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10.1038/s41598-018-23569-y http://scihub22266oqcxt.onion/10.1038/s41598-018-23569-y C5869712!5869712!29588471     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Sci+Rep 2018 ; 8 (ä): ä Nephropedia Template TP {{tp|p=29588471|t=2018. Discovery of a highly selective JAK3 inhibitor for the treatment of rheumatoid arthritis |pdf=|usr=}}{{29588471}} gab.com Text Discovery of a highly selective JAK3 inhibitor for the treatment of rheumatoid arthritis JO: Sci Rep http://www.kidney.de/pget.php?&tw=1&pmid=29588471 #FOAvip Janus tyrosine kinase 3 (JAK3) is expressed in lymphoid cells and is involved in the signalling of T cell functions. The development of a selective JAK3 inhibitor has been shown to have a potential benefit in the treatment of autoimmune disorders. In this article, we developed the 4-aminopiperidine-based compound RB1, which was highly selective for JAK3 inhibition, with an IC50 of value of 40?nM, but did not inhibit JAK1, JAK2 or tyrosine kinase 2 (TYK2) at concentrations up to 5?µM. Furthermore, RB1 also exhibited favourable selectivity against a panel of representative kinases. In a battery of cytokine-stimulated cell-based assays, this potent inhibitor of JAK3 activity with good selectivity against other kinases could potently inhibit JAK3 activity over the activity of JAK1 or JAK2 (over at least 100-fold). A combination of liquid chromatography-mass spectrometry (LC-MS) experiments validated that RB1 covalently modified the unique cysteine 909 residue in JAK3. In vivo, RB1 exerted significantly improved pathology in the joints of a collagen-induced arthritis mouse model. The reasonable pharmacokinetics properties (F?=?72.52%, T1/2?=?14.6?h) and favourable results of toxicology experiments (LD50?>?2?g/kg) suggest that RB1 has the potential to be an efficacious treatment for RA. Twit Text FOAVip Discovery of a highly selective JAK3 inhibitor for the treatment of rheumatoid arthritis ????Sci Rep http://www.kidney.de/pget.php?&tw=1&pmid=29588471 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=29588471 #FOAvip English Wikipedia <ref>{{Cite pmid|29588471}}</ref> Discovery of a highly selective JAK3 inhibitor for the treatment of rheumatoid arthritis #MMPMID29588471 Pei H; He L; Shao M; Yang Z; Ran Y; Li D; Zhou Y; Tang M; Wang T; Gong Y; Chen X; Yang S; Xiang M; Chen L Sci Rep 2018[]; 8 (ä): ä PMID29588471show ga Janus tyrosine kinase 3 (JAK3) is expressed in lymphoid cells and is involved in the signalling of T cell functions. The development of a selective JAK3 inhibitor has been shown to have a potential benefit in the treatment of autoimmune disorders. In this article, we developed the 4-aminopiperidine-based compound RB1, which was highly selective for JAK3 inhibition, with an IC50 of value of 40?nM, but did not inhibit JAK1, JAK2 or tyrosine kinase 2 (TYK2) at concentrations up to 5?µM. Furthermore, RB1 also exhibited favourable selectivity against a panel of representative kinases. In a battery of cytokine-stimulated cell-based assays, this potent inhibitor of JAK3 activity with good selectivity against other kinases could potently inhibit JAK3 activity over the activity of JAK1 or JAK2 (over at least 100-fold). A combination of liquid chromatography-mass spectrometry (LC-MS) experiments validated that RB1 covalently modified the unique cysteine 909 residue in JAK3. In vivo, RB1 exerted significantly improved pathology in the joints of a collagen-induced arthritis mouse model. The reasonable pharmacokinetics properties (F?=?72.52%, T1/2?=?14.6?h) and favourable results of toxicology experiments (LD50?>?2?g/kg) suggest that RB1 has the potential to be an efficacious treatment for RA. äDiscovery of a highly selective JAK3 inhibitor for the treatment of rh(epmc).pdf DeepDyve Pubget Overpricing