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Credit: Peter H. Seeberger
A novel compound can inhibit an enzyme that is essential for malaria parasite survival, according to research published in PLOS Biology.
Researchers believe that creating this compound, WEHI-916, is the first step toward developing a new class of antimalarial drugs that could cure and prevent malaria infections caused by all species of the parasite, including those resistant to existing drugs.
The group developed WEHI-916 to block the enzyme Plasmepsin V. They previously showed Plasmepsin V is responsible for controlling the transport of proteins in and out of the malaria parasite.
Now, they’ve used WEHI-916 to prove the importance of Plasmepsin V to the survival of both Plasmodium vivax and Plasmodium falciparum.
“Researchers, including us, had been trying, without success, to learn more about Plasmepsin V using standard genetic techniques,” said study author Just Boddey, PhD, of The Walter and Eliza Hall Institute of Medical Research in Parkville, Victoria, Australia.
“Our idea was to create a drug-like compound that would block Plasmepsin V so we could investigate its importance. We found that blocking Plasmepsin V kills malaria parasites and delivered a new and effective potential drug at the same time.”
Plasmepsin V was an ideal drug target because its inhibition effectively halted the transport of hundreds of malaria proteins, Dr Boddey noted.
“The Plasmodium parasite needs to produce and deliver over 300 different proteins to the red blood cell to survive in the body and hide from the host’s immune system,” he said. “Instead of targeting individual proteins, we can block Plasmepsin V and prevent all of those proteins from leaving the parasite.”
The researchers believe these findings could aid the development of drugs that are effective in curing malaria caused by all 5 species of Plasmodium parasite.
“Our study has shown that Plasmepsin V is a key enzyme in [P vivax and P falciparum], and WEHI-916 can inhibit Plasmepsin V isolated from both of them,” said study author Brad Sleebs, PhD, also of The Walter and Eliza Hall Institute.
“Not only does this compound enable us to prove Plasmepsin V is an excellent drug target, it is a starting point for a research program that could lead to a new class of antimalarial drugs.”
Now, the researchers have turned their attention to developing WEHI-916 and related compounds for human use.
“We are now examining in our insectary whether Plasmepsin V could be a target during other stages of the malaria lifecycle,” Dr Boddey said. “The enzyme is present in the parasites that first infect humans in the liver, as well as in parasite forms that exit humans and infect mosquitoes.”
“If WEHI-916 kills the parasite during these stages as well, it will mean any drugs that target Plasmepsin V can be used as a preventative as well as a cure.” 
Credit: Peter H. Seeberger
A novel compound can inhibit an enzyme that is essential for malaria parasite survival, according to research published in PLOS Biology.
Researchers believe that creating this compound, WEHI-916, is the first step toward developing a new class of antimalarial drugs that could cure and prevent malaria infections caused by all species of the parasite, including those resistant to existing drugs.
The group developed WEHI-916 to block the enzyme Plasmepsin V. They previously showed Plasmepsin V is responsible for controlling the transport of proteins in and out of the malaria parasite.
Now, they’ve used WEHI-916 to prove the importance of Plasmepsin V to the survival of both Plasmodium vivax and Plasmodium falciparum.
“Researchers, including us, had been trying, without success, to learn more about Plasmepsin V using standard genetic techniques,” said study author Just Boddey, PhD, of The Walter and Eliza Hall Institute of Medical Research in Parkville, Victoria, Australia.
“Our idea was to create a drug-like compound that would block Plasmepsin V so we could investigate its importance. We found that blocking Plasmepsin V kills malaria parasites and delivered a new and effective potential drug at the same time.”
Plasmepsin V was an ideal drug target because its inhibition effectively halted the transport of hundreds of malaria proteins, Dr Boddey noted.
“The Plasmodium parasite needs to produce and deliver over 300 different proteins to the red blood cell to survive in the body and hide from the host’s immune system,” he said. “Instead of targeting individual proteins, we can block Plasmepsin V and prevent all of those proteins from leaving the parasite.”
The researchers believe these findings could aid the development of drugs that are effective in curing malaria caused by all 5 species of Plasmodium parasite.
“Our study has shown that Plasmepsin V is a key enzyme in [P vivax and P falciparum], and WEHI-916 can inhibit Plasmepsin V isolated from both of them,” said study author Brad Sleebs, PhD, also of The Walter and Eliza Hall Institute.
“Not only does this compound enable us to prove Plasmepsin V is an excellent drug target, it is a starting point for a research program that could lead to a new class of antimalarial drugs.”
Now, the researchers have turned their attention to developing WEHI-916 and related compounds for human use.
“We are now examining in our insectary whether Plasmepsin V could be a target during other stages of the malaria lifecycle,” Dr Boddey said. “The enzyme is present in the parasites that first infect humans in the liver, as well as in parasite forms that exit humans and infect mosquitoes.”
“If WEHI-916 kills the parasite during these stages as well, it will mean any drugs that target Plasmepsin V can be used as a preventative as well as a cure.”
Credit: Peter H. Seeberger
A novel compound can inhibit an enzyme that is essential for malaria parasite survival, according to research published in PLOS Biology.
Researchers believe that creating this compound, WEHI-916, is the first step toward developing a new class of antimalarial drugs that could cure and prevent malaria infections caused by all species of the parasite, including those resistant to existing drugs.
The group developed WEHI-916 to block the enzyme Plasmepsin V. They previously showed Plasmepsin V is responsible for controlling the transport of proteins in and out of the malaria parasite.
Now, they’ve used WEHI-916 to prove the importance of Plasmepsin V to the survival of both Plasmodium vivax and Plasmodium falciparum.
“Researchers, including us, had been trying, without success, to learn more about Plasmepsin V using standard genetic techniques,” said study author Just Boddey, PhD, of The Walter and Eliza Hall Institute of Medical Research in Parkville, Victoria, Australia.
“Our idea was to create a drug-like compound that would block Plasmepsin V so we could investigate its importance. We found that blocking Plasmepsin V kills malaria parasites and delivered a new and effective potential drug at the same time.”
Plasmepsin V was an ideal drug target because its inhibition effectively halted the transport of hundreds of malaria proteins, Dr Boddey noted.
“The Plasmodium parasite needs to produce and deliver over 300 different proteins to the red blood cell to survive in the body and hide from the host’s immune system,” he said. “Instead of targeting individual proteins, we can block Plasmepsin V and prevent all of those proteins from leaving the parasite.”
The researchers believe these findings could aid the development of drugs that are effective in curing malaria caused by all 5 species of Plasmodium parasite.
“Our study has shown that Plasmepsin V is a key enzyme in [P vivax and P falciparum], and WEHI-916 can inhibit Plasmepsin V isolated from both of them,” said study author Brad Sleebs, PhD, also of The Walter and Eliza Hall Institute.
“Not only does this compound enable us to prove Plasmepsin V is an excellent drug target, it is a starting point for a research program that could lead to a new class of antimalarial drugs.”
Now, the researchers have turned their attention to developing WEHI-916 and related compounds for human use.
“We are now examining in our insectary whether Plasmepsin V could be a target during other stages of the malaria lifecycle,” Dr Boddey said. “The enzyme is present in the parasites that first infect humans in the liver, as well as in parasite forms that exit humans and infect mosquitoes.”
“If WEHI-916 kills the parasite during these stages as well, it will mean any drugs that target Plasmepsin V can be used as a preventative as well as a cure.”