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Your search keyword '"Fox, Anna M. W."' showing total 12 results
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12 results on '"Fox, Anna M. W."'

1. A Specific Inhibitor of PfCDPK4 Blocks Malaria Transmission: Chemical-genetic Validation

Author

Ojo, Kayode K., Eastman, Richard T., Vidadala, RamaSubbaRao, Zhang, Zhongsheng, Rivas, Kasey L., Choi, Ryan, Lutz, Justin D., Reid, Molly C., Fox, Anna M. W., Hulverson, Matthew A., Kennedy, Mark, Isoherranen, Nina, Kim, Laura M., Comess, Kenneth M., Kempf, Dale J., Verlinde, Christophe L. M. J., Su, Xin-zhuan, Kappe, Stefan H. I., Maly, Dustin J., Fan, Erkang, and Van Voorhis, Wesley C.

Published
2014

4. Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds

Author

Crowther, Gregory J., primary, Hillesland, Heidi K., additional, Keyloun, Katelyn R., additional, Reid, Molly C., additional, Lafuente-Monasterio, Maria Jose, additional, Ghidelli-Disse, Sonja, additional, Leonard, Stephen E., additional, He, Panqing, additional, Jones, Jackson C., additional, Krahn, Mallory M., additional, Mo, Jack S., additional, Dasari, Kartheek S., additional, Fox, Anna M. W., additional, Boesche, Markus, additional, El Bakkouri, Majida, additional, Rivas, Kasey L., additional, Leroy, Didier, additional, Hui, Raymond, additional, Drewes, Gerard, additional, Maly, Dustin J., additional, Van Voorhis, Wesley C., additional, and Ojo, Kayode K., additional

Published
2016
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5. Transmission of malaria to mosquitoes blocked by bumped kinase inhibitors

Author

Ojo, Kayode K, Pfander, Claudia, Mueller, Natascha R, Burstroem, Charlotte, Larson, Eric T, Bryan, Cassie M, Fox, Anna M W, Reid, Molly C, Johnson, Steven M, Murphy, Ryan C, Kennedy, Mark, Mann, Henning, Leibly, David J, Hewitt, Stephen N, Verlinde, Christophe L M J, Kappe, Stefan, Merritt, Ethan A, Maly, Dustin J, Billker, Oliver, Van Voorhis, Wesley C, Ojo, Kayode K, Pfander, Claudia, Mueller, Natascha R, Burstroem, Charlotte, Larson, Eric T, Bryan, Cassie M, Fox, Anna M W, Reid, Molly C, Johnson, Steven M, Murphy, Ryan C, Kennedy, Mark, Mann, Henning, Leibly, David J, Hewitt, Stephen N, Verlinde, Christophe L M J, Kappe, Stefan, Merritt, Ethan A, Maly, Dustin J, Billker, Oliver, and Van Voorhis, Wesley C

Abstract

Effective control and eradication of malaria will require new tools to prevent transmission. Current antimalarial therapies targeting the asexual stage of Plasmodium do not prevent transmission of circulating gametocytes from infected humans to mosquitoes. Here, we describe a new class of transmission-blocking compounds, bumped kinase inhibitors (BKIs), which inhibit microgametocyte exflagellation. Oocyst formation and sporozoite production, necessary for transmission to mammals, were inhibited in mosquitoes fed on either BKI-1-treated human blood or mice treated with BKI-1. BKIs are hypothesized to act via inhibition of Plasmodium calcium-dependent protein kinase 4 and predicted to have little activity against mammalian kinases. Our data show that BKIs do not inhibit proliferation of mammalian cell lines and are well tolerated in mice. Used in combination with drugs active against asexual stages of Plasmodium, BKIs could prove an important tool for malaria control and eradication.

Published
2012
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6. A Specific Inhibitor of PfCDPK4 Blocks Malaria Transmission: Chemical-genetic Validation

Author

Ojo, Kayode K., primary, Eastman, Richard T., additional, Vidadala, RamaSubbaRao, additional, Zhang, Zhongsheng, additional, Rivas, Kasey L., additional, Choi, Ryan, additional, Lutz, Justin D., additional, Reid, Molly C., additional, Fox, Anna M. W., additional, Hulverson, Matthew A., additional, Kennedy, Mark, additional, Isoherranen, Nina, additional, Kim, Laura M., additional, Comess, Kenneth M., additional, Kempf, Dale J., additional, Verlinde, Christophe L. M. J., additional, Su, Xin-zhuan, additional, Kappe, Stefan H. I., additional, Maly, Dustin J., additional, Fan, Erkang, additional, and Van Voorhis, Wesley C., additional

Published
2013
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7. Multiple Determinants for Selective Inhibition of Apicomplexan Calcium-Dependent Protein Kinase CDPK1

Author

Larson, Eric T., primary, Ojo, Kayode K., additional, Murphy, Ryan C., additional, Johnson, Steven M., additional, Zhang, Zhongsheng, additional, Kim, Jessica E., additional, Leibly, David J., additional, Fox, Anna M. W., additional, Reid, Molly C., additional, Dale, Edward J., additional, Perera, B. Gayani K., additional, Kim, Jae, additional, Hewitt, Stephen N., additional, Hol, Wim G. J., additional, Verlinde, Christophe L. M. J., additional, Fan, Erkang, additional, Van Voorhis, Wesley C., additional, Maly, Dustin J., additional, and Merritt, Ethan A., additional

Published
2012
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8. Development of Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitors with Potent Anti-Toxoplasma Activity

Author

Johnson, Steven M., primary, Murphy, Ryan C., additional, Geiger, Jennifer A., additional, DeRocher, Amy E., additional, Zhang, Zhongsheng, additional, Ojo, Kayode K., additional, Larson, Eric T., additional, Perera, B. Gayani K., additional, Dale, Edward J., additional, He, Panqing, additional, Reid, Molly C., additional, Fox, Anna M. W., additional, Mueller, Natascha R., additional, Merritt, Ethan A., additional, Fan, Erkang, additional, Parsons, Marilyn, additional, Van Voorhis, Wesley C., additional, and Maly, Dustin J., additional

Published
2012
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9. Multiple Determinantsfor Selective Inhibition ofApicomplexan Calcium-Dependent Protein Kinase CDPK1.

Author

Larson, Eric T., Ojo, Kayode K., Murphy, Ryan C., Johnson, Steven M., Zhang, Zhongsheng, Kim, Jessica E., Leibly, David J., Fox, Anna M. W., Reid, Molly C., Dale, Edward J., Perera, B. Gayani K., Kim, Jae, Hewitt, Stephen N., Hol, Wim G. J., Verlinde, Christophe L. M. J., Fan, Erkang, Van Voorhis, Wesley C., Maly, Dustin J., and Merritt, Ethan A.

Published
2012
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10. Development of Toxoplasma gondiiCalcium-DependentProtein Kinase 1 (TgCDPK1) Inhibitors with PotentAnti-ToxoplasmaActivity.

Author

Johnson, Steven M., Murphy, Ryan C., Geiger, Jennifer A., DeRocher, Amy E., Zhang, Zhongsheng, Ojo, Kayode K., Larson, Eric T., Perera, B. Gayani K., Dale, Edward J., He, Panqing, Reid, Molly C., Fox, Anna M. W., Mueller, Natascha R., Merritt, Ethan A., Fan, Erkang, Parsons, Marilyn, Van Voorhis, Wesley C., and Maly, Dustin J.

Published
2012
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11. Transmission of malaria to mosquitoes blocked by bumped kinase inhibitors.

Author

Ojo, Kayode K., Pfander, Claudia, Mueller, Natascha R., Burstroem, Charlotte, Larson, Eric T., Bryan, Cassie M., Fox, Anna M. W., Reid, Molly C., Johnson, Steven M., Murphy, Ryan C., Kennedy, Mark, Mann, Henning, Leibly, David J., Hewitt, Stephen N., Verlinde, Christophe L. M. J., Kappe, Stefan, Merritt, Ethan A., Maly, Dustin J., Billker, Oliver, and Van Voorhis, Wesley C.

Subjects
*MALARIA, *INFECTIOUS disease transmission, *MOSQUITOES, *KINASE inhibitors, *ANTIMALARIALS, *PLASMODIUM, *SPOROZOITES
Abstract

Effective control and eradication of malaria will require new tools to prevent transmission. Current antimalarial therapies targeting the asexual stage of Plasmodium do not prevent transmission of circulating gametocytes from infected humans to mosquitoes. Here, we describe a new class of transmission-blocking compounds, bumped kinase inhibitors (BKIs), which inhibit microgametocyte exflagellation. Oocyst formation and sporozoite production, necessary for transmission to mammals, were inhibited in mosquitoes fed on either BKI-1- treated human blood or mice treated with BKI-1. BKIs are hypothesized to act via inhibition of Plasmodium calcium-dependent protein kinase 4 and predicted to have little activity against mammalian kinases. Our data show that BKIs do not inhibit proliferation of mammalian cell lines and are well tolerated in mice. Used in combination with drugs active against asexual stages of Plasmodium, BKIs could prove an important tool for malaria control and eradication. [ABSTRACT FROM AUTHOR]

Published
2012
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12. Development of potent and selective Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) inhibitors that block the transmission of malaria to mosquitoes.

Author

Vidadala RS, Ojo KK, Johnson SM, Zhang Z, Leonard SE, Mitra A, Choi R, Reid MC, Keyloun KR, Fox AM, Kennedy M, Silver-Brace T, Hume JC, Kappe S, Verlinde CL, Fan E, Merritt EA, Van Voorhis WC, and Maly DJ

Subjects
Amino Acid Sequence, Animals, Molecular Sequence Data, Sequence Homology, Amino Acid, Antimalarials pharmacology, Calcium metabolism, Malaria, Falciparum transmission, Plasmodium falciparum enzymology, Protein Kinase Inhibitors pharmacology, Protein Kinases drug effects
Abstract

Malaria remains a major health concern for a large percentage of the world's population. While great strides have been made in reducing mortality due to malaria, new strategies and therapies are still needed. Therapies that are capable of blocking the transmission of Plasmodium parasites are particularly attractive, but only primaquine accomplishes this, and toxicity issues hamper its widespread use. In this study, we describe a series of pyrazolopyrimidine- and imidazopyrazine-based compounds that are potent inhibitors of PfCDPK4, which is a calcium-activated Plasmodium protein kinase that is essential for exflagellation of male gametocytes. Thus, PfCDPK4 is essential for the sexual development of Plasmodium parasites and their ability to infect mosquitoes. We demonstrate that two structural features in the ATP-binding site of PfCDPK4 can be exploited in order to obtain potent and selective inhibitors of this enzyme. Furthermore, we demonstrate that pyrazolopyrimidine-based inhibitors that are potent inhibitors of the in vitro activity of PfCDPK4 are also able to block Plasmodium falciparum exflagellation with no observable toxicity to human cells. This medicinal chemistry effort serves as a valuable starting point in the development of safe, transmission-blocking agents for the control of malaria., (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)

Published
2014
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