The Experts below are selected from a list of 27 Experts worldwide ranked by ideXlab platform
Francisco Gamarro - One of the best experts on this subject based on the ideXlab platform.
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Sitamaquine Sensitivity in Leishmania Species Is Not Mediated by Drug Accumulation in Acidocalcisomes
Antimicrobial agents and chemotherapy, 2008Co-Authors: Carmen López-martín, José M. Pérez-victoria, Luis Alberto Vieira De Carvalho, Santiago Castanys, Francisco GamarroAbstract:Sitamaquine (WR6026), an 8-Aminoquinoline Derivative, is a new antileishmanial oral drug. As a lipophilic weak base, it rapidly accumulates in acidic compartments, represented mainly by acidocalcisomes. In this work, we show that the antileishmanial action of sitamaquine is unrelated to its level of accumulation in these acidic vesicles. We have observed significant differences in sitamaquine sensitivity and accumulation between Leishmania species and strains, and interestingly, there is no correlation between them. However, there is a relationship between the levels of accumulation of sitamaquine and acidotropic probes, acidocalcisomes size, and polyphosphate levels. The Leishmania major AP3δ-null mutant line, in which acidocalcisomes are devoid of their usual polyphosphate and proton content, is unable to accumulate sitamaquine; however, both the parental strain and the AP3δ-null mutants showed similar sensitivities to sitamaquine. Our findings provide clear evidence that the antileishmanial action of sitamaquine is unrelated to its accumulation in acidocalcisomes.
Dawit A Ejigu - One of the best experts on this subject based on the ideXlab platform.
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tafenoquine and its potential in the treatment and relapse prevention of plasmodium vivax malaria the evidence to date
Drug Design Development and Therapy, 2016Co-Authors: Yehenew A Ebstie, Solomon M Abay, Wondimagegn Tamiru Tadesse, Dawit A EjiguAbstract:Despite declining global malaria incidence, the disease continues to be a threat to people living in endemic regions. In 2015, an estimated 214 million new malaria cases and 438,000 deaths due to malaria were recorded. Plasmodium vivax is the second most common cause of malaria next to Plasmodium falciparum. Vivax malaria is prevalent especially in Southeast Asia and the Horn of Africa, with enormous challenges in controlling the disease. Some of the challenges faced by vivax malaria-endemic countries include limited access to effective drugs treating liver stages of the parasite (schizonts and hypnozoites), emergence/spread of drug resistance, and misperception of vivax malaria as nonlethal. Primaquine, the only 8-Aminoquinoline Derivative approved by the US Food and Drug Administration, is intended to clear intrahepatic hypnozoites of P. vivax (radical cure). However, poor adherence to a prolonged treatment course, drug-induced hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency, and the emergence of resistance make it imperative to look for alternative drugs. Therefore, this review focuses on data accrued to date on tafenoquine and gives insight on the potential role of the drug in preventing relapse and radical cure of patients with vivax malaria.
Carmen López-martín - One of the best experts on this subject based on the ideXlab platform.
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Sitamaquine Sensitivity in Leishmania Species Is Not Mediated by Drug Accumulation in Acidocalcisomes
Antimicrobial agents and chemotherapy, 2008Co-Authors: Carmen López-martín, José M. Pérez-victoria, Luis Alberto Vieira De Carvalho, Santiago Castanys, Francisco GamarroAbstract:Sitamaquine (WR6026), an 8-Aminoquinoline Derivative, is a new antileishmanial oral drug. As a lipophilic weak base, it rapidly accumulates in acidic compartments, represented mainly by acidocalcisomes. In this work, we show that the antileishmanial action of sitamaquine is unrelated to its level of accumulation in these acidic vesicles. We have observed significant differences in sitamaquine sensitivity and accumulation between Leishmania species and strains, and interestingly, there is no correlation between them. However, there is a relationship between the levels of accumulation of sitamaquine and acidotropic probes, acidocalcisomes size, and polyphosphate levels. The Leishmania major AP3δ-null mutant line, in which acidocalcisomes are devoid of their usual polyphosphate and proton content, is unable to accumulate sitamaquine; however, both the parental strain and the AP3δ-null mutants showed similar sensitivities to sitamaquine. Our findings provide clear evidence that the antileishmanial action of sitamaquine is unrelated to its accumulation in acidocalcisomes.
Yehenew A Ebstie - One of the best experts on this subject based on the ideXlab platform.
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tafenoquine and its potential in the treatment and relapse prevention of plasmodium vivax malaria the evidence to date
Drug Design Development and Therapy, 2016Co-Authors: Yehenew A Ebstie, Solomon M Abay, Wondimagegn Tamiru Tadesse, Dawit A EjiguAbstract:Despite declining global malaria incidence, the disease continues to be a threat to people living in endemic regions. In 2015, an estimated 214 million new malaria cases and 438,000 deaths due to malaria were recorded. Plasmodium vivax is the second most common cause of malaria next to Plasmodium falciparum. Vivax malaria is prevalent especially in Southeast Asia and the Horn of Africa, with enormous challenges in controlling the disease. Some of the challenges faced by vivax malaria-endemic countries include limited access to effective drugs treating liver stages of the parasite (schizonts and hypnozoites), emergence/spread of drug resistance, and misperception of vivax malaria as nonlethal. Primaquine, the only 8-Aminoquinoline Derivative approved by the US Food and Drug Administration, is intended to clear intrahepatic hypnozoites of P. vivax (radical cure). However, poor adherence to a prolonged treatment course, drug-induced hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency, and the emergence of resistance make it imperative to look for alternative drugs. Therefore, this review focuses on data accrued to date on tafenoquine and gives insight on the potential role of the drug in preventing relapse and radical cure of patients with vivax malaria.
José M. Pérez-victoria - One of the best experts on this subject based on the ideXlab platform.
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Sitamaquine Sensitivity in Leishmania Species Is Not Mediated by Drug Accumulation in Acidocalcisomes
Antimicrobial agents and chemotherapy, 2008Co-Authors: Carmen López-martín, José M. Pérez-victoria, Luis Alberto Vieira De Carvalho, Santiago Castanys, Francisco GamarroAbstract:Sitamaquine (WR6026), an 8-Aminoquinoline Derivative, is a new antileishmanial oral drug. As a lipophilic weak base, it rapidly accumulates in acidic compartments, represented mainly by acidocalcisomes. In this work, we show that the antileishmanial action of sitamaquine is unrelated to its level of accumulation in these acidic vesicles. We have observed significant differences in sitamaquine sensitivity and accumulation between Leishmania species and strains, and interestingly, there is no correlation between them. However, there is a relationship between the levels of accumulation of sitamaquine and acidotropic probes, acidocalcisomes size, and polyphosphate levels. The Leishmania major AP3δ-null mutant line, in which acidocalcisomes are devoid of their usual polyphosphate and proton content, is unable to accumulate sitamaquine; however, both the parental strain and the AP3δ-null mutants showed similar sensitivities to sitamaquine. Our findings provide clear evidence that the antileishmanial action of sitamaquine is unrelated to its accumulation in acidocalcisomes.
