Search Results - "Wring, Stephen A"

SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis by Jacobs, Robert T, Nare, Bakela, Wring, Stephen A, Orr, Matthew D, Chen, Daitao, Sligar, Jessica M, Jenks, Matthew X, Noe, Robert A, Bowling, Tana S, Mercer, Luke T, Rewerts, Cindy, Gaukel, Eric, Owens, Jennifer, Parham, Robin, Randolph, Ryan, Beaudet, Beth, Bacchi, Cyrus J, Yarlett, Nigel, Plattner, Jacob J, Freund, Yvonne, Ding, Charles, Akama, Tsutomu, Zhang, Y-K, Brun, Reto, Kaiser, Marcel, Scandale, Ivan, Don, Robert

“…Human African trypanosomiasis (HAT) is an important public health problem in sub-Saharan Africa, affecting hundreds of thousands of individuals. An urgent need…”
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Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus by Dwyer, John J, Wilson, Karen L, Davison, Donna K, Freel, Stephanie A, Seedorff, Jennifer E, Wring, Stephen A, Tvermoes, Nicolai A, Matthews, Thomas J, Greenberg, Michael L, Delmedico, Mary K

“…Enfuvirtide (ENF), the first approved fusion inhibitor (FI) for HIV, is a 36-aa peptide that acts by binding to the heptad repeat 1 (HR1) region of gp41 and…”
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Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs by Mahar Doan, Kelly M, Humphreys, Joan E, Webster, Lindsey O, Wring, Stephen A, Shampine, Larry J, Serabjit-Singh, Cosette J, Adkison, Kimberly K, Polli, Joseph W

“…Membrane permeability and P-glycoprotein (Pgp) can be limiting factors for blood-brain barrier penetration. The objectives of this study were to determine…”
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Preclinical Pharmacokinetics and Pharmacodynamic Target of SCY-078, a First-in-Class Orally Active Antifungal Glucan Synthesis Inhibitor, in Murine Models of Disseminated Candidiasis by Wring, Stephen A, Randolph, Ryan, Park, SeongHee, Abruzzo, George, Chen, Qing, Flattery, Amy, Garrett, Graig, Peel, Michael, Outcalt, Russell, Powell, Kendall, Trucksis, Michelle, Angulo, David, Borroto-Esoda, Katyna

“…SCY-078 (MK-3118) is a novel, semisynthetic derivative of enfumafungin and represents the first compound of the triterpene class of antifungals. SCY-078…”
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Induction of P-Glycoprotein and Cytochrome P450 3A by HIV Protease Inhibitors by Huang, L, Wring, S A, Woolley, J L, Brouwer, K R, Serabjit-Singh, C, Polli, J W

“…P-Glycoprotein (Pgp) and cytochrome P450 3A (CYP3A) are important enzymes affecting the disposition of HIV protease inhibitors (HIV PIs). After multiple dosing…”
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MSG-10: a Phase 2 study of oral ibrexafungerp (SCY-078) following initial echinocandin therapy in non-neutropenic patients with invasive candidiasis by Spec, Andrej, Pullman, John, Thompson, George R, Powderly, William G, Tobin, Ellis H, Vazquez, Jose, Wring, Stephen A, Angulo, David, Helou, Silvia, Pappas, Peter G

“…Abstract Objectives To evaluate the safety and efficacy of two dosing regimens of oral ibrexafungerp (formerly SCY-078), a novel orally bioavailable β-glucan…”
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Topical Treatment for Cutaneous Leishmaniasis: Dermato-Pharmacokinetic Lead Optimization of Benzoxaboroles by Van Bocxlaer, Katrien, Gaukel, Eric, Hauser, Deirdre, Park, Seong Hee, Schock, Sara, Yardley, Vanessa, Randolph, Ryan, Plattner, Jacob J, Merchant, Tejal, Croft, Simon L, Jacobs, Robert T, Wring, Stephen A

“…Cutaneous leishmaniasis (CL) is caused by several species of the protozoan parasite , affecting an estimated 10 million people worldwide. Previously reported…”
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Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylase by Volkov, Oleg A, Brockway, Anthony J, Wring, Stephen A, Peel, Michael, Chen, Zhe, Phillips, Margaret A, De Brabander, Jef K

“…New therapeutic options are needed for treatment of human African trypanosomiasis (HAT) caused by protozoan parasite Trypanosoma brucei. S-Adenosylmethionine…”
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Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides by Thompson, Andrew M., Marshall, Andrew J., Maes, Louis, Yarlett, Nigel, Bacchi, Cyrus J., Gaukel, Eric, Wring, Stephen A., Launay, Delphine, Braillard, Stephanie, Chatelain, Eric, Mowbray, Charles E., Denny, William A.

“…[Display omitted] A 900 compound nitroimidazole-based library derived from our pretomanid backup program with TB Alliance was screened for utility against…”
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Synthesis and evaluation of analogs of 5′-(((Z)-4-amino-2-butenyl)methylamino)-5′-deoxyadenosine (MDL 73811, or AbeAdo) – An inhibitor of S-adenosylmethionine decarboxylase with antitrypanosomal activity by Brockway, Anthony J., Volkov, Oleg A., Cosner, Casey C., MacMillan, Karen S., Wring, Stephen A., Richardson, Thomas E., Peel, Michael, Phillips, Margaret A., De Brabander, Jef K.

“…[Display omitted] We describe our efforts to improve the pharmacokinetic properties of a mechanism-based suicide inhibitor of the polyamine biosynthetic enzyme…”
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Rational use of in vitro P-glycoprotein assays in drug discovery by Polli, J W, Wring, S A, Humphreys, J E, Huang, L, Morgan, J B, Webster, L O, Serabjit-Singh, C S

“…P-glycoprotein (Pgp) affects the absorption, distribution, and clearance of a variety of compounds. Thus, identification of compounds that are Pgp substrates…”
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Benzoxaboroles: a new class of potential drugs for human African trypanosomiasis by Jacobs, Robert T, Plattner, Jacob J, Nare, Bakela, Wring, Stephen A, Chen, Daitao, Freund, Yvonne, Gaukel, Eric G, Orr, Matthew D, Perales, Joe B, Jenks, Matthew, Noe, Robert A, Sligar, Jessica M, Zhang, Yong-Kang, Bacchi, Cyrus J, Yarlett, Nigel, Don, Robert

“…Human African trypanosomiasis, caused by the kinetoplastid parasite Trypanosoma brucei, affects thousands of people across sub-Saharan Africa, and is fatal if…”
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Interaction of native bile acids with human apical sodium-dependent bile acid transporter (hASBT) : Influence of steroidal hydroxylation pattern and C-24 conjugation by BALAKRISHNAN, Anand, WRING, Stephen A, POLLI, James E

“…The human apical sodium-dependent bile acid transporter (hASBT) is a potential target for drug delivery, but an understanding of hASBT substrate requirements…”
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Predicting P-glycoprotein substrates by a quantitative structure-activity relationship model by Gombar, Vijay K, Polli, Joseph W, Humphreys, Joan E, Wring, Stephen A, Serabjit-Singh, Cosette S

“…A quantitative structure-activity relationship (QSAR) model has been developed to predict whether a given compound is a P-glycoprotein (Pgp) substrate or not…”
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Identification of Trypanosoma brucei AdoMetDC Inhibitors Using a High-Throughput Mass Spectrometry-Based Assay by Volkov, Oleg A, Cosner, Casey C, Brockway, Anthony J, Kramer, Martin, Booker, Michael, Zhong, Shihua, Ketcherside, Ariel, Wei, Shuguang, Longgood, Jamie, McCoy, Melissa, Richardson, Thomas E, Wring, Stephen A, Peel, Michael, Klinger, Jeffrey D, Posner, Bruce A, De Brabander, Jef K, Phillips, Margaret A

“…Human African trypanosomiasis (HAT) is a fatal infectious disease caused by the eukaryotic pathogen Trypanosoma brucei (Tb). Available treatments are difficult…”
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Influence of Charge and Steric Bulk in the C-24 Region on the Interaction of Bile Acids with Human Apical Sodium-Dependent Bile Acid Transporter by Balakrishnan, Anand, Wring, Stephen A, Coop, Andrew, Polli, James E

“…The human apical sodium-dependent bile acid transporter (hASBT) is a potential target for drug delivery, but an understanding of hASBT substrate requirements…”
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Recent developments in the design and application of screen-printed electrochemical sensors for biomedical, environmental and industrial analyses by Hart, John P., Wring, Stephen A.

“…This review presents recent developments in the design and application of disposable, screen-printed electrochemical sensors for biomedical, environmental and…”
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Method to Screen Substrates of Apical Sodium-Dependent Bile Acid Transporter by Rais, Rana, Gonzalez, Pablo M., Zheng, Xiaowan, Wring, Stephen A., Polli, James E.

“…Human apical sodium-dependent bile acid transporter (hASBT) is a potential prodrug target under study. Development of prodrugs that target hASBT may yield…”
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Serotonin and Pulmonary Hypertension; Sex and Drugs and ROCK and Rho by MacLean, Margaret R, Fanburg, Barry, Hill, Nicolas, Lazarus, Howard M, Pack, Thomas F, Palacios, Michelle, Penumatsa, Krishna C, Wring, Stephen A

“…Serotonin is often referred to as a "happy hormone" as it maintains good mood, well-being, and happiness. It is involved in communication between nerve cells…”
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SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei by Perales, Joe B., Freeman, Jennifer, Bacchi, Cyrus J., Bowling, Tana, Don, Robert, Gaukel, Eric, Mercer, Luke, Moore III, Joseph A., Nare, Bakela, Nguyen, Tien M., Noe, Robert A., Randolph, Ryan, Rewerts, Cindy, Wring, Stephen A., Yarlett, Nigel, Jacobs, Robert T.

“…A series of 2,4-diaminopyrimidines was investigated and compounds were found to have in vivo efficacy against Trypanosoma brucei in an acute mouse model…”
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