
https://doi.org/10.1158/1538-7445.am2016-lb-159

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Lysosomal storage of oligosaccharide and glycosphingolipid in imino sugar treated cells

Autor: George W. J. Fleet, David C. A. Neville, Terry D. Butters, Stephanie D. Boomkamp, Raymond A. Dwek, J. S. Shane Rountree

Publikováno v: Glycoconjugate journal. 27(3)

Sandhoff and Tay-Sachs disease are autosomal recessive GM2 gangliosidoses where a deficiency of lysosomal beta-hexosaminidase results in storage of glycoconjugates. Imino sugar (2-acetamido-1,4-imino-1,2,4-trideoxy-L-arabinitol) inhibition of beta-he

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c764439002e48c593692515c4e1b6e57
https://pubmed.ncbi.nlm.nih.gov/20186478

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