Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Olivier A. Pierrat"'
Autor:
Olivier A. Pierrat, Manjuan Liu, Gavin W. Collie, Kartika Shetty, Matthew J. Rodrigues, Yann-Vaï Le Bihan, Emma A. Gunnell, P. Craig McAndrew, Mark Stubbs, Martin G. Rowlands, Norhakim Yahya, Erald Shehu, Rachel Talbot, Lisa Pickard, Benjamin R. Bellenie, Kwai-Ming J. Cheung, Ludovic Drouin, Paolo Innocenti, Hannah Woodward, Owen A. Davis, Matthew G. Lloyd, Ana Varela, Rosemary Huckvale, Fabio Broccatelli, Michael Carter, David Galiwango, Angela Hayes, Florence I. Raynaud, Christopher Bryant, Steven Whittaker, Olivia W. Rossanese, Swen Hoelder, Rosemary Burke, Rob L. M. van Montfort
Publikováno v:
Scientific Reports, Vol 12, Iss 1, Pp 1-15 (2022)
Abstract By suppressing gene transcription through the recruitment of corepressor proteins, B-cell lymphoma 6 (BCL6) protein controls a transcriptional network required for the formation and maintenance of B-cell germinal centres. As BCL6 deregulatio
Externí odkaz:
https://doaj.org/article/0430233ed30549f9969eadd4d689eff3
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones
Autor:
Alice C. Harnden, Owen A. Davis, Gary M. Box, Angela Hayes, Louise D. Johnson, Alan T. Henley, Alexis K. de Haven Brandon, Melanie Valenti, Kwai-Ming J. Cheung, Alfie Brennan, Rosemary Huckvale, Olivier A. Pierrat, Rachel Talbot, Michael D. Bright, Hafize Aysin Akpinar, Daniel S. J. Miller, Dalia Tarantino, Sharon Gowan, Selby de Klerk, Peter Craig McAndrew, Yann-Vaï Le Bihan, Mirco Meniconi, Rosemary Burke, Vladimir Kirkin, Rob L. M. van Montfort, Florence I. Raynaud, Olivia W. Rossanese, Benjamin R. Bellenie, Swen Hoelder
Publikováno v:
Journal of Medicinal Chemistry. 66:5892-5906
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c9094aa8cbb7b8cceb3273b677e3d3d9
https://doi.org/10.1021/acs.jmedchem.3c00155
https://doi.org/10.1021/acs.jmedchem.3c00155
Autor:
Owen A. Davis, Kwai-Ming J. Cheung, Alfie Brennan, Matthew G. Lloyd, Matthew J. Rodrigues, Olivier A. Pierrat, Gavin W. Collie, Yann-Vaï Le Bihan, Rosemary Huckvale, Alice C. Harnden, Ana Varela, Michael D. Bright, Paul Eve, Angela Hayes, Alan T. Henley, Michael D. Carter, P. Craig McAndrew, Rachel Talbot, Rosemary Burke, Rob L. M. van Montfort, Florence I. Raynaud, Olivia W. Rossanese, Mirco Meniconi, Benjamin R. Bellenie, Swen Hoelder
Publikováno v:
Journal of Medicinal Chemistry. 65:8169-8190
To identify new chemical series with enhanced binding affinity to the BTB domain of B-cell lymphoma 6 protein, we targeted a subpocket adjacent to Val18. With no opportunities for strong polar interactions, we focused on attaining close shape complem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3f6c02b01eed5ce5ede7cf979780c4e
https://doi.org/10.1021/acs.jmedchem.1c02174
https://doi.org/10.1021/acs.jmedchem.1c02174
Autor:
Rosemary Huckvale, Alice C. Harnden, Kwai-Ming J. Cheung, Olivier A. Pierrat, Rachel Talbot, Gary M. Box, Alan T. Henley, Alexis K. de Haven Brandon, Albert E. Hallsworth, Michael D. Bright, Hafize Aysin Akpinar, Daniel S. J. Miller, Dalia Tarantino, Sharon Gowan, Angela Hayes, Emma A. Gunnell, Alfie Brennan, Owen A. Davis, Louise D. Johnson, Selby de Klerk, Craig McAndrew, Yann-Vaï Le Bihan, Mirco Meniconi, Rosemary Burke, Vladimir Kirkin, Rob L. M. van Montfort, Florence I. Raynaud, Olivia W. Rossanese, Benjamin R. Bellenie, Swen Hoelder
Publikováno v:
Journal of Medicinal Chemistry. 65:8191-8207
The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. Herein, we report the optimization of our previously reported benzimidazolone molecular glue-type degrader
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c69d8cef8cdf04211cefb44860e5b55b
https://doi.org/10.1021/acs.jmedchem.1c02175
https://doi.org/10.1021/acs.jmedchem.1c02175
Autor:
Rob L. M. van Montfort, Kwai-Ming J. Cheung, L. Johnson, Mirco Meniconi, Florence I. Raynaud, P. Craig McAndrew, Rosemary Huckvale, Gavin W. Collie, Alan T. Henley, Olivier A. Pierrat, Emma Gunnell, Michael Carter, Matthew J. Rodrigues, Yann-Vaï Le Bihan, Mahad Gatti Iou, Matthew Garth Lloyd, Angela Hayes, Benjamin R. Bellenie, Rosemary Burke, Rachel Talbot, Olivia W. Rossanese, Michael D. Bright, Swen Hoelder, Owen Alexander Davis
Publikováno v:
Journal of Medicinal Chemistry
'Journal of Medicinal Chemistry ', vol: 64, pages: 17079-17097 (2021)
'Journal of Medicinal Chemistry ', vol: 64, pages: 17079-17097 (2021)
We describe the optimization of modestly active starting points to potent inhibitors of BCL6 by growing into a subpocket, which was occupied by a network of five stably bound water molecules. Identifying potent inhibitors required not only forming ne
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bcc591a63ed4a3f1d0ac4656dc9e279
http://europepmc.org/articles/PMC8667045
http://europepmc.org/articles/PMC8667045
Autor:
G. Meirion Richards, Arjun Thapaliya, Esther N. Arwert, Gary Newton, Bradleigh Whitton, Kathy Tomlin, Rosemary Burke, Rajesh Chopra, A. Elisa Pasqua, Matthew D. Cheeseman, Rob L. M. van Montfort, Erald Shehu, Angela Hayes, Agi Skawinska, Tamas Hahner, Keith Jones, Ramya Salimraj, Birgit Wilding, Florence I. Raynaud, Olivier A. Pierrat, Nicola E. A. Chessum
Publikováno v:
Bioorganic & Medicinal Chemistry Letters
Graphical abstract
ERAP1 is a zinc-dependent M1-aminopeptidase that trims lipophilic amino acids from the N-terminus of peptides. Owing to its importance in the processing of antigens and regulation of the adaptive immune response, dysregulation
ERAP1 is a zinc-dependent M1-aminopeptidase that trims lipophilic amino acids from the N-terminus of peptides. Owing to its importance in the processing of antigens and regulation of the adaptive immune response, dysregulation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ecdf1f131211583813ef222c70721360
http://europepmc.org/articles/PMC8188423
http://europepmc.org/articles/PMC8188423
Autor:
Benjamin R, Bellenie, Kwai-Ming J, Cheung, Ana, Varela, Olivier A, Pierrat, Gavin W, Collie, Gary M, Box, Michael D, Bright, Sharon, Gowan, Angela, Hayes, Matthew J, Rodrigues, Kartika N, Shetty, Michael, Carter, Owen A, Davis, Alan T, Henley, Paolo, Innocenti, Louise D, Johnson, Manjuan, Liu, Selby, de Klerk, Yann-Vaï, Le Bihan, Matthew G, Lloyd, P Craig, McAndrew, Erald, Shehu, Rachel, Talbot, Hannah L, Woodward, Rosemary, Burke, Vladimir, Kirkin, Rob L M, van Montfort, Florence I, Raynaud, Olivia W, Rossanese, Swen, Hoelder
Publikováno v:
Journal of Medicinal Chemistry
Deregulation of the transcriptional repressor BCL6 enables tumorigenesis of germinal center B-cells, and hence BCL6 has been proposed as a therapeutic target for the treatment of diffuse large B-cell lymphoma (DLBCL). Herein we report the discovery o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b69bcc50adc7e246cbc1312a1fd83ac1
https://pubmed.ncbi.nlm.nih.gov/32275432
https://pubmed.ncbi.nlm.nih.gov/32275432
Publikováno v:
Bioscience Reports
The exon junction complex (EJC) is the main mechanism by which cells select specific mRNAs\ud for translation into protein. We hypothesized that the EJC is involved in the regulation\ud of gene expression during the stress response in cardiac myocyte
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a22211da12eeea01b9d8cfbaca5cb7f2
https://doi.org/10.1042/bsr20170707
https://doi.org/10.1042/bsr20170707
Publikováno v:
Structure(London, England:1993)
Summary Rhomboids are evolutionarily conserved serine proteases that cleave transmembrane proteins within the membrane. The increasing number of known rhomboid functions in prokaryotes and eukaryotes makes them attractive drug targets. Here, we descr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b488863601b8f8253eb52ccd48d78610
https://doi.org/10.1016/j.str.2013.03.013
https://doi.org/10.1016/j.str.2013.03.013
Autor:
Jonathan M. Large, Ela Smiljanic, Kvido Strisovsky, Nathalie Bouloc, Matthew Freeman, Keith H. Ansell, Olivier A. Pierrat, Yonka Christova
Publikováno v:
ACS Chemical Biology
Rhomboids are relatively recently discovered intramembrane serine proteases that are conserved throughout evolution. They have a wide range of biological functions, and there is also much speculation about their potential medical relevance. Although
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b05d9a444b673fff86360ed54e8b61f3
https://doi.org/10.1021/cb100314y
https://doi.org/10.1021/cb100314y