On 2 October at 14:00 p.m. (Moscow time)
In this lecture, we describe novel all-on-resin strategies permitting the synthesis of super potent (nano- and picomolar) tubulysin and dolastatin analogs and their functionalization with cleavable linkers that allow their traceless release after the selective internalization into cancer cells. We also present synthetic methods towards novel targeting peptides and their conjugates to the cytotoxic payloads.
Daniel García Rivera — Full Professor, University of Havana (UH), Cuba.
The development of novel pharmaceuticals and therapeutic agents is one of the prioritized areas for the growth of a knowledge-based economy. In the field of cancer therapy, antibody-drug conjugates (ADCs) are among the most powerful tools for the development of oncology therapeutics. This class of anticancer agent consists of recombinant monoclonal antibodies (mAbs) covalently linked to highly potent cytotoxic small-molecule drugs, called payloads or warheads, thus comprising high selectivity for cancer cells and maintaining the typically favorable pharmacokinetics of mAbs. An important step of ADC development is the synthesis of highly cytotoxic compounds. Among them, antimitotic peptides such as auristatins, dolastatins and tubulysins are among the anticancer payloads of greatest promise due to their very high cytotoxicity, especially against multi-drug resistant cell lines.
Participants: students, postgraduates and scientific-pedagogical workers of the faculty of Sciences of RUDN and other Universities.