A High Throughput Screen Utilizing Newly Discovered Intramolecular Neuronal Calcium Channel interactions to Discover New Analgesics
This invention incorporates a newly discovered peptide which inhibits neural N-type calcium channels and the specific inter-molecular interaction that mediates the inhibitory effect of the peptide. This prototype peptide promises a beneficial profile for producing analgesia akin to opiates like morphine. The knowledge of the molecular interaction provides a target for drug discovery of compounds that mimic the effects of the prototype peptide. Additionally, this invention includes two hybridization assays that may be adapted for high-throughput screening of compounds or peptides that improve upon the profile of the prototype inhibitory peptide. All the discoveries may be generalized to other members of the CaV2 family of calcium channels. Description (Set) Proposed Use (Set) This invention, the prototype peptide inhibitor of N-type channels and the hybridization assays, point to a new approach to enhancing the analgesia currently induced by morphine and opiates. The prototype peptide is predicted to enhance effects seen with morphine thereby reducing the concentration of morphine administered to provide analgesia. The bi-molecular interaction discovered can serve as the basis of high-throughput screen for optimized peptides or compounds that can mimic the prototype peptide with improved delivery, clearance, and specificity. Finally this invention will enable testing of peptides that could inhibit other members of the CaV2 calcium channel family. Millions of people suffer yearly from chronic pain. Drawbacks to current treatment methods include addiction, nausea, sedation, and desensitization. N-type channel blockers have been found to have analgesic effects both alone and in conjunction with morphine, but these drugs still have serious side effects. Researchers have identified that G-protein mediated inhibition transiently reverses the inhibition of N-type channels, therefore identification of modulators, which work synergistically with opiates, may provide a new class of analgesics.
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