Search Results - "Verlinde, Christophe"

Rational Modification of a Candidate Cancer Drug for Use Against Chagas Disease by Kraus, James M, Verlinde, Christophe L. M. J, Karimi, Mandana, Lepesheva, Galina I, Gelb, Michael H, Buckner, Frederick S

“…Chagas disease is one of the major neglected diseases of the world. Existing drug therapies are limited, ineffective, and highly toxic. We describe a novel…”
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Genomic-scale prioritization of drug targets: the TDR Targets database by Agüero, Fernán, Berriman, Matthew, Nwaka, Solomon, Ralph, Stuart A, Roos, David S, Van Voorhis, Wesley C, Al-Lazikani, Bissan, Aslett, Martin, Buckner, Frederick S, Campbell, Robert K, Carmona, Santiago, Carruthers, Ian M, Chan, A. W. Edith, Chen, Feng, Crowther, Gregory J, Doyle, Maria A, Hertz-Fowler, Christiane, Hopkins, Andrew L, McAllister, Gregg, Overington, John P, Pain, Arnab, Paolini, Gaia V, Pieper, Ursula, Riechers, Aaron, Sali, Andrej, Shanmugam, Dhanasekaran, Suzuki, Takashi, Verlinde, Christophe L. M. J

“…The wealth of genomic data for pathogens that cause tropical diseases hold considerable promise for the discovery of novel drugs. An international consortium…”
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Toxoplasma gondii calcium-dependent protein kinase 1 is a target for selective kinase inhibitors by Ojo, Kayode K, Larson, Eric T, Keyloun, Katelyn R, Castaneda, Lisa J, DeRocher, Amy E, Inampudi, Krishna K, Kim, Jessica E, Arakaki, Tracy L, Murphy, Ryan C, Zhang, Li, Napuli, Alberto J, Maly, Dustin J, Verlinde, Christophe L M J, Buckner, Frederick S, Parsons, Marilyn, Hol, Wim G J, Merritt, Ethan A, Van Voorhis, Wesley C

“…A family of calcium-dependent protein kinases (CDPK) is present in apicomplexan parasites but not in animals, indicating their potential as targets for…”
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Optimization of Methionyl tRNA-Synthetase Inhibitors for Treatment of Cryptosporidium Infection by Buckner, Frederick S, Ranade, Ranae M, Gillespie, J Robert, Shibata, Sayaka, Hulverson, Matthew A, Zhang, Zhongsheng, Huang, Wenlin, Choi, Ryan, Verlinde, Christophe L M J, Hol, Wim G J, Ochida, Atsuko, Akao, Yuichiro, Choy, Robert K M, Van Voorhis, Wesley C, Arnold, Sam L M, Jumani, Rajiv S, Huston, Christopher D, Fan, Erkang

“…Cryptosporidiosis is one of the leading causes of moderate to severe diarrhea in children in low-resource settings. The therapeutic options for…”
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Spontaneous Selection of Cryptosporidium Drug Resistance in a Calf Model of Infection by Hasan, Muhammad M, Stebbins, Erin E, Choy, Robert K M, Gillespie, J Robert, de Hostos, Eugenio L, Miller, Peter, Mushtaq, Aisha, Ranade, Ranae M, Teixeira, José E, Verlinde, Christophe L M J, Sateriale, Adam, Zhang, Zhongsheng, Osbourn, Damon M, Griggs, David W, Fan, Erkang, Buckner, Frederick S, Huston, Christopher D

“…The intestinal protozoan is a leading cause of diarrheal disease and mortality in young children. There is currently no fully effective treatment for…”
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Development of Methionyl-tRNA Synthetase Inhibitors as Antibiotics for Gram-Positive Bacterial Infections by Faghih, Omeed, Zhang, Zhongsheng, Ranade, Ranae M, Gillespie, J Robert, Creason, Sharon A, Huang, Wenlin, Shibata, Sayaka, Barros-Álvarez, Ximena, Verlinde, Christophe L M J, Hol, Wim G J, Fan, Erkang, Buckner, Frederick S

“…Antibiotic-resistant bacteria are widespread and pose a growing threat to human health. New antibiotics acting by novel mechanisms of action are needed to…”
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Inhibitors of methionyl-tRNA synthetase have potent activity against Giardia intestinalis trophozoites by Ranade, Ranae M, Zhang, Zhongsheng, Gillespie, J Robert, Shibata, Sayaka, Verlinde, Christophe L M J, Hol, Wim G J, Fan, Erkang, Buckner, Frederick S

“…The methionyl-tRNA synthetase (MetRS) is a novel drug target for the protozoan pathogen Giardia intestinalis. This protist contains a single MetRS that is…”
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A Specific Inhibitor of PfCDPK4 Blocks Malaria Transmission: Chemical-genetic Validation by 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, Van Voorhis, Wesley C.

“…Malaria parasites are transmitted by mosquitoes, and blocking parasite transmission is critical in reducing or eliminating malaria in endemic regions. Here, we…”
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Second Generation Analogues of the Cancer Drug Clinical Candidate Tipifarnib for Anti-Chagas Disease Drug Discovery by Kraus, James M, Tatipaka, Hari Babu, McGuffin, Sarah A, Chennamaneni, Naveen Kumar, Karimi, Mandana, Arif, Jenifer, Verlinde, Christophe L. M. J, Buckner, Frederick S, Gelb, Michael H

“…We previously reported that the cancer drug clinical candidate tipifarnib kills the causative agent of Chagas disease, Trypanosoma cruzi, by blocking…”
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Transmission of malaria to mosquitoes blocked by bumped kinase inhibitors by 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

“…Effective control and eradication of malaria will require new tools to prevent transmission. Current antimalarial therapies targeting the asexual stage of…”
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Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1 by Zhang, Zhongsheng, Ojo, Kayode K., Johnson, Steven M., Larson, Eric T., He, Penqing, Geiger, Jennifer A., Castellanos-Gonzalez, Alejandro, White, A. Clinton, Parsons, Marilyn, Merritt, Ethan A., Maly, Dustin J., Verlinde, Christophe L.M.J., Van Voorhis, Wesley C., Fan, Erkang

“…Calcium-dependent protein kinase-1 (CDPK1) from Cryptosporidium parvum (CpCDPK1) and Toxoplasma gondii (TgCDPK1) have become attractive targets for discovering…”
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Distinct States of Methionyl-tRNA Synthetase Indicate Inhibitor Binding by Conformational Selection by Koh, Cho Yeow, Kim, Jessica E., Shibata, Sayaka, Ranade, Ranae M., Yu, Mingyan, Liu, Jiyun, Gillespie, J. Robert, Buckner, Frederick S., Verlinde, Christophe L.M.J., Fan, Erkang, Hol, Wim G.J.

“…To guide development of new drugs targeting methionyl-tRNA synthetase (MetRS) for treatment of human African trypanosomiasis, crystal structure determinations…”
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Urea-Based Inhibitors of Trypanosoma brucei Methionyl-tRNA Synthetase: Selectivity and in Vivo Characterization by Shibata, Sayaka, Gillespie, J. Robert, Ranade, Ranae M, Koh, Cho Yeow, Kim, Jessica E, Laydbak, Joy U, Zucker, Frank H, Hol, Wim G. J, Verlinde, Christophe L. M. J, Buckner, Frederick S, Fan, Erkang

“…Urea-based methionyl-tRNA synthetase inhibitors were designed, synthesized, and evaluated for their potential toward treating human African trypanosomiasis…”
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Structures of Trypanosoma brucei methionyl-tRNA synthetase with urea-based inhibitors provide guidance for drug design against sleeping sickness by Koh, Cho Yeow, Kim, Jessica E, Wetzel, Allan B, de van der Schueren, Will J, Shibata, Sayaka, Ranade, Ranae M, Liu, Jiyun, Zhang, Zhongsheng, Gillespie, J Robert, Buckner, Frederick S, Verlinde, Christophe L M J, Fan, Erkang, Hol, Wim G J

“…Methionyl-tRNA synthetase of Trypanosoma brucei (TbMetRS) is an important target in the development of new antitrypanosomal drugs. The enzyme is essential,…”
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Selective Inhibitors of Methionyl-tRNA Synthetase Have Potent Activity against Trypanosoma brucei Infection in Mice by SHIBATA, Sayaka, GILLESPIE, J. Robert, MERRITT, Ethan A, HOL, Wim G. J, VERLINDE, Christophe L. M. J, ERKANG FAN, BUCKNER, Frederick S, KELLEY, Angela M, NAPULI, Alberto J, ZHONGSHENG ZHANG, KOVZUN, Kuzma V, PEFLEY, Ranae M, LAM, Jocelyn, ZUCKER, Frank H, VAN VOORHIS, Wesley C

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Pharmacological Characterization, Structural Studies, and In Vivo Activities of Anti-Chagas Disease Lead Compounds Derived from Tipifarnib by BUCKNER, Frederick S, TEREZINHA BAHIA, Maria, VERLINDE, Christophe L. M. J, CHARMAN, Susan A, LEPESHEVA, Galina I, GELBC, Michael H, KUMAR SURYADEVARA, Praveen, WHITE, Karen L, SHACKLEFORD, David M, KUMAR CHENNAMANENI, Naveen, HULVERSON, Matthew A, LAYDBAK, Joy U, CHATELAIN, Eric, SCANDALE, Ivan

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Glycogen Synthase Kinase 3 Is a Potential Drug Target for African Trypanosomiasis Therapy by OJO, Kayode K, GILLESPIE, J. Robert, WELLS, Timothy N. C, VAN VOORHIS, Wesley C, RIECHERS, Aaron J, NAPULI, Alberto J, VERLINDE, Christophe L. M. J, BUCKNER, Frederick S, GELB, Michael H, DOMOSTOJ, Mathias M, WELLS, Susan J, SCHEER, Alexander

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Missense Mutations in the Regulatory Domain of PKCγ: A New Mechanism for Dominant Nonepisodic Cerebellar Ataxia by Chen, Dong-Hui, Brkanac, Zoran, Christophe Verlinde, L.M.J., Tan, Xiao-Jian, Bylenok, Laura, Nochlin, David, Matsushita, Mark, Lipe, Hillary, Wolff, John, Fernandez, Magali, Cimino, P.J., Thomas Bird, D., Raskind, Wendy H.

“…We report a nonepisodic autosomal dominant (AD) spinocerebellar ataxia (SCA) not caused by a nucleotide repeat expansion that is, to our knowledge, the first…”
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Identification of CD46 Binding Sites within the Adenovirus Serotype 35 Fiber Knob by HONGJIE WANG, LIAW, Yen-Chywan, LIEBER, André, STONE, Daniel, KALYUZHNIY, Oleksandr, AMIRASLANOV, Imameddin, TUVE, Sebastian, VERLINDE, Christophe L. M. J, SHAYAKHMETOV, Dmitry, STEHLE, Thilo, ROFFLER, Steve

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Multiple Determinants for Selective Inhibition of Apicomplexan Calcium-Dependent Protein Kinase CDPK1 by 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, Merritt, Ethan A

“…Diseases caused by the apicomplexan protozoans Toxoplasma gondii and Cryptosporidium parvum are a major health concern. The life cycle of these parasites is…”
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