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Ligand-based drug design considering specific features of aldose reductase
Published on Jul 09, 2018393 Views
Aldose reductase is as a rate-limiting enzyme in the polyol pathway, one of the main mechanisms of glucose toxicity. Inhibitors of aldose reductase showed to be helpful in prevention of diabetic compl
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Ligand-based drug design considering specific features of aldose reductase00:00
Department of Biochemical Pharmacology00:22
G-LUCK - Pharmacological intervention in glucose-toxicity in type 2 diabetes01:07
Aldo-keto reductases02:07
Late (chronic) diabetic complications 03:02
Patients with T2DM – insulin resistance03:46
Polyol pathway05:06
ALR2 - 105:31
ALR2 - 206:37
MEP dependance on pH08:05
MEP of aldose reductase - 108:56
MEP of aldose reductase - 209:12
2 substrates mechanism10:22
Inhibitors12:12
Safety belt13:39
History13:55
Hexahydropyridoindoles – efficient radical scavengers - 114:05
Hexahydropyridoindoles – efficient radical scavengers - 214:35
Carboxymethylated pyridoindoles14:55
3-D structure15:09
basic (protonated) nitrogen + acidic (dissociated) >COO- => zwitterion15:12
tetrahydropyridoindoles16:02
Indole acetic acids 16:26
Database of indole derivatives for in silico ADMET and activity study16:43
methylation at R2 and R316:53
tricyclic structure of cemtirestat - 117:09
tricyclic structure of cemtirestat - 217:23
Rat ALR2 - 117:47
Rat ALR2 - 218:05
Rat ALR2 - 319:13
Rat ALR2 - 419:15
Rat ALR2 - 519:32
2nd substrate-protein-cofactor 19:46
Software20:05
Acknowledgements:20:11
Funding20:43