Pain remains a significant public health issue with two-thirds of patients achieving little to no pain relief from the myriad of currently available pharmacotherapies and dosing regimens. The use of opioid (e.g. morphine) pharmacotherapies produces several rewarding and reinforcing side effects, which result in the drugs’ diversion to abuse settings. Glial cells have been found to play a critical role in initiating and maintaining increased nociception in response to peripheral nerve injury. The opioids-induced glial cell activation attenuates opioid-induced pain suppression and enhances the development of opioid tolerance and dependence, the drug reward, and other negative side effects such as respiratory depression. We are interested in employing structure-based drug design and high-throughput screening techniques to identify novel small-molecule inhibitors of the cell surface receptors that regulate glial cell activation. The identified agents will potentially serve as therapeutics that suppresses opioid-dependence and tolerance.

Fig (Left) Potentiation of opioid analgesics by targeting the TLR4-mediated glial activation. (A) Opioids activate glia by triggering the signal transduction mediated by the TLR4 (dimeric form in complex with MD-2), resulting in the release of cytokine intercellular mediator, interleukin-1 (IL-1), and suppressing the desired opioid-induced neuronal analgesia effect. (B) In the presence of the antagonists of the TLR4-signaling, such as inhibitors of the critical TLR4 homodimerization or the TLR4/MD-2 interactions, glia stay in the resting state. Opioids (red star) cause analgesia by binding to opioid receptors (orange hexagon). (Right) Designs of peptide antagonists of the TLR4/MD-2 binding based on the TLR4-binding region of MD-2.

Moscow, July 15 2008
Quantum Pharmaceuticals announce drug discovery collaboration with University of Colorado at Boulder. Under the terms of agreement Quantum Pharmaceuticals will apply its state-of-the-art in-house drug discovery technology to discover novel small molecule inhibitors in inflammation area. CU-Boulder is to further develop the discovered inhibitors. The targets and financial terms were not disclosed.
About Quantum Pharmaceuticals
Quantum Pharmaceuticals is a drug discovery company based in Moscow, Russia specializing in small molecule screening and design through the use of its proprietary technology platform.
About CU-Boulder
As the flagship university of the state of Colorado, CU-Boulder is a dynamic community of scholars and learners. As one of 34 U.S. public institutions belonging to the prestigious Association of American Universities (AAU) – and the only member in the Rocky Mountain region – we have a proud tradition of academic excellence, with four Nobel laureates and more than 50 members of prestigious academic academies. CU-Boulder has blossomed in size and quality since we opened our doors in 1877 – attracting superb faculty, staff, and students and building strong programs in the sciences, engineering, business, law, arts, humanities, education, music, and many other disciplines. Today, with our sights set on becoming the standard for the great comprehensive public research universities of the new century, we strive to serve the people of Colorado and to engage with the world through excellence in our teaching, research, creative work, and service.