Protein degradation induced by PROTAC molecules as an emerging drug discovery strategy

Autor: Mladen Koravovic, Bojan Markovic, Milena Kovacevic, Milena Rmandic, Gordana Tasic

Publikováno v: Journal of the Serbian Chemical Society

The traditional concept of drug discovery is based on the occupancydriven pharmacology model. It implies the development of inhibitors occupying binding sites that directly affect protein functions. Therefore, proteins that do not have such binding s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99948ebd7001ecd84f7e2d326e658ef9
https://farfar.pharmacy.bg.ac.rs/handle/123456789/4296

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

Tento výsledek nelze pro nepřihlášené uživatele zobrazit.
K zobrazení výsledku je třeba se přihlásit.