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10.1016/j.chembiol.2016.04.009 http://scihub22266oqcxt.onion/10.1016/j.chembiol.2016.04.009 C4898890!4898890!27203377     free     free     free       Cell+Chem+Biol 2016 ; 23 (5): 579-86 Nephropedia Template TP {{tp|p=27203377|t=2016. Controlling Sulfuryl-Transfer |pdf=|usr=}}{{27203377}} gab.com Text Controlling Sulfuryl-Transfer JO: Cell Chem Biol http://www.kidney.de/pget.php?&tw=1&pmid=27203377 #FOAvip In humans, the cytosolic sulfotransferases (SULTs) catalyze regiospecific transfer of the sulfuryl-moiety (?SO3) from PAPS to thousands of metabolites, including numerous signaling small molecules, and thus regulates their activities and half-lives. Imbalances in the in vivo set-points of these reaction leads to disease. Here, with the goal of controlling sulfonation in vivo, molecular ligand-recognition principles in the SULT and nuclear-receptor families are integrated in creating a strategy that can prevent sulfonation of a compound without significantly altering its receptor affinity, or inhibiting SULTS. The strategy is validated by using it to control the sulfonation and estrogen-receptor (ER) activating activity of raloxifene (an FDA-approved SERM) and its derivatives. Preventing sulfonation is shown to enhance ER-activation efficacy 104-fold in studies using Ishikawa cells. The strategy offers the opportunity to control sulfuryl-transfer on a compound-by-compound basis, to enhance the efficacy of sulfonated drugs, and to explore the biology of sulfuryl-transfer with unprecedented precision. Twit Text FOAVip Controlling Sulfuryl-Transfer ????Cell Chem Biol http://www.kidney.de/pget.php?&tw=1&pmid=27203377 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=27203377 #FOAvip English Wikipedia <ref>{{Cite pmid|27203377}}</ref> Controlling Sulfuryl-Transfer #MMPMID27203377 Cook I; Wang T; Wang W; Kopp F; Wu P; Leyh TS Cell Chem Biol 2016[May]; 23 (5): 579-86 PMID27203377show ga In humans, the cytosolic sulfotransferases (SULTs) catalyze regiospecific transfer of the sulfuryl-moiety (?SO3) from PAPS to thousands of metabolites, including numerous signaling small molecules, and thus regulates their activities and half-lives. Imbalances in the in vivo set-points of these reaction leads to disease. Here, with the goal of controlling sulfonation in vivo, molecular ligand-recognition principles in the SULT and nuclear-receptor families are integrated in creating a strategy that can prevent sulfonation of a compound without significantly altering its receptor affinity, or inhibiting SULTS. The strategy is validated by using it to control the sulfonation and estrogen-receptor (ER) activating activity of raloxifene (an FDA-approved SERM) and its derivatives. Preventing sulfonation is shown to enhance ER-activation efficacy 104-fold in studies using Ishikawa cells. The strategy offers the opportunity to control sulfuryl-transfer on a compound-by-compound basis, to enhance the efficacy of sulfonated drugs, and to explore the biology of sulfuryl-transfer with unprecedented precision. äControlling Sulfuryl-Transfer (epmc).pdf DeepDyve Pubget Overpricing