Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade

F1000Research

Volumn 5, Issue , 2016, Pages

  Watson, Amanda J ^a   Hopkins, Gemma V ^a   Hitchin, Samantha ^a   Begum, Habiba ^a   Jones, Stuart ^a   Jordan, Allan ^a   Holt, Sarah ^a   Nikki March, H ^a   Newton, Rebecca ^a   Small, Helen ^a   Stowell, Alex ^a   Waddell, Ian D ^a   Waszkowycz, Bohdan ^a   Ogilvie, Donald J ^a  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN RET; PROTEIN TYROSINE KINASE INHIBITOR; QUINAZOLINE DERIVATIVE; RET INHIBITOR; UNCLASSIFIED DRUG; VANDETANIB;

ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG IDENTIFICATION; DRUG SCREENING; DRUG SELECTIVITY; ENZYME ASSAY; HEK293 CELL LINE; HUMAN; HUMAN CELL; IC50; VALIDATION PROCESS; WESTERN BLOTTING;

EID: 85010952920     PISSN: 20461402     EISSN: 1759796X     Source Type: Journal    
DOI: 10.12688/F1000RESEARCH.8724.2     Document Type: Article

References (33)

1. Newton R, Bowler KA, Burns EM, et al.: The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. Eur J Med Chem. 2016; 112: 20-32
2. Arighi E, Borrello MG, Sariola H: RET tyrosine kinase signaling in development and cancer. Cytokine Growth Factor Rev. 2005; 16(4-5): 441-467
3. Santoro M, Carlomagno F, Melillo RM, et al.: Dysfunction of the RET receptor in human cancer. Cell Mol Life Sci. 2004; 61(23): 2954-2964
4. Santoro M, Carlomagno F: Drug insight: Small-molecule inhibitors of protein kinases in the treatment of thyroid cancer. Nat Clin Pract Endocrinol Metab. 2006; 2(1): 42-52
5. Wells SA Jr, Santoro M: Targeting the RET pathway in thyroid cancer. Clin Cancer Res. 2009; 15(23): 7119-23
6. Elisei R, Cosci B, Romei C, et al.: Prognostic significance of somatic RET oncogene mutations in sporadic medullary thyroid cancer: a 10-year follow-up study. J Clin Endocrinol Metab. 2008; 93(3): 682-687
7. Ju YS, Lee WC, Shin JY, et al.: A transforming KIF5B and RET gene fusion in lung adenocarcinoma revealed from whole-genome and transcriptome sequencing. Genome Res. 2012; 22(3): 436-45
8. Kohno T, Ichikawa H, Totoki Y, et al.: KIF5B-RET fusions in lung adenocarcinoma. Nat Med. 2012; 18(3): 375-377
9. Takeuchi K, Soda M, Togashi Y, et al.: RET, ROS1 and ALK fusions in lung cancer. Nat Med. 2012; 18(3): 378-381
10. Lipson D, Capelletti M, Yelensky R, et al.: Identification of new ALK and RET gene fusions from colorectal and lung cancer biopsies. Nat Med. 2012; 18(3): 382-384
11. Drilon A, Wang L, Hasanovic A, et al.: Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas. Cancer Discov. 2013; 3(6): 630-635
12. Wells SA Jr, Robinson BG, Gagel RF, et al.: Vandetanib in patients with locally advanced or metastatic medullary thyroid cancer: a randomized, double-blind phase III trial. J Clin Oncol. 2012; 30(2): 134-141
13. Elisei R, Schlumberger MJ, Müller SP, et al.: Cabozantinib in progressive medullary thyroid cancer. J Clin Oncol. 2013; 31(29): 3639-3646
14. https://clinicaltrials.gov/(accessed February 2016)
15. Gautschi O, Zander T, Keller FA, et al.: A patient with lung adenocarcinoma and RET fusion treated with vandetanib. J Thorac Oncol. 2013; 8(5): e43-44
16. Suguwara M, Ly T, Hershman JM: Medullary thyroid cancer-current treatment strategy, novel therapies and perspectives for the future. Horm Cancer. 2012; 3(5-6): 218-226
17. Mulligan LM: RET revisited: expanding the oncogenic portfolio. Nat Rev Cancer. 2014; 14(3): 173-186
18. Song M: Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem. 2015; 58(9): 3672-3681
19. Schlumberger M, Jarzab B, Cabanillas ME, et al.: A Phase II Trial of the Multitargeted Tyrosine Kinase Inhibitor Lenvatinib (E7080) in Advanced Medullary Thyroid Cancer. Clin Cancer Res. 2016; 22(1): 44-53
20. De Falco V, Buonocore P, Muthu M, et al.: Ponatinib (AP24534) is a novel potent inhibitor of oncogenic RET mutants associated with thyroid cancer. J Clin Enocrinol Metab. 2013; 98(5): E811-E819
21. Kodama T, Tsukaguchi T, Satoh Y, et al.: Alectinib shows potent antitumor activity against RET-rearranged non-small cell lung cancer. Mol Cancer Ther. 2014; 13(12): 2910-2918
22. Alfano L, Guida T, Provitero L, et al.: RET is a heat shock protein 90 (HSP90) client protein and is knocked down upon HSP90 pharmacological block. J Clin Endocrinol Metab. 2010; 95(7): 3552-3557
23. Taipale M, Jarosz DF, Lindquist S: HSP90 at the hub of protein homeostasis: emerging mechanistic insights. Nat Rev Mol Cell Biol. 2010; 11(7): 515-528
24. Vichai V, Kirtikara K: Sulforhodamine B colorimetric assay for cytotoxicity screening. Nat Protoc. 2006; 1(3): 1112-1116
25. Rudolph J, Xiao Y, Pardi A, et al.: Slow inhibition and conformation selective properties of extracellular signal-regulated kinase 1 and 2 inhibitors. Biochemistry. 2015; 54(1): 22-31
26. Wu P, Nielsen TE, Clausen MH: FDA-approved small-molecule kinase inhibitors. Trends Pharmacol Sci. 2015; 36(7): 422-39
27. Knowles PP, Murray-Rust J, Kjaer S, et al.: Structure and chemical inhibition of the RET tyrosine kinase domain. J Biol Chem. 2006; 281(44): 33577-33587
28. Verbeek HH, Alves MM, de Groot JW, et al.: The effects of four different tyrosine kinase inhibitors on medullary and papillary thyroid cancer cells. J Clin Endocrinol Metab. 2011; 96(6): E991-5
29. Carlomagno F, Salvatore D, Santoro M, et al.: Point mutation of the RET proto-oncogene in the TT human medullary thyroid carcinoma cell line. Biochem Biophys Res Commun. 1995; 207(3): 1022-1028
30. Matsubara D, Kanai Y, Ishikawa S, et al.: Identification of CCDC6-RET fusion in the human lung adenocarcinoma cell line, LC-2/ad. J Thorac Oncol. 2012; 7(12): 1872-1876
31. Suzuki M, Makinoshima H, Matsumoto S, et al.: Identification of a lung adenocarcinoma cell line with CCDC6-RET fusion gene and the effect of RET inhibitors in vitro and in vivo. Cancer Sci. 2013; 104(7): 896-903
32. Sakamoto H, Tsukaguchi T, Hiroshima S, et al.: CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011; 19(5): 679-690
33. Watson AJ, Hopkins GV, Hitchin S, et al.: Dataset 1 in: identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade. F1000Research. 2016