New Frontiers in Kinases Editorial

New Frontiers in Kinases: Second Generation Inhibitors–Going beyond Cancer Stefan Laufer 1-1 Full: PDF (124 K)

In This Issue

In This Issue, Volume 6, Issue 1 Janice Elaine Y. Silverman 2-2 Full: PDF (644 K)

Viewpoint

Class II but Not Second Class—Prospects for the Development of Class II PI3K Inhibitors Simon J. Mountford, Zhaohua Zheng, Krithika Sundaram, Ian G. Jennings, Justin R. Hamilton, and Philip E. Thompson 3-6 Full: PDF (2410 K)

Patent Highlights

Combination of Novel Imidazopyridazine Mps-1 Kinase Inhibitors and Bcl-2 Family Protein Inhibitors Gerard Rosse 7-8 Full: PDF (262 K)

Pyrrolopyrimidine Analogues as MKNK Inhibitors Jean-Francois Brazeau and Gerard Rosse 9-10 Full: PDF (228 K)

Dual Leucine Zipper Kinase Inhibitors: Potential Treatments for Neurodegenerative Diseases Ahmed F. Abdel-Magid 11-12 Full: PDF (254 K)

RET Kinase Inhibitors May Treat Cancer and Gastrointestinal Disorders Ahmed F. Abdel-Magid 13-14 Full: PDF (252 K)

Quinalozinones as Inhibitors of Class I PI3K Kinases Gerard Rosse 15-16 Full: PDF (322 K)

P21-Activated Kinase 4 (PAK4) Inhibitors as Potential Cancer Therapy Ahmed F. Abdel-Magid 17-18 Full: PDF (261 K)

Novel Azaindazole Sulfonamides Inhibitors of Serum and Glucocorticoid Regulated Kinase Gerard Rosse 19-20 Full: PDF (278 K)

Pyrrolopyridines-quinazolines Inhibitors of PKR-Like ER Kinase Gerard Rosse 21-22 Full: PDF (253 K)

Novel Disubstituted Pyrimidines as Inhibitors of Bruton’s Tyrosine Kinase Gerard Rosse 23-24 Full: PDF (232 K)

Letters

Fragment-Based Discovery of Type I Inhibitors of Maternal Embryonic Leucine Zipper Kinase Christopher N. Johnson, Valerio Berdini, Lijs Beke, Pascal Bonnet, Dirk Brehmer, Joseph E. Coyle, Phillip J. Day, Martyn Frederickson, Eddy J. E. Freyne, Ron A. H. J. Gilissen, Christopher C. F. Hamlett, Steven Howard, Lieven Meerpoel, Rachel McMenamin, Sahil Patel, David C. Rees, Andrew Sharff, François Sommen, Tongfei Wu, and Joannes T. M. Linders 25-30 Full: PDF (2366 K)

Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase Christopher N. Johnson, Christophe Adelinet, Valerio Berdini, Lijs Beke, Pascal Bonnet, Dirk Brehmer, Frederick Calo, Joseph E. Coyle, Phillip J. Day, Martyn Frederickson, Eddy J. E. Freyne, Ron A. H. J. Gilissen, Christopher C. F. Hamlett, Steven Howard, Lieven Meerpoel, Laurence Mevellec, Rachel McMenamin, Elisabeth Pasquier, Sahil Patel, David C. Rees, and Joannes T. M. Linders 31-36 Full: PDF (2040 K)

Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors Paul A Barsanti, Robert J. Aversa, Xianming Jin, Yue Pan, Yipin Lu, Robert Elling, Rama Jain, Mark Knapp, Jiong Lan, Xiaodong Lin, Patrick Rudewicz, Janet Sim, Lorena Taricani, George Thomas, Linda Xiao, and Qin Yue 37-41 Full: PDF (2070 K)

Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors Paul A Barsanti, Yue Pan, Yipin Lu, Rama Jain, Matthew Cox, Robert J. Aversa, Michael P. Dillon, Robert Elling, Cheng Hu, Xianming Jin, Mark Knapp, Jiong Lan, Savithri Ramurthy, Patrick Rudewicz, Lina Setti, Sharadha Subramanian, Michelle Mathur, Lorena Taricani, George Thomas, Linda Xiao, and Qin Yue 42-46 Full: PDF (1689 K)

Quantification of a Pharmacodynamic ERK End Point in Melanoma Cell Lysates: Toward Personalized Precision Medicine Mangalika Warthaka, Charles H. Adelmann, Tamer S. Kaoud, Ramakrishna Edupuganti, Chunli Yan, William H. Johnson, Jr., Scarlett Ferguson, Clint D. Tavares, Lindy J. Pence, Eric V. Anslyn, Pengyu Ren, Kenneth Y. Tsai, and Kevin N. Dalby 47-52 Full: PDF (1361 K)

Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation Nicole C. Goodwin, Giovanni Cianchetta, Hugh A. Burgoon, Jason Healy, Ross Mabon, Eric D. Strobel, Jason Allen, Shuli Wang, Brian D. Hamman, and David B. Rawlins 53-57 Full: PDF (1504 K)

Pyrimidine-Based Tricyclic Molecules as Potent and Orally Efficacious Inhibitors of Wee1 Kinase Yunsong Tong, Maricel Torrent, Alan S. Florjancic, Kenneth D. Bromberg, Fritz G. Buchanan, Debra C. Ferguson, Eric F. Johnson, Loren M. Lasko, David Maag, Philip J. Merta, Amanda M. Olson, Donald J. Osterling, Nirupama Soni, Alexander R. Shoemaker, and Thomas D. Penning 58-62 Full: PDF (2120 K)

Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors Yong Xu, Benjamin G. Brenning, Steven G. Kultgen, Jason M. Foulks, Adrianne Clifford, Shuping Lai, Ashley Chan, Shannon Merx, Michael V. McCullar, Steven B. Kanner, and Koc-Kan Ho 63-67 Full: PDF (468 K)

Unfolded Protein Response in Cancer: IRE1α Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability Paul E. Harrington, Kaustav Biswas, David Malwitz, Andrew S. Tasker, Christopher Mohr, Kristin L. Andrews, Ken Dellamaggiore, Richard Kendall, Holger Beckmann, Peter Jaeckel, Silvia Materna-Reichelt, Jennifer R. Allen, and J. Russell Lipford 68-72 Full: PDF (1693 K)

Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors Nis Halland, Friedemann Schmidt, Tilo Weiss, Joachim Saas, Ziyu Li, Jörg Czech, Matthias Dreyer, Armin Hofmeister, Katharina Mertsch, Uwe Dietz, Carsten Strübing, and Marc Nazare 73-78 Full: PDF (1180 K)

Structural Analysis of the Binding of Type I, I1/2, and II Inhibitors to Eph Tyrosine Kinases Jing Dong, Hongtao Zhao, Ting Zhou, Dimitrios Spiliotopoulos, Chitra Rajendran, Xiao-Dan Li, Danzhi Huang, and Amedeo Caflisch 79-83 Full: PDF (3414 K)

Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma Bryce A. Harrison, Zheng Y. Almstead, Hugh Burgoon, Michael Gardyan, Nicole C. Goodwin, Jason Healy, Ying Liu, Ross Mabon, Brett Marinelli, Lakshman Samala, Yulian Zhang, Terry R. Stouch, N. Andrew Whitlock, Suma Gopinathan, Beth McKnight, Shuli Wang, Nita Patel, Alan G. E. Wilson, Brian D. Hamman, Dennis S. Rice, and David B. Rawlins 84-88 Full: PDF (986 K)

Distinct Binding Mode of Multikinase Inhibitor Lenvatinib Revealed by Biochemical Characterization Kiyoshi Okamoto, Megumi Ikemori-Kawada, Anja Jestel, Konstanze von König, Yasuhiro Funahashi, Tomohiro Matsushima, Akihiko Tsuruoka, Atsushi Inoue, and Junji Matsui 89-94 Full: PDF (4054 K)

Synthesis and Structure–Activity Relationship Study of 5a-Carbasugar Analogues of SL0101 Mingzong Li, Yu Li, Roman M. Mrozowski, Zachary M. Sandusky, Mingde Shan, Xiwen Song, Bulan Wu, Qi Zhang, Deborah A. Lannigan, and George A. O’Doherty 95-99 Full: PDF (1830 K)