Ligand-based drug design considering specific features of aldose reductase

author: Magdalena Majekova, Institute of Pharmacology and Toxicology, University of Zurich
published: July 9, 2018,   recorded: May 2018,   views: 382


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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 complications and other disorders connected related to a glucose toxicity. Aldose reductase (EC:, the three-dimensional structure of AR has been explored in many research works, belongs to the aldo-keto reductase superfamily. Aldose reductase catalyzes many substrates, as lipid aldehydes, methyl glyoxal, aliphatic and aromatic aldehydes, daunorubicin, doxorubicin, etc. With the exception of PGH2 transformation to PGD2, which proceeds in the absence of cofactors NADPH or NADP + , all other known catalytic processes of AR are NADPH-dependent. We present a survey of ligand-based drug design, which resulted in identification of efficient inhibitors (1), with highlighting the specific features of aldose reductase.

(1) Majekova M, Ballekova J, Prnova M, et al.. Structure optimization of tetrahydropyridoindole-based aldose reductase inhibitors improved their efficacy and selectivity. Bioorg. Med. Chem. 2017;25: 6353-6360. Available from: doi: 10.1016/j.bmc.2017.10.005.

Financing: Slovak Research and Development Agency under the contract No. APVV-15-0455 and the Scientific Grant Agency VEGA grant 2/0127/18

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