Molecular Docking Study: Application to the Epidermal Growth Factor Receptor

With the development of computer tools over the past 20 years, molecular modeling, and more precisely molecular docking (molecular docking), has very quickly entered the field of pharmaceutical research. Our work consists of studying the inhibition of the enzyme EGFR (1M17) involved in cancer with d...

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Main Authors: Faiza Asli, Imane Bensahbane
Format: Article
Language:English
Published: MDPI AG 2024-11-01
Series:Chemistry Proceedings
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Online Access:https://www.mdpi.com/2673-4583/16/1/82
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author Faiza Asli
Imane Bensahbane
author_facet Faiza Asli
Imane Bensahbane
author_sort Faiza Asli
collection DOAJ
description With the development of computer tools over the past 20 years, molecular modeling, and more precisely molecular docking (molecular docking), has very quickly entered the field of pharmaceutical research. Our work consists of studying the inhibition of the enzyme EGFR (1M17) involved in cancer with deferent inhibitors derived from quinazoline and quinoline by molecular docking. Ligands L_1 and L_2 are the best ligands for inhibiting the activity of 1M17 since they form a stable complex with this enzyme by better binding to the active site. The results obtained show that ligands L1 and L2 have weak interactions with the active site residue EGFR (1M17), which stabilize the complexes formed with these ligands, allow better binding at the level of the active site, and give an RMSD of L_1 [1.9563 Å] and of L_2 [1.2483 Å]. All the newly designed compounds passed the pharmacokinetic analysis (ADME–TOX) (adsorption, distribution, metabolism, excretion, and other physicochemical tests), passed the drug-likeness test, and also adhered to the Lipinski rule of five.
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spelling doaj-art-cb6702398c1448af9cc801e90fd9a2be2025-08-20T03:27:21ZengMDPI AGChemistry Proceedings2673-45832024-11-011618210.3390/ecsoc-28-20219Molecular Docking Study: Application to the Epidermal Growth Factor ReceptorFaiza Asli0Imane Bensahbane1Group of Computational and Medicinal Chemistry LMCE Laboratory, University Mohamed Khider, Biskra 07000, AlgeriaGroup of Computational and Medicinal Chemistry LMCE Laboratory, University Mohamed Khider, Biskra 07000, AlgeriaWith the development of computer tools over the past 20 years, molecular modeling, and more precisely molecular docking (molecular docking), has very quickly entered the field of pharmaceutical research. Our work consists of studying the inhibition of the enzyme EGFR (1M17) involved in cancer with deferent inhibitors derived from quinazoline and quinoline by molecular docking. Ligands L_1 and L_2 are the best ligands for inhibiting the activity of 1M17 since they form a stable complex with this enzyme by better binding to the active site. The results obtained show that ligands L1 and L2 have weak interactions with the active site residue EGFR (1M17), which stabilize the complexes formed with these ligands, allow better binding at the level of the active site, and give an RMSD of L_1 [1.9563 Å] and of L_2 [1.2483 Å]. All the newly designed compounds passed the pharmacokinetic analysis (ADME–TOX) (adsorption, distribution, metabolism, excretion, and other physicochemical tests), passed the drug-likeness test, and also adhered to the Lipinski rule of five.https://www.mdpi.com/2673-4583/16/1/82molecular dockingEGFRquinazoline and quinoliène derivativesADME-TinteractionsMOE
spellingShingle Faiza Asli
Imane Bensahbane
Molecular Docking Study: Application to the Epidermal Growth Factor Receptor
Chemistry Proceedings
molecular docking
EGFR
quinazoline and quinoliène derivatives
ADME-T
interactions
MOE
title Molecular Docking Study: Application to the Epidermal Growth Factor Receptor
title_full Molecular Docking Study: Application to the Epidermal Growth Factor Receptor
title_fullStr Molecular Docking Study: Application to the Epidermal Growth Factor Receptor
title_full_unstemmed Molecular Docking Study: Application to the Epidermal Growth Factor Receptor
title_short Molecular Docking Study: Application to the Epidermal Growth Factor Receptor
title_sort molecular docking study application to the epidermal growth factor receptor
topic molecular docking
EGFR
quinazoline and quinoliène derivatives
ADME-T
interactions
MOE
url https://www.mdpi.com/2673-4583/16/1/82
work_keys_str_mv AT faizaasli moleculardockingstudyapplicationtotheepidermalgrowthfactorreceptor
AT imanebensahbane moleculardockingstudyapplicationtotheepidermalgrowthfactorreceptor