Researchers at Harvard University (USA) define their research as a “turning point in drug discovery”. In an article published in the Harvard Gazette on June 17, they describe how they managed to synthesize a molecule, thehalichondrin, known to be a anticancer agent. If it occurs naturally in sea sponges, in very small amounts, it was so complex that it had never been created in the laboratory.
“Four billion ways to be wrong”
More specifically, the team of Yoshito Kishi, professor of the chemistry department at Harvard, synthesized sufficient quantities ofE7130, a “potential drug” from the class of halichondrins. In preclinical studies, Japanese researchers had already identified this compound as a promising agent to target the tumor. That was thirty-three years ago already. It took three decades to finally produce enough.
This molecule is actually particularly difficult to manufacture due to the fact that it has 31 centers of chirality, that is to say 31 points which define how it is oriented in space. According to scientists, there were therefore approximately “four billion ways to be wrong”. “It’s an unprecedented success […] No one had been able to produce halichondrins at the 10 gram scale. One milligram is all “, develops Takashi Owa, co-author of the study and head of drug creation for the Japanese pharmaceutical company Eisai, collaborator of the project.
Encouraging results
“Professor Kishi’s expertise provided us with a unique and exciting opportunity to test the molecule in our systems., he continues. [Il a réalisé] a remarkable total synthesis, which allowed us to initiate a clinical trial of the E7130. “ Studies in vitro and in vivo on mice have been launched to better understand its mode of action. It seems that the molecule is beautiful and very inhibitory of microtubule dynamics, molecules important for cell division. As a reminder, tumors develop following a disruption of cell growth.
There were already treatments capable of targeting cancer cells, such as paclitaxel or vinblastine. But it seems that this compound performs much better, although it has not yet been tested on humans. The team of researchers now hopes to start a second clinical trial in the United States.
The full study was published in Scientific Reports June 17.
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