Choragudi Shechinah Felice, Veeramachaneni Ganesh Kumar, Raman Bv, Js Bondili
Department of Biotechnology, K L University, Green fields, Vaddeswaram, Guntur, A.P-522502.
Department of Basic Sciences, Madanapalle Institute of Technology and sciences, Madanapalle, A.P-517325.
Bioinformation. 2014 Aug 30;10(8):507-11. doi: 10.6026/97320630010507. eCollection 2014.
Endo- β-N-acetylgucosaminidases (ENGases) are the enzymes that catalyze both hydrolysis and transglycosylation reactions. It is of interest to study ENGases because of their ability to synthesize glycopeptides. Homology models of Human, Arabidopsis thaliana and Sorghum ENGases were developed and their active sites marked based on information available from Arthrobacter protophormiae (PDB ID: 3FHQ) ENGase. Further, these models were docked with the natural substrate GlcNAc-Asn and the inhibitor Man3GlcNAc-thiazoline. The catalytic triad of Asn, Glu and Tyr (N171, E173 and Y205 of bacteria) were found to be conserved across the phyla. The crucial Y299F mutation showing 3 times higher transglycosylation activity than in wild type Endo-A is known. The hydrolytic activity remained unchanged in bacteria, while the transglycosylation activity increased. This Y to F change is found to be naturally evolved and should be attributing higher transglycosylation rates in human and Arabidopsis thaliana ENGases. Ligand interactions Ligplots revealed the interaction of amino acids with hydrophobic side chains and polar uncharged side chain amino acids. Thus, structure based molecular model-ligand interactions provide insights into the catalytic mechanism of ENGases and assist in the rational engineering of ENGases.
内切-β-N-乙酰葡糖胺酶(ENGases)是催化水解和转糖基化反应的酶。由于其合成糖肽的能力,对ENGases的研究很有意义。基于来自原噬菌体节杆菌(PDB ID:3FHQ)ENGase的可用信息,构建了人、拟南芥和高粱ENGases的同源模型,并标记了它们的活性位点。此外,将这些模型与天然底物GlcNAc-Asn和抑制剂Man3GlcNAc-噻唑啉进行对接。发现Asn、Glu和Tyr的催化三联体(细菌中的N171、E173和Y205)在不同门中是保守的。已知关键的Y299F突变的转糖基化活性比野生型内切-A高3倍。在细菌中水解活性保持不变,而转糖基化活性增加。发现这种Y到F的变化是自然进化的,并且应该归因于人和拟南芥ENGases中更高的转糖基化速率。配体相互作用Ligplots揭示了氨基酸与疏水侧链和极性不带电侧链氨基酸的相互作用。因此,基于结构的分子模型-配体相互作用为ENGases的催化机制提供了见解,并有助于ENGases的合理工程设计。