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EphB1 as a Novel Drug Target to Combat Pain and Addiction

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Technical Report,01 Sep 2016,31 Aug 2017

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The University of Texas Southwestern Medical Center Dallas United States

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The synaptic receptor protein known as EphB1 is a central player in nerve injury-induced neuropathic pain and the related pain symptoms associated with the withdrawal from opioidmorphine addiction. Our hypothesis is that postsynaptic EphB1 participates in pain through the ability of its extracellular domain to form protein-protein interactions with its presynaptic ligand, ephrin-B2, and the NR1 subunit of the postsynaptic NMDA receptor to inappropriately strengthen the synapses in the spinal cord that transmit pain signals into the brain. Our project is to carry out high-throughput screens HTS to identify small molecular weight drug-like compounds from a 200,000 complex library that antagonize EphB1 protein-protein interactions. While we originally set out to target the EphB1NR1 protein-protein interaction, we changed directions in Year 2 due to technical difficulties and focused on the interaction of EphB1 with ephrin-B2. In Year 3 we developed a robust HTS assay and screened the full 200,000 compound library for antagonists that disrupt the EphB1ephrin-B2 interaction. We identified two highly related lead compounds from the 200,000 compound library and are presently focusing on characterizing them further.

Subject Categories:

  • Medicine and Medical Research
  • Biochemistry
  • Pharmacology

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