Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140
Ghiboub, Mohammed, Koster, Jan, Craggs, Peter D, Li Yim, Andrew Y. F, Shillings, Anthony, Hutchinson, Sue, Bingham, Ryan P, Gatfield, Kelly, Hageman, Ishtu L, Yao, Gang, O'Keefe, Heather P, Coffin, Aaron, Patel, Amish, Sloan, Lisa A, Mitchell, Darren J, Hayhow, Thomas G, Lunven, Laurent, Watson, Robert J, Blunt, Christopher E, Harrison, Lee A, Bruton, Gordon, Kumar, Umesh, Hamer, Natalie, Spaull, John R, Zwijnenburg, Danny A, Welting, Olaf, Hakvoort, Theodorus B. M, te Velde, Anje A, van Limbergen, Johan, Henneman, Peter, Prinjha, Rab K, de Winther, Menno P. J, Harker, Nicola R, Tough, David F, de Jonge, Wouter J
Published in BMC biology (19.08.2022)
Published in BMC biology (19.08.2022)
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Journal Article
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor
Seal, Jonathan T, Atkinson, Stephen J, Aylott, Helen, Bamborough, Paul, Chung, Chun-wa, Copley, Royston C. B, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Lindon, Matthew, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors
Seal, Jonathan T, Atkinson, Stephen J, Bamborough, Paul, Bassil, Anna, Chung, Chun-wa, Foley, James, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Kruger, Ryan G, Matteo, Jeanne J, McCabe, Michael T, Messenger, Cassie, Mitchell, Darren, Phillipou, Alex, Preston, Alex, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Wyce, Anastasia, Zhang, Xi-Ping, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors
Aylott, Helen E, Atkinson, Stephen J, Bamborough, Paul, Bassil, Anna, Chung, Chun-wa, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Messenger, Cassie, Mitchell, Darren, Phillipou, Alexander, Preston, Alex, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Seal, Jonathan T, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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Journal Article
Design, Synthesis, and Characterization of I‑BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate
Humphreys, Philip G, Atkinson, Stephen J, Bamborough, Paul, Bit, Rino A, Chung, Chun-wa, Craggs, Peter D, Cutler, Leanne, Davis, Rob, Ferrie, Alan, Gong, GangLi, Gordon, Laurie J, Gray, Matthew, Harrison, Lee A, Hayhow, Thomas G, Haynes, Andrea, Henley, Nick, Hirst, David J, Holyer, Ian D, Lindon, Matthew J, Lovatt, Cerys, Lugo, David, McCleary, Scott, Molnar, Judit, Osmani, Qendresa, Patten, Chris, Preston, Alex, Rioja, Inmaculada, Seal, Jonathan T, Smithers, Nicholas, Sun, Fenglai, Tang, Dalin, Taylor, Simon, Theodoulou, Natalie H, Thomas, Clare, Watson, Robert J, Wellaway, Christopher R, Zhu, Linrong, Tomkinson, Nicholas C. O, Prinjha, Rab K
Published in Journal of medicinal chemistry (10.02.2022)
Published in Journal of medicinal chemistry (10.02.2022)
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Journal Article
Identification of a Series of N‑Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins
Harrison, Lee A, Atkinson, Stephen J, Bassil, Anna, Chung, Chun-wa, Grandi, Paola, Gray, James R. J, Levernier, Etienne, Lewis, Antonia, Lugo, David, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren J, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Seal, Jonathan T, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family
Preston, Alex, Atkinson, Stephen J, Bamborough, Paul, Chung, Chun-wa, Gordon, Laurie J, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Lewis, Antonia J, Lugo, David, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Rioja, Inmaculada, Seal, Jon, Taylor, Simon, Thesmar, Pierre, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in ACS medicinal chemistry letters (13.08.2020)
Published in ACS medicinal chemistry letters (13.08.2020)
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Journal Article
Discovery of Further Pyrrolidine trans-Lactams as Inhibitors of Human Neutrophil Elastase (HNE) with Potential as Development Candidates and the Crystal Structure of HNE Complexed with an Inhibitor (GW475151)
Macdonald, Simon J. F, Dowle, Michael D, Harrison, Lee A, Clarke, Geoffrey D. E, Inglis, Graham G. A, Johnson, Martin R, Shah, Pritom, Smith, Robin A, Amour, Augustin, Fleetwood, Gill, Humphreys, Davina C, Molloy, Christopher R, Dixon, Mary, Godward, Rosalind E, Wonacott, Alan J, Singh, Onkar M. P, Hodgson, Simon T, Hardy, George W
Published in Journal of medicinal chemistry (29.08.2002)
Published in Journal of medicinal chemistry (29.08.2002)
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Journal Article
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase—GW311616A a development candidate
Macdonald, Simon J.F, Dowle, Michael D, Harrison, Lee A, Shah, Pritom, Johnson, Martin R, Inglis, Graham G.A, Clarke, Geoffrey D.E, Smith, Robin A, Humphreys, Davina, Molloy, Christopher R, Amour, Augustin, Dixon, Mary, Murkitt, Graham, Godward, Rosalind E, Padfield, Tony, Skarzynski, Tadeusz, Singh, Onkar M.P, Kumar, K.Abhhilash, Fleetwood, Gill, Hodgson, Simon T, Hardy, George W, Finch, Harry
Published in Bioorganic & medicinal chemistry letters (09.04.2001)
Published in Bioorganic & medicinal chemistry letters (09.04.2001)
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Journal Article
A Flexible, Practical, and Stereoselective Synthesis of Enantiomerically Pure trans-5-Oxohexahydropyrrolo[3,2-b]pyrroles (Pyrrolidine-trans-lactams), a New Class of Serine Protease Inhibitors, Using Acyliminium Methodology
Macdonald, Simon J. F, Clarke, Geoffrey D. E, Dowle, Michael D, Harrison, Lee A, Hodgson, Simon T, Inglis, Graham G. A, Johnson, Martin R, Shah, Prit, Upton, Richard J, Walls, Steven B
Published in Journal of organic chemistry (09.07.1999)
Published in Journal of organic chemistry (09.07.1999)
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Journal Article
Syntheses of trans-5- Oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-Oxo-hexahydro-furo[3,2-b]pyrroles (Pyrrolidine trans-Lactams and trans-Lactones): New Pharmacophores for Elastase Inhibition
Macdonald, Simon J. F, Belton, David J, Buckley, Doreen M, Spooner, Julie E, Anson, Michael S, Harrison, Lee A, Mills, Keith, Upton, Richard J, Dowle, Michael D, Smith, Robin A, Molloy, Christopher R, Risley, Catherine
Published in Journal of medicinal chemistry (08.10.1998)
Published in Journal of medicinal chemistry (08.10.1998)
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Journal Article
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams
MACDONALD, Simon J. F, DOWLE, Michael D, MOLLOY, Christopher R, DIXON, Mary, MURKITT, Graham, GODWARD, Rosalind E, SKARZYNSKI, Tadeusz, SINGH, Onkar M. P, KUMAR, K. Abhhilash, HODGSON, Simon T, MCDONALD, Edward, HARDY, George W, HARRISON, Lee A, FINCH, Harry, SPOONER, Julie E, SHAH, Pritom, JOHNSON, Martin R, INGLIS, Graham G. A, CLARKE, Geoffrey D. E, BELTON, David J, SMITH, Robin A
Published in Bioorganic & medicinal chemistry letters (22.01.2001)
Published in Bioorganic & medicinal chemistry letters (22.01.2001)
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Journal Article
Discovery of a Brain-Penetrant S1P(3)-Sparing Direct Agonist of the S1P(1) and S1P(5) Receptors Efficacious at Low Oral Dose
Demont, Emmanuel H., Arpino, Sandra, Bit, Rino A., Campbell, Colin A., Deeks, Nigel, Desai, Sapna, Dowell, Simon J., Gaskin, Pam, Gray, James R. J., Harrison, Lee A., Haynes, Andrea, Heightman, Tom D., Holmes, Duncan S., Humphreys, Philip G., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Panchal, Terry, Philpott, Karen L., Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Journal Article
Discovery of a Brain-Penetrant S1P 3 -Sparing Direct Agonist of the S1P 1 and S1P 5 Receptors Efficacious at Low Oral Dose
Demont, Emmanuel H., Arpino, Sandra, Bit, Rino A., Campbell, Colin A., Deeks, Nigel, Desai, Sapna, Dowell, Simon J., Gaskin, Pam, Gray, James R. J., Harrison, Lee A., Haynes, Andrea, Heightman, Tom D., Holmes, Duncan S., Humphreys, Philip G., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Panchal, Terry, Philpott, Karen L., Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Journal Article
Three- Dimensional Synthetic Aperture Radar Image Formation
Harrison, Lee A., Marciszewski, Mateusz, Abreu, William
Published in 2024 International Applied Computational Electromagnetics Society Symposium (ACES) (19.05.2024)
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Published in 2024 International Applied Computational Electromagnetics Society Symposium (ACES) (19.05.2024)
Conference Proceeding
Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1 and S1P5 Receptors Efficacious at Low Oral Dose
Demont, Emmanuel H, Arpino, Sandra, Bit, Rino A, Campbell, Colin A, Deeks, Nigel, Desai, Sapna, Dowell, Simon J, Gaskin, Pam, Gray, James R. J, Harrison, Lee A, Haynes, Andrea, Heightman, Tom D, Holmes, Duncan S, Humphreys, Philip G, Kumar, Umesh, Morse, Mary A, Osborne, Greg J, Panchal, Terry, Philpott, Karen L, Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Journal Article
A novel series of arylpiperazines with high affinity and selectivity for the dopamine D3 receptor
John Murray, P., Harrison, Lee A., Johnson, Martin R., Robertson, Graeme M., Scopes, David I.C., Bull, David R., Graham, Elizabeth A., Hayes, Ann G., Kilpatrick, Gavin J., Daas, Izaak Den, Large, Charles, Sheehan, Michael J., Stubbs, Carole M., Turpin, Michael P.
Published in Bioorganic & medicinal chemistry letters (02.02.1995)
Published in Bioorganic & medicinal chemistry letters (02.02.1995)
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Journal Article
A novel series of arylpiperazines with high affinity and selectivity for the dopamine D 3 receptor
John Murray, P., Harrison, Lee A., Johnson, Martin R., Robertson, Graeme M., Scopes, David I.C., Bull, David R., Graham, Elizabeth A., Hayes, Ann G., Kilpatrick, Gavin J., Daas, Izaak Den, Large, Charles, Sheehan, Michael J., Stubbs, Carole M., Turpin, Michael P.
Published in Bioorganic & medicinal chemistry letters (02.02.1995)
Published in Bioorganic & medicinal chemistry letters (02.02.1995)
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Journal Article
Corrigendum to “Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine- trans-lactams” : [Bioorg. Med. Chem. Lett. 11 (2001) 243]
Macdonald, Simon J.F., Dowle, Michael D., Harrison, Lee A., Spooner, Julie E., Shah, Pritom, Johnson, Martin R., Inglis, Graham G.A., Clarke, Geoffrey D.E., Belton, David J., Smith, Robin A., Molloy, Christopher R., Dixon, Mary, Murkitt, Graham, Godward, Rosalind E., Skarzynski, Tadeusz, Singh, Onkar M.P., Kumar, K.Abhhilash, Hodgson, Simon T., McDonald, Edward, Hardy, George W., Finch, Harry, Humphreys, Davina C., Fleetwood, Gill
Published in Bioorganic & medicinal chemistry letters (01.05.2001)
Published in Bioorganic & medicinal chemistry letters (01.05.2001)
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Journal Article