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Tag, H.

Publications and source records attributed to Tag, H..

2 recordsLinked to original sources

Computational Screening of Zanthoxylum armatum DC Phytochemicals for Inhibiting Mutant P53 in Throat Cancer Therapy

AimTo investigate the potential of phytochemicals from Zanthoxylum armatum DC in targeting mutant p53 as a therapeutic strategy for throat cancer using an in-silico approach. BackgroundThroat cancer is increasingly associated with mutations in the TP53 gene, leading to dysfunctional p53 proteins. Current synthetic drugs targeting mutant p53 face challenges of toxicity and off-target effects, necessitating the exploration of alternative natural compounds. MethodsWe employed molecular docking, molecular dynamics simulations, MMPBSA analysis, and ADMET studies to identify and characterize effective inhibitors of mutant p53 from Z. armatum DC phytochemicals. ResultsThree compounds - Z3, Z7, and Z33 - demonstrated superior binding affinities to mutant p53 compared to the commercial drug Prima. These phytochemicals induced more compact and stable protein conformations, with Z3 and Z7 notably restricting active site residual motion. MMPBSA analysis confirmed favourable binding energetics, while ADMET studies indicated drug-like properties with potentially lower toxicity than Prima. ConclusionThis study provides compelling evidence for the potential of Z. armatum DC phytochemicals, particularly Z3 and Z7, as novel therapeutic agents targeting mutant p53 in throat cancer. These findings offer a foundation for future experimental validation and drug development efforts.

bioinformatics↗

In silico analysis of Bacopa monnieri (L.) Wettst. compounds for drug development against Neurodegenerative Disorders

Neurotrophins play a crucial role in the development and regulation of neurons. Alterations in the functioning of these Neurotrophins leads to several Neurodegenerative Disorders. Albeit engineered medications which are accessible for the treatment of Neurodegenerative Disorders, due to their numerous side-effects, it becomes imperative to formulate and synthesize novel drug candidates. Plants could be utilized as an alternative for these manufactured medications because of their low incidental effects in contrast with the engineered drugs. Bacopa monnieri has been traditionally known to be utilized to treat Neurodegenerative Disorders. Therefore, in current study an in-silico based study was carried out to evaluate the pharmacological effect of Bacopa monnieri. Molecular Docking was carried out to screen the active phytochemicals of Bacopa monnieri which can act as potential drug candidates against the causative proteins of Neurodegenerative Disorders. A total of 105 biologically active phytochemicals from Bacopa monnieri were docked against the receptors of brain-derived neurotrophic factor, neurotrophin-3, neurotrophin-4, and nerve growth factor. Based on molecular docking study it was observed that the phytocompounds Vitamin E, Benzene propanoic acid, 3,5-bis(1,1dimethylethyl)4-hydroxy-, methyl ester (BPA), Stigmasterol, and Nonacosane of Bacopa monnieri significantly fits to the active residues of the four selected drug targets. Further Molecular Dynamics simulation study was performed to examine the stability of the binding of these phytochemicals with the selected targets. Drug likeness properties as well as related physico-chemical properties were analyzed through ADMETox study. Our findings suggested that the phytocompounds Vitamin E, BPA, Stigmasterol and Nonacosane significantly bind against brain-derived neurotrophic factor, neurotrophin-3, neurotrophin4, and nerve growth factor, respectively which may be the potential drug candidates for the treatment of neurodegenerative disorders. Graphic Abstract O_FIG O_LINKSMALLFIG WIDTH=200 HEIGHT=140 SRC="FIGDIR/small/486025v1_ufig1.gif" ALT="Figure 1"> View larger version (55K): org.highwire.dtl.DTLVardef@2c39aforg.highwire.dtl.DTLVardef@17f4fd9org.highwire.dtl.DTLVardef@1534e13org.highwire.dtl.DTLVardef@2ad383_HPS_FORMAT_FIGEXP M_FIG C_FIG

pharmacology and toxicology↗