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10.1080/14756366.2017.1419221 http://scihub22266oqcxt.onion/10.1080/14756366.2017.1419221 C6009951!6009951 !29338454     free     free     free Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 265.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 265.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 265.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\29338454 .jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       J+Enzyme+Inhib+Med+Chem 2018 ; 33 (1 ): 349-358 Nephropedia Template TP {{tp|p=29338454 |t=2018. Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61 |pdf=|usr=}}{{29338454 }} gab.com Text Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61 JO: J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=29338454 #FOAvip This work aims at elucidating the mechanism and kinetics of hydrolysis of GANT61, the first and most-widely used inhibitor of the Hedgehog (Hh) signalling pathway that targets Glioma-associated oncogene homologue (Gli) proteins, and at confirming the chemical nature of its bioactive form. GANT61 is poorly stable under physiological conditions and rapidly hydrolyses into an aldehyde species (GANT61-A), which is devoid of the biological activity against Hh signalling, and a diamine derivative (GANT61-D), which has shown inhibition of Gli-mediated transcription. Here, we combined chemical synthesis, NMR spectroscopy, analytical studies, molecular modelling and functional cell assays to characterise the GANT61 hydrolysis pathway. Our results show that GANT61-D is the bioactive form of GANT61 in NIH3T3 Shh-Light II cells and SuFu(-/-) mouse embryonic fibroblasts, and clarify the structural requirements for GANT61-D binding to Gli1. This study paves the way to the design of GANT61 derivatives with improved potency and chemical stability. Twit Text FOAVip Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61 ????J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=29338454 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=29338454 #FOAvip English Wikipedia <ref>{{Cite pmid|29338454 }}</ref> Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61 #MMPMID29338454 Calcaterra A ; Iovine V ; Botta B ; Quaglio D ; D'Acquarica I ; Ciogli A ; Iazzetti A ; Alfonsi R ; Lospinoso Severini L ; Infante P ; Di Marcotullio L ; Mori M ; Ghirga F J Enzyme Inhib Med Chem 2018[Dec]; 33 (1 ): 349-358 PMID29338454 show ga This work aims at elucidating the mechanism and kinetics of hydrolysis of GANT61, the first and most-widely used inhibitor of the Hedgehog (Hh) signalling pathway that targets Glioma-associated oncogene homologue (Gli) proteins, and at confirming the chemical nature of its bioactive form. GANT61 is poorly stable under physiological conditions and rapidly hydrolyses into an aldehyde species (GANT61-A), which is devoid of the biological activity against Hh signalling, and a diamine derivative (GANT61-D), which has shown inhibition of Gli-mediated transcription. Here, we combined chemical synthesis, NMR spectroscopy, analytical studies, molecular modelling and functional cell assays to characterise the GANT61 hydrolysis pathway. Our results show that GANT61-D is the bioactive form of GANT61 in NIH3T3 Shh-Light II cells and SuFu(-/-) mouse embryonic fibroblasts, and clarify the structural requirements for GANT61-D binding to Gli1. This study paves the way to the design of GANT61 derivatives with improved potency and chemical stability. |Animals [MESH] |Dose-Response Relationship, Drug [MESH] |Fibroblasts/drug effects [MESH] |Hedgehog Proteins/*antagonists & inhibitors/metabolism [MESH] |Hydrolysis [MESH] |Kinetics [MESH] |Mice [MESH] |Models, Molecular [MESH] |Molecular Structure [MESH] |NIH 3T3 Cells [MESH] |Pyridines/chemical synthesis/chemistry/*pharmacology [MESH] |Pyrimidines/chemical synthesis/chemistry/*pharmacology [MESH] |Signal Transduction/drug effects [MESH]Chemical, computational and functional insights into the chemical stab(epmc).pdf DeepDyve Pubget Overpricing