Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Alan T. Henley"'
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:
A. Elisa Pasqua, Swee Y. Sharp, Nicola E. A. Chessum, Angela Hayes, Loredana Pellegrino, Michael J. Tucker, Asadh Miah, Birgit Wilding, Lindsay E. Evans, Carl S. Rye, N. Yi Mok, Manjuan Liu, Alan T. Henley, Sharon Gowan, Emmanuel De Billy, Robert te Poele, Marissa Powers, Suzanne A. Eccles, Paul A. Clarke, Florence I. Raynaud, Paul Workman, Keith Jones, Matthew D. Cheeseman
Publikováno v:
Journal of Medicinal Chemistry. 66:5907-5936
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::719374538241e3474602d329b097d75c
https://doi.org/10.1021/acs.jmedchem.3c00156
https://doi.org/10.1021/acs.jmedchem.3c00156
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:
Florence I. Raynaud, Johann S. de Bono, Paul Workman, Stan B. Kaye, Suzanne A. Eccles, Bart Vanhaesebroeck, Mika Derynck, Lori Friedman, Richard D. Baird, Alexis de Haven Brandon, Gary Box, Melanie Valenti, Alan T. Henley, Yasmin J. Asad, Joo Chew Ang, Rupinder Pandher, Joo Ern Ang
Metabolite changes that constitute the Venn diagram in Figure 2. Significant changes listed are reductions (labelled "-1") or increases (labelled "1") in concentrations relative to the relevant controls.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35242fa0e3a742cbb6b034b2187e5495
https://doi.org/10.1158/1535-7163.22503601
https://doi.org/10.1158/1535-7163.22503601
Autor:
Florence I. Raynaud, Johann S. de Bono, Paul Workman, Stan B. Kaye, Suzanne A. Eccles, Bart Vanhaesebroeck, Mika Derynck, Lori Friedman, Richard D. Baird, Alexis de Haven Brandon, Gary Box, Melanie Valenti, Alan T. Henley, Yasmin J. Asad, Joo Chew Ang, Rupinder Pandher, Joo Ern Ang
Summary of baseline reproducibility of candidate plasma metabolite biomarkers (n=17 patients).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca4f1e3fff57a56a184d3e834e92b978
https://doi.org/10.1158/1535-7163.22503598.v1
https://doi.org/10.1158/1535-7163.22503598.v1
Autor:
Florence I. Raynaud, Johann S. de Bono, Paul Workman, Stan B. Kaye, Suzanne A. Eccles, Bart Vanhaesebroeck, Mika Derynck, Lori Friedman, Richard D. Baird, Alexis de Haven Brandon, Gary Box, Melanie Valenti, Alan T. Henley, Yasmin J. Asad, Joo Chew Ang, Rupinder Pandher, Joo Ern Ang
Characteristics of dose-dependent changes in candidate plasma metabolite pharmacodynamic biomarker concentrations in 41 patients, as determined on day 1 of pictilisib clinical trial. Cells with p-values
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4068e9bc95db86ee6248750810664f56
https://doi.org/10.1158/1535-7163.22503595
https://doi.org/10.1158/1535-7163.22503595
Autor:
Florence I. Raynaud, Johann S. de Bono, Paul Workman, Stan B. Kaye, Suzanne A. Eccles, Bart Vanhaesebroeck, Mika Derynck, Lori Friedman, Richard D. Baird, Alexis de Haven Brandon, Gary Box, Melanie Valenti, Alan T. Henley, Yasmin J. Asad, Joo Chew Ang, Rupinder Pandher, Joo Ern Ang
Changes in candidate plasma metabolite pharmacodynamic biomarker concentrations over first 2 weeks in 17 patients treated with {greater than or equal to}330 mg once-daily of pictilisib. Cells with p-values
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::146f091d32f617a6f33545ed2ab9f842
https://doi.org/10.1158/1535-7163.22503592.v1
https://doi.org/10.1158/1535-7163.22503592.v1
Autor:
Florence I. Raynaud, Johann S. de Bono, Paul Workman, Stan B. Kaye, Suzanne A. Eccles, Bart Vanhaesebroeck, Mika Derynck, Lori Friedman, Richard D. Baird, Alexis de Haven Brandon, Gary Box, Melanie Valenti, Alan T. Henley, Yasmin J. Asad, Joo Chew Ang, Rupinder Pandher, Joo Ern Ang
Heat map of changes (relative to vehicle control) in candidate plasma and tumor metabolite biomarkers at 8 hours post-dosing of mice bearing U87MG xenografts with pictilisib 75mg/kg or buparlisib 60mg/kg (a, acyl; aa, acyl-acyl; ae, acyl-alkyl; Cx:y,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::783e2038908da754470e738776ff331e
https://doi.org/10.1158/1535-7163.22503604
https://doi.org/10.1158/1535-7163.22503604
Autor:
Florence I. Raynaud, Johann S. de Bono, Paul Workman, Stan B. Kaye, Suzanne A. Eccles, Bart Vanhaesebroeck, Mika Derynck, Lori Friedman, Richard D. Baird, Alexis de Haven Brandon, Gary Box, Melanie Valenti, Alan T. Henley, Yasmin J. Asad, Joo Chew Ang, Rupinder Pandher, Joo Ern Ang
Changes in plasma metabolites across timepoints by patient/sample.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3403e56e36b8dc398b621ff78430c7a3
https://doi.org/10.1158/1535-7163.22503589.v1
https://doi.org/10.1158/1535-7163.22503589.v1