2012
DOI: 10.1016/j.semcdb.2011.10.023
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Targeting Eph receptors with peptides and small molecules: Progress and challenges

Abstract: The Eph receptors are a large family of receptor tyrosine kinases. Their kinase activity and downstream signaling ability are stimulated by the binding of cell surface-associated ligands, the ephrins. The ensuing signals are bidirectional because the ephrins can also transduce signals (known as reverse signals) following their interaction with Eph receptors. The ephrin-binding pocket in the extracellular N-terminal domain of the Eph receptors and the ATP-binding pocket in the intracellular kinase domain repres… Show more

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Cited by 90 publications
(105 citation statements)
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“…In terms of therapeutic potential, ephrinB1 is expressed at the cell surface and could potentially be targeted. Although there are no inhibitors of ephrins in clinical use, a number of peptides and chemical compounds that target Eph receptors and inhibit ephrin binding or downstream kinase activation have been identified (56). These molecules show promise as probes to study Eph receptor/ephrin biology, as lead compounds for drug development and as targeting agents to deliver drugs or imaging agents to tumors.…”
Section: Discussionmentioning
confidence: 99%
“…In terms of therapeutic potential, ephrinB1 is expressed at the cell surface and could potentially be targeted. Although there are no inhibitors of ephrins in clinical use, a number of peptides and chemical compounds that target Eph receptors and inhibit ephrin binding or downstream kinase activation have been identified (56). These molecules show promise as probes to study Eph receptor/ephrin biology, as lead compounds for drug development and as targeting agents to deliver drugs or imaging agents to tumors.…”
Section: Discussionmentioning
confidence: 99%
“…immunogenic or allergic responses). Thus, it is advantageous to use peptide that selectively bind to EphA2 and use its ability to mediate internalization (46). The normal tissues have low EphA2 expression compare to tumor tissues and based on our bio-distribution data, the use of the YSA peptide for drug delivery may reduce toxic side-effects by reducing exposure of cytotoxic drugs to normal cells.…”
Section: Discussionmentioning
confidence: 99%
“…Dasatinib and nilotinib are two multikinase inhibitors that have been shown to inhibit EphB2, along with BCR-abl, c-Kit, PDGFR-β, other Eph receptors, and members of the src family [ 102 ]. The effect of nilotinib in osteosarcoma has not been investigated.…”
Section: Ephb2mentioning
confidence: 99%