Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Ian Edward David Smith"'
Autor:
Don T. Fisher, Gillian F. Watt, Ian Churcher, Laurie J. Gordon, Andrea D Gonçalves, Alina Mares, Phoebe Dace, Rakesh Nagilla, Bartholomew J. Votta, Ian Edward David Smith, John D. Harling, Pamela A. Haile, Afjal Hussain Miah, Paul Giffen, Paul Scott-Stevens, Aditya R. Thawani, Mark David Rackham, Jane Denyer
Publikováno v:
Journal of Medicinal Chemistry. 64:12978-13003
Receptor-interacting serine/threonine protein kinase 2 (RIPK2) is an important kinase of the innate immune system. Herein, we describe the optimization of a series of RIPK2 PROTACs which recruit members of the inhibitor of apoptosis (IAP) family of E
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd70a2b845dd3036fbf167fdc5991ce9
https://doi.org/10.1021/acs.jmedchem.1c01118
https://doi.org/10.1021/acs.jmedchem.1c01118
Autor:
Peter Stacey, Gopal P. Sapkota, Georgina Green, Hannah Lithgow, Marcel Muelbaier, Glenn A. Burley, Andrew B. Benowitz, Ian Edward David Smith, Xiao Qing Lewell, Ryan Whatling, Markus A. Queisser, Agnieszka Konopacka, Robert P. Law, Stephen Besley, John D. Harling, Sascha Röth
Publikováno v:
SLAS Discovery. 26:885-895
Targeted protein degradation is an emerging new strategy for the modulation of intracellular protein levels with applications in chemical biology and drug discovery. One approach to enable this strategy is to redirect the ubiquitin-proteasome system
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a25d36af593c2fa67d1af3c8cf9adc5d
https://doi.org/10.1177/24725552211017517
https://doi.org/10.1177/24725552211017517
Autor:
Jenni Cryan, Don T. Fisher, Michael Reilly, Ian Edward David Smith, Anna Vossenkämper, Gillian F. Watt, Ian Churcher, John D. Harling, Allison M. Beal, Thomas T. MacDonald, Alina Mares, Phoebe Dace, Bartholomew J. Votta, Marcus Bantscheff, Jane Denyer, Paul Scott-Stevens, Afjal Hussain Miah, Andrew B. Benowitz, Aditya R. Thawani, Carol A. Capriotti, Mark David Rackham, Nico Zinn, Pamela A. Haile
Publikováno v:
Communications Biology, Vol 3, Iss 1, Pp 1-13 (2020)
Communications Biology
Communications Biology
Proteolysis-Targeting Chimeras (PROTACs) are heterobifunctional small-molecules that can promote the rapid and selective proteasome-mediated degradation of intracellular proteins through the recruitment of E3 ligase complexes to non-native protein su
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db0dc940ac613e6d44979be8bc358056
http://link.springer.com/article/10.1038/s42003-020-0868-6
http://link.springer.com/article/10.1038/s42003-020-0868-6
Autor:
Harley Green, Lydia Barnes, Jolyon Matthews-Wright, Rachel Szpara, Luke Francis, Nuria S. Lima, Hollie Blaber, Carrie K. W. Wong, Alexander Seal, Charlotte S. Payne, Matthew F. Meehan, C. Elizabeth Killalea, Rohan J. Trainor, Katherine Wood, Jack M. J. Grace, Oliver Williams, Liam Cochrane, Edmund J. P. Hogarth, Katherine Louise Jones, Zoe J. Lee, Shusha Mahdy, Anna Gruszka, Lisa Morrison, Freya Taday, Leyla Jusu, Oliver King, May-Li Mackinnon, Joe Stillibrand, Daniel Buckley, Edward Cooney, Z.A. Henley, Simon J. F. Macdonald, Christina L. Long, Daniel Fu He, Craig Pike, Zoe C. Byron, Keenan M. Smith, Ian Edward David Smith, Antony M. Threadgould, Lewis Byers, Kamile Stanelyte, Hal R. I. Parke, Nick Barton, Rosa Cookson, James E. Rowedder, Andrew Nortcliffe, Aaron J. Senior, Alan Nadin, Makenzie J. Millward, Joseph Lambert, Lawrence Payne, David T. K. Brooks, Christopher Merrett, Heather A. Damian, Jordan Waters, Richard G. Chilvers
Publikováno v:
Journal of Medicinal Chemistry. 62:10402-10422
Phosphoinositide-3-kinase δ (PI3Kδ) is a critical regulator of cell growth and transformation and has been explored as a therapeutic target for a range of diseases. Through the exploration of the t...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e3c565e07f6df53b788d687eb5d9b250
https://doi.org/10.1021/acs.jmedchem.9b01499
https://doi.org/10.1021/acs.jmedchem.9b01499
Autor:
John D. Harling, Hannah Lithgow, William J. Kerr, Marcus Bantscheff, Zuni I. Bassi, Marcel Muelbaier, Han Dai, Ian Edward David Smith, Christopher P. Tinworth, Sophie E. Hughes, Lars Dittus, Glenn A. Burley
The impact of covalent binding on PROTAC-mediated degradation of BTK was investigated through the preparation of both covalent binding and reversible binding PROTACs derived from the covalent BTK inhibitor ibrutinib. It was determined that a covalent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16bdbf2c7c16f7218b63c1d96ac63bb6
https://strathprints.strath.ac.uk/67192/1/Tinworth_etal_ACS_CB_2019_PROTAC_mediated_degradation_of_Brutons_tyrosine_kinase.pdf
https://strathprints.strath.ac.uk/67192/1/Tinworth_etal_ACS_CB_2019_PROTAC_mediated_degradation_of_Brutons_tyrosine_kinase.pdf
Autor:
Chuck Poole, Alan R. Rendina, Andrew L. Larkin, Heather Hobbs, Helen F. Sneddon, Lee T. Schaller, Gordon Saxty, Jonathan P. Hutchinson, David N. Deaton, Jeffrey Guss, Young Do, Tianshun Xu, Karen Affleck, Simon Teanby Hodgson, Stephen A. Thomson, H. Fritz Kramer, Caterina Musetti, Peckham Gregory, Ian Edward David Smith, Melanie Leveridge, Harry Nicholls, Jason A. Holt, Don O. Somers, Ying Shen, J. Darren Stuart, Sorif Uddin, Anne Cleasby, Paul N. Mortenson, Caroline Richardson, Daniel J. Price, Lisa M. Shewchuk, Eugene L. Stewart, Michael R. Jeune, David Anders, Lisa A. Orband-Miller, Ashley Paul Hancock, Paris Ward, Joseph W. Wilson
Publikováno v:
Bioorganicmedicinal chemistry. 27(8)
With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits were sorted
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19cd1125a360e08da732c75d2aa1d7f2
https://pubmed.ncbi.nlm.nih.gov/30858025
https://pubmed.ncbi.nlm.nih.gov/30858025
Autor:
Natasha Routly, Giovanna Bergamini, Jeffrey L. Gustafson, Ko Eunhwa, Kristoffer Famm, Paola Grandi, John J. Flanagan, Daniel P. Bondeson, Maria Faelth-Savitski, Afjal Hussain Miah, Nico Zinn, Deborah A. Gordon, Craig M. Crews, Laurens Kruidenier, Paul S. Carter, Ian Edward David Smith, Marcus Bantscheff, Alina Mares, Dennis L. Buckley, John D. Harling, Linda N. Casillas, Sebastien Andre Campos, Ryan R. Willard, Bartholomew J. Votta, Willem den Besten, Satoko Shimamura, Carly S. Cox, Ian Churcher, Katie E Mulholland
Publikováno v:
Nature Chemical Biology. 11:611-617
The current predominant therapeutic paradigm is based on maximizing drug-receptor occupancy to achieve clinical benefit. This strategy, however, generally requires excessive drug concentrations to ensure sufficient occupancy, often leading to adverse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91cded625a4a254a72d85709b447840b
https://doi.org/10.1038/nchembio.1858
https://doi.org/10.1038/nchembio.1858
A series of aromatic heterocycles, thiazoles, imidazoles, and dimethoxyindoles, can be synthesised directly from alkenes via a ketoiodination-cyclisation protocol. The alkene starting materials are themselves easily accessible by many different and w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07ba58a59c851722ce544403843565a8
https://doi.org/10.1055/s-0030-1259034
https://doi.org/10.1055/s-0030-1259034
Autor:
Jeffrey L. Gustafson, Ian Edward David Smith, Kanak Raina, Craig M. Crews, John Hines, John D. Harling, Dennis L. Buckley, Afjal Hussain Miah, Nicole Darricarrère
Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use of PROTACs, heterobifunctional molecules that can recruit specific E3 l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::177c0160bb8c80ad3723f2efae7df395
https://europepmc.org/articles/PMC4629848/
https://europepmc.org/articles/PMC4629848/
Publikováno v:
Tetrahedron: Asymmetry. 20:723-725
The preparation of enantiomerically pure threo-β-amino-α-hydroxy acids via 1,3-dipolar cycloadditions of imine dipolarophiles with the chiral isomunchnone derived from (5R)-5-phenylmorpholin-3-one 1 is described. The cycloadducts were obtained with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e3fdd0073fd6b703ad88f8c3ea1bd319
https://doi.org/10.1016/j.tetasy.2009.02.029
https://doi.org/10.1016/j.tetasy.2009.02.029