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10.1021/acsptsci.0c00076 http://scihub22266oqcxt.onion/10.1021/acsptsci.0c00076 32821882!7409933!32821882     free     free     free Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       ACS+Pharmacol+Transl+Sci 2020 ; 3 (4): 613-626 Nephropedia Template TP {{tp|p=32821882|t=2020. Metabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm |pdf=|usr=}}{{32821882}} gab.com Text Metabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm JO: ACS Pharmacol Transl Sci http://www.kidney.de/pget.php?&tw=1&pmid=32821882 #FOAvip Drugs that contain phosphates (and phosphonates or phosphinates) have intrinsic absorption issues and are therefore often delivered in prodrug forms to promote their uptake. Effective prodrug forms distribute their payload to the site of the intended target and release it efficiently with minimal byproduct toxicity. The ability to balance unwanted payload release during transit with desired release at the site of action is critical to prodrug efficacy. Despite decades of research on prodrug forms, choosing the ideal prodrug form remains a challenge which is often solved empirically. The recent emergency use authorization of the antiviral remdesivir for COVID-19 exemplifies a new approach for delivery of phosphate prodrugs by parenteral dosing, which minimizes payload release during transit and maximizes tissue payload distribution. This review focuses on the role of metabolic activation in efficacy during oral and parenteral dosing of phosphate, phosphonate, and phosphinate prodrugs. Through examining prior structure-activity studies on prodrug forms and the choices that led to development of remdesivir and other clinical drugs and drug candidates, a better understanding of their ability to distribute to the planned site of action, such as the liver, plasma, PBMCs, or peripheral tissues, can be gained. The structure-activity relationships described here will facilitate the rational design of future prodrugs. Twit Text FOAVip Metabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm ????ACS Pharmacol Transl Sci http://www.kidney.de/pget.php?&tw=1&pmid=32821882 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=32821882 #FOAvip English Wikipedia <ref>{{Cite pmid|32821882}}</ref> Metabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm #MMPMID32821882 Wiemer AJ ACS Pharmacol Transl Sci 2020[Aug]; 3 (4): 613-626 PMID32821882show ga Drugs that contain phosphates (and phosphonates or phosphinates) have intrinsic absorption issues and are therefore often delivered in prodrug forms to promote their uptake. Effective prodrug forms distribute their payload to the site of the intended target and release it efficiently with minimal byproduct toxicity. The ability to balance unwanted payload release during transit with desired release at the site of action is critical to prodrug efficacy. Despite decades of research on prodrug forms, choosing the ideal prodrug form remains a challenge which is often solved empirically. The recent emergency use authorization of the antiviral remdesivir for COVID-19 exemplifies a new approach for delivery of phosphate prodrugs by parenteral dosing, which minimizes payload release during transit and maximizes tissue payload distribution. This review focuses on the role of metabolic activation in efficacy during oral and parenteral dosing of phosphate, phosphonate, and phosphinate prodrugs. Through examining prior structure-activity studies on prodrug forms and the choices that led to development of remdesivir and other clinical drugs and drug candidates, a better understanding of their ability to distribute to the planned site of action, such as the liver, plasma, PBMCs, or peripheral tissues, can be gained. The structure-activity relationships described here will facilitate the rational design of future prodrugs. äMetabolic Efficacy of Phosphate Prodrugs and the Remdesivir Paradigm (epmc).pdf DeepDyve Pubget Overpricing