Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects

<p dir="ltr">Lung cancer is a major cause of cancer deaths worldwide, and has a very low survival rate. Non-small cell lung cancer (NSCLC) is the largest subset of lung cancers, which accounts for about 85% of all cases. It has been well established that a mutation in the epidermal g...

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Main Author: Rizwan Qureshi (15279193) (author)
Other Authors: Bin Zou (539731) (author), Tanvir Alam (638619) (author), Jia Wu (169990) (author), Victor H. F. Lee (10738845) (author), Hong Yan (27984) (author)
Published: 2023
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author Rizwan Qureshi (15279193)
author2 Bin Zou (539731)
Tanvir Alam (638619)
Jia Wu (169990)
Victor H. F. Lee (10738845)
Hong Yan (27984)
author2_role author
author
author
author
author
author_facet Rizwan Qureshi (15279193)
Bin Zou (539731)
Tanvir Alam (638619)
Jia Wu (169990)
Victor H. F. Lee (10738845)
Hong Yan (27984)
author_role author
dc.creator.none.fl_str_mv Rizwan Qureshi (15279193)
Bin Zou (539731)
Tanvir Alam (638619)
Jia Wu (169990)
Victor H. F. Lee (10738845)
Hong Yan (27984)
dc.date.none.fl_str_mv 2023-01-10T09:00:00Z
dc.identifier.none.fl_str_mv 10.1109/tcbb.2022.3141697
dc.relation.none.fl_str_mv https://figshare.com/articles/journal_contribution/Computational_Methods_for_the_Analysis_and_Prediction_of_EGFR-Mutated_Lung_Cancer_Drug_Resistance_Recent_Advances_in_Drug_Design_Challenges_and_Future_Prospects/26827777
dc.rights.none.fl_str_mv CC BY 4.0
info:eu-repo/semantics/openAccess
dc.subject.none.fl_str_mv Biomedical and clinical sciences
Clinical sciences
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
Non-small cell lung cancer (NSCLC)
epidermal growth factor receptor (EGFR)
molecular modeling
computational methods
molecular dynamics (MD) simulation
AlphaFold2
deep learning
Drugs
Immune system
Proteins
Lung cancer
Computational modeling
Inhibitors
Biological system modeling
dc.title.none.fl_str_mv Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
dc.type.none.fl_str_mv Text
Journal contribution
info:eu-repo/semantics/publishedVersion
text
contribution to journal
description <p dir="ltr">Lung cancer is a major cause of cancer deaths worldwide, and has a very low survival rate. Non-small cell lung cancer (NSCLC) is the largest subset of lung cancers, which accounts for about 85% of all cases. It has been well established that a mutation in the epidermal growth factor receptor (EGFR) can lead to lung cancer. EGFR Tyrosine Kinase Inhibitors (TKIs) are developed to target the kinase domain of EGFR. These TKIs produce promising results at the initial stage of therapy, but the efficacy becomes limited due to the development of drug resistance. In this paper, we provide a comprehensive overview of computational methods, for understanding drug resistance mechanisms. The important EGFR mutants and the different generations of EGFR–TKIs, with the survival and response rates are discussed. Next, we evaluate the role of important EGFR parameters in drug resistance mechanism, including structural dynamics, hydrogen bonds, stability, dimerization, binding free energies, and signaling pathways. Personalized drug resistance prediction models, drug response curve, drug synergy, and other data-driven methods are also discussed. Recent advancements in deep learning; such as AlphaFold2, deep generative models, big data analytics, and the applications of statistics and permutation are also highlighted. We explore limitations in the current methodologies, and discuss strategies to overcome them. We believe this review will serve as a reference for researchers; to apply computational techniques for precision medicine, analyzing structures of protein-drug complexes, drug discovery, and understanding the drug response and resistance mechanisms in lung cancer patients.</p><h2>Other Information</h2><p dir="ltr">Published in: IEEE/ACM Transactions on Computational Biology and Bioinformatics<br>License: <a href="https://creativecommons.org/licenses/by/4.0" target="_blank">https://creativecommons.org/licenses/by/4.0</a><br>See article on publisher's website: <a href="https://dx.doi.org/10.1109/tcbb.2022.3141697" target="_blank">https://dx.doi.org/10.1109/tcbb.2022.3141697</a></p>
eu_rights_str_mv openAccess
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identifier_str_mv 10.1109/tcbb.2022.3141697
network_acronym_str Manara2
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oai_identifier_str oai:figshare.com:article/26827777
publishDate 2023
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spelling Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future ProspectsRizwan Qureshi (15279193)Bin Zou (539731)Tanvir Alam (638619)Jia Wu (169990)Victor H. F. Lee (10738845)Hong Yan (27984)Biomedical and clinical sciencesClinical sciencesOncology and carcinogenesisPharmacology and pharmaceutical sciencesNon-small cell lung cancer (NSCLC)epidermal growth factor receptor (EGFR)molecular modelingcomputational methodsmolecular dynamics (MD) simulationAlphaFold2deep learningDrugsImmune systemProteinsLung cancerComputational modelingInhibitorsBiological system modeling<p dir="ltr">Lung cancer is a major cause of cancer deaths worldwide, and has a very low survival rate. Non-small cell lung cancer (NSCLC) is the largest subset of lung cancers, which accounts for about 85% of all cases. It has been well established that a mutation in the epidermal growth factor receptor (EGFR) can lead to lung cancer. EGFR Tyrosine Kinase Inhibitors (TKIs) are developed to target the kinase domain of EGFR. These TKIs produce promising results at the initial stage of therapy, but the efficacy becomes limited due to the development of drug resistance. In this paper, we provide a comprehensive overview of computational methods, for understanding drug resistance mechanisms. The important EGFR mutants and the different generations of EGFR–TKIs, with the survival and response rates are discussed. Next, we evaluate the role of important EGFR parameters in drug resistance mechanism, including structural dynamics, hydrogen bonds, stability, dimerization, binding free energies, and signaling pathways. Personalized drug resistance prediction models, drug response curve, drug synergy, and other data-driven methods are also discussed. Recent advancements in deep learning; such as AlphaFold2, deep generative models, big data analytics, and the applications of statistics and permutation are also highlighted. We explore limitations in the current methodologies, and discuss strategies to overcome them. We believe this review will serve as a reference for researchers; to apply computational techniques for precision medicine, analyzing structures of protein-drug complexes, drug discovery, and understanding the drug response and resistance mechanisms in lung cancer patients.</p><h2>Other Information</h2><p dir="ltr">Published in: IEEE/ACM Transactions on Computational Biology and Bioinformatics<br>License: <a href="https://creativecommons.org/licenses/by/4.0" target="_blank">https://creativecommons.org/licenses/by/4.0</a><br>See article on publisher's website: <a href="https://dx.doi.org/10.1109/tcbb.2022.3141697" target="_blank">https://dx.doi.org/10.1109/tcbb.2022.3141697</a></p>2023-01-10T09:00:00ZTextJournal contributioninfo:eu-repo/semantics/publishedVersiontextcontribution to journal10.1109/tcbb.2022.3141697https://figshare.com/articles/journal_contribution/Computational_Methods_for_the_Analysis_and_Prediction_of_EGFR-Mutated_Lung_Cancer_Drug_Resistance_Recent_Advances_in_Drug_Design_Challenges_and_Future_Prospects/26827777CC BY 4.0info:eu-repo/semantics/openAccessoai:figshare.com:article/268277772023-01-10T09:00:00Z
spellingShingle Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
Rizwan Qureshi (15279193)
Biomedical and clinical sciences
Clinical sciences
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
Non-small cell lung cancer (NSCLC)
epidermal growth factor receptor (EGFR)
molecular modeling
computational methods
molecular dynamics (MD) simulation
AlphaFold2
deep learning
Drugs
Immune system
Proteins
Lung cancer
Computational modeling
Inhibitors
Biological system modeling
status_str publishedVersion
title Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
title_full Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
title_fullStr Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
title_full_unstemmed Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
title_short Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
title_sort Computational Methods for the Analysis and Prediction of EGFR-Mutated Lung Cancer Drug Resistance: Recent Advances in Drug Design, Challenges and Future Prospects
topic Biomedical and clinical sciences
Clinical sciences
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
Non-small cell lung cancer (NSCLC)
epidermal growth factor receptor (EGFR)
molecular modeling
computational methods
molecular dynamics (MD) simulation
AlphaFold2
deep learning
Drugs
Immune system
Proteins
Lung cancer
Computational modeling
Inhibitors
Biological system modeling