Discovery of novel biaryl sulfonamide based Mcl-1 inhibitors

Autor: Bruce Follows, Shawn Fessler, Timm Baumeister, Ann-Marie Campbell, Mary Margaret Zablocki, Hongbin Li, Deepali Gotur, Zhongguo Wang, Xiaozhang Zheng, Lisa Molz, Cokey Nguyen, Torsten Herbertz, Liann Wang, Kenneth Bair

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 29:2375-2382

Mcl-1 is an anti-apoptotic protein overexpressed in hematological malignancies and several human solid tumors. Small molecule inhibition of Mcl-1 would offer an effective therapy to Mcl-1 mediated resistance. Subsequently, it has been the target of e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c397dc7a19ede1383733b944a5d0534
https://doi.org/10.1016/j.bmcl.2019.06.008

A global benchmark study using affinity-based biosensors

Autor: Aykut Üren, Stephen G. Brohawn, Eva Muñoz, Kenneth Miller, Mike Scott, Heather Hughes, Yasmina Noubia Abdiche, Rohn Lee Millican, Anne W Emerick, Jonathan Brooks, Michael B. Murphy, Charlene S. Lee, Carmelo Di Primo, Joshua Ballard, Quyhn Trinh, Giuseppe A. Papalia, Cynthia S. Hinck, Kevin Thompson, Peter Flynn, Joshua S. Klein, Martin A. Wear, Mark Toews, Richard N. Bohnsack, Mohammed Yousef, Daniel Malashock, Gaetano Barbato, Jill Raymond, Alison Joyce, Min Hsiang Yang, Julie Rothacker, Patrick England, Ashique Rafique, Jacinto López-Sagaseta, Scott L. Klakamp, Daulet Satpaev, Monica Dines, Danny Terwey, Islay Campbell, Joshua Thompson, Ben Busby, Tanmoy Ganguly, Gerardo Gutierrez-Sanchez, Sergei Shikov, Kevin Lindquist, Momchilo Vuyisich, Asya Grinberg, Krista Witte, Yun Hee Cho, Yue Ji Li, Hubert Mantz, Ewa Pol, Gonzalo Obal, Brian J. Pak, María J. Hernáiz, Peter Kainz, Erk Gedig, Mary M. Murphy, Tsafir Bravman, Janus Krarup, Gabrielle Zeder-Lutz, John Quinn, Thomas E. Ryan, Pietro Brandani, Dawn Kernaghan, Anca Clabbers, M. Brent Waddell, Agnes Puskas, Petr Skládal, Sanjay Nilapwar, Kara Herlihy, Gregor Anderluh, Federico Torta, Eric Hommema, Andrej Bavdek, Rejane Guimaraes, Anthony M. Giannetti, Eric Fang, Henrik Anderson, Anne Birgitte Bagge Hagel, Schuyler B Corry, Mark R. Witmer, Phillippe Neuner, Sébastien Wieckowski, Nico Dankbar, Alanna Pinkerton, Suparna Mundodo, Trevor D. Chapman, Sylvie Canepa, Satya P. Yadav, Rostislav Skrabana, Oleksandr Kalyuzhniy, Phini S Katsamba, Vidya Chandrasekaran, Eugene G. Chomey, Dana Reichmann, Katy McGirr, Dotzlaf Joe Edward, Mireille Baltzinger, Ite A. Laird-Offringa, Liann Wang, Erica Boni, Tiffany Tsang, Zaneta Nikolovska-Coleska, Andreas Schoenemann, Yuki Abe, Jamie Furneisen, Kenneth T. Lewis, Eileen M. Lafer, John Corbin, Satyen Gautam, Yuguo Feng, Olan Dolezal, Sylviane Hoos, James R. Horn, Bianca Beusink, Jinlin Peng, Otto Pritsch, Kristian H. Schlick, Ryan James Darling, Malgorzata Mikolajczyk, Quincy L. Carter, Jason T. Schuman, Yang Liu, Abdelkrim Khadir, Loïc Martin, Mark Alan Lewis, Ganeshram Krishnamoorthy, Andrew W. Drake, Jason Baardsnes, George Korza, Jesper Pass, Judie Berlier, Melicia Gainey, Nguyen Ly, James R. Partridge, Rosy Calvert, Roberta D'Agata, Rebecca L. Rich, Monica E. Ferreira, Phillip Page, Frank John Podlaski, Jay Duffner, Ruchira Das Gupta, Melanie Wong, Sergei Bibikov, Jiejin Li, Paola Torreri, Bruce A. Andrien, Peter Spies, Christina Boozer, David G. Myszka

Publikováno v: Analytical Biochemistry
Analytical Biochemistry, Elsevier Masson, 2009, 386 (2), pp.194-216. ⟨10.1016/j.ab.2008.11.021⟩
Analytical biochemistry, 386(2):10.1016/j.ab.2008.11.021, 194-216. Academic Press Inc.
Analytical Biochemistry, 2009, 386 (2), pp.194-216. ⟨10.1016/j.ab.2008.11.021⟩
Rich, R L, Papalia, G A, Flynn, P J, Furneisen, J, Quinn, J, Klein, J S, Katsamba, P S, Waddell, M B, Scott, M, Thompson, J, Berlier, J, Corry, S, Baltzinger, M, Zeder-Lutz, G, Schoenemann, A, Clabbers, A, Wieckowski, S, Murphy, M M, Page, P, Ryan, T E, Duffner, J, Ganguly, T, Corbin, J, Gautam, S, Anderluh, G, Bavdek, A, Reichmann, D, Yadav, S P, Hommema, E, Pol, E, Drake, A, Klakamp, S, Chapman, T, Kernaghan, D, Miller, K, Schuman, J, Lindquist, K, Herlihy, K, Murphy, M B, Bohnsack, R, Andrien, B, Brandani, P, Terwey, D, Millican, R, Darling, R J, Wang, L, Carter, Q, Dotzlaf, J, Lopez-Sagaseta, J, Campbell, I, Torreri, P, Hoos, S, England, P, Liu, Y, Abdiche, Y, Malashock, D, Pinkerton, A, Wong, M, Lafer, E, Hinck, C, Thompson, K, Primo, C D, Joyce, A, Brooks, J, Torta, F, Bagge Hagel, A B, Krarup, J, Pass, J, Ferreira, M, Shikov, S, Mikolajczyk, M, Abe, Y, Barbato, G, Giannetti, A M, Krishnamoorthy, G, Beusink, B, Satpaev, D, Tsang, T, Fang, E, Partridge, J, Brohawn, S, Horn, J, Pritsch, O, Obal, G, Nilapwar, S, Busby, B, Gutierrez-Sanchez, G, Gupta, R D, Canepa, S, Witte, K, Nikolovska-Coleska, Z, Cho, Y H, D'Agata, R, Schlick, K, Calvert, R, Munoz, E M, Hernaiz, M J, Bravman, T, Dines, M, Yang, M-H, Puskas, A, Boni, E, Li, J, Wear, M, Grinberg, A, Baardsnes, J, Dolezal, O, Gainey, M, Anderson, H, Peng, J, Lewis, M, Spies, P, Trinh, Q, Bibikov, S, Raymond, J, Yousef, M, Chandrasekaran, V, Feng, Y, Emerick, A, Mundodo, S, Guimaraes, R, McGirr, K, Li, Y-J, Hughes, H, Mantz, H, Skrabana, R, Witmer, M, Ballard, J, Martin, L, Skladal, P, Korza, G, Laird-Offringa, I, Lee, C S, Khadir, A, Podlaski, F, Neuner, P, Rothacker, J, Rafique, A, Dankbar, N, Kainz, P, Gedig, E, Vuyisich, M, Boozer, C, Ly, N, Toews, M, Uren, A, Kalyuzhniy, O, Lewis, K, Chomey, E, Pak, B J & Myszka, D G 2009, ' A global benchmark study using affinity-based biosensors ', Analytical Biochemistry, vol. 386, no. 2, pp. 194-216 . https://doi.org/10.1016/j.ab.2008.11.021

International audience; To explore the variability in biosensor studies, 150 participants from 20 countries were given the same protein samples and asked to determine kinetic rate constants for the interaction. We chose a protein system that was amen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15f0511d7d5e8ed6e3424eec0c582e12
https://hal.archives-ouvertes.fr/hal-01527917

Crystallographic Identification of a Noncompetitive Inhibitor Binding Site on the Hepatitis C Virus NS5B RNA Polymerase Enzyme

Autor: Robert A. Love, Hilary Wriggers, Anne Ekker, Michael J. Hickey, James Arthur Thomson, Hans E. Parge, Jingjin Gao, Xiu Yu, Liann Wang, Wade Diehl, Peter S. Dragovich, Shella A. Fuhrman

Publikováno v: Journal of Virology. 77:10176-10176

The virus-encoded nonstructural protein 5B (NS5B) of hepatitis C virus (HCV) is an RNA-dependent RNA polymerase and is absolutely required for replication of the virus. NS5B exhibits significant differences from cellular polymerases and therefore has

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ecfd3dda560813b0e57e4460caf0090
https://doi.org/10.1128/jvi.77.18.10176.2003