Enzymatic synthesis of 2-chloropurine arabinonucleosides with chiral amino acid amides at the c6 position and an evaluation of antiproliferative activity in vitro
A number of purine arabinosides containing chiral amino acid amides at the C6 position of the purine were synthesized using a transglycosylation reaction with recombinant E. coli nucleoside phosphorylases. Arsenolysis of 2-chloropurine ribosides with chiral amino acid amides at C6 was used for the enzymatic synthesis, and the reaction equilibrium shifted towards the synthesis of arabinonucleosides. The synthesized nucleosides were shown to be resistant to the action of E. coli adenosine deaminase. The antiproliferative activity of the synthesized nucleosides was studied on human acute myeloid leukemia cell line U937. Among all the compounds, the serine derivative exhibited an activity level (IC50 = 16 μM) close to that of Nelarabine (IC50 = 3 μM) and was evaluated as active. The work is published in the International Journal of Molecular Sciences. Learn more
News 
- New structural data made it possible to decipher the mechanism of human oncochannel TRPV6 inhibition by the natural phytoestrogen genistein
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V.23 Calcium-selective oncochannel TRPV6 is the major driver of cell proliferation in human body and its overexpression was found in some of the most severe human cancers, including leukemia, breast, prostate, colon, ovarian, thyroid, and endometrial cancers. While significant effort has been invested in the development of synthetic TRPV6 inhibitors, natural channel blockers have been largely neglected despite of their pharmacological value.
- Enzymatic synthesis of 2-chloropurine arabinonucleosides with chiral amino acid amides at the c6 position and an evaluation of antiproliferative activity in vitro
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IV.5 A number of purine arabinosides containing chiral amino acid amides at the C6 position of the purine were synthesized using a transglycosylation reaction with recombinant E. coli nucleoside phosphorylases.
- Doxorubicin-Loaded Polyelectrolyte Multilayer Capsules Modified with Antitumor DR5-Specific TRAIL Variant
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III.29 Carriers providing active targeted delivery of anticancer drugs to tumor cells are promising for cancer chemotherapy. A team of scientists from the Laboratory of protein engineering and the Laboratory of Biomedical Materials IBCh RAS in collaboration with collegues from other Russian Institutes have developed biodegradable polyelectrolyte microcapsules which have been modified with the DR5-B ligand.
Events
- "Molecular Brain" seminar, Epilepsy and channelopathies: from molecular mechanisms to the clinic and back
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IX.22.22 (This event is over) The seminar will take place on September 22 at 16:00 in the Minor hall. Three presentations will focus on the current understanding of epilepsy and channelopathies and will consider various aspects: molecular and physiological mechanisms, as well as approaches to therapy. Everyone is cordially invited!