Search Results - "Belshaw, Simone"

Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer by Unbekandt, Mathieu, Belshaw, Simone, Bower, Justin, Clarke, Maeve, Cordes, Jacqueline, Crighton, Diane, Croft, Daniel R, Drysdale, Martin J, Garnett, Mathew J, Gill, Kathryn, Gray, Christopher, Greenhalgh, David A, Hall, James A M, Konczal, Jennifer, Lilla, Sergio, McArthur, Duncan, McConnell, Patricia, McDonald, Laura, McGarry, Lynn, McKinnon, Heather, McMenemy, Carol, Mezna, Mokdad, Morrice, Nicolas A, Munro, June, Naylor, Gregory, Rath, Nicola, Schüttelkopf, Alexander W, Sime, Mairi, Olson, Michael F

“…The myotonic dystrophy-related Cdc42-binding kinases MRCKα and MRCKβ contribute to the regulation of actin-myosin cytoskeleton organization and dynamics,…”
Get full text

A novel small-molecule MRCK inhibitor blocks cancer cell invasion by Unbekandt, Mathieu, Croft, Daniel R, Crighton, Diane, Mezna, Mokdad, McArthur, Duncan, McConnell, Patricia, Schüttelkopf, Alexander W, Belshaw, Simone, Pannifer, Andrew, Sime, Mairi, Bower, Justin, Drysdale, Martin, Olson, Michael F

“…The myotonic dystrophy kinase-related CDC42-binding kinases MRCKα and MRCKβ regulate actin-myosin contractility and have been implicated in cancer metastasis…”
Get full text

Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys by Hoyt, Scott B, Park, Min K, London, Clare, Xiong, Yusheng, Tata, Jim, Bennett, D. Jonathan, Cooke, Andrew, Cai, Jiaqiang, Carswell, Emma, Robinson, John, MacLean, John, Brown, Lindsay, Belshaw, Simone, Clarkson, Thomas R, Liu, Kun, Liang, Gui-Bai, Struthers, Mary, Cully, Doris, Wisniewski, Tom, Ren, Ning, Bopp, Charlene, Sok, Andrea, Cai, Tian-Quan, Stribling, Sloan, Pai, Lee-Yuh, Ma, Xiuying, Metzger, Joe, Verras, Andreas, McMasters, Daniel, Chen, Qing, Tung, Elaine, Tang, Wei, Salituro, Gino, Buist, Nicole, Kuethe, Jeff, Rivera, Nelo, Clemas, Joe, Zhou, Gaochao, Gibson, Jack, Maxwell, Carrie Ann, Lassman, Mike, McLaughlin, Theresa, Castro-Perez, Jose, Szeto, Daphne, Forrest, Gail, Hajdu, Richard, Rosenbach, Mark, Ali, Amjad

“…We report the discovery of a benzimidazole series of CYP11B2 inhibitors. Hit-to-lead and lead optimization studies identified compounds such as 32, which…”
Get full text

Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors by Cai, Jiaqiang, Robinson, John, Belshaw, Simone, Everett, Kathryn, Fradera, Xavier, van Zeeland, Mario, van Berkom, Leon, van Rijnsbergen, Peter, Popplestone, Lucy, Baugh, Mark, Dempster, Maureen, Bruin, John, Hamilton, William, Kinghorn, Emma, Westwood, Paul, Kerr, Jennifer, Rankovic, Zoran, Arbuckle, Wullie, Bennett, D. Jonathan, Jones, Philip S., Long, Clive, Martin, Iain, Uitdehaag, Joost C.M., Meulemans, Tommi

“…By using a small atom (Cl, F, or Me) to increase the torsion angle between the phenyl ring and the attached secondary amide, trifluoromethylphenyl motif was…”
Get full text

1H-Imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: Separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pkₐ by Arbuckle, Wullie, Baugh, Mark, Belshaw, Simone, Bennett, D. Jonathan, Bruin, John, Cai, Jiaqiang, Cameron, Kenneth S, Claxton, Chris, Dempster, Maureen, Everett, Kathryn, Fradera, Xavier, Hamilton, William, Jones, Philip S, Kinghorn, Emma, Long, Clive, Martin, Iain, Robinson, John, Westwood, Paul

“…Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pkₐ of basic nitrogen containing cathepsin S inhibitors, a set of…”
Get full text

1H-Imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: Separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pk sub(a) by Arbuckle, Wullie, Baugh, Mark, Belshaw, Simone, Bennett, DJonathan, Bruin, John, Cai, Jiaqiang, Cameron, Kenneth S, Claxton, Chris, Dempster, Maureen, Everett, Kathryn, Fradera, Xavier, Hamilton, William, Jones, Philip S, Kinghorn, Emma, Long, Clive, Martin, Iain, Robinson, John, Westwood, Paul

“…Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pk sub(a) of basic nitrogen containing cathepsin S inhibitors, a set of…”
Get full text

1 H-Imidazo[4,5- c]pyridine-4-carbonitrile as cathepsin S inhibitors: Separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen p k a by Arbuckle, Wullie, Baugh, Mark, Belshaw, Simone, Bennett, D. Jonathan, Bruin, John, Cai, Jiaqiang, Cameron, Kenneth S., Claxton, Chris, Dempster, Maureen, Everett, Kathryn, Fradera, Xavier, Hamilton, William, Jones, Philip S., Kinghorn, Emma, Long, Clive, Martin, Iain, Robinson, John, Westwood, Paul

“…Based on the theoretical understanding of the in vivo lysosomotropism, by manipulating the p k a of the cathepsin S inhibitors, a set of compounds with p k a…”
Get full text