Departamento de Biofísica e Farmacologia , Universidade Federal do Rio Grande do Norte , 59072-970 Natal-RN , Brazil.
Departamento de Física Teórica e Experimental , Universidade Federal do Rio Grande do Norte , 59072-970 Natal-RN , Brazil.
J Phys Chem B. 2019 Aug 1;123(30):6421-6429. doi: 10.1021/acs.jpcb.9b04468. Epub 2019 Jul 22.
We intend to investigate the drug-binding energy of each nucleotide inside the aminoglycoside hygromycin B (hygB) binding site of 30S ribosomal RNA (rRNA) subunit by using the molecular fractionation with conjugate caps (MFCC) strategy based on the density functional theory (DFT), considering the functional LDA/PWC, OBS, and the dielectric constant parametrization. Aminoglycosides are bactericidal antibiotics that have high affinity to the prokaryotic rRNA, inhibiting the synthesis of proteins by acting on the main stages of the translation mechanism, whereas binding to rRNA 16S, a component of the 30S ribosomal subunit in prokaryotes. The identification of the nucleotides presenting the most negative binding energies allows us to stabilize hygB in a suitable binding pocket of the 30S ribosomal subunit. In addition, it should be highlighted that mutations in these residues may probably lead to resistance to ribosome-targeting antibiotics. Quantum calculations of aminoglycoside hygromycin B-ribosome complex might contribute to further quantum studies with antibiotics like macrolides and other aminoglycosides.
我们拟采用基于密度泛函理论(DFT)的共轭帽分子分段(MFCC)策略,考虑功能 LDA/PWC、OBS 和介电常数参数化,研究氨基糖苷类抗生素潮霉素 B(hygB)结合位点 30S 核糖体 RNA(rRNA)亚基中每个核苷酸的药物结合能。氨基糖苷类抗生素是一种杀菌抗生素,与原核 rRNA 具有高亲和力,通过作用于翻译机制的主要阶段来抑制蛋白质的合成,而与原核生物 30S 核糖体亚基的组成部分 16S rRNA 结合。确定具有最负结合能的核苷酸,可以使 hygB 稳定在 30S 核糖体亚基的合适结合口袋中。此外,值得强调的是,这些残基的突变可能导致对核糖体靶向抗生素的耐药性。氨基糖苷类抗生素潮霉素 B-核糖体复合物的量子计算可能有助于对大环内酯类抗生素和其他氨基糖苷类抗生素进行进一步的量子研究。