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RET inhibition: implications in cancer therapy

, Biol Sci D PhD, , Biol Sci D PhD, , MD, , Biol Sci D PhD, , MD & , Biol Sci D PhD
Pages 403-419 | Published online: 06 Mar 2013

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (3)

Guodong Zheng, Shenqian Xu, Wuxia Liu, Tingting Du, Jingfeng Zhang, Minyu Li, Chen Cai & Hong Shi. (2021) Deciphering the resistance mechanism of RET kinase mutant against vandetanib and nintedanib using molecular dynamics simulations. Journal of Experimental Nanoscience 16:1, pages 278-293.
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Luca Mologni, Carlo Gambacorti-Passerini, Peter Goekjian & Leonardo Scapozza. (2017) RET kinase inhibitors: a review of recent patents (2012–2015). Expert Opinion on Therapeutic Patents 27:1, pages 91-99.
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Chen Lin, Shanshan Wang, Weiwei Xie, Jianhua Chang & Yu Gan. (2015) The RET fusion gene and its correlation with demographic and clinicopathological features of non-small cell lung cancer: a meta-analysis. Cancer Biology & Therapy 16:7, pages 1019-1028.
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Articles from other publishers (34)

Gabriele La Monica, Giuseppe Pizzolanti, Concetta Baiamonte, Alessia Bono, Federica Alamia, Francesco Mingoia, Antonino Lauria & Annamaria Martorana. (2023) Design and Synthesis of Novel Thieno[3,2- c ]quinoline Compounds with Antiproliferative Activity on RET-Dependent Medullary Thyroid Cancer Cells . ACS Omega.
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Anil Verma & Pankaj Wadhwa. (2023) An Identification of RET Inhibitor: A Computational Study. Current Signal Transduction Therapy 18:2.
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Priyanka Ramesh, Woong-Hee Shin & Shanthi Veerappapillai. (2021) Discovery of a Potent Candidate for RET-Specific Non-Small-Cell Lung Cancer—A Combined In Silico and In Vitro Strategy. Pharmaceutics 13:11, pages 1775.
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Zhibo Luo, Lingli Wang, Zhifei Fu, Bin Shuai, Miaorong Luo, Guoping Hu, Jian Chen, Jikui Sun, Jiansong Wang, Jian Li, Shuhui Chen & Yang Zhang. (2021) Discovery and optimization of selective RET inhibitors via scaffold hopping. Bioorganic & Medicinal Chemistry Letters 47, pages 128149.
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Thais Cristina Mendonça Nogueira & Marcus Vinicius Nora de Souza. (2021) New FDA oncology small molecule drugs approvals in 2020: Mechanism of action and clinical applications. Bioorganic & Medicinal Chemistry 46, pages 116340.
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Cong-Cong Jia, Wang Chen, Zi-Li Feng & Zhao-Peng Liu. (2021) Recent developments of RET protein kinase inhibitors with diverse scaffolds as hinge binders. Future Medicinal Chemistry 13:1, pages 45-62.
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Zhichao Tian, Xiaohui Niu & Weitao Yao. (2020) Receptor Tyrosine Kinases in Osteosarcoma Treatment: Which Is the Key Target?. Frontiers in Oncology 10.
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Aishwarya Laxmi, Pawan Gupta & Jeena Gupta. (2019) CCDC6, a gene product in fusion with different protoncogenes, as a potential chemotherapeutic target. Cancer Biomarkers 24:4, pages 383-393.
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John P. Russell, Ehsan Mohammadi, Casey O. Ligon, Anthony C. Johnson, Michael D. Gershon, Meenakshi Rao, Yuhong Shen, Chi-Chung Chan, Hilary S. Eidam, Michael P. DeMartino, Mui Cheung, Allen I. Oliff, Sanjay Kumar & Beverley Greenwood-Van Meerveld. (2019) Exploring the Potential of RET Kinase Inhibition for Irritable Bowel Syndrome: A Preclinical Investigation in Rodent Models of Colonic Hypersensitivity. Journal of Pharmacology and Experimental Therapeutics 368:2, pages 299-307.
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Yucong Wang, Yinghui Xu, Xu Wang, Chao Sun, Ye Guo, Guoguang ShaoZhiguang YangShi Qiu & Kewei Ma. (2019) RET fusion in advanced non-small-cell lung cancer and response to cabozantinib. Medicine 98:3, pages e14120.
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Aniello Cerrato, Roberta Visconti & Angela Celetti. (2018) The rationale for druggability of CCDC6-tyrosine kinase fusions in lung cancer. Molecular Cancer 17:1.
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Valeria La Pietra, Stefania Sartini, Lorenzo Botta, Alessandro Antonelli, Silvia Martina Ferrari, Poupak Fallahi, Alessio Moriconi, Vito Coviello, Luca Quattrini, Yi-Yu Ke, Hsieh Hsing-Pang, Federico Da Settimo, Ettore Novellino, Concettina La Motta & Luciana Marinelli. (2018) Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. European Journal of Medicinal Chemistry 150, pages 491-505.
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Sara Redaelli, Ivan Plaza-Menacho & Luca Mologni. (2018) Novel targeted therapeutics for MEN2. Endocrine-Related Cancer 25:2, pages T53-T68.
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Sandra Salvi, Jean Louis Ravetti, Giuseppe Arena, Clementina Musso, Serena Varesano, Maria Pia Pistillo, Pier Aldo Canessa, Paola Ferro, Franco Fedeli & Silvio Roncella. (2018) Evaluation of RET Gene Rearrangement by Fluorescence In Situ Hybridization in Malignant Mesothelioma. Journal of Thoracic Oncology 13:1, pages e12-e14.
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Dennis Plenker, Maximilian Riedel, Johannes Brägelmann, Marcel A. DammertRakhee ChauhanPhillip P. KnowlesCarina LorenzMarina Keul, Mike BührmannOliver Pagel, Verena TischlerAndreas H. Scheel, Daniel SchütteYanrui Song, Justina Stark, Florian MrugallaYannic AlberAndré RichtersJulian EngelFrauke LeendersJohannes M. Heuckmann, Jürgen WolfJoachim DieboldGeorg PallMartin PeiferMaarten Aerts, Kris GevaertRené P. ZahediReinhard BuettnerKevan M. ShokatNeil Q. McDonald, Stefan M. KastOliver GautschiRoman K. ThomasMartin L. Sos. (2017) Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors. Science Translational Medicine 9:394.
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Saoirse O. Dolly, Dearbhaile C. Collins, Raghav Sundar, Sanjay Popat & Timothy A. Yap. (2017) Advances in the Development of Molecularly Targeted Agents in Non-Small-Cell Lung Cancer. Drugs 77:8, pages 813-827.
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Mei Han, Shan Li, Jing Ai, Rong Sheng, Yongzhou Hu, Youhong Hu & Meiyu Geng. (2016) Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 26:23, pages 5679-5684.
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Louise A Moyle, Eric Blanc, Oihane Jaka, Johanna Prueller, Christopher RS Banerji, Francesco Saverio Tedesco, Stephen DR Harridge, Robert D Knight & Peter S Zammit. (2016) Ret function in muscle stem cells points to tyrosine kinase inhibitor therapy for facioscapulohumeral muscular dystrophy. eLife 5.
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Chen Lin, Shanshan Wang, Weiwei Xie, Rongliang Zheng, Yu Gan & Jianhua Chang. (2016) Apatinib inhibits cellular invasion and migration by fusion kinase KIF5B-RET via suppressing RET/Src signaling pathway. Oncotarget 7:37, pages 59236-59244.
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Sarah Levinson & Ross L. Cagan. (2016) Drosophila Cancer Models Identify Functional Differences between Ret Fusions. Cell Reports 16:11, pages 3052-3061.
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Balazs Jóri, Rick Kamps, Sofia Xanthoulea, Bert Delvoux, Marinus J. Blok, Koen K. Van de Vijver, Bart de Koning, Felicia Trups Oei, Carli M. Tops, Ernst J. M. Speel, Roy F. Kruitwagen, Encarna B. Gomez-Garcia & Andrea Romano. (2015) Germ-line variants identified by next generation sequencing in a panel of estrogen and cancer associated genes correlate with poor clinical outcome in Lynch syndrome patients. Oncotarget 6:38, pages 41108-41122.
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Henriette Franz, Holger Greschik, Dominica Willmann, Luka Ozretić, Cordula Annette Jilg, Eva Wardelmann, Manfred Jung, Reinhard Buettner & Roland Schüle. (2015) The histone code reader SPIN1 controls RET signaling in liposarcoma. Oncotarget 6:7, pages 4773-4789.
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Tianwei Zhang, Yachao Lu, Qingqing Ye, Meizhuo Zhang, Li Zheng, Xiaolu Yin, Paul Gavine, Zhongsheng Sun, Qunsheng Ji, Guanshan Zhu & Xinying Su. (2015) An evaluation and recommendation of the optimal methodologies to detect RET gene rearrangements in papillary thyroid carcinoma . Genes, Chromosomes and Cancer 54:3, pages 168-176.
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John P Alao, Sona Michlikova, Peter Dinér, Morten Grøtli & Per Sunnerhagen. (2014) Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer 14:1.
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Alona Zer & Natasha Leighl. (2014) Promising Targets and Current Clinical Trials in Metastatic Non-Squamous NSCLC. Frontiers in Oncology 4.
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I. Plaza-Menacho, L. Mologni & N.Q. McDonald. (2014) Mechanisms of RET signaling in cancer: Current and future implications for targeted therapy. Cellular Signalling 26:8, pages 1743-1752.
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Xin Ku, Stephanie Heinzlmeir, Dominic Helm, Guillaume Médard & Bernhard Kuster. (2014) New Affinity Probe Targeting VEGF Receptors for Kinase Inhibitor Selectivity Profiling by Chemical Proteomics. Journal of Proteome Research 13:5, pages 2445-2452.
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Ross A Okimoto & Trever G Bivona. (2014) Recent advances in personalized lung cancer medicine. Personalized Medicine 11:3, pages 309-321.
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Qi-Zheng Sun, Yong Xu, Jing-Jing Liu, Chun-Hui Zhang, Ze-Rong Wang, Ren-Lin Zheng, Wen-Jing Wang, Lin-Li Li & Sheng-Yong Yang. (2014) Structural modification of an EGFR inhibitor that showed weak off-target activity against RET leading to the discovery of a potent RET inhibitor. Molecular Diversity 18:2, pages 403-409.
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Lois M. Mulligan. (2014) RET revisited: expanding the oncogenic portfolio. Nature Reviews Cancer 14:3, pages 173-186.
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Alessia Lopergolo, Valentina Nicolini, Enrica Favini, Laura Dal Bo, Monica Tortoreto, Denis Cominetti, Marco Folini, Paola Perego, Vittoria Castiglioni, Eugenio Scanziani, Maria Grazia Borrello, Nadia Zaffaroni, Giuliana Cassinelli & Cinzia Lanzi. (2014) Synergistic Cooperation Between Sunitinib and Cisplatin Promotes Apoptotic Cell Death in Human Medullary Thyroid Cancer. The Journal of Clinical Endocrinology & Metabolism 99:2, pages 498-509.
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A. Mortlock, K. Foote, J. Kettle & B. Aquila. 2014. Reference Module in Chemistry, Molecular Sciences and Chemical Engineering. Reference Module in Chemistry, Molecular Sciences and Chemical Engineering.
Takashi Kohno, Koji Tsuta, Katsuya Tsuchihara, Takashi Nakaoku, Kiyotaka Yoh & Koichi Goto. (2013) RET fusion gene: Translation to personalized lung cancer therapy . Cancer Science 104:11, pages 1396-1400.
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Luca Mologni, Sara Redaelli, Andrea Morandi, Ivan Plaza-Menacho & Carlo Gambacorti-Passerini. (2013) Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase. Molecular and Cellular Endocrinology 377:1-2, pages 1-6.
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