Ephrin Receptor InhibitorChemicals ResearchUpdated on Apr 11, 2019 View more like this | Visit SHIRLEY, NY | Contact BOCSCI INC |
BOC Sciences offers Ephrin Receptor Inhibitors for research use.
Small molecule antagonists that target Eph receptors so far display weak binding affinities in the micromolar range, probably due to the large size and flexibility of the ephrin-binding pocket. Efforts to elevate affinity have contributed to more potential but larger (>500 kDa) compounds. Small molecules match the ATP-binding pocket better in the Eph kinase domain. Advantages of small molecule kinase inhibitors are their extensive track record as drugs, potential for oral bioavailability, and in many cases ease of synthesis. However, most kinase inhibitors exhibit poor selectivity and target multiple kinases. Indeed, several small molecules identified as inhibitors of other kinase families, taking dasatinib as an example, can also strongly inhibit Eph receptors. Accidentally, recently dasatinib was reported to also inhibit kinase-independent EphA2 oncogenic signaling in cells through an indirect mechanism. Various types of screens to identify Eph kinase inhibitors have also produced several potential compounds.
Small molecule antagonists that target Eph receptors so far display weak binding affinities in the micromolar range, probably due to the large size and flexibility of the ephrin-binding pocket. Efforts to elevate affinity have contributed to more potential but larger (>500 kDa) compounds. Small molecules match the ATP-binding pocket better in the Eph kinase domain. Advantages of small molecule kinase inhibitors are their extensive track record as drugs, potential for oral bioavailability, and in many cases ease of synthesis. However, most kinase inhibitors exhibit poor selectivity and target multiple kinases. Indeed, several small molecules identified as inhibitors of other kinase families, taking dasatinib as an example, can also strongly inhibit Eph receptors. Accidentally, recently dasatinib was reported to also inhibit kinase-independent EphA2 oncogenic signaling in cells through an indirect mechanism. Various types of screens to identify Eph kinase inhibitors have also produced several potential compounds.
