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1 November 2013
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Cover Image
Cover Image
Ribbon representation of a homology model of the c-Met specific Anticalin PRS-110. Anticalins are engineered human lipocalins that represent a next generation class of drug molecules. The lipocalins have a structurally conserved β-barrel architecture that forms a cup-shaped ligand binding pocket that can accommodate small and large ligands. The β strands (blue) of the lipocalin form the base of the ligand-binding pocket and the entry of the pocket is comprised of four loops connecting the β strands. Novel, target-specific Anticalins are generated by engineering mutations (pink regions, PRS-110 mutations) within these four loops and then selecting variants with the desired binding activity. For details, see article by Olwill and colleagues on page 2459. - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Highlights
Small Molecule Therapeutics
Developing Lipid Nanoparticle-Based siRNA Therapeutics for Hepatocellular Carcinoma Using an Integrated Approach
Leiming Li; Rongqi Wang; Denise Wilcox; Aparna Sarthy; Xiaoyu Lin; Xiaoli Huang; Lu Tian; Prasad Dande; Robert D. Hubbard; Todd M. Hansen; Carol Wada; Xiaobin Zhao; William M. Kohlbrenner; Stephen W. Fesik; Yu Shen
Author Choice
BAY 80-6946 Is a Highly Selective Intravenous PI3K Inhibitor with Potent p110α and p110δ Activities in Tumor Cell Lines and Xenograft Models
Ningshu Liu; Bruce R. Rowley; Cathy O. Bull; Claudia Schneider; Andrea Haegebarth; Christoph A. Schatz; Paul R. Fracasso; Dean P. Wilkie; Martin Hentemann; Scott M. Wilhelm; William J. Scott; Dominik Mumberg; Karl Ziegelbauer
Synergistic Targeting of PI3K/AKT Pathway and Androgen Receptor Axis Significantly Delays Castration-Resistant Prostate Cancer Progression In Vivo
Christian Thomas; Francois Lamoureux; Claire Crafter; Barry R. Davies; Eliana Beraldi; Ladan Fazli; Soojin Kim; Daksh Thaper; Martin E. Gleave; Amina Zoubeidi
AMG 900, a Small-Molecule Inhibitor of Aurora Kinases, Potentiates the Activity of Microtubule-Targeting Agents in Human Metastatic Breast Cancer Models
Tammy L. Bush; Marc Payton; Scott Heller; Grace Chung; Kelly Hanestad; James B. Rottman; Robert Loberg; Gregory Friberg; Richard L. Kendall; Douglas Saffran; Robert Radinsky
UNC569, a Novel Small-Molecule Mer Inhibitor with Efficacy against Acute Lymphoblastic Leukemia In Vitro and In Vivo
Sandra Christoph; Deborah DeRyckere; Jennifer Schlegel; J. Kimble Frazer; Lance A. Batchelor; Alesia Y. Trakhimets; Susan Sather; Debra M. Hunter; Christopher T. Cummings; Jing Liu; Chao Yang; Dmitri Kireev; Catherine Simpson; Jacqueline Norris-Drouin; Emily A. Hull-Ryde; William P. Janzen; Gary L. Johnson; Xiaodong Wang; Stephen V. Frye; H. Shelton Earp, III; Douglas K. Graham
Paclitaxel–Hyaluronic NanoConjugates Prolong Overall Survival in a Preclinical Brain Metastases of Breast Cancer Model
Rajendar K. Mittapalli; Xinli Liu; Chris E. Adkins; Mohamed I. Nounou; Kaci A. Bohn; Tori B. Terrell; Hussaini S. Qhattal; Werner J. Geldenhuys; Diane Palmieri; Patricia S. Steeg; Quentin R. Smith; Paul R. Lockman
Isolation of a Novel Thioflavin S–Derived Compound That Inhibits BAG-1–Mediated Protein Interactions and Targets BRAF Inhibitor–Resistant Cell Lines
Marion Enthammer; Emmanouil S. Papadakis; Maria Salomé Gachet; Martin Deutsch; Stefan Schwaiger; Katarzyna Koziel; Muhammad Imtiaz Ashraf; Sana Khalid; Gerhard Wolber; Graham Packham; Ramsey I. Cutress; Hermann Stuppner; Jakob Troppmair
The Novel ATP-Competitive Inhibitor of the MET Hepatocyte Growth Factor Receptor EMD1214063 Displays Inhibitory Activity against Selected MET-Mutated Variants
Michaela Medová; Benoît Pochon; Bruno Streit; Wieslawa Blank-Liss; Paola Francica; Deborah Stroka; Adrian Keogh; Daniel M. Aebersold; Andree Blaukat; Friedhelm Bladt; Yitzhak Zimmer
Characterization of a New Class of Androgen Receptor Antagonists with Potential Therapeutic Application in Advanced Prostate Cancer
Huifang Li; Mohamed D.H. Hassona; Nathan A. Lack; Peter Axerio-Cilies; Eric Leblanc; Peyman Tavassoli; Natalia Kanaan; Kate Frewin; Kriti Singh; Hans Adomat; Konrad J. Böhm; Helge Prinz; Emma Tomlinson Guns; Paul S. Rennie; Artem Cherkasov
Large Molecule Therapeutics
Author Choice
A Highly Potent and Specific MET Therapeutic Protein Antagonist with Both Ligand-Dependent and Ligand-Independent Activity
Shane A. Olwill; Christian Joffroy; Hendrik Gille; Elisa Vigna; Gabriele Matschiner; Andrea Allersdorfer; Bradley M. Lunde; Jakub Jaworski; James F. Burrows; Cristina Chiriaco; Hans Jürgen Christian; Martin Hülsmeyer; Stefan Trentmann; Kristian Jensen; Andreas M. Hohlbaum; Laurent Audoly
Cancer Therapeutics Insights
In Vitro and In Vivo Therapeutic Efficacy of Carfilzomib in Mantle Cell Lymphoma: Targeting the Immunoproteasome
Liang Zhang; Lan V. Pham; Kate J. Newberry; Zhishuo Ou; Rong Liang; Jianfei Qian; Luhong Sun; Marzenna Blonska; Yun You; Jing Yang; Xin Lin; Alex Rollo; Archito T. Tamayo; John Lee; Richard J. Ford; Xiurong Zhao; Larry W. Kwak; Qing Yi; Michael Wang
Tools and Technologies
Letter to the Editor
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