Department of Biotechnology, Lahore College for Women University, Lahore, Pakistan.
Panjwani Center for Molecular Medicine and Drug Research, University of Karachi, Karachi, Pakistan.
PLoS One. 2024 Aug 2;19(8):e0307448. doi: 10.1371/journal.pone.0307448. eCollection 2024.
Cancer is a leading concern and important cause of death worldwide. Cancer is a non-communicable illness defined as uncontrolled division of cells. It can develop into metastatic cancer when tumor cells migrate to other organs. In recent years evidence has emerged that the bioavailability of Asn play a crucial role in cancer metastasis. Asn is a non-essential amino acid formed from an ATP dependent catalyzed reaction by the enzyme asparagine synthetase (ASNS), where Asp and Gln are converted to Asn and Glu, respectively. The human ASNS enzyme consist of 561 amino acids, with a molecular weight of 64 KDa. ASNS governs the activation of transcriptional factors that regulate the process of metastasis. In this work the 3D model of ASNS in E. coli (AS-B) and the human ASNS docked with its different ligands have been used to study the 3D mechanism of the conversion of Asp and Gln to Asn and Glu, in human ASNS. The stability evaluation of the docked complexes was checked by molecular dynamic simulation through the bioinformatic tool Desmond. The binding residues and their interactions can be exploited for the development of inhibitors, as well as for finding new drug molecules against ASNS and prevention of metastatic cancer.
癌症是全球主要关注的问题和重要死因。癌症是非传染性疾病,定义为细胞不受控制的分裂。当肿瘤细胞迁移到其他器官时,它可能发展成转移性癌症。近年来有证据表明,Asn 的生物利用度在癌症转移中起着至关重要的作用。Asn 是一种非必需氨基酸,由酶天冬酰胺合成酶 (ASNS) 催化的 ATP 依赖性反应形成,其中 Asp 和 Gln 分别转化为 Asn 和 Glu。人 ASNS 酶由 561 个氨基酸组成,分子量为 64 kDa。ASNS 调节转录因子的激活,从而调节转移过程。在这项工作中,使用了大肠杆菌中的 ASNS 的 3D 模型(AS-B)和与人 ASNS 对接的不同配体,以研究人 ASNS 中天冬氨酸和谷氨酰胺转化为天冬酰胺和谷氨酸的 3D 机制。通过生物信息学工具 Desmond 进行分子动力学模拟检查对接复合物的稳定性评估。可以利用结合残基及其相互作用来开发抑制剂,以及寻找针对 ASNS 和预防转移性癌症的新药物分子。