Journal ArticleDOI
Species Difference of Esterase Expression and Hydrolase Activity in Plasma
TLDR
In conclusion, the esterase expression and hydrolyzing pattern of dog plasma were found to be closest to that of human plasma, and should be considered when selecting model animals for preclinical studies.About:
This article is published in Journal of Pharmaceutical Sciences.The article was published on 2012-10-01. It has received 219 citations till now. The article focuses on the topics: Esterase & Butyrylcholinesterase.read more
Citations
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Journal ArticleDOI
Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys
Travis K. Warren,Robert Jordan,Michael K. Lo,Adrian S. Ray,Richard L. Mackman,Veronica Soloveva,Dustin Siegel,Michel Perron,Roy Bannister,Hui Hon Chung,Nate Larson,Robert G. Strickley,Jay Wells,Kelly S. Stuthman,Sean A. Van Tongeren,Nicole L. Garza,Ginger Donnelly,Amy C. Shurtleff,Cary Retterer,Dima N. Gharaibeh,Rouzbeh Zamani,Tara Kenny,Brett P. Eaton,Elizabeth C. Grimes,Lisa S. Welch,Laura Gomba,Catherine L. Wilhelmsen,Donald K. Nichols,Jonathan E. Nuss,Elyse R. Nagle,Jeffrey R. Kugelman,Gustavo Palacios,Edward Doerffler,Sean Neville,Ernest Carra,Michael O. Clarke,Lijun Zhang,Willard Lew,Bruce Ross,Queenie Wang,Kwon Soo Chun,Lydia Wolfe,Darius Babusis,Yeojin Park,Kirsten M. Stray,Iva Trancheva,Joy Y. Feng,Ona Barauskas,Yili Xu,Pamela Wong,Molly R. Braun,Mike Flint,Laura K. McMullan,Shan Shan Chen,Rachel Fearns,S. Swaminathan,Douglas L. Mayers,Christina F. Spiropoulou,William A. Lee,Stuart T. Nichol,Tomas Cihlar,Sina Bavari +61 more
TL;DR: These results show the first substantive post-exposure protection by a small-molecule antiviral compound against EBOV in nonhuman primates, and the broad-spectrum antiviral activity of GS-5734 in vitro against other pathogenic RNA viruses, including filoviruses, arenavirus, and coronavirus suggests the potential for wider medical use.
Journal ArticleDOI
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses
Dustin Siegel,Hui Hon Chung,Edward Doerffler,Michael O'neil Hanrahan Clarke,Kwon Soo Chun,Lijun Zhang,Sean Neville,Ernest Carra,Willard Lew,Bruce Ross,Queenie Wang,Lydia Wolfe,Robert Jordan,Veronica Soloveva,John E. Knox,Jason K. Perry,Michel Perron,Kirsten M. Stray,Ona Barauskas,Joy Y. Feng,Yili Xu,Gary Lee,Arnold L. Rheingold,Adrian S. Ray,Roy Bannister,Robert G. Strickley,S. Swaminathan,William A. Lee,Sina Bavari,Tomas Cihlar,Michael K. Lo,Travis K. Warren,Richard L. Mackman +32 more
TL;DR: A robust diastereoselective synthesis provided sufficient quantities of 4b to enable preclinical efficacy in a non-human-primate EBOV challenge model and structure activity relationships established that the 1′-CN group and C-linked nucleobase were critical for optimal anti-EBOV potency and selectivity against host polymerases.
Journal ArticleDOI
The expanding role of prodrugs in contemporary drug design and development
TL;DR: This Review highlights prodrug design strategies for improved formulation and pharmacokinetic and targeting properties, with a focus on the most recently marketed prodrugs.
Journal ArticleDOI
A comprehensive review of UDP-glucuronosyltransferase and esterases for drug development.
TL;DR: An overview of recent findings in UGT and esterases studies focusing on tissue distribution, gene regulation, substrate and inhibitor specificity, and species differences is given.
Journal ArticleDOI
Remdesivir against COVID-19 and Other Viral Diseases.
TL;DR: Remdesivir reduces the time to recovery of hospitalized patients who require supplemental oxygen and may have a positive impact on mortality outcomes while having a favorable safety profile, and approval of this drug will not be sufficient to solve the public health issues caused by the ongoing pandemic.
References
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THE MAMMALIAN CARBOXYLESTERASES: From Molecules to Functions
Tetsuo Satoh,Masakiyo Hosokawa +1 more
TL;DR: A comparison of the nucleotide and amino acid sequence of the mammalian carboxylesterases shows that all forms expressed in the rat can be assigned to one of three gene subfamilies with structural identities of more than 70% within each subfamily.
Journal ArticleDOI
Serum esterases. 1. Two types of esterase (A and B) hydrolysing p-nitrophenyl acetate, propionate and butyrate, and a method for their determination
Journal ArticleDOI
Crystal structure of human butyrylcholinesterase and of its complexes with substrate and products.
TL;DR: The crystal structures of several recombinant truncated human BChE complexes and conjugates are reported and a description for mechanistically relevant non-productive substrate and product binding is provided and is similar to a previously published theoretical model of this enzyme.
Journal ArticleDOI
The effect of the human serum paraoxonase polymorphism is reversed with diazoxon, soman and sarin
Holly G. Davies,Rebecca J. Richter,Matthew C. Keifer,Clarence A. Broomfield,Jason Sowalla,Clement E. Furlong +5 more
TL;DR: A simple enzyme analysis is reported that provides a clear resolution of PON1 genotypes and phenotypes allowing for a reasonable assessment of an individual's probable susceptibility or resistance to a given OR, extending earlier studies on this system.
Journal ArticleDOI
Structure and Evolution of the Serum Paraoxonase Family of Detoxifying and Anti-Atherosclerotic Enzymes
Michal Harel,Amir Aharoni,Leonid Gaidukov,Boris Brumshtein,Olga Khersonsky,Ran Meged,Hay Dvir,Raimond B. G. Ravelli,Andrew A. McCarthy,Lilly Toker,Israel Silman,Joel L. Sussman,Dan S. Tawfik +12 more
TL;DR: The first crystal structure of a PON family member, a variant of PON1 obtained by directed evolution, is described, a six-bladed β-propeller with a unique active site lid that is also involved in HDL binding.