Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Bohdan Waszkowycz"'
Autor:
Alba Maiques-Diaz, Gary J. Spencer, James T. Lynch, Filippo Ciceri, Emma L. Williams, Fabio M.R. Amaral, Daniel H. Wiseman, William J. Harris, Yaoyong Li, Sudhakar Sahoo, James R. Hitchin, Daniel P. Mould, Emma E. Fairweather, Bohdan Waszkowycz, Allan M. Jordan, Duncan L. Smith, Tim C.P. Somervaille
Publikováno v:
Cell Reports, Vol 22, Iss 13, Pp 3641-3659 (2018)
Summary: Pharmacologic inhibition of LSD1 promotes blast cell differentiation in acute myeloid leukemia (AML) with MLL translocations. The assumption has been that differentiation is induced through blockade of LSD1’s histone demethylase activity.
Externí odkaz:
https://doaj.org/article/62c57f81e288426abeec246fcdba9441
Autor:
Amanda J. Watson, Gemma V. Hopkins, Samantha Hitchin, Habiba Begum, Stuart Jones, Allan Jordan, Sarah Holt, H. Nikki March, Rebecca Newton, Helen Small, Alex Stowell, Ian D. Waddell, Bohdan Waszkowycz, Donald J. Ogilvie
Publikováno v:
F1000Research, Vol 5 (2016)
RET (REarranged during Transfection) is a receptor tyrosine kinase, which plays pivotal roles in regulating cell survival, differentiation, proliferation, migration and chemotaxis. Activation of RET is a mechanism of oncogenesis in medullary thyroid
Externí odkaz:
https://doaj.org/article/96b9e34465224e6ea3077ebb933196a0
Autor:
Amanda J. Watson, Gemma V. Hopkins, Samantha Hitchin, Habiba Begum, Stuart Jones, Allan Jordan, Sarah Holt, H. Nikki March, Rebecca Newton, Helen Small, Alex Stowell, Ian D. Waddell, Bohdan Waszkowycz, Donald J. Ogilvie
Publikováno v:
F1000Research, Vol 5 (2016)
RET (REarranged during Transfection) is a receptor tyrosine kinase, which plays pivotal roles in regulating cell survival, differentiation, proliferation, migration and chemotaxis. Activation of RET is a mechanism of oncogenesis in medullary thyroid
Externí odkaz:
https://doaj.org/article/129cb938044645b4be8abc534fed27f3
Autor:
Bohdan Waszkowycz, Habiba Begum, Chitra Seewooruthun, Aude Echalier, Amanda J. Watson, Stuart Donald Jones, Richard Bayliss, Mark W. Richards, Rebecca Newton, Li-Ying Lin, Daniel Burschowsky, Allan M. Jordan, Donald J. Ogilvie, Niall M. Hamilton, Samantha Hitchin, Eleanor French, Ian D. Waddell
Publikováno v:
ACS Med Chem Lett
[Image: see text] A combination of focused library and virtual screening, hit expansion, and rational design has resulted in the development of a series of inhibitors of RET(V804M) kinase, the anticipated drug-resistant mutant of RET kinase. These ag
Autor:
Julie A. Tucker, Ben Acton, Ian D. Waddell, Alexandra Stowell, Nicola Hamilton, Niall M. Hamilton, Kate M. Smith, Stuart Donald Jones, James R. Hitchin, Bohdan Waszkowycz, Alison E. McGonagle, Dominic I. James, Allan M. Jordan, Daniel P. Mould, Clifford David Jones, Colin Hutton, Helen F. Small, Emma E. Fairweather, Donald J. Ogilvie, Louise A. Griffiths
Publikováno v:
Waszkowycz, B, Smith, K, Mcgonagle, A, Jordan, A, Acton, B, Fairweather, E, Griffiths, L, Hamilton, N M, Hamilton, N, Hitchin, J R, Hutton, C, James, D I, Jones, C D, Jones, S, Mould, D, Small, H F, Stowell, A, Tucker, J, Waddell, I & Ogilvie, D J 2018, ' Cell-active Small Molecule Inhibitors of the DNA-damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides ', Journal of Medicinal Chemistry, vol. 61, no. 23, pp. 10767–10792 . https://doi.org/10.1021/acs.jmedchem.8b01407
DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The enzyme poly(ADP-ribose) glycohydrolase (PARG) plays a pivotal role in the regulation of DNA r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e713bd6a754c7026f2f63ab3b3df4e2
https://doi.org/10.1021/acs.jmedchem.8b01407
https://doi.org/10.1021/acs.jmedchem.8b01407
Autor:
Alison E. McGonagle, Graeme J. Thomson, Paul Depledge, Gemma Hopkins, Bohdan Waszkowycz, Mathew Rushbrooke, Nicola Hamilton, Allan M. Jordan, Kate M. Smith, James R. Hitchin, Daniel P. Mould, Helen F. Small, Fabrice Turlais, Ian D. Waddell, Amanda J. Watson, Laura A. Maguire, Donald J. Ogilvie, Niall M. Hamilton, Ali Raoof
Publikováno v:
Journal of Medicinal Chemistry. 56:6352-6370
The recently discovered enzyme tyrosyl-DNA phosphodiesterase 2 (TDP2) has been implicated in the topoisomerase-mediated repair of DNA damage. In the clinical setting, it has been hypothesized that TDP2 may mediate drug resistance to topoisomerase II
Autor:
Gillian I. Rice, Marcin Szynkiewicz, Nicole Fabien, Patrick M. Gaffney, Sarah B. Daly, James O'Sullivan, Alexandre Belot, John Brognard, Shameem Fawdar, Pierre Cochat, Anne Perrine Foray, Jill E. Urquhart, Jonathan E. Dickerson, Natalie Stephenson, Marie Therese Zabot, Josephine Mayer, Flore Rozenberg, Paul R. Kasher, Graeme C.M. Black, Yanick J. Crow, Eleanor W. Trotter, Laurent Juillard, Anne Laure Debaud, Bruno Ranchin, Christophe Malcus, Michael W. Beresford, Pierre Lebon, Jean Francois Eliaou, Nathalie Bonnefoy, Bohdan Waszkowycz, Sanjeev S. Bhaskar, Céline René, Isabelle Rouvet, Leslie G. Biesecker, Anna A. Marusiak
Publikováno v:
Arthritis & Rheumatism. 65:2161-2171
Objective: Systemic lupus erythematosus (SLE) is a prototype autoimmune disease, assumed to occur due to a complex interplay of environmental and genetic factors. Rare causes of monogenic SLE have been described, providing unique insights into fundam
Autor:
John Brognard, Anna A. Marusiak, Bohdan Waszkowycz, Franziska Hanke, Natalie L. Stephenson, Shameem Fawdar, Eleanor W. Trotter, Crispin J. Miller, Sara Ientile, Yaoyong Li, Zoe C. Edwards
Publikováno v:
Proceedings of the National Academy of Sciences. 110:12426-12431
Approximately 70% of patients with non–small-cell lung cancer present with late-stage disease and have limited treatment options, so there is a pressing need to develop efficacious targeted therapies for these patients. This remains a major challen
Autor:
Guoqing Chen, Kexue Li, Zhulun Wang, Lawrence R. McGee, Timothy D. Cushing, Paul Faulder, Ben Fisher, John Eksterowicz, Merrill Ayres, Mohmed K. Anwer, Fei Lee, Jinsong Liu, Bohdan Waszkowycz, Steven M. Rubenstein, Youngsook Shin, Ellyn Farrelly, Olga Plotnikova, Shou-Hua Xiao, Athena Sudom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1238-1244
The discovery, structure-based design, synthesis, and optimization of NIK inhibitors are described. Our work began with an HTS hit, imidazopyridinyl pyrimidinamine 1. We utilized homology modeling and conformational analysis to optimize the indole sc
Autor:
Jonathan Gilley, Robert Adalbert, Jonathan Clark, Bohdan Waszkowycz, Melanie Wong, David E. Clark, Peter Lockey, Michael P. Coleman
Publikováno v:
Clark, D E, Waszkowycz, B, Wong, M, Lockey, P M, Adalbert, R, Gilley, J, Clark, J & Coleman, M P 2016, ' Application of virtual screening to the discovery of novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with potential for the treatment of cancer and axonopathies ', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 12, pp. 2920-2926 . https://doi.org/10.1016/j.bmcl.2016.04.039
NAMPT may represent a novel target for drug discovery in various therapeutic areas, including oncology and inflammation. Additionally, recent work has suggested that targeting NAMPT has potential in treating axon degeneration. In this work, publicly
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76067925156b34bd3fe4c153740dcd0e
https://www.repository.cam.ac.uk/handle/1810/276166
https://www.repository.cam.ac.uk/handle/1810/276166