Search Results - "Pollastri, Michael P."

The Aryl Hydrocarbon Receptor is a Critical Regulator of Tissue Factor Stability and an Antithrombotic Target in Uremia by Shivanna, Sowmya, Kolandaivelu, Kumaran, Shashar, Moshe, Belghasim, Mostafa, Al-Rabadi, Laith, Balcells, Mercedes, Zhang, Anqi, Weinberg, Janice, Francis, Jean, Pollastri, Michael P, Edelman, Elazer R, Sherr, David H, Chitalia, Vipul C

“…Patients with CKD suffer high rates of thrombosis, particularly after endovascular interventions, yet few options are available to improve management and…”
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Identification of cinnabarinic acid as a novel endogenous aryl hydrocarbon receptor ligand that drives IL-22 production by Lowe, Margaret M, Mold, Jeff E, Kanwar, Bittoo, Huang, Yong, Louie, Alexander, Pollastri, Michael P, Wang, Cuihua, Patel, Gautam, Franks, Diana G, Schlezinger, Jennifer, Sherr, David H, Silverstone, Allen E, Hahn, Mark E, McCune, Joseph M

“…The aryl hydrocarbon receptor (AHR) binds to environmental toxicants including synthetic halogenated aromatic hydrocarbons and is involved in a diverse array…”
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The single cyclic nucleotide-specific phosphodiesterase of the intestinal parasite Giardia lamblia represents a potential drug target by Kunz, Stefan, Balmer, Vreni, Sterk, Geert Jan, Pollastri, Michael P, Leurs, Rob, Müller, Norbert, Hemphill, Andrew, Spycher, Cornelia

“…Giardiasis is an intestinal infection correlated with poverty and poor drinking water quality, and treatment options are limited. According to the Center for…”
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Finding new collaboration models for enabling neglected tropical disease drug discovery by Pollastri, Michael P

“…  [...]the time between experimental result and data sharing is too long for others in the field to use these results for their own projects in real time, and…”
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Fexinidazole: A New Drug for African Sleeping Sickness on the Horizon by Pollastri, Michael P.

“…Decades after the last new chemical entity was added to the pharmacopeia for human African trypanosomiasis (or sleeping sickness), orally dosed fexinidazole…”
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Anilinoquinoline based inhibitors of trypanosomatid proliferation by Ferrins, Lori, Sharma, Amrita, Thomas, Sarah M, Mehta, Naimee, Erath, Jessey, Tanghe, Scott, Leed, Susan E, Rodriguez, Ana, Mensa-Wilmot, Kojo, Sciotti, Richard J, Gillingwater, Kirsten, Pollastri, Michael P

“…We recently reported the medicinal chemistry re-optimization of a series of compounds derived from the human tyrosine kinase inhibitor, lapatinib, for activity…”
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Identification and characterization of hundreds of potent and selective inhibitors of Trypanosoma brucei growth from a kinase-targeted library screening campaign by Diaz, Rosario, Luengo-Arratta, Sandra A, Seixas, João D, Amata, Emanuele, Devine, William, Cordon-Obras, Carlos, Rojas-Barros, Domingo I, Jimenez, Elena, Ortega, Fatima, Crouch, Sabrinia, Colmenarejo, Gonzalo, Fiandor, Jose Maria, Martin, Jose Julio, Berlanga, Manuela, Gonzalez, Silvia, Manzano, Pilar, Navarro, Miguel, Pollastri, Michael P

“…In the interest of identification of new kinase-targeting chemotypes for target and pathway analysis and drug discovery in Trypanosomal brucei, a…”
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The susceptibility of trypanosomatid pathogens to PI3/mTOR kinase inhibitors affords a new opportunity for drug repurposing by Diaz-Gonzalez, Rosario, Kuhlmann, F Matthew, Galan-Rodriguez, Cristina, Madeira da Silva, Luciana, Saldivia, Manuel, Karver, Caitlin E, Rodriguez, Ana, Beverley, Stephen M, Navarro, Miguel, Pollastri, Michael P

“…Target repurposing utilizes knowledge of "druggable" targets obtained in one organism and exploits this information to pursue new potential drug targets in…”
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Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents by Klug, Dana M, Diaz-Gonzalez, Rosario, Pérez-Moreno, Guiomar, Ceballos-Pérez, Gloria, García-Hernández, Raquel, Gomez-Pérez, Veronica, Ruiz-Pérez, Luis Miguel, Rojas-Barros, Domingo I, Gamarro, Francisco, González-Pacanowska, Dolores, Martínez-Martínez, María S, Manzano, Pilar, Ferrins, Lori, Caffrey, Conor R, Navarro, Miguel, Pollastri, Michael P

“…New treatments are needed for neglected tropical diseases (NTDs) such as Human African trypanosomiasis (HAT), Chagas disease, and schistosomiasis. Through a…”
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A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes by Galvin, Brendan D, Li, Zhiru, Villemaine, Estelle, Poole, Catherine B, Chapman, Melissa S, Pollastri, Michael P, Wyatt, Paul G, Carlow, Clotilde K S

“…Myristoylation is a lipid modification involving the addition of a 14-carbon unsaturated fatty acid, myristic acid, to the N-terminal glycine of a subset of…”
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Repurposing strategies for tropical disease drug discovery by Klug, Dana M., Gelb, Michael H., Pollastri, Michael P.

“…[Display omitted] Neglected tropical diseases (NTDs) and other diseases of the developing world, such as malaria, attract research investments that are…”
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Application of l‑Threonine Aldolase to on-DNA Reactions by Chai, Jing, Lu, Xiaojie, Arico-Muendel, Christopher C, Ding, Yun, Pollastri, Michael P

“…Enzymatic catalysis is a highly attractive approach to the DNA encoded library technology (DEL) that has not been widely explored. In this paper, we report an…”
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Synthesis of a DNA-Encoded Macrocyclic Library Utilizing Intramolecular Benzimidazole Formation by Chai, Jing, Arico-Muendel, Christopher C., Ding, Yun, Pollastri, Michael P., Scott, Sarah, Mantell, Mark A., Yao, Gang

“…Macrocycles occupy chemical space “beyond the rule of five”. They bridge traditional bioactive small molecule drugs and macromolecules and have the potential…”
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Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1) by Amata, Emanuele, Bland, Nicholas D., Campbell, Robert K., Pollastri, Michael P.

“…[Display omitted] Human African trypanosomiasis (HAT) is a parasitic disease, caused by the protozoan pathogen Trypanosoma brucei, which affects thousands…”
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Kinases as Druggable Targets in Trypanosomatid Protozoan Parasites by Merritt, Christopher, Silva, Lisseth E., Tanner, Angela L., Stuart, Kenneth, Pollastri, Michael P.

“…Merritt et al examine kinases as druggable targets in trypanosomatid protozoan parasites…”
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Physiologic Targets and Modes of Action for CBL0137, a Lead for Human African Trypanosomiasis Drug Development by Sanz-Rodríguez, Carlos E, Hoffman, Benjamin, Guyett, Paul J, Purmal, Andrei, Singh, Baljinder, Pollastri, Michael P, Mensa-Wilmot, Kojo

“…CBL0137 is a lead drug for human African trypanosomiasis, caused by Herein, we use a four-step strategy to 1) identify physiologic targets and 2) determine…”
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Chemical Optimization of CBL0137 for Human African Trypanosomiasis Lead Drug Discovery by Singh, Baljinder, Sharma, Amrita, Gunaganti, Naresh, Rivers, Mitch, Gadekar, Pradip K., Greene, Brady, Chichioco, Michael, Sanz-Rodriguez, Carlos E., Fu, Courtney, LeBlanc, Catherine, Burchfield, Erin, Sharif, Nyle, Hoffman, Benjamin, Kumar, Gaurav, Purmal, Andrei, Mensa-Wilmot, Kojo, Pollastri, Michael P.

“…The carbazole CBL0137 (1) is a lead for drug development against human African trypanosomiasis (HAT), a disease caused by Trypanosoma brucei. To advance 1 as a…”
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Medicinal Chemistry Optimization of a Diaminopurine Chemotype: Toward a Lead for Trypanosoma brucei Inhibitors by Singh, Baljinder, Diaz-Gonzalez, Rosario, Ceballos-Perez, Gloria, Rojas-Barros, Domingo I, Gunaganti, Naresh, Gillingwater, Kirsten, Martinez-Martinez, Maria Santos, Manzano, Pilar, Navarro, Miguel, Pollastri, Michael P

“…Human African trypanosomiasis (HAT), or sleeping sickness, is caused by the protozoan parasite Trypanosoma brucei and transmitted through the bite of infected…”
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Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery by Devine, William, Woodring, Jennifer L., Swaminathan, Uma, Amata, Emanuele, Patel, Gautam, Erath, Jessey, Roncal, Norma E., Lee, Patricia J., Leed, Susan E., Rodriguez, Ana, Mensa-Wilmot, Kojo, Sciotti, Richard J., Pollastri, Michael P.

“…Tropical protozoal infections are a significant cause of morbidity and mortality worldwide; four in particular (human African trypanosomiasis (HAT), Chagas…”
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Pharmacophore Identification and Structure–Activity Relationship Analysis of a Series of Substituted Azaindoles as Inhibitors of Trypanosoma brucei by Ferrins, Lori, Diaz, Rosario, Cordon-Obras, Carlos, Rojas-Barros, Domingo, Quotadamo, Antonio, Oehme, Daniel P., Ceballos-Pérez, Gloria, Swaminathan, Uma, Pérez-Moreno, Guiomar, Bosch-Navarrete, Cristina, García-Hernández, Raquel, Gomez-Liñan, Claudia, Saura, Andreu, Ruiz-Perez, Luis Miguel, Gamarro, Francisco, Martinez-Martinez, Maria Santos, Manzano, Pilar, González-Pacanowska, Dolores, Navarro, Miguel, Pollastri, Michael P.

“…Human African trypanosomiasis is among the World Health Organization’s designated neglected tropical diseases. Repurposing strategies are often employed in…”
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