Zobrazeno 1 - 10
of 36
pro vyhledávání: '"Kevin J. Embrey"'
Autor:
Adriana E. Tron, Matthew A. Belmonte, Ammar Adam, Brian M. Aquila, Lawrence H. Boise, Elisabetta Chiarparin, Justin Cidado, Kevin J. Embrey, Eric Gangl, Francis D. Gibbons, Gareth P. Gregory, David Hargreaves, J. Adam Hendricks, Jeffrey W. Johannes, Ricky W. Johnstone, Steven L. Kazmirski, Jason G. Kettle, Michelle L. Lamb, Shannon M. Matulis, Ajay K. Nooka, Martin J. Packer, Bo Peng, Philip B. Rawlins, Daniel W. Robbins, Alwin G. Schuller, Nancy Su, Wenzhan Yang, Qing Ye, Xiaolan Zheng, J. Paul Secrist, Edwin A. Clark, David M. Wilson, Stephen E. Fawell, Alexander W. Hird
Publikováno v:
Nature Communications, Vol 9, Iss 1, Pp 1-14 (2018)
High expression of Mcl-1 promotes tumorigenesis and resistance to anticancer therapies. Here they report a macrocyclic molecule with high selectivity and affinity for Mcl-1 that exhibits potent anti-tumor effects as single agent and in combination wi
Externí odkaz:
https://doaj.org/article/814ff3ef6b204d84917e2b025f3e1da9
Autor:
Sven Wernersson, Romel Bobby, Liz Flavell, Alexander G. Milbradt, Geoffrey A. Holdgate, Kevin J. Embrey, Mikael Akke
Publikováno v:
Biochemistry. 61:2303-2318
The bromodomain and extra-terminal (BET) protein BRD4 regulates gene expression via recruitment of transcriptional regulatory complexes to acetylated chromatin. Like other BET proteins, BRD4 contains two bromodomains, BD1 and BD2, that can interact c
Autor:
Jeffrey W. Johannes, Fiona Pachl, Amber Balazs, Tieguang Yao, C. Larner, Lisa McWilliams, Marianne Schimpl, Scott W. Martin, Kevin J. Embrey, Tom D. Heightman, Paul Hemsley, Jonathan P. Orme, Derek Barratt, Giuditta Illuzzi, Andrew Madin, Paolo Di Fruscia, Avipsa Ghosh, Martin J. Packer, Scott D. Edmondson, Elisabetta Leo, Xiaolan Zheng, Matthew D. Chuba, Xiaohui Pei, Mark J. O'Connor, Verity Talbot, Ke Zhang, Stephen Fawell, Elizabeth Underwood, Anna Staniszewska, Lina Liu, Lin Xue, Sonja J. Gill, Anders Gunnarsson, Andrew Pike, Susan E. Critchlow, Jeffrey G. Varnes, Andrew X. Zhang, Sébastien L. Degorce, J. Lane, Sudhir M. Hande, Hongyao She, Sabina Cosulich, Michal Bista
Publikováno v:
Journal of Medicinal Chemistry. 64:14498-14512
Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA mutation. However, some have failed in combination with first-line chemotherapies, usually
Autor:
Simon C. C. Lucas, Ulf Börjesson, Mark J. Bostock, John Cuff, Fredrik Edfeldt, Kevin J. Embrey, Per-Olof Eriksson, Andrea Gohlke, Anders Gunnarson, Michael Lainchbury, Alexander G. Milbradt, Rachel Moore, Philip B. Rawlins, Ian Sinclair, Christopher Stubbs, R. Ian Storer
Publikováno v:
RSC Med Chem
Fragment based drug discovery is a critical part of the lead generation toolbox and relies heavily on a readily available, high quality fragment library. Over years of use, the AstraZeneca fragment set had become partially depleted and instances of c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::446ddff84fa8641f08a20b101425dc2e
https://europepmc.org/articles/PMC9491351/
https://europepmc.org/articles/PMC9491351/
Autor:
Marie-France Langelier, Michael McCauley, Elizabeth Underwood, Laura E. Easton, Ji-Chun Yang, David Neuhaus, Kevin J. Embrey, Philip B. Rawlins, John M. Pascal, Marianne Schimpl, Tom E. H. Ogden
Publikováno v:
Nucleic Acids Research
PARP-1 is a key early responder to DNA damage in eukaryotic cells. An allosteric mechanism links initial sensing of DNA single-strand breaks by PARP-1’s F1 and F2 domains via a process of further domain assembly to activation of the catalytic domai
Autor:
Iacovos N Michaelides, Christopher D. Stubbs, Puneet Khurana, Kun Song, Kevin J. Embrey, R. Ian Storer, Christopher R. Phillips, Gavin W. Collie, Ian L. Dale, Arjan Snijder, Louise Barlind, Ulf Börjesson
Publikováno v:
ACS Medicinal Chemistry Letters
We report here a fragment screen directed toward the c-MET kinase from which we discovered a series of inhibitors able to bind to a rare conformation of the protein in which the P-loop adopts a collapsed, or folded, arrangement. Preliminary SAR explo
Publikováno v:
ADMET and DMPK
Volume 7
Issue 4
ADMET and DMPK, Vol 7, Iss 4, Pp 222-241 (2019)
Volume 7
Issue 4
ADMET and DMPK, Vol 7, Iss 4, Pp 222-241 (2019)
Biophysical methods such as mass spectrometry, surface plasmon resonance, nuclear magnetic resonance, and both differential scanning isothermal titration calorimetry are now well established as key components of the early drug discovery process. Thes
Autor:
Nancy Su, Brian Aquila, Gareth P. Gregory, Stephen Fawell, J. Adam Hendricks, Ammar Adam, Lawrence H. Boise, Jeffrey W. Johannes, Kevin J. Embrey, Edwin Clark, Philip B. Rawlins, Justin Cidado, Francis D. Gibbons, Ricky W. Johnstone, Qing Ye, Elisabetta Chiarparin, Steven L. Kazmirski, Michelle Lamb, J. Paul Secrist, Wenzhan Yang, Alexander Hird, Daniel W. Robbins, Adriana E. Tron, Alwin Schuller, Martin J. Packer, David J. Hargreaves, Xiaolan Zheng, Matthew A. Belmonte, Eric Gangl, Ajay K. Nooka, Shannon M. Matulis, Jason Grant Kettle, Bo Peng, David Matthew Wilson
Publikováno v:
Nature Communications, Vol 9, Iss 1, Pp 1-14 (2018)
Nature Communications
Nature Communications
Mcl-1 is a member of the Bcl-2 family of proteins that promotes cell survival by preventing induction of apoptosis in many cancers. High expression of Mcl-1 causes tumorigenesis and resistance to anticancer therapies highlighting the potential of Mcl
Autor:
Mark J. O'Connor, Philip B. Rawlins, Kevin J. Embrey, Anders Gunnarsson, Sudhir M. Hande, Anna Staniszewska, Fiona Pachl, Andrew X. Zhang, Jonathan P. Orme, Giuditta Illuzzi, Lisa McWilliams, Sonja J. Gill, Jeffrey W. Johannes, J. Lane, Sébastien L. Degorce, Amber Balazs, Martin J. Packer, Andrew Madin, Marianne Schimpl, Andrew Pike, Elisabetta Leo, Xiaolan Zheng, Avipsa Ghosh, C. Larner
Publikováno v:
Cancer Research. 81:296-296
Since the approval of olaparib in 2014 for BRCA mutated (BRCAm) ovarian cancer, many PARP inhibitors have been developed and have seen widespread success. However, as a class, these drugs are not without adverse events which have limited their abilit
Autor:
Pavel Macek, Jonathan P. Waltho, J. Willem M. Nissink, Matthew J. Cliff, Kevin J. Embrey, Rick Davies, Martin Blackledge, Stanislava Panova, Malene Ringkjøbing Jensen
Publikováno v:
Structure
Structure, Elsevier (Cell Press), 2019, 27 (10), pp.1537-1546.e4. ⟨10.1016/j.str.2019.07.006⟩
Panova, S, Cliff, M, Macek, P, Blackledge, M, Jensen, M R, Nissink, J W M, Embrey, K J, Davies, R & Waltho, J 2019, ' Mapping hidden residual structure within the Myc bHLH-LZ domain using chemical denaturant titration ', Structure . https://doi.org/10.1016/j.str.2019.07.006
Structure, 2019, 27 (10), pp.1537-1546.e4. ⟨10.1016/j.str.2019.07.006⟩
Structure, Elsevier (Cell Press), 2019, 27 (10), pp.1537-1546.e4. ⟨10.1016/j.str.2019.07.006⟩
Panova, S, Cliff, M, Macek, P, Blackledge, M, Jensen, M R, Nissink, J W M, Embrey, K J, Davies, R & Waltho, J 2019, ' Mapping hidden residual structure within the Myc bHLH-LZ domain using chemical denaturant titration ', Structure . https://doi.org/10.1016/j.str.2019.07.006
Structure, 2019, 27 (10), pp.1537-1546.e4. ⟨10.1016/j.str.2019.07.006⟩
International audience; Intrinsically disordered proteins (IDPs) underpin biological regulation and hence are highly desirable drug-development targets. NMR is normally the tool of choice for studying the conformational preferences of IDPs, but the a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2279504f4c486d035e0b61eb94e5db50
https://hal.univ-grenoble-alpes.fr/hal-03016176/document
https://hal.univ-grenoble-alpes.fr/hal-03016176/document