Bioinformatics Infrastructure Facility, Sri Venkateswara College, New Delhi, India.
J Mol Model. 2011 Feb;17(2):301-13. doi: 10.1007/s00894-010-0727-3. Epub 2010 May 8.
Tuberculosis (TB) is a global health problem and the situation has become more precarious due to the advent of HIV infections and continuous rise in the number of multi-drug resistant strains of Mycobacterium tuberculosis (M. tb). Biochemical studies on Fatty Acyl-CoA Synthetases (FadD13), one of the gene products of mymA operon, have provided insights into the involvement of this protein in the activation of fatty acids. Due to non-availability of the crystal structure of FadD13, we have employed in silico approaches to resolve and characterize the structure of this important protein of M. tb. A three dimensional model of M. tb FadD13 was predicted by a de novo structure prediction server that integrates fragment assembly with SimFold energy function. With the aid of molecular mechanics and dynamics methods, the final model was obtained and assessed subsequently for global and local accuracy by various assessment programs. With this model, a flexible docking study with the substrates was performed. Results of ligand interactions with key amino acids in the binding site are also summarized. The molecular model for the M. tb FadD13 obtained sheds light on the topographical features of the binding pocket of the protein and provides atomic insight into the possible modes of substrate recognition. The three-dimensional model of FadD13 presented here would be helpful in guiding both enzymatic studies as well as design of specific inhibitors.
结核病(TB)是一个全球性的健康问题,由于 HIV 感染的出现以及结核分枝杆菌(M. tb)多药耐药株数量的持续增加,情况变得更加危急。对脂肪酸酰基辅酶 A 合成酶(FadD13)的生化研究,mycA 操纵子的一个基因产物,提供了有关该蛋白在激活脂肪酸中作用的见解。由于 FadD13 的晶体结构不可用,我们采用了计算方法来解决和表征 M. tb 的这种重要蛋白质的结构。通过整合片段组装和 SimFold 能量函数的从头结构预测服务器,预测了 M. tb FadD13 的三维模型。借助分子力学和动力学方法,获得了最终模型,并随后通过各种评估程序评估其全局和局部准确性。使用该模型,对配体与底物的柔性对接进行了研究。还总结了配体与结合位点关键氨基酸相互作用的结果。获得的 M. tb FadD13 分子模型阐明了该蛋白结合口袋的地形特征,并提供了原子水平上对底物识别可能模式的深入了解。这里提出的 FadD13 的三维模型将有助于指导酶学研究以及特异性抑制剂的设计。