In This Issue

In This Issue, Volume 5, Issue 11 Janice Elaine Y. Silverman 1175-1175 Full: PDF (1113 K)

Viewpoint

Recent Progress in Antitumoral Synthetic Vaccines Cristina Nativi and Olivier Renaudet 1176-1178 Full: PDF (153 K)

Treatment of Amyotrophic Lateral Sclerosis: Lessons Learned from Many Failures P. Hande Özdinler and Richard B. Silverman 1179-1181 Full: PDF (165 K)

Patent Highlights

Neutrophil Elastase Inhibitors as Potential Anti-Inflammatory Therapies Ahmed F. Abdel-Magid 1182-1183 Full: PDF (262 K)

Inhibitors of Mutant IDH for the Treatment of Cancer Ahmed F. Abdel-Magid 1184-1185 Full: PDF (238 K)

Liver X Receptor Agonists for the Treatment of Coronary Heart Disease and Other Disorders Ahmed F. Abdel-Magid 1186-1187 Full: PDF (255 K)

Pyrazolsulfonamide Agonists of Oxytocin Receptor Gerard Rosse 1188-1189 Full: PDF (244 K)

Featured Letter

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain Emmanuel H. Demont, Paul Bamborough, Chun-wa Chung, Peter D. Craggs, David Fallon, Laurie J. Gordon, Paola Grandi, Clare I. Hobbs, Jameed Hussain, Emma J. Jones, Armelle Le Gall, Anne-Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Andy D. Roberts, Robert J. Sheppard, and Robert J. Watson 1190-1195 Full: PDF (3345 K)

Letters

Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands Oluseye K. Onajole, J. Brek Eaton, Ronald J. Lukas, Dani Brunner, Lucinda Thiede, Barbara J. Caldarone, and Alan P. Kozikowski 1196-1201 Full: PDF (757 K)

Nanomolar-Potency Small Molecule Inhibitor of STAT5 Protein Abbarna A. Cumaraswamy, Andrew M. Lewis, Mulu Geletu, Aleksandra Todic, Diego B. Diaz, Xin Ran Cheng, Carla E. Brown, Rob C. Laister, David Muench, Kagan Kerman, H. Leighton Grimes, Mark D. Minden, and Patrick T. Gunning 1202-1206 Full: PDF (2600 K)

Structure Activity Relationships of αv Integrin Antagonists for Pulmonary Fibrosis by Variation in Aryl Substituents James Adams, Edward C. Anderson, Emma E. Blackham, Yin Wa Ryan Chiu, Thomas Clarke, Natasha Eccles, Luke A. Gill, Joshua J. Haye, Harvey T. Haywood, Christian R. Hoenig, Marius Kausas, Joelle Le, Hannah L. Russell, Christopher Smedley, William J. Tipping, Tom Tongue, Charlotte C. Wood, Jason Yeung, James E. Rowedder, M. Jonathan Fray, Thomas McInally, and Simon J. F. Macdonald 1207-1212 Full: PDF (441 K)

Synthesis, Structure, and SAR of Tetrahydropyran-Based LpxC Inhibitors Kerry E. Murphy-Benenato, Nelson Olivier, Allison Choy, Philip L. Ross, Matthew D. Miller, Jason Thresher, Ning Gao, and Michael R. Hale 1213-1218 Full: PDF (2030 K)

Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer Zhenfu Han, Peter K. W. Harris, Darin E. Jones, Ryan Chugani, Tommy Kim, Manjula Agarwal, Wei Shen, Scott A. Wildman, and James W. Janetka 1219-1224 Full: PDF (2266 K)

Synthesis and Biological Evaluation of Sophoridinol Derivatives as a Novel Family of Potential Anticancer Agents Chongwen Bi, Caixia Zhang, Yinghong Li, Sheng Tang, Shenggang Wang, Rongguang Shao, Haigen Fu, Feng Su, and Danqing Song 1225-1229 Full: PDF (862 K)

Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist Satoshi Itadani, Shinya Takahashi, Masaki Ima, Tetsuya Sekiguchi, Manabu Fujita, Yoshisuke Nakayama, and Jun Takeuchi 1230-1234 Full: PDF (522 K)

Dihydropyrrolo[2,3-d]pyrimidines: Selective Toll-Like Receptor 9 Antagonists from Scaffold Morphing Efforts Manabu Watanabe, Mai Kasai, Hideyuki Tomizawa, Masamitsu Aoki, Kazuo Eiho, Yoshiaki Isobe, and Shigehiro Asano 1235-1239 Full: PDF (530 K)

Aptamer-Facilitated Cryoprotection of Viruses Shahrokh M. Ghobadloo, Ana Gargaun, Rebecca Casselman, Darija Muharemagic, and Maxim V. Berezovski 1240-1244 Full: PDF (2496 K)

Synthesis, in Vitro Covalent Binding Evaluation, and Metabolism of 14C-Labeled Inhibitors of 11β-HSD1 Daqing Sun, Qiuping Ye, Xuelei Yan, Yosup Rew, Peter Fan, Xiao He, Min Jiang, Dustin L. McMinn, Mario Monshouwer, Hua Tu, and Jay P. Powers 1245-1250 Full: PDF (717 K)

Structure–Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors Sarah C. Zimmermann, Rana Rais, Jesse Alt, Caitlin Burzynski, Barbara S. Slusher, and Takashi Tsukamoto 1251-1253 Full: PDF (262 K)

Design of Fluorine-Containing 3,4-Diarylfuran-2(5H)-ones as Selective COX-1 Inhibitors Md. Jashim Uddin, Anna V. Elleman, Kebreab Ghebreselasie, Cristina K. Daniel, Brenda C. Crews, Kellie D. Nance, Tamanna Huda, and Lawrence J. Marnett 1254-1258 Full: PDF (283 K)

Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers Won-Gil Lee, Kathleen M. Frey, Ricardo Gallardo-Macias, Krasimir A. Spasov, Mariela Bollini, Karen S. Anderson, and William L. Jorgensen 1259-1262 Full: PDF (2517 K)