Scorpion venom to carry drugs in the mind [Report]



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The Peptide and Protein Laboratory of the Institute for Research in Biomedicine (IRB Barcelona) published an article in Chemical Communications describing the use of a peptide derived from chlorotoxin, present in scorpion venom, to transport drugs across the blood-brain barrier.

The barrier serves to protect the brain from toxic substances, but it also prevents many potential therapeutic drugs from entering. "About 98% of the drugs that can have therapeutic applications can not be used because they can not cross this barrier," explains laboratory manager Ernest Giralt.

The researchers chemically synthesized the chlorotoxin and a series of analogues that retain some of the properties of the parent peptide. They investigated the efficacy of these compounds in cellular models of BBB and demonstrated that the MiniCTX3 peptide had the ability to transport compounds across the BBB "with high efficiency".

In the same way that traditional medicine uses natural products such as plants and flowers to treat various diseases, the IRB laboratory in Barcelona is inspired by venom to identify peptide shuttles. "Our goal is to allow drugs to enter the brain. To do this, we link them to peptides specifically designed to cross the BBB. The combination of these drugs with the shuttles would improve their efficiency, "says Meritxell Teixidó, co-head of research. "There are only two or three groups in the world dedicated to peptide shuttles. We are working on a number of strategies, one of which is venom, "Giralt said.

In previous studies, scientists have developed a shuttle peptide with BBB permeability inspired by a peptide of bee venom, namely apamin.

After these positive results, the laboratory wanted to determine if the venom could be a universal source of peptide shuttles. "Thousands of venoms containing millions of shuttle potential peptides have been described. We chose chlorotoxin because it has already been reported that it acts as a toxin in the brain, "says Teixidó.

More information:
Cristina Diaz-Perlas et al. From venoms to BBB shuttles. MiniCTX3: a molecular vector derived from scorpion venom, Chemical Communications (2018). DOI: 10.1039 / C8CC06725B

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The Peptide and Protein Laboratory of the Institute for Research in Biomedicine (IRB Barcelona) published an article in Chemical Communications describing the use of a peptide derived from chlorotoxin, present in scorpion venom, to transport drugs across the blood-brain barrier.

The barrier serves to protect the brain from toxic substances, but it also prevents many potential therapeutic drugs from entering. "About 98% of the drugs that can have therapeutic applications can not be used because they can not cross this barrier," explains laboratory manager Ernest Giralt.

The researchers chemically synthesized the chlorotoxin and a series of analogues that retain some of the properties of the parent peptide. They investigated the efficacy of these compounds in cellular models of BBB and demonstrated that the MiniCTX3 peptide had the ability to transport compounds across the BBB "with high efficiency".

In the same way that traditional medicine uses natural products such as plants and flowers to treat various diseases, the IRB laboratory in Barcelona is inspired by venom to identify peptide shuttles. "Our goal is to allow drugs to enter the brain. To do this, we link them to peptides specifically designed to cross the BBB. The combination of these drugs with the shuttles would improve their efficiency, "says Meritxell Teixidó, co-head of research. "There are only two or three groups in the world dedicated to peptide shuttles. We are working on a number of strategies, one of which is venom, "Giralt said.

In previous studies, scientists have developed a shuttle peptide with BBB permeability inspired by a peptide of bee venom, namely apamin.

After these positive results, the laboratory wanted to determine if the venom could be a universal source of peptide shuttles. "Thousands of venoms containing millions of shuttle potential peptides have been described. We chose chlorotoxin because it has already been reported that it acts as a toxin in the brain, "says Teixidó.

More information:
Cristina Diaz-Perlas et al. From venoms to BBB shuttles. MiniCTX3: a molecular vector derived from scorpion venom, Chemical Communications (2018). DOI: 10.1039 / C8CC06725B

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