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Prous Institute Presents in Silico and Experimental Findings on Targets for Neuroplasticity Modulation and Cancer Research at 22nd International Symposium on Medicinal Chemistry

Berlin, Germany: Prous Institute for Biomedical Research has announced the presentation of study results using its proprietary computational platform, Symmetry®, to identify molecular and cellular targets involved in neuroplasticity and tumor cell proliferation at the 22nd International Symposium on Medicinal Chemistry organized by the European Federation of Medicinal Chemistry (EFMC).

Prous Institute's in silico solution for drug discovery and toxicity screening, Symmetry®, was used to construct predictive computational systems mimicking the different processes involved in order to design new molecules with potential pharmacological activity.

 

Neuroplasticity Modulation

Neuroplasticity is widely considered to be a cellular mechanism underlying learning and memory and covers broad disease areas. A series of compounds identified at Prous Institute exhibit cognitive effects in behavioral learning tests after acute administration and last several days after a single dose. This is an important finding as existing compounds only show their effects on memory improvement after chronic administration.

In the study presented, Prous Institute used Symmetry® to assess more than 30 molecular and cellular targets involved in neuroplasticity. Behavioral studies in mice showed that while the selected compounds did not affect exploration, they did enhance short- and long-term memory in passive avoidance and object recognition tests. In addition, the psychoactive effect measured in comparison to previous hippocampal and cortico-hippocampal tests indicated a procognitive action. The results support the hypothesis of neuroplasticity-mediated cognitive enhancement and have thus served to foster the development of selected compounds.

 

Tumor cell proliferation

Prous Institute has also designed, synthesized and tested magnolol and honokiol derivatives that exhibit a potent, broad spectrum of activity against a wide variety of tumor cells compared with the parent compounds. The synthesized compounds inhibited both Src and EGFR kinases, thus making them promising candidates for the treatment of cancer as they are likely to show a reduced tendency to develop cancer cell resistance.

Magnolol and honokiol are the main components of Magnolia officinalis, a plant which has been used for millennia in traditional Chinese medicine and in Japanese Kampo medicine. Both compounds have been reported to exhibit multiple pharmacological actions, including antitumor, antiplatelet, antibacterial, anxiolytic and antidepressant activities.

The newly identified compounds presented at the conference were also active as inhibitors of Akt3 kinase, CDK2 kinase and MAPK1 kinase. Some compounds were also found to have modulating effects on the Wnt/β-catenin signaling pathway, which is hyperactivated in most human cancers and is suggested to represent an attractive therapeutic target. Based on this finding, Prous Institute has initiated a new drug discovery cycle to translate this finding into the development of modulators of the Wnt/β-catenin pathway.

Full results of these studies were presented at the 22nd International Symposium on Medicinal Chemistry, EFMC (European Federation for Medicinal Chemistry)–ISMC 2012 held in Berlin, Germany from September 2-6, 2012.  

 

About Prous Institute for Biomedical Research

Prous Institute for Biomedical Research (PIBR) is a privately-held biotechnology company focused on the discovery of novel therapeutics through the application of its proprietary drug discovery platform, Symmetry®, and expertise in synthetic chemistry, molecular and cellular biology, and pharmacology. Our uniqueness and our core competencies reflect 50 years of experience creating and managing biomedical knowledge.