Normally siRNA do not penetrate cell membranes without transfection reagents. In Quantum Pharmaceutical we developed a new nanoscale complex with ability to transport siRNA over cell membranes of a cancer cell. In experiments with fluorescent siRNA molecules coupled with our proprietory transport system we conformed the ability of the complex to penetrate the cell membrane already in nanomolar concentration range. To demonstrate that we performed the experiments on lung cancer cells A549 and H1299 incubated with 20 nM concentration of our lead compound QP-654 and observed after overnight incubation.

The graphs above show uptake of the flourescent siRNA complex by the cancer cells. The left upper picture represents nuclear staining of A549 cells with Hoechst dye. The right upper picture represent uptake of fluorescent siRNA complex by the cancer cells. The lower picture corresponds to superposition of upper pictures and indicates the accumulation of the siRNA-containing complex in the cancer sells and thus proves the efficacy of the transport system.

Moscow, October, 28 2008

Quantum Pharmaceuticals announce drug discovery collaboration with Children's Cancer Institute Australia's (CCIA). Under the terms of the agreement Quantum Pharmaceuticals gets access to CCIA in-house disease target data. Quantum Pharmaceuticals will contribute its technological breakthroughs and expertise in small molecule drug discovery to feed the portfolio of CCIA with new drug candidates. CCIA 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 CCIA

Children's Cancer Institute Australia's (CCIA) vision is to save the lives of all children with cancer and eliminate their suffering.Our mission is to be a leader in preventing cancer, to find new ways of curing cancer in children through world-class research, to ensure the best possible quality of life for these children and their families, to share the vision with others and to increase awareness, participation and funding.

Quantum Pharmaceuticals announce drug discovery collaboration with Fox Chase Cancer Center 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 cancer area. The targets and financial terms were not disclosed.

Fox Chase Cancer Center is one of the US nation's first comprehensive cancer centers designated by the National Cancer Institute in 1974. Fox Chase's activities include basic, clinical and prevention research; detection and treatment of cancer; and community outreach programs.
Researchers at Fox Chase investigate problems that range from understanding the fundamental mechanisms of biomolecular reactions all the way to the treatment of neoplastic diseases in the clinic.

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

Following the classic thrombine study, we catch up with a more important target: PDK1 kinase.

Pyruvate dehydrogenase kinase, isozyme 1, also known as PDK1, is a human gene.It codes for an isozyme of pyruvate dehydrogenase kinase (PDK).Pyruvate dehydrogenase (PDH) is a part of a mitochondrial multienzyme complex that catalyzes the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. The enzymatic activity is regulated by a phosphorylation/dephosphorylation cycle. Phosphorylation of PDH by a specific pyruvate dehydrogenase kinase (PDK) results in inactivation.

There are no as much known inhibitors as for thrombine. BindingDB gives a few more than 70 compounds with measured binding affinities, all relatively strong binders, many of them similar to each other. We run our QUANTUM software to perform docking and the affinity calculations. The results are represented on the graph and demonstrate a solid correlation. In fact the correlation shows QUANTUM's ability to identify strong binders and distinguish between similar compounds (selectivity).