Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Rebecca H Graves"'
Autor:
Alison E. John, Rebecca H. Graves, K. Tao Pun, Giovanni Vitulli, Ellen J. Forty, Paul F. Mercer, Josie L. Morrell, John W. Barrett, Rebecca F. Rogers, Maryam Hafeji, Lloyd I. Bibby, Elaine Gower, Valerie S. Morrison, Yim Man, James A. Roper, Jeni C. Luckett, Lee A. Borthwick, Ben S. Barksby, Rachel A. Burgoyne, Rory Barnes, Joelle Le, David J. Flint, Susan Pyne, Anthony Habgood, Louise A. Organ, Chitra Joseph, Rochelle C. Edwards-Pritchard, Toby M. Maher, Andrew J. Fisher, Natasja Stæhr Gudmann, Diana J. Leeming, Rachel C. Chambers, Pauline T. Lukey, Richard P. Marshall, Simon J. F. Macdonald, R. Gisli Jenkins, Robert J. Slack
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-14 (2020)
The αvβ6 integrin is key in activating the pro-fibrotic cytokine TGFβ in idiopathic pulmonary fibrosis. Here, the authors show an inhaled small molecule αvβ6 inhibitor GSK3008348 induces prolonged inhibition of TGFβ signaling pathways in human
Externí odkaz:
https://doaj.org/article/0b6e5916f4cb4d2e9b4186f07f1b86ee
Autor:
Natasja Stæhr Gudmann, Richard P. Marshall, Jeni Luckett, Rebecca F. Rogers, Robert J. Slack, Simon J. F. Macdonald, Diana Julie Leeming, Rachel C. Chambers, Joelle Le, Pauline T. Lukey, Anthony Habgood, Paul F. Mercer, Rachel A. Burgoyne, Ben S. Barksby, Lloyd I. Bibby, Yim Man, Maryam Hafeji, Andrew J. Fisher, David J. Flint, Toby M. Maher, Louise Organ, Susan Pyne, Lee A. Borthwick, James A. Roper, Valerie S. Morrison, Alison E. John, Giovanni Vitulli, Rebecca H. Graves, Rochelle C. Edwards-Pritchard, R. Gisli Jenkins, John Barrett, Josie Morrell, K. Tao Pun, Elaine Gower, Rory Barnes, Ellen J. Forty, Chitra Joseph
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-14 (2020)
Nature Communications
Nature Communications
The αvβ6 integrin plays a key role in the activation of transforming growth factor-β (TGFβ), a pro-fibrotic mediator that is pivotal to the development of idiopathic pulmonary fibrosis (IPF). We identified a selective small molecule αvβ6 RGD-mi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e5b4959cf67302e9783a88dddd530b0b
https://doaj.org/article/0b6e5916f4cb4d2e9b4186f07f1b86ee
https://doaj.org/article/0b6e5916f4cb4d2e9b4186f07f1b86ee
Autor:
Chris D. Edwards, Edward Taylor, Rebecca H Graves, Olivia J. Robb, Brett O'Brien, Andrew W Harrell, Edith M. Hessel, Augustin Amour, Aarti Patel, Neil A Miller
Publikováno v:
Clinical pharmacokinetics. 61(2)
Physiologically based pharmacokinetic (PBPK) modelling has evolved to accommodate different routes of drug administration and enables prediction of drug concentrations in tissues as well as plasma. The inhalation route of administration has proven su
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d81f740786cad5a758f64fe8d78e115d
https://pubmed.ncbi.nlm.nih.gov/34458976
https://pubmed.ncbi.nlm.nih.gov/34458976
Autor:
Rebecca H. Graves, Panayiotis A. Procopiou, Simon Teanby Hodgson, Afjal Hussain Miah, Jonathan M. Percy, Aurelie C. Champigny
Publikováno v:
Bioorganicmedicinal chemistry. 25(20)
A novel 4-aminoindazole sulfonamide hit (13) was identified as a human CCR4 antagonists from testing a focussed library of compounds in the primary GTPγS assay. Replacing the indazole core with a pyrazolopyrimidine, and introduction of a methoxy gro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3143f291710aea03db432202ed36e178
https://pubmed.ncbi.nlm.nih.gov/28801066
https://pubmed.ncbi.nlm.nih.gov/28801066
Autor:
John Barrett, Catherine Nye, Don O. Somers, Roberto Solari, John D. Harling, Sebastien Andre Campos, Rachel Grimley, Rebecca H. Graves, Christina M. Bessant, Angela M. Deakin, Laura Hanns, William J. Kerr, Oxana Polyakova, Nick Barton, Laiq Chaudry
Publikováno v:
Journal of Biological Chemistry. 288:28195-28206
IL-2-inducible tyrosine kinase (Itk) plays a key role in antigen receptor signaling in T cells and is considered an important target for anti-inflammatory drug discovery. In order to generate inhibitors with the necessary potency and selectivity, a c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3ae4f29a0279ef07ef494bc4aa68fb8c
https://doi.org/10.1074/jbc.m113.474114
https://doi.org/10.1074/jbc.m113.474114
Autor:
Rebecca H. Graves, Alan P. Hill, David E. Clapham, Steven L. Sollis, Karen M. L. Morriss, Robert J. Slack, Nick Barton, Ashley Paul Hancock, Heather Hobbs, Afjal Hussain Miah, Coline Jumeaux, Alison J. Ford, Claire E. Smith, Deborah Needham, Emma B. Sheriff, Panayiotis A. Procopiou, Simon Teanby Hodgson, John Barrett, Malcolm Begg, David A. Hall, Yannick M. L. Lacroix, Royston C. B. Copley, Hugo Staton
Publikováno v:
Journal of Medicinal Chemistry. 56:1946-1960
A series of indazole arylsulfonamides were synthesized and examined as human CCR4 antagonists. Methoxy- or hydroxyl-containing groups were the more potent indazole C4 substituents. Only small groups were tolerated at C5, C6, or C7, with the C6 analog
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ae8d8293ba0da5bc006f2fa7aeae3c0
https://doi.org/10.1021/jm301572h
https://doi.org/10.1021/jm301572h
Autor:
Rebecca H. Graves, Elaine Gower, Richard P. Marshall, Pan Procopiou, Andrew J. Fisher, Giovanni Vitulli, Ellen J. Forty, Tao Pun, Steve Ludbrook, Simon J. F. Macdonald, Anderson Niall Andrew, Jane Denyer, Alison E. John, David C. Budd, Susan Pyne, Gisli Jenkins, John Pritchard, Pauline T. Lukey, David J. Flint, John Marshall, Rachel C. Chambers, Valerie S. Morrison, Carmel B. Nanthakumar, Paul F. Mercer, Robert J. Slack
Publikováno v:
QJM: An International Journal of Medicine.
Fibrosis is the formation of scar tissue due to injury or long-term inflammation and is a leading cause of morbidity and mortality in disorders that include IPF. The αvβ6 integrin has been identified as playing a key role in the activation of TGFβ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7464da6e9014e4cc1e1841f8366720bf
https://doi.org/10.1093/qjmed/hcw120.013
https://doi.org/10.1093/qjmed/hcw120.013
Autor:
Jonathan M. Percy, Simon Teanby Hodgson, Sean M. Lynn, Brian Evans, Panayiotis A. Procopiou, Rebecca H. Graves, Laura Ajram, Stephen A. Richards, Afjal Hussain Miah, Malcolm Begg, Robert J. Slack, Lena Shukla
A number of potent 2,8-diazaspiro[4.5]decan-8-yl)pyrimidin-4-amine CCR4 antagonists binding to the extracellular allosteric site were synthesised. (R)-N-(2,4-Dichlorobenzyl)-2-(2-(pyrrolidin-2-ylmethyl)-2,8-diazaspiro[4.5]decan-8-yl)pyrimidin-4-amine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e553624afbf87efcffffc8f5b3ffa92
https://strathprints.strath.ac.uk/57543/1/Shukla_etal_EJMC2016_2_8_Diazaspiro_4.5_decan_8_yl_pyrimidin_4_amine_potent_CCR4.pdf
https://strathprints.strath.ac.uk/57543/1/Shukla_etal_EJMC2016_2_8_Diazaspiro_4.5_decan_8_yl_pyrimidin_4_amine_potent_CCR4.pdf
Autor:
David A. Hall, Yannick M. L. Lacroix, Alison J. Ford, Deborah Needham, Rebecca H. Graves, Robert J. Slack, Panayiotis A. Procopiou, Simon Teanby Hodgson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2730-2733
Synthesis and preliminary SAR of the N1 substituent of a novel series of indazole sulfonamide chemokine receptor 4 (CCR4) antagonist is reported. Compound 7r was identified for further development.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5236d775d1e575285ec5ad4362f26615
https://doi.org/10.1016/j.bmcl.2012.02.104
https://doi.org/10.1016/j.bmcl.2012.02.104
Autor:
Anthony Cahn, Simon Teanby Hodgson, Rebecca H. Graves, Steve Hughes, Joanna Watson, Misba Beerahee, Robert Wilson, Sjoerd van Marle, Roberto Solari, Jonathan Robertson, Graeme Young, David A. Hall
Publikováno v:
BMC Pharmacology & Toxicology
Background The CC-chemokine receptor 4 (CCR4) is thought potentially to play a critical role in asthma pathogenesis due to its ability to recruit type 2 T-helper lymphocytes to the inflamed airways. Therefore, CCR4 provides an excellent target for an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2df3b428d2aef98dcf9516eecf37ca87
https://pubmed.ncbi.nlm.nih.gov/23448278
https://pubmed.ncbi.nlm.nih.gov/23448278