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PY873、PY899和DIA对甘氨酰胺核苷酸转甲酰基酶的抑制作用分析

analysis of glycinamide ribonucleotide transformylase inhibition by PY873, PY899 and DIA.

作者信息

Batool Sidra, Nawaz Muhammad Sulaman, Mushtaq Gohar, Parvaiz Fahed, Kamal Mohammad A

机构信息

Department of BioSciences, COMSATS Institute of Information Technology, Park Road, Chak Shahzad, Islamabad 44000, Pakistan.

Department of Biochemistry, College of Science, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

Saudi J Biol Sci. 2017 Sep;24(6):1155-1161. doi: 10.1016/j.sjbs.2014.11.008. Epub 2014 Nov 22.

DOI:10.1016/j.sjbs.2014.11.008
PMID:28855807
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5562383/
Abstract

In humans, purine synthesis pathway consists of multi-functional enzymes. Nucleotide metabolism enzymes are potential drug targets for treating cancer and autoimmune diseases. Glycinamide ribonucleotide transformylase (GART) is one of the most important trifunctional enzymes involved in purine synthesis. Previous studies have demonstrated the role of folate inhibitors against tumor activity. In this present study, three components of GART enzyme were targeted as receptor dataset and analysis was carried out with folate ligand dataset. To accomplish the task, Autodock 4.2 was used for determining the docking compatibilities of ligand and receptor dataset. Taken together, it has been suggested that folate ligands could be potentially used as inhibitors of GART.

摘要

在人类中,嘌呤合成途径由多功能酶组成。核苷酸代谢酶是治疗癌症和自身免疫性疾病的潜在药物靶点。甘氨酰胺核糖核苷酸转甲酰基酶(GART)是参与嘌呤合成的最重要的三功能酶之一。先前的研究已经证明了叶酸抑制剂对肿瘤活性的作用。在本研究中,将GART酶的三个组分作为受体数据集,并与叶酸配体数据集进行分析。为完成该任务,使用Autodock 4.2来确定配体和受体数据集的对接兼容性。综上所述,有人提出叶酸配体可能潜在地用作GART的抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/bbb0de9ea7b5/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/111636511cc2/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/c2871a26195f/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/20a6993b4fbf/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/bbb0de9ea7b5/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/111636511cc2/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/c2871a26195f/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/20a6993b4fbf/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe87/5562383/bbb0de9ea7b5/gr4.jpg

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