A disalicylic acid-furanyl derivative inhibits ephrin binding to a subset of Eph receptorsRoberta Noberini
Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
Chem Biol Drug Des 78:667-78. 2011
..These findings suggest that salicylic acid derivatives could be used as starting points to design new small molecule antagonists of Eph receptors...
Inhibition of Eph receptor-ephrin ligand interaction by tea polyphenolsRoberta Noberini
Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Pharmacol Res 66:363-73. 2012
..Thus, the Eph receptor tyrosine kinase family represents an important class of targets for tea-derived phytochemicals...
- Distinctive binding of three antagonistic peptides to the ephrin-binding pocket of the EphA4 receptor
Ilaria Lamberto
Sanford Burnham Medical Research Institute, 10901 N Torrey Pines Rd, La Jolla, CA 92037, USA
Biochem J 445:47-56. 2012
..The peptides exhibit a long half-life in cell culture medium which, with their substantial binding affinity and selectivity for EphA4, makes them excellent research tools to modulate EphA4 function...
- Targeted delivery of paclitaxel to EphA2-expressing cancer cells
Si Wang
Cancer Research Center, Sanford Burnham Medical Research Institute, La Jolla, CA 90237, USA
Clin Cancer Res 19:128-37. 2013
..YSA is an EphA2-targeting peptide that effectively delivers anticancer agents to prostate cancer tumors. Here, we report on how we increased the drug-like properties of this delivery system...
- PEGylation potentiates the effectiveness of an antagonistic peptide that targets the EphB4 receptor with nanomolar affinity
Roberta Noberini
Sanford Burnham Medical Research Institute, La Jolla, California, United States of America
PLoS ONE 6:e28611. 2011
..Furthermore, the PEGylated peptide is suitable for other cell culture and in vivo applications requiring prolonged EphB4 receptor targeting...
- Novel targeted system to deliver chemotherapeutic drugs to EphA2-expressing cancer cells
Si Wang
Cancer Research Center, Sanford Burnham Medical Research Institute, 10901 N Torrey Pines Road, La Jolla, California 92037, USA
J Med Chem 55:2427-36. 2012
..We believe these studies open the way to the development of a new class of therapeutic compounds that exploit the EphA2 receptor for drug delivery to cancer cells...
- HTS by NMR of combinatorial libraries: a fragment-based approach to ligand discovery
Bainan Wu
Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Chem Biol 20:19-33. 2013
..We used the method to identify compounds that target protein-protein interactions...
- Targeting Eph receptors with peptides and small molecules: progress and challenges
Roberta Noberini
Sanford Burnham Medical Research Institute, 10901 N Torrey Pines Rd, La Jolla, CA 92037, USA
Semin Cell Dev Biol 23:51-7. 2012
..Strategies that could also be explored include targeting additional Eph receptor interfaces and the ephrin ligands...
- Profiling Eph receptor expression in cells and tissues: a targeted mass spectrometry approach
Roberta Noberini
Sanford Burnham Medical Research Institute, La Jolla, CA, USA
Cell Adh Migr 6:102-12. 2012
..The new mass spectrometry approach we have developed represents a useful tool for the identification of the spectrum of Eph receptors present in a biological sample and could also be extended to profiling ephrin expression...
- Characterization of a novel angiogenic model based on stable, fluorescently labelled endothelial cell lines amenable to scale-up for high content screening
Natalie L Prigozhina
Sanford Burnham Medical Research Institute, 10901 N Torrey Pines Road, La Jolla, CA 92037, USA
Biol Cell 103:467-81. 2011
..We then evaluated HMEC cultures, both alone and co-cultured with an EMC (epicardial mesothelial cell) line that contributes vascular smooth muscle cells, to determine the suitability for HTS or HCS...
- Proliferation and tumor suppression: not mutually exclusive for Eph receptors
Roberta Noberini
Burnham Institute for Medical Research, La Jolla, CA 92037, USA
Cancer Cell 16:452-4. 2009
..These separate pathways simultaneously promote proliferation but suppress invasive growth of intestinal adenomas...
- Small molecules can selectively inhibit ephrin binding to the EphA4 and EphA2 receptors
Roberta Noberini
Burnham Institute for Medical Research, La Jolla, California 92037, USA
J Biol Chem 283:29461-72. 2008
..Furthermore, the newly identified inhibitors represent possible leads for the development of therapies to treat pathologies in which EphA4 and EphA2 are involved, including nerve injuries and cancer...
