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Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain.

<div class='caption-title'>Comparison of erlotinib binding to active and inactive EGFR-TKD models</div>
<div class='caption-title'>Crystal structures of TKI-bound EGFR-TKD</div>
<div class='caption-title'>Erlotinib binding to inactive EGFR-TKD</div>
Park JH, Liu Y, Lemmon MA, Radhakrishnan R
OpenAccess logo Biochem J 448 417-23 (2012)
Cited: 121 times
EuropePMC logo PMID: 23101586

Abstract

Erlotinib and gefitinib, tyrosine kinase inhibitors used to block EGFR (epidermal growth factor receptor) signalling in cancer, are thought to bind only the active conformation of the EGFR-TKD (tyrosine kinase domain). Through parallel computational and crystallographic studies, we show in the present study that erlotinib also binds the inactive EGFR-TKD conformation, which may have significant implications for its use in EGFR-mutated cancers.

Reviews - 4hjo mentioned but not cited (7)

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Articles - 4hjo mentioned but not cited (67)

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  22. Allele-Specific Role of ERBB2 in the Oncogenic Function of EGFR L861Q in EGFR-Mutant Lung Cancers. Sato H, Offin M, Kubota D, Yu HA, Wilhelm C, Toyooka S, Somwar R, Kris MG, Ladanyi M. J Thorac Oncol 16 113-126 (2021)
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  36. Analysis of the Molecular Mechanism of Punicalagin in the Treatment of Alzheimer's Disease by Computer-Aided Drug Research Technology. Xu P, Xu L, Huang S, Li D, Liu Y, Guo H, Dai N, Hong Z, Zhong S. ACS Omega 7 6121-6132 (2022)
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  38. Direct Synthesis of Diamides from Dicarboxylic Acids with Amines Using Nb2O5 as a Lewis Acid Catalyst and Molecular Docking Studies as Anticancer Agents. Ali MA, Nath A, Jannat M, Islam MM. ACS Omega 6 25002-25009 (2021)
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  44. BTEAC Catalyzed Ultrasonic-Assisted Synthesis of Bromobenzofuran-Oxadiazoles: Unravelling Anti-HepG-2 Cancer Therapeutic Potential through In Vitro and In Silico Studies. Irfan A, Zahoor AF, Rasul A, Al-Hussain SA, Faisal S, Ahmad S, Noor R, Muhammed MT, Zaki MEA. Int J Mol Sci 24 3008 (2023)
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  54. Antimicrobial, Cytotoxic, and α-Glucosidase Inhibitory Activities of Ethanol Extract and Chemical Constituents Isolated from Homotrigona apicalis Propolis-In Vitro and Molecular Docking Studies. Phuong DTL, Van Phuong N, Le Tuan N, Cong NT, Hang NT, Thanh LN, Hue VT, Vuong NQ, Ha NTT, Popova M, Trusheva B, Bankova V. Life (Basel) 13 1682 (2023)
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  56. Computer-Assisted Drug Discovery of a Novel Theobromine Derivative as an EGFR Protein-Targeted Apoptosis Inducer. Eissa IH, Yousef RG, Elkaeed EB, Alsfouk AA, Husein DZ, Ibrahim IM, El-Mahdy HA, Elkady H, Metwaly AM. Evol Bioinform Online 19 11769343231217916 (2023)
  57. Design, Synthesis, and Molecular Docking Studies of Some New Quinoxaline Derivatives as EGFR Targeting Agents. Badithapuram V, Nukala SK, Thirukovela NS, Dasari G, Manchal R, Bandari S. Russ J Bioorg Chem 48 565-575 (2022)
  58. Design, synthesis, X-ray crystal structures, anticancer, DNA binding, and molecular modelling studies of pyrazole-pyrazoline hybrid derivatives. Rana M, Hungyo H, Parashar P, Ahmad S, Mehandi R, Tandon V, Raza K, Assiri MA, Ali TE, El-Bahy ZM, Rahisuddin. RSC Adv 13 26766-26779 (2023)
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