Discovery of Novel Amphipathic Ligands for the Dynorphin Binding Site on the Bradykinin Receptor

InventionThe invention disclosed in UA12-097 is a dynorphin analog designed to interact with a receptor that is partly responsible for pain sensations. Dyrnphin analog targets the bradykinin receptors instead of the f NMDA receptors. The ligands are novel in the deletion of an arginine residue in position 7 which has been recognized as an essential residue for opioid and non-opioid activities. This deletion has been shown to retain biological activity for the receptor. The researchers have also identified the minimum pharmacophore (combination of more than 2 basic amino acids and 2 hydrophobic amino acids) for the bradykinin receptor. BackgroundAdvantagesThe dynorphin analog targets a different pathway, bradykinin receptors instead of NMDA receptors, to offer pain relief without the standard side effects.The series of dimorphic A analogs show therapeutic benefit to modulate pain, since it has been shown that up-regulation of dynorphin causes hyperalgesia by interacting with the bradykinin receptor.ApplicationsUse as an analgesic, specifically analgesia against chronic pain (Burgess and Williams 3756).Another potential application for this invention is use as an anti-inflammatory drug.There is a possibility, that with little to no modification. This particular dynorphin analog can be used to treat mild inflammationHas potential application in pain modulation and analgesiaInventorsVictor HrubyJosephine LaiYeon Sun LeeFrank Porreca ContactPaul EynottLicensing Manager, Tech Launch ArizonaPaulE@tla.arizona.edu Refer to technology #UA12-097

USA