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Literature DB >> 28911727

The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer.

Valentina De Falco¹, Francesca Carlomagno², Hong-Yu Li³, Massimo Santoro⁴.

Abstract

RET receptor tyrosine kinase acts as a mutated oncogenic driver in several human malignancies and it is over-expressed in other cancers. Small molecule compounds with RET tyrosine kinase inhibitory activity are being investigated for the targeted treatment of these malignancies. Multi-targeted compounds with RET inhibitory concentration in the nanomolar range have entered clinical practice. This review summarizes mechanisms of RET oncogenic activity and properties of new compounds that, at the preclinical stage, have demonstrated promising anti-RET activity.

Entities: CellLine Chemical Disease Gene Mutation Species

Keywords: MEN; RET; TKI; targeted therapy; thyroid cancer; tyrosine kinase

Mesh：

Substances：

Year: 2017 PMID： 28911727 PMCID： PMC5624797 DOI： 10.1016/j.beem.2017.04.013

Source DB: PubMed Journal: Best Pract Res Clin Endocrinol Metab ISSN： 1521-690X Impact factor: 4.690

125 in total

1. RET inhibitors for patients with RET fusion-positive and RET wild-type non-small-cell lung cancer.

Authors: Rafael Rosell; Niki Karachaliou
Journal: Lancet Oncol Date: 2016-11-04 Impact factor: 41.316

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Authors: M Takahashi; J Ritz; G M Cooper
Journal: Cell Date: 1985-09 Impact factor: 41.582

Review 3. Revised American Thyroid Association guidelines for the management of medullary thyroid carcinoma.

Authors: Samuel A Wells; Sylvia L Asa; Henning Dralle; Rossella Elisei; Douglas B Evans; Robert F Gagel; Nancy Lee; Andreas Machens; Jeffrey F Moley; Furio Pacini; Friedhelm Raue; Karin Frank-Raue; Bruce Robinson; M Sara Rosenthal; Massimo Santoro; Martin Schlumberger; Manisha Shah; Steven G Waguespack
Journal: Thyroid Date: 2015-06 Impact factor: 6.568

4. Alectinib shows potent antitumor activity against RET-rearranged non-small cell lung cancer.

Authors: Tatsushi Kodama; Toshiyuki Tsukaguchi; Yasuko Satoh; Miyuki Yoshida; Yoshiaki Watanabe; Osamu Kondoh; Hiroshi Sakamoto
Journal: Mol Cancer Ther Date: 2014-10-27 Impact factor: 6.261

5. Oncogenic RET kinase domain mutations perturb the autophosphorylation trajectory by enhancing substrate presentation in trans.

Authors: Iván Plaza-Menacho; Karin Barnouin; Kerry Goodman; Rubén J Martínez-Torres; Annabel Borg; Judith Murray-Rust; Stephane Mouilleron; Phillip Knowles; Neil Q McDonald
Journal: Mol Cell Date: 2014-02-20 Impact factor: 17.970

6. Vandetanib in pretreated patients with advanced non-small cell lung cancer-harboring RET rearrangement: a phase II clinical trial.

Authors: S-H Lee; J-K Lee; M-J Ahn; D-W Kim; J-M Sun; B Keam; T M Kim; D S Heo; J S Ahn; Y-L Choi; H-S Min; Y K Jeon; K Park
Journal: Ann Oncol Date: 2017-02-01 Impact factor: 32.976

7. Design, Synthesis and Inhibitory Activity of Photoswitchable RET Kinase Inhibitors.

Authors: Rubén Ferreira; Jesper R Nilsson; Carlos Solano; Joakim Andréasson; Morten Grøtli
Journal: Sci Rep Date: 2015-05-06 Impact factor: 4.379

Review 8. Landscape of gene fusions in epithelial cancers: seq and ye shall find.

Authors: Chandan Kumar-Sinha; Shanker Kalyana-Sundaram; Arul M Chinnaiyan
Journal: Genome Med Date: 2015-12-18 Impact factor: 11.117

9. RET Functions as a Dual-Specificity Kinase that Requires Allosteric Inputs from Juxtamembrane Elements.

Authors: Iván Plaza-Menacho; Karin Barnouin; Rachael Barry; Annabel Borg; Mariam Orme; Rakhee Chauhan; Stephane Mouilleron; Rubén J Martínez-Torres; Pascal Meier; Neil Q McDonald
Journal: Cell Rep Date: 2016-12-20 Impact factor: 9.423

10. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.

Authors: Scott M Wilhelm; Christopher Carter; Liya Tang; Dean Wilkie; Angela McNabola; Hong Rong; Charles Chen; Xiaomei Zhang; Patrick Vincent; Mark McHugh; Yichen Cao; Jaleel Shujath; Susan Gawlak; Deepa Eveleigh; Bruce Rowley; Li Liu; Lila Adnane; Mark Lynch; Daniel Auclair; Ian Taylor; Rich Gedrich; Andrei Voznesensky; Bernd Riedl; Leonard E Post; Gideon Bollag; Pamela A Trail
Journal: Cancer Res Date: 2004-10-01 Impact factor: 13.312

13 in total

Review 1. Evolution of Our Understanding of the Hyperparathyroid Syndromes: A Historical Perspective.

Authors: Stephen J Marx; David Goltzman
Journal: J Bone Miner Res Date: 2018-12-10 Impact factor: 6.741

Review 2. RET kinase inhibitors for RET-altered thyroid cancers.

Authors: Danica M Vodopivec; Mimi I Hu
Journal: Ther Adv Med Oncol Date: 2022-06-21 Impact factor: 5.485

Review 3. The importance of the RET gene in thyroid cancer and therapeutic implications.

Authors: Domenico Salvatore; Massimo Santoro; Martin Schlumberger
Journal: Nat Rev Endocrinol Date: 2021-02-18 Impact factor: 43.330

4. Biallelic variants in genes previously associated with dominant inheritance: CACNA1A, RET and SLC20A2.

Authors: A Arteche-López; M I Álvarez-Mora; M T Sánchez Calvin; J M Lezana Rosales; C Palma Milla; M J Gómez Rodríguez; I Gomez Manjón; A Blázquez; A Juarez Rufián; P Ramos Gómez; O Sierra Tomillo; I Hidalgo Mayoral; R Pérez de la Fuente; I J Posada Rodríguez; L I González Granado; Miguel A Martin; J F Quesada-Espinosa; M Moreno-García
Journal: Eur J Hum Genet Date: 2021-07-15 Impact factor: 5.351

Review 5. Metabolic Reprogramming in Thyroid Carcinoma.

Authors: Raquel Guimaraes Coelho; Rodrigo S Fortunato; Denise P Carvalho
Journal: Front Oncol Date: 2018-03-23 Impact factor: 6.244

Review 6. RET Gene Fusions in Malignancies of the Thyroid and Other Tissues.

Authors: Massimo Santoro; Marialuisa Moccia; Giorgia Federico; Francesca Carlomagno
Journal: Genes (Basel) Date: 2020-04-15 Impact factor: 4.096

7. Molecular Modelling Studies on Pyrazole Derivatives for the Design of Potent Rearranged during Transfection Kinase Inhibitors.

Authors: Swapnil P Bhujbal; Seketoulie Keretsu; Seung Joo Cho
Journal: Molecules Date: 2021-01-28 Impact factor: 4.411