Ligand-based drug design considering specific features of aldose reductase
published: July 9, 2018, recorded: May 2018, views: 380
Report a problem or upload filesIf you have found a problem with this lecture or would like to send us extra material, articles, exercises, etc., please use our ticket system to describe your request and upload the data.
Enter your e-mail into the 'Cc' field, and we will keep you updated with your request's status.
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: 126.96.36.199), 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
Download slides: biophysics2018_majekova_aldose_reductase_01.pdf (2.6 MB)
Link this pageWould you like to put a link to this lecture on your homepage?
Go ahead! Copy the HTML snippet !