Lung adenocarcinoma with BRAF G469L mutation refractory to vemurafenib.

作者: Oliver Gautschi , Solange Peters , Vincent Zoete , Franziska Aebersold-Keller , Klaus Strobel

DOI: 10.1016/J.LUNGCAN.2013.08.012

关键词:

摘要: BRAF V600E is an emerging drug target in lung cancer, but the clinical significance of non-V600 mutations cancer and other malignancies less clear. Here, we report case a patient with metastatic adenocarcinoma G469L mutation refractory to vemurafenib. We calculated structure model this very rare type mutated kinase explain molecular mechanism resistance. This information may help develop effective targeted therapies for cancers mutations.

参考文章(17)
Hong Yang, Brian Higgins, Kenneth Kolinsky, Kathryn Packman, Zenaida Go, Raman Iyer, Stanley Kolis, Sylvia Zhao, Richard Lee, Joseph F. Grippo, Kathleen Schostack, Mary Ellen Simcox, David Heimbrook, Gideon Bollag, Fei Su, RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models Cancer Research. ,vol. 70, pp. 5518- 5527 ,(2010) , 10.1158/0008-5472.CAN-10-0646
Shin Yup Lee, Min Jung Kim, Guang Jin, Seung Soo Yoo, Ji Young Park, Jin Eun Choi, Hyo Sung Jeon, Sukki Cho, Eung Bae Lee, Seung Ick Cha, Tae-In Park, Chang Ho Kim, Tae Hoon Jung, Jae Yong Park, Somatic Mutations in Epidermal Growth Factor Receptor Signaling Pathway Genes in Non-small Cell Lung Cancers Journal of Thoracic Oncology. ,vol. 5, pp. 1734- 1740 ,(2010) , 10.1097/JTO.0B013E3181F0BECA
Gideon Bollag, Peter Hirth, James Tsai, Jiazhong Zhang, Prabha N. Ibrahim, Hanna Cho, Wayne Spevak, Chao Zhang, Ying Zhang, Gaston Habets, Elizabeth A. Burton, Bernice Wong, Garson Tsang, Brian L. West, Ben Powell, Rafe Shellooe, Adhirai Marimuthu, Hoa Nguyen, Kam Y. J. Zhang, Dean R. Artis, Joseph Schlessinger, Fei Su, Brian Higgins, Raman Iyer, Kurt D’Andrea, Astrid Koehler, Michael Stumm, Paul S. Lin, Richard J. Lee, Joseph Grippo, Igor Puzanov, Kevin B. Kim, Antoni Ribas, Grant A. McArthur, Jeffrey A. Sosman, Paul B. Chapman, Keith T. Flaherty, Xiaowei Xu, Katherine L. Nathanson, Keith Nolop, Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF -mutant melanoma Nature. ,vol. 467, pp. 596- 599 ,(2010) , 10.1038/NATURE09454
Oliver Gautschi, Chantal Pauli, Klaus Strobel, Astrid Hirschmann, Gert Printzen, Stefan Aebi, Joachim Diebold, A Patient With BRAF V600E Lung Adenocarcinoma Responding to Vemurafenib Journal of Thoracic Oncology. ,vol. 7, pp. e23- e24 ,(2012) , 10.1097/JTO.0B013E3182629903
Peng Xie, Craig Streu, Jie Qin, Howard Bregman, Nicholas Pagano, Eric Meggers, Ronen Marmorstein, The crystal structure of BRAF in complex with an organoruthenium inhibitor reveals a mechanism for inhibition of an active form of BRAF kinase. Biochemistry. ,vol. 48, pp. 5187- 5198 ,(2009) , 10.1021/BI802067U
Thomas Zander, Matthias Scheffler, Lucia Nogova, Carsten Kobe, Walburga Engel-Riedel, Martin Hellmich, Irini Papachristou, Karin Toepelt, Andreas Draube, Lukas Heukamp, Reinhard Buettner, Yon D. Ko, Roland T. Ullrich, Egbert Smit, Ronald Boellaard, Adriaan A. Lammertsma, Michael Hallek, Andreas H. Jacobs, Andreas Schlesinger, Karin Schulte, Silvia Querings, Erich Stoelben, Bernd Neumaier, Roman K. Thomas, Markus Dietlein, Jürgen Wolf, Early Prediction of Nonprogression in Advanced Non–Small-Cell Lung Cancer Treated With Erlotinib By Using [18F]Fluorodeoxyglucose and [18F]Fluorothymidine Positron Emission Tomography Journal of Clinical Oncology. ,vol. 29, pp. 1701- 1708 ,(2011) , 10.1200/JCO.2010.32.4939
Gerald S Falchook, Georgina V Long, Razelle Kurzrock, Kevin B Kim, Tobias H Arkenau, Michael P Brown, Omid Hamid, Jeffrey R Infante, Michael Millward, Anna C Pavlick, Steven J O’Day, Samuel C Blackman, C Martin Curtis, Peter Lebowitz, Bo Ma, Daniele Ouellet, Richard F Kefford, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. The Lancet. ,vol. 379, pp. 1893- 1901 ,(2012) , 10.1016/S0140-6736(12)60398-5
B. Sen, S. Peng, X. Tang, H. S. Erickson, H. Galindo, T. Mazumdar, D. J. Stewart, I. Wistuba, F. M. Johnson, Kinase-Impaired BRAF Mutations in Lung Cancer Confer Sensitivity to Dasatinib Science Translational Medicine. ,vol. 4, ,(2012) , 10.1126/SCITRANSLMED.3003513
Christine A. Pratilas, Aphrothiti J. Hanrahan, Ensar Halilovic, Yogindra Persaud, Junichi Soh, Dhananjay Chitale, Hisayuki Shigematsu, Hiromasa Yamamoto, Ayana Sawai, Manickam Janakiraman, Barry S. Taylor, William Pao, Shinichi Toyooka, Marc Ladanyi, Adi Gazdar, Neal Rosen, David B. Solit, Genetic predictors of MEK-dependence in non-small cell lung cancer Cancer Research. ,vol. 68, pp. 9375- 9383 ,(2008) , 10.1158/0008-5472.CAN-08-2223