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1 February 2014
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Cover Image
The ALK/MET inhibitor crizotinib has already shown efficacy in ALK-driven non–small cell lung cancer patients, but the treatment is not curative with rapid acquisition of resistance, which is partly attributable to the gatekeeper-residue mutation L1196M of ALK. Computational modeling suggested that ASP3026, a novel small molecule ALK inhibitor, is well docked with both wild-type and L1196M ALK, and fits more deeply within the ATP-binding pocket of the L1196M form, with the larger side-chain of methionine compared to leucine, than crizotinib. Thismight explain why ASP3026 showedmore potent efficacy against the L1196M mutant within the therapeutic margin compared with crizotinib. For details, see article by Mori and colleagues on page 329. - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Highlights
Review
Small Molecule Therapeutics
Selective Inhibition of Pancreatic Ductal Adenocarcinoma Cell Growth by the Mitotic MPS1 Kinase Inhibitor NMS-P715
Roger B. Slee; Brenda R. Grimes; Ruchi Bansal; Jesse Gore; Corinne Blackburn; Lyndsey Brown; Rachel Gasaway; Jaesik Jeong; Jose Victorino; Keith L. March; Riccardo Colombo; Brittney-Shea Herbert; Murray Korc
The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice
Masamichi Mori; Yoko Ueno; Satoshi Konagai; Hiroshi Fushiki; Itsuro Shimada; Yutaka Kondoh; Rika Saito; Kenichi Mori; Nobuaki Shindou; Takatoshi Soga; Hideki Sakagami; Takashi Furutani; Hitoshi Doihara; Masafumi Kudoh; Sadao Kuromitsu
Characterization of LY2228820 Dimesylate, a Potent and Selective Inhibitor of p38 MAPK with Antitumor Activity
Robert M. Campbell; Bryan D. Anderson; Nathan A. Brooks; Harold B. Brooks; Edward M. Chan; Alfonso De Dios; Raymond Gilmour; Jeremy R. Graff; Enrique Jambrina; Mary Mader; Denis McCann; Songqing Na; Stephen H. Parsons; Susan E. Pratt; Chuan Shih; Louis F. Stancato; James J. Starling; Courtney Tate; Juan A. Velasco; Yong Wang; Xiang S. Ye
Large Molecule Therapeutics
Novel Neutralizing Hedgehog Antibody MEDI-5304 Exhibits Antitumor Activity by Inhibiting Paracrine Hedgehog Signaling
Neil R. Michaud; Youzhen Wang; Kristen A. McEachern; Jerold J. Jordan; Anne Marie Mazzola; Axel Hernandez; Sanjoo Jalla; Jon W. Chesebrough; Mark J. Hynes; Matthew A. Belmonte; Lidong Wang; Jaspal S. Kang; Jelena Jovanović; Naomi Laing; David W. Jenkins; Elaine Hurt; Meina Liang; Christopher Frantz; Robert E. Hollingsworth; Diane M. Simeone; David C. Blakey; Vahe Bedian
Author Choice
Pharmacodynamic and Antineoplastic Activity of BI 836845, a Fully Human IGF Ligand-Neutralizing Antibody, and Mechanistic Rationale for Combination with Rapamycin
Katrin Friedbichler; Marco H. Hofmann; Monika Kroez; Elinborg Ostermann; Herbert R. Lamche; Christian Koessl; Eric Borges; Michael N. Pollak; Günther Adolf; Paul J. Adam
Author Choice
MM-141, an IGF-IR– and ErbB3-Directed Bispecific Antibody, Overcomes Network Adaptations That Limit Activity of IGF-IR Inhibitors
Jonathan B. Fitzgerald; Bryan W. Johnson; Jason Baum; Sharlene Adams; Sergio Iadevaia; Jian Tang; Victoria Rimkunas; Lihui Xu; Neeraj Kohli; Rachel Rennard; Maja Razlog; Yang Jiao; Brian D. Harms; Kenneth J. Olivier, Jr; Birgit Schoeberl; Ulrik B. Nielsen; Alexey A. Lugovskoy
Cancer Biology and Signal Transduction
MiR-134/487b/655 Cluster Regulates TGF-β–Induced Epithelial–Mesenchymal Transition and Drug Resistance to Gefitinib by Targeting MAGI2 in Lung Adenocarcinoma Cells
Kazuhiro Kitamura; Masahiro Seike; Tetsuya Okano; Kuniko Matsuda; Akihiko Miyanaga; Hideaki Mizutani; Rintaro Noro; Yuji Minegishi; Kaoru Kubota; Akihiko Gemma
OATP1A/1B Transporters Affect Irinotecan and SN-38 Pharmacokinetics and Carboxylesterase Expression in Knockout and Humanized Transgenic Mice
Dilek Iusuf; Marion Ludwig; Ahmed Elbatsh; Anita van Esch; Evita van de Steeg; Els Wagenaar; Martin van der Valk; Fan Lin; Olaf van Tellingen; Alfred H. Schinkel
Companion Diagnostics and Cancer Biomarkers
Plastin Polymorphisms Predict Gender- and Stage-Specific Colon Cancer Recurrence after Adjuvant Chemotherapy
Yan Ning; Armin Gerger; Wu Zhang; Diana L. Hanna; Dongyun Yang; Thomas Winder; Takeru Wakatsuki; Melissa J. Labonte; Sebastian Stintzing; Nico Volz; Yu Sunakawa; Stefan Stremitzer; Rita El-Khoueiry; Heinz-Josef Lenz
Nonclinical Evaluation of the Serum Pharmacodynamic Biomarkers HGF and Shed MET following Dosing with the Anti-MET Monovalent Monoclonal Antibody Onartuzumab
Elaine Mai; Zhong Zheng; Youjun Chen; Jing Peng; Christophe Severin; Ellen Filvaroff; Mally Romero; William Mallet; Surinder Kaur; Thomas Gelzleichter; Ihsan Nijem; Mark Merchant; Judy C. Young
Correction
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