Home LiteratureArticle Details
PMID: 22286373 Published · ppublish English Journal Article Review

RET TKI: potential role in thyroid cancers.

Current oncology reports ·Vol. 14 ·No. 2 ·2012-04-00 ·Pages 97-104

Antonelli A, Fallahi P, Ferrari SM, Mancusi C, Colaci M, Santarpia L, Ferri C

Abstract

The increasing incidence of thyroid cancer is associated with a higher number of advanced disease characterized by the loss of cancer differentiation and metastatic spread. The knowledge of the molecular pathways involved in the pathogenesis of thyroid cancer has made possible the development of new therapeutic drugs able to blockade the oncogenic kinases (RET/PTC) or signaling kinases (vascular endothelial growth factor receptor [VEGFR]) involved in cellular growth and proliferation. Some clinical trials have been conducted showing the ability of targeted therapies able to inhibit RET(sorafenib, imatinib, vandetanib) in stabilizing the course of the disease. The aim of the introduction of these targeted therapies is to extend life duration assuring a good quality of life; however, further studies are needed to reach these goals.

MeSH Terms
Antineoplastic Agents/therapeutic use Carcinoma, Medullary/drug therapy Carcinoma, Papillary/drug therapy Humans Molecular Targeted Therapy/methods Proto-Oncogene Proteins c-ret/antagonists & inhibitors Receptor Protein-Tyrosine Kinases/antagonists & inhibitors Thyroid Neoplasms/drug therapy
Chemicals
Antineoplastic Agents Proto-Oncogene Proteins c-ret Receptor Protein-Tyrosine Kinases
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Antonelli Alessandro
Department of Internal Medicine, University of Pisa, School of Medicine, Via Roma 67, 56100 Pisa, Italy. alessandro.antonelli@med.unipi.it
Fallahi Poupak
Ferrari Silvia Martina
Mancusi Caterina
Colaci Michele
Santarpia Libero
Ferri Clodoveo
References (66)
66 references, click to expand
  1. Beneficial effects of sorafenib on tumor progression, but not on radioiodine uptake, in patients with differentiated thyroid carcinoma.
    Eur J Endocrinol. 2009 Dec;161(6):923-31 PMID: 19773371
  2. Cellular effects and antitumor activity of RET inhibitor RPI-1 on MEN2A-associated medullary thyroid carcinoma.
    J Natl Cancer Inst. 2004 Jul 7;96(13):1006-14 PMID: 15240784
  3. The Ret receptor protein tyrosine kinase associates with the SH2-containing adapter protein Grb10.
    J Biol Chem. 1995 Sep 15;270(37):21461-3 PMID: 7665556
  4. Distinct pattern of ret oncogene rearrangements in morphological variants of radiation-induced and sporadic thyroid papillary carcinomas in children.
    Cancer Res. 1997 May 1;57(9):1690-4 PMID: 9135009
  5. Primary cell cultures from anaplastic thyroid cancer obtained by fine-needle aspiration used for chemosensitivity tests.
    Clin Endocrinol (Oxf). 2008 Jul;69(1):148-52 PMID: 18194485
  6. BRAF mediates RET/PTC-induced mitogen-activated protein kinase activation in thyroid cells: functional support for requirement of the RET/PTC-RAS-BRAF pathway in papillary thyroid carcinogenesis.
    Endocrinology. 2006 Feb;147(2):1014-9 PMID: 16254036
  7. A novel RET inhibitor with potent efficacy against medullary thyroid cancer in vivo.
    Surgery. 2010 Dec;148(6):1228-36; discussion 1236 PMID: 21134556
  8. Mechanisms of Disease: cancer targeting and the impact of oncogenic RET for medullary thyroid carcinoma therapy.
    Nat Clin Pract Oncol. 2006 Oct;3(10):564-74 PMID: 17019434
  9. Hirschsprung's disease in a family with multiple endocrine neoplasia type 2.
    J Pediatr Gastroenterol Nutr. 1982;1(4):603-7 PMID: 6136579
  10. Development of thyroid papillary carcinomas secondary to tissue-specific expression of the RET/PTC1 oncogene in transgenic mice.
    Oncogene. 1996 Apr 18;12(8):1821-6 PMID: 8622903
  11. Dedifferentiated thyroid cancer: a therapeutic challenge.
    Biomed Pharmacother. 2008 Oct;62(8):559-63 PMID: 18725177
  12. Disabling Abl-perspectives on Abl kinase regulation and cancer therapeutics.
    Cancer Cell. 2002 Feb;1(1):13-5 PMID: 12086882
  13. RET tyrosine kinase signaling in development and cancer.
    Cytokine Growth Factor Rev. 2005 Aug-Oct;16(4-5):441-67 PMID: 15982921
  14. Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine (PP2).
    J Clin Endocrinol Metab. 2003 Apr;88(4):1897-902 PMID: 12679489
  15. Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer.
    J Clin Oncol. 2010 Feb 10;28(5):767-72 PMID: 20065189
  16. Therapeutic potential of novel selective-spectrum kinase inhibitors in oncology.
    Expert Opin Investig Drugs. 2008 Jul;17(7):1013-28 PMID: 18549338
  17. Multiple mucosal neuromata with endocrine tumours: a syndrome allied to von Recklinghausen's disease.
    J Pathol Bacteriol. 1966 Jan;91(1):71-80 PMID: 4957444
  18. Lobectomy versus total thyroidectomy in children with post-Chernobyl thyroid cancer: a 15 year follow-up.
    Endocrine. 2011 Dec;40(3):432-6 PMID: 21698517
  19. Thyroid carcinoma.
    Curr Opin Oncol. 2006 Jan;18(1):30-5 PMID: 16357561
  20. Increasing incidence of thyroid cancer in the United States, 1973-2002.
    JAMA. 2006 May 10;295(18):2164-7 PMID: 16684987
  21. Familial medullary thyroid carcinoma without associated endocrinopathies: a distinct clinical entity.
    Br J Surg. 1986 Apr;73(4):278-81 PMID: 3697657
  22. Roles of trk family neurotrophin receptors in medullary thyroid carcinoma development and progression.
    Proc Natl Acad Sci U S A. 1999 Apr 13;96(8):4540-5 PMID: 10200298
  23. PP1 inhibitor induces degradation of RETMEN2A and RETMEN2B oncoproteins through proteosomal targeting.
    Cancer Res. 2003 May 1;63(9):2234-43 PMID: 12727845
  24. Growth factor receptors expression in anaplastic thyroid carcinoma: potential markers for therapeutic stratification.
    Hum Pathol. 2008 Jan;39(1):15-20 PMID: 17949783
  25. Methods and goals for the use of in vitro and in vivo chemosensitivity testing.
    Mol Biotechnol. 2007 Feb;35(2):185-97 PMID: 17435285
  26. The ret/PTC mutations are common in sporadic papillary thyroid carcinoma of children and young adults.
    J Clin Endocrinol Metab. 2000 Mar;85(3):1170-5 PMID: 10720057
  27. The physical map of the human RET proto-oncogene.
    Oncogene. 1995 Nov 2;11(9):1737-43 PMID: 7478601
  28. ZD6474, an orally available inhibitor of KDR tyrosine kinase activity, efficiently blocks oncogenic RET kinases.
    Cancer Res. 2002 Dec 15;62(24):7284-90 PMID: 12499271
  29. Evaluation of the sensitivity to chemotherapeutics or thiazolidinediones of primary anaplastic thyroid cancer cells obtained by fine-needle aspiration.
    Eur J Endocrinol. 2008 Sep;159(3):283-91 PMID: 18583391
  30. Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer.
    J Clin Oncol. 2010 May 10;28(14):2323-30 PMID: 20368568
  31. Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer.
    J Clin Oncol. 2011 Jul 1;29(19):2660-6 PMID: 21606412
  32. Epidemiologic and clinical evaluation of thyroid cancer in children from the Gomel region (Belarus).
    World J Surg. 1996 Sep;20(7):867-71 PMID: 8678964
  33. RET/PTC-induced cell growth is mediated in part by epidermal growth factor receptor (EGFR) activation: evidence for molecular and functional interactions between RET and EGFR.
    Cancer Res. 2008 Jun 1;68(11):4183-91 PMID: 18519677
  34. Current concepts in RET-related genetics, signaling and therapeutics.
    Trends Genet. 2006 Nov;22(11):627-36 PMID: 16979782
  35. A phase II trial of imatinib therapy for metastatic medullary thyroid carcinoma.
    J Clin Endocrinol Metab. 2007 Sep;92(9):3466-9 PMID: 17579194
  36. RET as a diagnostic and therapeutic target in sporadic and hereditary endocrine tumors.
    Endocr Rev. 2006 Aug;27(5):535-60 PMID: 16849421
  37. Molecular characterization of RET/PTC3; a novel rearranged version of the RETproto-oncogene in a human thyroid papillary carcinoma.
    Oncogene. 1994 Feb;9(2):509-16 PMID: 8290261
  38. Multiple endocrine neoplasia type 2a associated with cutaneous lichen amyloidosis.
    Ann Intern Med. 1989 Nov 15;111(10):802-6 PMID: 2573304
  39. Thiazolidinediones and antiblastics in primary human anaplastic thyroid cancer cells.
    Clin Endocrinol (Oxf). 2009 Jun;70(6):946-53 PMID: 18785992
  40. Molecular genetics and diagnosis of thyroid cancer.
    Nat Rev Endocrinol. 2011 Aug 30;7(10):569-80 PMID: 21878896
  41. Tyrosines 1015 and 1062 are in vivo autophosphorylation sites in ret and ret-derived oncoproteins.
    J Clin Endocrinol Metab. 2000 Oct;85(10):3898-907 PMID: 11061555
  42. The effects of four different tyrosine kinase inhibitors on medullary and papillary thyroid cancer cells.
    J Clin Endocrinol Metab. 2011 Jun;96(6):E991-5 PMID: 21470995
  43. Phase II trial of sorafenib in metastatic thyroid cancer.
    J Clin Oncol. 2009 Apr 1;27(10):1675-84 PMID: 19255327
  44. Increasing world incidence of thyroid cancer: increased detection or higher radiation exposure?
    Hormones (Athens). 2010 Apr-Jun;9(2):103-8 PMID: 20687393
  45. Genetic alterations in the RAS/RAF/mitogen-activated protein kinase and phosphatidylinositol 3-kinase/Akt signaling pathways in the follicular variant of papillary thyroid carcinoma.
    Cancer. 2010 Jun 15;116(12):2974-83 PMID: 20564403
  46. Vandetanib: first global approval.
    Drugs. 2011 Jul 9;71(10):1355-65 PMID: 21770481
  47. Dysregulated RET signaling in thyroid cancer.
    Endocrinol Metab Clin North Am. 2008 Jun;37(2):363-74, viii PMID: 18502331
  48. Vandetanib (100 mg) in patients with locally advanced or metastatic hereditary medullary thyroid cancer.
    J Clin Endocrinol Metab. 2010 Jun;95(6):2664-71 PMID: 20371662
  49. Tyrosine kinases as targets for cancer therapy.
    N Engl J Med. 2005 Jul 14;353(2):172-87 PMID: 16014887
  50. Kinase inhibitors for refractory thyroid cancers.
    Lancet Oncol. 2010 Oct;11(10):912-3 PMID: 20851683
  51. Repair by Src kinase of function-impaired RET with multiple endocrine neoplasia type 2A mutation with substitutions of tyrosines in the COOH-terminal kinase domain for phenylalanine.
    Cancer Res. 2002 Apr 15;62(8):2414-22 PMID: 11956105
  52. Novel pyrazolopyrimidine derivatives as tyrosine kinase inhibitors with antitumoral activity in vitro and in vivo in papillary dedifferentiated thyroid cancer.
    J Clin Endocrinol Metab. 2011 Feb;96(2):E288-96 PMID: 21147882
  53. Targeted therapy of thyroid cancer.
    Biochem Pharmacol. 2010 Sep 1;80(5):592-601 PMID: 20471374
  54. Endocrine effects of the tyrosine kinase inhibitor vandetanib in patients treated for thyroid cancer.
    J Clin Endocrinol Metab. 2011 Sep;96(9):2741-9 PMID: 21715537
  55. CEP-701 and CEP-751 inhibit constitutively activated RET tyrosine kinase activity and block medullary thyroid carcinoma cell growth.
    Cancer Res. 2003 Sep 1;63(17):5559-63 PMID: 14500395
  56. Epidermal growth factor receptor as a therapeutic target in human thyroid carcinoma: mutational and functional analysis.
    J Clin Endocrinol Metab. 2006 Sep;91(9):3662-6 PMID: 16822827
  57. Medullary thyroid cancer.
    Curr Treat Options Oncol. 2000 Oct;1(4):359-67 PMID: 12057161
  58. Phase II trial of sorafenib in advanced thyroid cancer.
    J Clin Oncol. 2008 Oct 10;26(29):4714-9 PMID: 18541894
  59. Rationale and design of decision: a double-blind, randomized, placebo-controlled phase III trial evaluating the efficacy and safety of sorafenib in patients with locally advanced or metastatic radioactive iodine (RAI)-refractory, differentiated thyroid cancer.
    BMC Cancer. 2011 Aug 11;11:349 PMID: 21834960
  60. Molecular modeling of the extracellular domain of the RET receptor tyrosine kinase reveals multiple cadherin-like domains and a calcium-binding site.
    J Biol Chem. 2001 Sep 21;276(38):35808-17 PMID: 11445581
  61. A National Cancer Data Base report on 53,856 cases of thyroid carcinoma treated in the U.S., 1985-1995 [see commetns].
    Cancer. 1998 Dec 15;83(12):2638-48 PMID: 9874472
  62. New targeted molecular therapies for dedifferentiated thyroid cancer.
    J Oncol. 2010;2010:921682 PMID: 20628483
  63. Expression of vascular endothelial growth factor (VEGF) and its receptors in thyroid carcinomas of follicular origin: a potential autocrine loop.
    Eur J Endocrinol. 2005 Nov;153(5):701-9 PMID: 16260429
  64. Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer.
    J Clin Oncol. 2009 Aug 10;27(23):3794-801 PMID: 19564535
  65. Cancer statistics, 2007.
    CA Cancer J Clin. 2007 Jan-Feb;57(1):43-66 PMID: 17237035
  66. The RET/PTC3 oncogene: metastatic solid-type papillary carcinomas in murine thyroids.
    Cancer Res. 1998 Dec 1;58(23):5523-8 PMID: 9850089
Article Info
Journal
Current oncology reports
Abbr.
Curr Oncol Rep
ISSN
1534-6269
Published
2012-04-00
Pages
97-104
Language
English
Region
United States
NLM ID
100888967
Subset
IM
Analysis Services
Analysis Services

Contact

No. 2 Wenbo Road, Zhangqiu District, Jinan, Shandong

Qilu Normal University · Genelibs Bioinformatics Lab

750 Shunhua Rd, Jinan

2F, Bldg F, University Science Park

Tel: 0531-88819269

WeChat Official Account

Follow our WeChat subscription account for real-time updates and the latest in medical and biological research.


Business Email

E-mail: product@genelibs.com