Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

SdiA is a LuxR-type receptor that controls the virulence of Klebsiella pneumoniae, a Gram-negative bacterium that causes various infections in humans. SdiA senses exogenous acyl-homoserine lactones (AHLs) and autoinducer-2 (AI-2), two types of quorum sensing signals produced by other bacterial species. However, the molecular details of how SdiA recognizes and binds to different ligands and how this affects its function and regulation in K. pneumoniae still need to be better understood. This study uses computational methods to explore the protein-ligand binding dynamics of SdiA with 11 AHLs and 2 AI-2 ligands. The 3D structure of SdiA was predicted through homology modeling, followed by molecular docking with AHLs and AI-2 ligands. Binding affinities were quantified using MM-GBSA, and complex stability was assessed via Molecular Dynamics (MD) simulations. Results demonstrated that SdiA in Klebsiella pneumoniae exhibits a degenerate binding nature, capable of interacting with multiple AHLs and AI-2. Specific ligands, namely C10-HSL, C8-HSL, 3-oxo-C8-HSL, and 3-oxo-C10-HSL, were found to have high binding affinities and formed critical hydrogen bonds with key amino acid residues of SdiA. This finding aligns with the observed preference of SdiA for AHLs having 8 to 10 carbon-length acyl chains and lacking hydroxyl groups. In contrast, THMF and HMF demonstrated poor binding properties. Furthermore, AI-2 exhibited a low affinity, corroborating the inference that SdiA is not the primary receptor for AI-2 in K. pneumoniae. These findings provide insights into the protein-ligand binding dynamics of SdiA and its role in quorum sensing and virulence of K. pneumoniae.

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11030-023-10785-6DOI Listing

Publication Analysis

Top Keywords

binding dynamics
12
dynamics sdia
12
klebsiella pneumoniae
12
ahls ai-2
12
sdia
11
quorum sensing
8
protein-ligand binding
8
sdia ahls
8
ai-2 ligands
8
binding affinities
8

Similar Publications

This study utilized integrated sensory-guided, machine learning, and bioinformatics strategies identify umami-enhancing peptides from , investigated their mechanism of umami enhancement, and confirmed their umami-enhancing properties through sensory evaluations and electronic tongue. Three umami-enhancing peptides (APDGLPTGQ, SDDGFQ, and GLGDDL) demonstrated synergistic/additive effects by significantly enhancing umami intensity and duration in monosodium glutamate (MSG). Furthermore, molecular docking showed that these umami-enhancing peptides enhanced both the binding affinity and interaction forces between MSG and the T1R1/T1R3 receptor system, thereby enhancing umami perception.

View Article and Find Full Text PDF

Mammalian ALOX15 are allosteric enzymes but the mechanism of allosteric regulation remains a matter of discussion. Octyl (-(5-(1-indol-2-yl)-2-methoxyphenyl)sulfamoyl)carbamate inhibits the linoleate oxygenase activity of ALOX15 at nanomolar concentrations, but oxygenation of arachidonic acid is hardly affected. The mechanism of substrate selective inhibition suggests inter-monomer communication within the allosteric ALOX15 dimer complex, in which the inhibitor binding to monomer A induces conformational alterations in the structure of the active site of monomer B.

View Article and Find Full Text PDF

Phosphorylation plays an important role in the activity of CDK2 and inhibitor binding, but the corresponding molecular mechanism is still insufficiently known. To address this gap, the current study innovatively integrates molecular dynamics (MD) simulations, deep learning (DL) techniques, and free energy landscape (FEL) analysis to systematically explore the action mechanisms of two inhibitors (SCH and CYC) when CDK2 is in a phosphorylated state and bound state of CyclinE. With the help of MD trajectory-based DL, key functional domains such as the loops L3 loop and L7 are successfully identified.

View Article and Find Full Text PDF

, a causative agent of lymphatic filariasis, relies on its endosymbiont for survival. MurE ligase, a key enzyme in peptidoglycan biosynthesis, serves as a promising drug target for anti-filarial therapy. In this study, we employed a hierarchical virtual screening pipeline to identify phytochemical inhibitors targeting the MurE enzyme of the endosymbiont of (MurE).

View Article and Find Full Text PDF

Background: Differentially expressed genes (DEGs) have been known to provide important information on disease mechanisms and potential therapeutic targets. The traditional Chinese medicine (TCM) offers a large reservoir of bioactive compounds that could modulate at these targets. This study is an attempt to investigate the biomarkers in Sepsis and COVID-19 using gene expression analysis and molecular modeling validation of TCM-derived candidate compounds targeting key DEGs associated with sepsis.

View Article and Find Full Text PDF