Abdulaal Wesam H, Bakhrebah Muhammed A, Nassar Majed S, Almazni Ibrahim Abdullah, Almutairi Wael Abdullah, Natto Zuhair S, Khattab Amin K
Department of Biochemistry, Faculty of Science, Cancer and Mutagenesis Unit, King Fahd Medical Research Center, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Centre for Artificial Intelligence in Precision Medicines, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Bioinformation. 2022 Nov 30;18(11):1044-1049. doi: 10.6026/973206300181044. eCollection 2022.
SGLT2 inhibitors are a novel class of FDA approved anti-diabetes drugs. They act by blocking the SGLT2 protein, which prevents glucose reabsorption, leading in enhance glucose excretion and lower blood glucose levels. In diabetic patients, SGLT2 inhibitors have been linked to urinary tract infections (UTIs). Therefore, the development of novel SGLT2 inhibitors with no adverse effects is a need of time. With this purpose, in this study, 48164natural compounds from ZINC database were screened targeting both the SGLT2 and FimH protein using insilico approaches. FimH has been discovered as a promising target for preventing and treating UTIs. The hit compounds ZINC69481892, ZINC1612996, and ZINC4039265 exhibited strong binding with both SGLT2 and FimH with binding energies values of -9.88, -8.96, and -10.57 kcal/mol for SGLT2, and -7.86, -7.01, and -8.92 kcal/mol for FimH, which is higher than that of controls (-6.78 kcal/mol (Empaglifozolin for SGLT2) and -5.14 kcal/mol (Heptyl α-d-mannopyranoside for FimH)). Hits were found to bind with key residues of both SGLT2 and FimH protein. In addition, physiochemical properties showed that these compounds have good drug-likeness properties. Therefore, we anticipate that if these compounds are investigated further, might be potential SGLT2 inhibitors with less uropathogenic adverse effects.
钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂是一类经美国食品药品监督管理局(FDA)批准的新型抗糖尿病药物。它们通过阻断SGLT2蛋白发挥作用,该蛋白可阻止葡萄糖重吸收,从而增加葡萄糖排泄并降低血糖水平。在糖尿病患者中,SGLT2抑制剂与尿路感染(UTIs)有关。因此,开发无不良影响的新型SGLT2抑制剂是当务之急。为此,在本研究中,使用计算机模拟方法从ZINC数据库中筛选了48164种天然化合物,这些化合物同时针对SGLT2和FimH蛋白。FimH已被发现是预防和治疗尿路感染的一个有前景的靶点。命中化合物ZINC69481892、ZINC1612996和ZINC4039265与SGLT2和FimH均表现出强烈结合,SGLT2的结合能值分别为-9.88、-8.96和-10.57千卡/摩尔,FimH的结合能值分别为-7.86、-7.01和-8.92千卡/摩尔,高于对照值(SGLT2的恩格列净为-6.78千卡/摩尔,FimH的庚基α-D-甘露吡喃糖苷为-5.14千卡/摩尔)。发现命中化合物与SGLT2和FimH蛋白的关键残基结合。此外,物理化学性质表明这些化合物具有良好的类药性质。因此,我们预计,如果对这些化合物进行进一步研究,它们可能是具有较少尿路致病性不良影响的潜在SGLT2抑制剂。