RAF inhibitors that evade paradoxical MAPK pathway activation

Autor: K. B. Nolop, Garson Tsang, Yan Ma, Heidi Carias, D. Fong, Marika Nespi, Peter Hirth, Rafe Shellooe, Elizabeth A. Burton, Paul S. Lin, Jason Walters, Wayne Spevak, Todd Ewing, Ben Powell, Gideon Bollag, Hanna Cho, Womack Patrick, Bernice Matusow, Ying Zhang, Guoxian Wu, Jiazhong Zhang, Hamid Rezaei, Gary Conard Visor, Hoa Nguyen, Laura Sanftner, Brian L. West, Prabha N. Ibrahim, Gaston Habets, Weiru Wang, Jack Lin, Adhirai Marimuthu, James Tsai, Chao Zhang, Songyuan Shi, Emily Light

Publikováno v: Nature. 526:583-586

Oncogenic activation of BRAF fuels cancer growth by constitutively promoting RAS-independent mitogen-activated protein kinase (MAPK) pathway signalling. Accordingly, RAF inhibitors have brought substantially improved personalized treatment of metasta

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::295d12d8d17d3f824dfd2e4bd4b36dea
https://doi.org/10.1038/nature14982

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

Autor: Cromm, Philipp M., Crews, Craig M., Mainolfi, Nello, Rasmusson, Tim, Poulikakos, Poulikos I., Zhang, Chao, Bollag, Gideon, Shokat, Kevan M., Rosen, Neal, Agianian, Bogos, Gavathiotis, Evripidis, Raina, Kanak, Durrant, David E., Morrison, Deborah K., Neklesa, Taavi K., Winkler, James D., Chang, F., Steelman, L. S., Lee, J. T., Shelton, J. G., Navolanic, P. M., Blalock, W. L., Franklin, R. A., McCubrey, J. A., Burslem, George M., Smith, Blake E., Lai, Ashton C., Jaime-Figueroa, Saul, McQuaid, Daniel C., Bondeson, Daniel P., Toure, Momar, Dong, Hanqing, Qian, Yimin, Wang, Jing, Crew, Andrew P., Hines, John, Sanchez, Jaquelyn N., Wang, Ton, Cohen, Mark S., Shelledy, PharmD, Lindsay, Roman, PharmD, BCOP, Danielle, Davies, Helen, Bignell, Graham R., Cox, Charles, Stephens, Philip, Edkins, Sarah, Clegg, Sheila, Teague, Jon, Woffendin, Hayley, Garnett, Mathew J., Bottomley, William, Davis, Neil, Dicks, Ed, Ewing, Rebecca, Floyd, Yvonne, Gray, Kristian, Hall, Sarah, Hawes, Rachel, Hughes, Jaime, Kosmidou, Vivian, Menzies, Andrew, Mould, Catherine, Parker, Adrian, Stevens, Claire, Watt, Stephen, Hooper, Steven, Jayatilake, Hiran, Gusterson, Barry A., Cooper, Colin, Shipley, Janet, Hargrave, Darren, Pritchard-Jones, Katherine, Maitland, Norman, Chenevix-Trench, Georgia, Riggins, Gregory J., Bigner, Darell D., Palmieri, Giuseppe, Cossu, Antonio, Flanagan, Adrienne, Nicholson, Andrew, Ho, Judy W.C., Leung, Suet Y., Yuen, Siu T., Weber, Barbara L., Seigler, Hilliard F., Darrow, Timothy L., Paterson, Hugh, Wooster, Richard, Stratton, Michael R., Futreal, P. Andrew, Spevak, Wayne, Zhang, Ying, Burton, Elizabeth A., Ma, Yan, Habets, Gaston, Zhang, Jiazhong, Lin, Jack, Ewing, Todd, Matusow, Bernice, Tsang, Garson, Marimuthu, Adhirai, Cho, Hanna, Wu, Guoxian, Wang, Weiru, Fong, Daniel, Nguyen, Hoa, Shi, Songyuan, Womack, Patrick, Nespi, Marika, Shellooe, Rafe, Carias, Heidi, Powell, Ben, Light, Emily, Sanftner, Laura, Walters, Jason, Tsai, James, West, Brian L., Visor, Gary, Rezaei, Hamid, Lin, Paul S., Nolop, Keith, Ibrahim, Prabha N., Hirth, Peter, Arozarena, Imanol, Wellbrock, Claudia, Samatar, Ahmed A., Karoulia, Zoi, Chapman, Paul B., Hauschild, Axel, Robert, Caroline, Haanen, John B., Ascierto, Paolo, Larkin, James, Dummer, Reinhard, Garbe, Claus, Testori, Alessandro, Maio, Michele, Hogg, David, Lorigan, Paul, Lebbe, Celeste, Jouary, Thomas, Schadendorf, Dirk, Ribas, Antoni, O'Day, Steven J., Sosman, Jeffrey A., Kirkwood, John M., Eggermont, Alexander M.M., Dreno, Brigitte, Li, Jiang, Nelson, Betty, Hou, Jeannie, Lee, Richard J., Flaherty, Keith T., McArthur, Grant A., Vogelstein, Bert, Papadopoulos, Nickolas, Velculescu, Victor E., Zhou, Shibin, Diaz, Luis A., Kinzler, Kenneth W., Millington, G. W.M., Buhimschi, Alexandru D., Hamman, Brian D., Ishchenko, Alexey

Publikováno v: Cromm, P M, Crews, C M, Mainolfi, N, Rasmusson, T, Poulikakos, P I, Zhang, C, Bollag, G, Shokat, K M, Rosen, N, Crews, C M, Agianian, B, Gavathiotis, E, Raina, K, Crews, C M, Durrant, D E, Morrison, D K, Neklesa, T K, Winkler, J D, Crews, C M, Chang, F, Steelman, L S, Lee, J T, Shelton, J G, Navolanic, P M, Blalock, W L, Franklin, R A, McCubrey, J A, Burslem, G M, Smith, B E, Lai, A C, Jaime-Figueroa, S, McQuaid, D C, Bondeson, D P, Toure, M, Dong, H, Qian, Y, Wang, J, Crew, A P, Hines, J, Crews, C M, Sanchez, J N, Wang, T, Cohen, M S, Shelledy, PharmD, L, Roman, PharmD, BCOP, D, Davies, H, Bignell, G R, Cox, C, Stephens, P, Edkins, S, Clegg, S, Teague, J, Woffendin, H, Garnett, M J, Bottomley, W, Davis, N, Dicks, E, Ewing, R, Floyd, Y, Gray, K, Hall, S, Hawes, R, Hughes, J, Kosmidou, V, Menzies, A, Mould, C, Parker, A, Stevens, C, Watt, S, Hooper, S, Jayatilake, H, Gusterson, B A, Cooper, C, Shipley, J, Hargrave, D, Pritchard-Jones, K, Maitland, N, Chenevix-Trench, G, Riggins, G J, Bigner, D D, Palmieri, G, Cossu, A, Flanagan, A, Nicholson, A, Ho, J W C, Leung, S Y, Yuen, S T, Weber, B L, Seigler, H F, Darrow, T L, Paterson, H, Wooster, R, Wooster, R, Stratton, M R, Futreal, P A, Zhang, C, Spevak, W, Zhang, Y, Burton, E A, Ma, Y, Habets, G, Zhang, J, Lin, J, Ewing, T, Matusow, B, Tsang, G, Marimuthu, A, Cho, H, Wu, G, Wang, W, Fong, D, Nguyen, H, Shi, S, Womack, P, Nespi, M, Shellooe, R, Carias, H, Powell, B, Light, E, Sanftner, L, Walters, J, Tsai, J, West, B L, Visor, G, Rezaei, H, Lin, P S, Nolop, K, Ibrahim, P N, Hirth, P, Bollag, G, Arozarena, I, Wellbrock, C, Samatar, A A, Poulikakos, P I, Karoulia, Z, Gavathiotis, E, Poulikakos, P I, Chapman, P B, Hauschild, A, Robert, C, Haanen, J B, Ascierto, P, Larkin, J, Dummer, R, Garbe, C, Testori, A, Maio, M, Hogg, D, Lorigan, P, Lebbe, C, Jouary, T, Schadendorf, D, Ribas, A, O'Day, S J, Sosman, J A, Kirkwood, J M, Eggermont, A M M, Dreno, B, Nolop, K, Li, J, Nelson, B, Hou, J, Lee, R J, Flaherty, K T, McArthur, G A, Vogelstein, B, Papadopoulos, N, Velculescu, V E, Zhou, S, Diaz, L A, Kinzler, K W, Millington, G W M, Bondeson, D P, Smith, B E, Burslem, G M, Buhimschi, A D, Hines, J, Jaime-Figueroa, S, Wang, J, Hamman, B D, Ishchenko, A & Crews, C M 2018, ' The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study ', Cell Chemical Biology, pp. 67-77.e3 . https://doi.org/10.1016/j.chembiol.2017.09.009

Proteolysis targeting chimera (PROTAC) technology has emerged over the last two decades as a powerful tool for targeted degradation of endogenous proteins. Herein we describe the development of PROTACs for receptor tyrosine kinases, a protein family

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::361df2b1e3e643d7e80d0d128cb88ce3
https://doi.org/10.1016/j.chembiol.2017.09.009

Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent

Autor: Brian L. West, Weiru Wang, D. Erbe, John Cantwell, Ben Powell, J. Arnold, M. Perreault, B.P. England, G. P. Vlasuk, Womack Patrick, Michael V. Milburn, J. Kral, Kam Y. J. Zhang, Prabha N. Ibrahim, K. P. Hirth, Alexander N. Plotnikov, D. Fong, Shenghua Shi, Adhirai Marimuthu, S. Will, K. B. Nolop, Dean R. Artis, H.I. Krupka, Gaston Habets, C. Settachatgull, James Tobin, M. Signaevsky, J. J. Lin, Angela Oh, Hoa Nguyen, Gideon Bollag, U. Mehra, Chao Zhang, D. S. Yan

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America. 106(1)

In a search for more effective anti-diabetic treatment, we used a process coupling low-affinity biochemical screening with high-throughput co-crystallography in the design of a series of compounds that selectively modulate the activities of all three

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3efd4191219eb4895f357d4c4cb6cd2
https://pubmed.ncbi.nlm.nih.gov/19116277

Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3

Autor: Swahn, Britt-Marie, Huerta, Fernando, Kallin, Elisabet, Malmström, Jonas, Weigelt, Tatjana, Viklund, Jenny, Womack, Patrick, Xue, Yafeng, Öhberg, Liselotte

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 2005 15(22):5095-5099