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Akpa, A.

Publications and source records attributed to Akpa, A..

2 recordsLinked to original sources

The Structure-Based Virtual Screening for Natural Compounds that Bind with the Activating Receptors of Natural Killer Cells

AimThis study is aimed at prospecting for natural compounds that have strong binding affinity for the Activating Receptors of Natural Killer (NK) cells. BackgroundNK cells are responsible for the immunosurveillance of tumor and virally- infected cells. The cytotoxic potentials of this unique population of immune cells are triggered by the activating receptors. Through ligand-binding, these receptors induce the tyrosine phosphorylation of adapter proteins through their Immunoreceptor Tyrosine-based Activation Motif ITAM sequences and this triggers direct cytotoxicity and the production of cytokines through different signal pathways. ObjectiveTo computationally predict the selectivity, specificity, and efficacy of natural compounds to be used as immunostimulatory agents for cancer treatment. MethodIn this study, 1,697 natural compounds were obtained from 82 edible tropical plants through data mining. The molecular docking simulations of these compounds were executed against 18 activating NK cells receptor targets using the Python Prescription 0.8. An arbitrary docking score [≥] -7.0 kcal/mol was chosen as cut off value. Further screening for oral bioavailability, promiscuity, molecular complexity and pharmacokinetic properties using the Swissadme and pkCSM webservers. The ligand similarity analysis and phylogenetic analysis of the receptors was carried out with the ChemMine and Clustal Omega webservers respectively. Binding site analyses and bioactivity prediction were also done with the Protein-Ligand Interaction Profiler and Molinspiration webservers respectively. Normal mode analyses were carried out with the CABS-flex 2.0 server. ResultSeventeen bioactive and non-promiscuous lead compounds with good physicochemical and pharmacokinetic properties were identified. ConclusionFurther tests are required to evaluate the efficacy of the lead compounds.

bioinformatics

IN SILICO SCREENING AND MOLECULAR DYNAMIC SIMULATION STUDIES OF POTENTIAL SMALL MOLECULE IMMUNOMODULATORS OF THE KIR2DS2 RECEPTOR

The World Health Organization reports that cancer is one of the most common causes of death worldwide and it accounted for an estimated 9.6 million deaths in 2018. As compared with chemotherapy or radiotherapy, immunotherapy offers a safer, less stressful and selective strategy in the destruction of cancer cells. The killer cell immunoglobulin-like receptor 2DS2 (KIR2DS2) expressed on Natural Killer (NK) cells are involved in signal transduction processes that produce pro-inflammatory cytokines and directly destroy cancer and virally infected cells. The aim of this study is to identify small molecules from natural products that have strong binding affinity with KIR2DS2 and possible bioactivity. A library of small molecule natural compounds obtained from edible African plants was used for in Silico molecular docking simulations of KIR2DS2 (PDBID: 1m4k) using Pyrx. An arbitrary docking score [≥] -7.0 kcal/mol was chosen as cut off value. Screening for drug-likeness and ligand efficiency was based on the molecular descriptors of the compounds as provided by Pubchem. Further screening for saturation, molar refractivity, promiscuity, pharmacokinetic properties, and bioactivity was done using SWISSADME, PKCSM, and Molinspiration respectively. The molecular dynamic simulation and analyses was done using the Galaxy webserver which uses the GROMACS software. Analyses of molecular dynamic simulation were done using Galaxy and MDWEB webservers. Gibberellin A20 and A29 were obtained as the lead compounds and they show better promise as drug candidates for KIR2DS2 than the standard. It is recommended that the immuno-stimulatory effect of the lead compounds on KIR2DS2 be further investigated.

bioinformatics