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Pathway Description
Erlotinib Action Pathway
Homo sapiens
Drug Action Pathway
Created: 2013-08-22
Last Updated: 2019-08-16
Erlotinib is an anti-EGFR drug used in the treatment of some cancers. EGFR is linked multiple signalling pathways involved in tumour growth and angiogenesis such as the Ras/Raf pathway and the PI3K/Akt pathways. These pathways ultimately lead to the activation of transcription factors such as Jun, Fos, and Myc, as well as cyclin D1, which stimulates cell growth and mitosis. Uncontrolled cell growth and mitosis leads to cancer. Erlotinib acts as an anticancer drug by binding to the intracellular tyrosine kinase domain of the EGFR and blocking its activity. This in turn inhibits downstream signalling and prevents tumour growth.
References
Erlotinib Pathway References
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Pubmed: 3138233
Itoda M, Saito Y, Komamura K, Ueno K, Kamakura S, Ozawa S, Sawada J: Twelve novel single nucleotide polymorphisms in ABCB1/MDR1 among Japanese patients with ventricular tachycardia who were administered amiodarone. Drug Metab Pharmacokinet. 2002;17(6):566-71.
Pubmed: 15618713
Chen CJ, Chin JE, Ueda K, Clark DP, Pastan I, Gottesman MM, Roninson IB: Internal duplication and homology with bacterial transport proteins in the mdr1 (P-glycoprotein) gene from multidrug-resistant human cells. Cell. 1986 Nov 7;47(3):381-9. doi: 10.1016/0092-8674(86)90595-7.
Pubmed: 2876781
Chen CJ, Clark D, Ueda K, Pastan I, Gottesman MM, Roninson IB: Genomic organization of the human multidrug resistance (MDR1) gene and origin of P-glycoproteins. J Biol Chem. 1990 Jan 5;265(1):506-14.
Pubmed: 1967175
Zhang W, Mojsilovic-Petrovic J, Andrade MF, Zhang H, Ball M, Stanimirovic DB: The expression and functional characterization of ABCG2 in brain endothelial cells and vessels. FASEB J. 2003 Nov;17(14):2085-7. doi: 10.1096/fj.02-1131fje. Epub 2003 Sep 4.
Pubmed: 12958161
Ozvegy-Laczka C, Koblos G, Sarkadi B, Varadi A: Single amino acid (482) variants of the ABCG2 multidrug transporter: major differences in transport capacity and substrate recognition. Biochim Biophys Acta. 2005 Feb 1;1668(1):53-63. doi: 10.1016/j.bbamem.2004.11.005.
Pubmed: 15670731
Henriksen U, Gether U, Litman T: Effect of Walker A mutation (K86M) on oligomerization and surface targeting of the multidrug resistance transporter ABCG2. J Cell Sci. 2005 Apr 1;118(Pt 7):1417-26. doi: 10.1242/jcs.01729. Epub 2005 Mar 15.
Pubmed: 15769853
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