Zobrazeno 1 - 10
of 76
pro vyhledávání: '"Andrew, Madin"'
Autor:
Amanda J. Kennedy, Linda Sundström, Stefan Geschwindner, Eunice K. Y. Poon, Yuhong Jiang, Rongfeng Chen, Rob Cooke, Shawn Johnstone, Andrew Madin, Junxian Lim, Qingqi Liu, Rink-Jan Lohman, Anneli Nordqvist, Maria Fridén-Saxin, Wenzhen Yang, Dean G. Brown, David P. Fairlie, Niek Dekker
Publikováno v:
Communications Biology, Vol 3, Iss 1, Pp 1-13 (2020)
Kennedy et al. report the pharmacological and in vivo profiling of two small molecule PAR2 inhibitors and an agonist. They conclude that while the small molecule agonist and one of the inhibitors bind to the orthosteric PAR2 binding site, the other i
Externí odkaz:
https://doaj.org/article/e6a39fb1480d47f3b76e5e7e14d4b26c
Autor:
Grace Q. Gong, Benoit Bilanges, Ben Allsop, Glenn R. Masson, Victoria Roberton, Trevor Askwith, Sally Oxenford, Ralitsa R. Madsen, Sarah E. Conduit, Dom Bellini, Martina Fitzek, Matt Collier, Osman Najam, Zhenhe He, Ben Wahab, Stephen H. McLaughlin, A. W. Edith Chan, Isabella Feierberg, Andrew Madin, Daniele Morelli, Amandeep Bhamra, Vanesa Vinciauskaite, Karen E. Anderson, Silvia Surinova, Nikos Pinotsis, Elena Lopez-Guadamillas, Matthew Wilcox, Alice Hooper, Chandni Patel, Maria A. Whitehead, Tom D. Bunney, Len R. Stephens, Phillip T. Hawkins, Matilda Katan, Derek M. Yellon, Sean M. Davidson, David M. Smith, James B. Phillips, Richard Angell, Roger L. Williams, Bart Vanhaesebroeck
Publikováno v:
Nature. 618:159-168
Autor:
Neil T. Thompson, David R. Newell, Christopher Murray, Julie Irving, John Lyons, Eddy Freyne, Edward J. Lewis, Jose Cosme, Andrew Pike, Brent L. Graham, Lindsay A. Devine, Susanne Bethell, Abarna Thiru, Ruth Feltell, Darcey Miller, Maria Carr, Sharna Rich, Michael A. Batey, Christopher Hamlett, Michael Reader, Martyn Frederickson, Alistair O'Brien, Emma Vickerstaffe, Rajdeep K. Benning, Andrew Madin, Charlotte Griffiths Jones, Douglas Ross, Lynsey Fazal, Tim Perera, Patrick Angibaud, Peter King, Anne Cleasby, Valerio Berdini, Gordan Saxty, George Ward, Matthew Squires
We describe here the identification and characterization of 2 novel inhibitors of the fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases. The compounds exhibit selective inhibition of FGFR over the closely related VEGFR2 rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::605eebdec9c9d2137ffcbba68a3b82cd
https://doi.org/10.1158/1535-7163.c.6535227
https://doi.org/10.1158/1535-7163.c.6535227
Autor:
Neil T. Thompson, David R. Newell, Christopher Murray, Julie Irving, John Lyons, Eddy Freyne, Edward J. Lewis, Jose Cosme, Andrew Pike, Brent L. Graham, Lindsay A. Devine, Susanne Bethell, Abarna Thiru, Ruth Feltell, Darcey Miller, Maria Carr, Sharna Rich, Michael A. Batey, Christopher Hamlett, Michael Reader, Martyn Frederickson, Alistair O'Brien, Emma Vickerstaffe, Rajdeep K. Benning, Andrew Madin, Charlotte Griffiths Jones, Douglas Ross, Lynsey Fazal, Tim Perera, Patrick Angibaud, Peter King, Anne Cleasby, Valerio Berdini, Gordan Saxty, George Ward, Matthew Squires
PDF file - 475K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fe1a33d4a31585a984d85c6194526c9
https://doi.org/10.1158/1535-7163.22496319
https://doi.org/10.1158/1535-7163.22496319
Autor:
Bryan K. Chan, Eileen Seward, Michael Lainchbury, Thomas F. Brewer, Le An, Toby Blench, Matthew W. Cartwright, Grace Ka Yan Chan, Edna F. Choo, Jason Drummond, Richard L. Elliott, Emanuela Gancia, Lewis Gazzard, Baihua Hu, Graham E. Jones, Xifeng Luo, Andrew Madin, Sushant Malhotra, John G. Moffat, Jodie Pang, Laurent Salphati, Christopher J. Sneeringer, Craig E. Stivala, Binqing Wei, Weiru Wang, Ping Wu, Timothy P. Heffron
Publikováno v:
ACS Med Chem Lett
[Image: see text] Hematopoietic progenitor kinase 1 (HPK1) is implicated as a negative regulator of T-cell receptor-induced T-cell activation. Studies using HPK1 kinase-dead knock-in animals have demonstrated the loss of HPK1 kinase activity resulted
Autor:
Michael J. Waring, Andrew Madin, James H. Hunter, Garry Pairaudeau, Andreas Brunschweiger, Harriet A. Stanway-Gordon, Marco Potowski
Publikováno v:
The Journal of Organic Chemistry. 86:17930-17935
DNA-encoded libraries (DELs) offer great promise for the discovery of new ligands for proteins. Many current reactions used for DEL synthesis do not proceed efficiently over a wide range of substrates. Combining a diverse array of multicomponent reac
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:
Dean G. Brown, Wenzhen Yang, Rongfeng Chen, Shawn Donald Johnstone, Maria Fridén-Saxin, Stefan Geschwindner, Anneli Nordqvist, Junxian Lim, Linda Sundström, Yuhong Jiang, Qingqi Liu, David P. Fairlie, Rob Cooke, Andrew Madin, Rink-Jan Lohman, Amanda J. Kennedy, Eunice K. Y. Poon, Niek Dekker
Publikováno v:
Communications Biology, Vol 3, Iss 1, Pp 1-13 (2020)
Communications Biology
Communications Biology
Protease-activated receptor-2 (PAR2) has been implicated in multiple pathophysiologies but drug discovery is challenging due to low small molecule tractability and a complex activation mechanism. Here we report the pharmacological profiling of a pote
Autor:
Avipsa Ghosh, Sudhir M. Hande, Amber Balazs, Derek Barratt, Sabina Cosulich, Barry Davies, Sébastien Degorce, Kevin Embrey, Sonja Gill, Anders Gunnarsson, Giuditta Illuzzi, Peter Johnström, Jordan Lane, Carrie Larner, Rachel Lawrence, Elisabetta Leo, Andrew Madin, Elizabeth Martin, Lisa McWilliams, Lenka O’Connor, Mark O’Connor, Jonathan Orme, Fiona Pachl, Martin Packer, Andy Pike, Philip Rawlins, Marianne Schimpl, Magnus Schou, Anna Staniszewska, Wenzhan Yang, James Yates, Andrew Zhang, XiaoLa Zheng, Stephen Fawell, Petra Hamerlik, Jeffrey Johannes
Publikováno v:
Cancer Research. 82:6302-6302
PARP inhibitors exploit defects in DNA repair pathways to selectively target cancerous cells via PARP1 catalytic inhibition and PARP1 trapping onto the DNA. All known clinical PARP1 inhibitors bind at the same site at the catalytic center of the enzy
Autor:
David M. Smith, Gregory Weitsman, Michael Hirsch, Ambrosius P. Snijders, Svend Kjaer, Roger George, Peter J. Parker, Shahid Mehmood, Daniel J. Rolfe, Marisa L. Martin-Fernandez, Jeroen Claus, Tony Ng, Selene K. Roberts, Martina Fitzek, Laura C. Zanetti-Domingues, Audrey Colomba, Andrew Madin
Publikováno v:
Biochemical Journal
Despite being catalytically defective, pseudokinases are typically essential players of cellular signalling, acting as allosteric regulators of their active counterparts. Deregulation of a growing number of pseudokinases has been linked to human dise