Department of Chemistry, Osmania University, Hyderabad, Telangana, 500007, India.
Department of Chemistry, Tara Government College (A), Sangareddy, Telangana, India.
Biol Trace Elem Res. 2023 Oct;201(10):5037-5052. doi: 10.1007/s12011-023-03557-8. Epub 2023 Jan 18.
The medical field now needs more novel drugs to treat obesity and type-2 diabetes mellitus (T2D) than ever before. Obesity and T2D are both characterized by resistance to the hormones leptin and insulin. PTP-1B is a promising target for drug growth, as strong genetic, pharmacological, and biochemical evidence points to the possibility of treating diabetes and obesity by blocking the PTP-1B enzyme. Studies have also found that PTP-1B is overexpressed in patients with diabetes and obesity, suggesting that inhibiting PTP-1B may be a useful technique in their care. There are no clinically used PTP-1B inhibitors, despite the fact that numerous naturally occurring PTP-1B inhibitors have demonstrated great therapeutic promise. This is most likely due to their low activity or lack of selectivity. It is still important to look for more effective and focused PTP-1B inhibitors. A few organovanadium metal complexes were synthesized and characterized, and binding studies on vanadium complexes with PTP-B were also performed using fluorescence emission spectroscopy. Additionally, we theoretically (molecular modeling) and experimentally (enzyme kinetics) examined the PTP-1B inhibitory effects of these vanadium metal complexes and found that they have excellent PTP-1B inhibitory properties.
如今,医学领域比以往任何时候都更需要新型药物来治疗肥胖症和 2 型糖尿病(T2D)。肥胖症和 T2D 的特征均为对瘦素和胰岛素等激素产生抗性。PTP-1B 是药物研发的一个有前途的靶点,因为强有力的遗传、药理学和生物化学证据表明,通过抑制 PTP-1B 酶可能是治疗糖尿病和肥胖症的一种有效方法。研究还发现,PTP-1B 在糖尿病和肥胖症患者中过度表达,这表明抑制 PTP-1B 可能是他们治疗中的一种有用技术。尽管有许多天然存在的 PTP-1B 抑制剂显示出巨大的治疗潜力,但目前尚无临床应用的 PTP-1B 抑制剂。这很可能是由于它们的活性低或缺乏选择性。寻找更有效和有针对性的 PTP-1B 抑制剂仍然很重要。我们合成并表征了一些有机钒金属配合物,并使用荧光发射光谱法对钒配合物与 PTP-B 的结合进行了研究。此外,我们还从理论(分子建模)和实验(酶动力学)两个方面研究了这些钒金属配合物对 PTP-1B 的抑制作用,发现它们具有出色的 PTP-1B 抑制特性。