Journal of biomolecular structure & dynamics · 2018
Pharmacophore and structure-based drug design, molecular dynamics and admet/tox studies to design novel potential pad4 inhibitors.
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Barcellos Mariana P, Santos Cleydson B R, Federico Leonardo B, Almeida Paulo Fernando de, da Silva Carlos H T de Paula, Taft Carlton A
Аннотация
We have used docking (GLIDE), pharmacophore modeling (Discovery Studio), long trajectory molecular dynamics (Discovery Studio) and ADMET/Tox (QikProp and DEREK) to investigate PAD4 in order to determine potential novel inhibitors and hits. We have carried out virtual screening in the ZINC natural compounds database. Pharmacokinetics and Toxicity of the best hits were assessed using databases implemented in softwares that create models based on chemical structures taking into account consideration about the toxicophoric groups. A wide variety of pharmaceutical relevant properties are determined in order to make decisions about molecular suitability. After screening and analysis, the 6 most promising PAD4 inhibitors are suggested, with strong interactions (pi-stacking, hydrogen bonds, hydrophobic contacts) and suitable pharmacotherapeutic profile as well.
Предметные рубрики MeSH
Catalytic DomainDatabases, PharmaceuticalDrug DesignDrug-Related Side Effects and Adverse ReactionsEnzyme InhibitorsHigh-Throughput Screening AssaysHumansHydrophobic and Hydrophilic InteractionsLigandsModels, MolecularMolecular Docking SimulationMolecular Dynamics SimulationProtein-Arginine Deiminase Type 4Quantitative Structure-Activity Relationship