In This Issue
| In This Issue, Volume 4, Issue 2 Janice Elaine Y. Silverman 146-146 |
| Full: PDF (577 K) |
Viewpoint
| Nanomaterials for (Nano)medicine Silvia Marchesan and Maurizio Prato 147-149  |
| Full: PDF (484 K) |
| Pharmaceutical Profiling Case Study in Disruption Edward H. Kerns 150-152  |
| Full: PDF (425 K) |
Patent Highlights
| Toll-Like Receptor Agonists for Treatment of Viral Infections Ahmed F. Abdel-Magid 153-154 |
| Full: PDF (224 K) |
| Modulation of TRPV1 Receptor for Treatment of Pain and Other Disorders Ahmed F. Abdel-Magid 155-156 |
| Full: PDF (158 K) |
| Aldosterone Synthase Inhibitors: Targeting Chronic Kidney Disease and Diabetic Nephropathy Ahmed F. Abdel-Magid 157-158 |
| Full: PDF (211 K) |
| TRPV4 Antagonists: Potential Treatment for Congestive Heart Failure, Bladder Dysfunctions, and Pain Ahmed F. Abdel-Magid 159-160 |
| Full: PDF (182 K) |
| PDE10 Inhibitors as Potential Treatment for Schizophrenia Ahmed F. Abdel-Magid 161-162 |
| Full: PDF (217 K) |
| Irreversible Inhibitors of Cysteine Proteases Gerard Rosse 163-164 |
| Full: PDF (264 K) |
Letters
| Synthesis and Antimalarial Activity of 3,3-Spiroanellated 5,6-Disubstituted 1,2,4-Trioxanes Ranjani Maurya, Awakash Soni, Devireddy Anand, Makthala Ravi, Kanumuri S. R. Raju, Isha Taneja, Niraj K. Naikade, S. K. Puri, Wahajuddin, Sanjeev Kanojiya, and Prem P. Yadav 165-169  |
| Full: PDF (593 K) |
| Synthesis of 8-Hydroxyquinoline Derivatives as Novel Antitumor Agents Sau Hing Chan, Chung Hin Chui, Shun Wan Chan, Stanton Hon Lun Kok, Dessy Chan, Miriam Yuen Tung Tsoi, Polly Hang Mei Leung, Alfred King Yin Lam, Albert Sun Chi Chan, Kim Hung Lam, and Johnny Cheuk On Tang 170-174  |
| Full: PDF (1086 K) |
| Improving the Affinity of SL0101 for RSK Using Structure-Based Design Roman M. Mrozowski, Rajender Vemula, Bulan Wu, Qi Zhang, Benjamin R. Schroeder, Michael K. Hilinski, David E. Clark, Sidney M. Hecht, George A. O’Doherty, and Deborah A. Lannigan 175-179  |
| Full: PDF (2123 K) |
| Discovery of O-Alkylamino-Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents Haijun Chen, Zhengduo Yang, Chunyong Ding, Lili Chu, Yusong Zhang, Kristin Terry, Huiling Liu, Qiang Shen, and Jia Zhou 180-185  |
| Full: PDF (2047 K) |
| The Role of the Acidity of N-Heteroaryl Sulfonamides as Inhibitors of Bcl-2 Family Protein–Protein Interactions B. Barry Touré, Karen Miller-Moslin, Naeem Yusuff, Lawrence Perez, Michael Doré, Carol Joud, Walter Michael, Lucian DiPietro, Simon van der Plas, Michael McEwan, Francois Lenoir, Madelene Hoe, Rajesh Karki, Clayton Springer, John Sullivan, Kymberly Levine, Catherine Fiorilla, Xiaoling Xie, Raviraj Kulathila, Kara Herlihy, Dale Porter, and Michael Visser 186-190  |
| Full: PDF (3081 K) |
| Discovery of a Series of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion Shilong Zheng, Qiu Zhong, Quan Jiang, Madhusoodanan Mottamal, Qiang Zhang, Naijue Zhu, Matthew E. Burow, Rebecca A. Worthylake, and Guangdi Wang 191-196  |
| Full: PDF (4165 K) |
| Metal Impurities Cause False Positives in High-Throughput Screening Campaigns Johannes C. Hermann, Yingsi Chen, Charles Wartchow, John Menke, Lin Gao, Shelley K. Gleason, Nancy-Ellen Haynes, Nathan Scott, Ann Petersen, Stephen Gabriel, Binh Vu, Kelly M. George, Arjun Narayanan, Shirley H. Li, Hong Qian, Nanda Beatini, Linghao Niu, and Qing-Fen Gan 197-200  |
| Full: PDF (302 K) |
| Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors Satoshi Sogabe, Youichi Kawakita, Shigeru Igaki, Hidehisa Iwata, Hiroshi Miki, Douglas R. Cary, Terufumi Takagi, Shinji Takagi, Yoshikazu Ohta, and Tomoyasu Ishikawa 201-205  |
| Full: PDF (3499 K) |
| l-Aminoacyl-triazine Derivatives Are Isoform-Selective PI3Kβ Inhibitors That Target Nonconserved Asp862 of PI3Kβ Jo-Anne Pinson, Zhaohua Zheng, Michelle S. Miller, David K. Chalmers, Ian G. Jennings, and Philip E. Thompson 206-210  |
| Full: PDF (1527 K) |
| Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195 Yunsong Tong, Kent D. Stewart, Alan S. Florjancic, John E. Harlan, Philip J. Merta, Magdalena Przytulinska, Nirupama Soni, Kerren K. Swinger, Haizhong Zhu, Eric F. Johnson, Alexander R. Shoemaker, and Thomas D. Penning 211-215  |
| Full: PDF (1365 K) |
| Gadolinium Complex of 125I/127I-RGD-DOTA Conjugate as a Tumor-Targeting SPECT/MR Bimodal Imaging Probe Ji-Ae Park, Jung Young Kim, Yong Jin Lee, Wonho Lee, Sang Moo Lim, Tae-Jeong Kim, Jeongsoo Yoo, Yongmin Chang, and Kyeong Min Kim 216-219  |
| Full: PDF (1449 K) |
| Novel Hybrid-Type Antimicrobial Agents Targeting the Switch Region of Bacterial RNA Polymerase Fumika Yakushiji, Yuko Miyamoto, Yuki Kunoh, Reiko Okamoto, Hidemasa Nakaminami, Yuri Yamazaki, Norihisa Noguchi, and Yoshio Hayashi 220-224  |
| Full: PDF (1973 K) |
| A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer’s and Prion Diseases Matteo Staderini, Suzana Aulić, Manuela Bartolini, Hoang Ngoc Ai Tran, Víctor González-Ruiz, Daniel I. Pérez, Nieves Cabezas, Ana Martínez, M. Antonia Martín, Vincenza Andrisano, Giuseppe Legname, J. Carlos Menéndez, and Maria Laura Bolognesi 225-229  |
| Full: PDF (1487 K) |
| [3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors Hongyi Yu, Michael L. Moore, Karl Erhard, Mary Ann Hardwicke, Hong Lin, Juan I. Luengo, Jeanelle McSurdy-Freed, Ramona Plant, Junya Qu, Kaushik Raha, Cynthia M. Rominger, Michael D. Schaber, Michael D. Spengler, and Ralph A. Rivero 230-234  |
| Full: PDF (1347 K) |
| Development of N-Hydroxycinnamamide-Based Histone Deacetylase Inhibitors with an Indole-Containing Cap Group Yingjie Zhang, Penghui Yang, C. James Chou, Chunxi Liu, Xuejian Wang, and Wenfang Xu 235-238  |
| Full: PDF (1517 K) |
| Inhibition of Ebola Virus Infection: Identification of Niemann-Pick C1 as the Target by Optimization of a Chemical Probe Kyungae Lee, Tao Ren, Marceline Côté, Berahman Gholamreza, John Misasi, Anna Bruchez, and James Cunningham 239-243  |
| Full: PDF (1363 K) |
| Discovery of Novel N-Substituted Oxindoles as Selective M1 and M4 Muscarinic Acetylcholine Receptors Partial Agonists Takaaki Sumiyoshi, Takeshi Enomoto, Kentaro Takai, Yoko Takahashi, Yasuko Konishi, Yoshiharu Uruno, Kengo Tojo, Atsushi Suwa, Harumi Matsuda, Tomokazu Nakako, Mutsuko Sakai, Atsushi Kitamura, Yasuaki Uematsu, and Akihiko Kiyoshi 244-248  |
| Full: PDF (744 K) |
| Interrogation of the Active Sites of Protein Arginine Deiminases (PAD1, -2, and -4) Using Designer Probes Angelica M. Bello, Ewa Wasilewski, Lianhu Wei, Mario A. Moscarello, and Lakshmi P. Kotra 249-253  |
| Full: PDF (1419 K) |
| Synthesis of Novel Analogs of Cabergoline: Improving Cardiovascular Safety by Removing 5-HT2B Receptor Agonism Peter I. Dosa, Tim Ward, Michael A. Walters, and Suck Won Kim 254-258  |
| Full: PDF (434 K) |
| Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors Jin-Jun Liu, Brian Higgins, Grace Ju, Kenneth Kolinsky, Kin-Chun Luk, Kathryn Packman, Giacomo Pizzolato, Yi Ren, Kshitij Thakkar, Christian Tovar, Zhuming Zhang, and Peter M. Wovkulich 259-263  |
| Full: PDF (2010 K) |
| Synthesis and Antimycobacterial Activity of 2,1′-Dihydropyridomycins Oliver P. Horlacher, Ruben C. Hartkoorn, Stewart T. Cole, and Karl-Heinz Altmann 264-268  |
| Full: PDF (475 K) |
| Bodilisant—A Novel Fluorescent, Highly Affine Histamine H3 Receptor Ligand Miriam Tomasch, J. Stephan Schwed, Alexander Paulke, and Holger Stark 269-273  |
| Full: PDF (1526 K) |
| Probing the Binding Site of Abl Tyrosine Kinase Using in Situ Click Chemistry Cristina Peruzzotti, Stella Borrelli, Micol Ventura, Rebecca Pantano, Gaia Fumagalli, Michael S. Christodoulou, Damiano Monticelli, Marcello Luzzani, Anna Lucia Fallacara, Cristina Tintori, Maurizio Botta, and Daniele Passarella 274-277  |
| Full: PDF (1309 K) |
| Antimalarial and Structural Studies of Pyridine-Containing Inhibitors of 1-Deoxyxylulose-5-phosphate Reductoisomerase Jian Xue, Jiasheng Diao, Guobin Cai, Lisheng Deng, Baisong Zheng, Yuan Yao, and Yongcheng Song 278-282  |
| Full: PDF (996 K) |
| C-Terminus of Botulinum A Protease Has Profound and Unanticipated Kinetic Consequences upon the Catalytic Cleft Peter Šilhár, Matthew A. Lardy, Mark S. Hixon, Charles B. Shoemaker, Joseph T. Barbieri, Anjali K. Struss, Jenny M. Lively, Sacha Javor, and Kim D. Janda 283-287  |
| Full: PDF (1471 K) |
| Discovery of a Novel Broad-Spectrum Antifungal Agent Derived from Albaconazole Rémi Guillon, Fabrice Pagniez, Carine Picot, Damien Hédou, Alain Tonnerre, Elizabeth Chosson, Muriel Duflos, Thierry Besson, Cédric Logé, and Patrice Le Pape 288-292  |
| Full: PDF (475 K) |
| Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema Mark A. Hilfiker, Tram H. Hoang, Johan Cornil, Hilary S. Eidam, Daniel S. Matasic, Theresa J. Roethke, Michael Klein, Kevin S. Thorneloe, and Mui Cheung 293-296  |
| Full: PDF (391 K) |
| Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors Hidemitsu Minegishi, Shinji Fukashiro, Hyun Seung Ban, and Hiroyuki Nakamura 297-301  |
| Full: PDF (1298 K) |
| Immune-Stimulatory Dinucleotide at the 5′-End of Oligodeoxynucleotides Is Critical for TLR9-Mediated Immune Responses Mallikarjuna R. Putta, Lakshmi Bhagat, Daqing Wang, Fu-Gang Zhu, Ekambar R. Kandimalla, and Sudhir Agrawal 302-305  |
| Full: PDF (537 K) |
Technology Notes
| High-Throughput Selectivity Assays for Small-Molecule Inhibitors of β-Catenin/T-Cell Factor Protein–Protein Interactions Min Zhang, J. Leon Catrow, and Haitao Ji 306-311  |
| Full: PDF (1083 K) |