Literature DB >> 32292556

Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase.

Rebecca Newton1, Bohdan Waszkowycz1, Chitra Seewooruthun2, Daniel Burschowsky2, Mark Richards3, Samantha Hitchin1, Habiba Begum1, Amanda Watson1, Eleanor French1, Niall Hamilton1, Stuart Jones1, Li-Ying Lin4, Ian Waddell1, Aude Echalier2, Richard Bayliss3, Allan M Jordan1, Donald Ogilvie1.   

Abstract

A combination of focused library and virtual screening, hit expansion, and rational design has resulted in the development of a series of inhibitors of RETV804M kinase, the anticipated drug-resistant mutant of RET kinase. These agents do not inhibit the wild type (wt) isoforms of RET or KDR and therefore offer a potential adjunct to RET inhibitors currently undergoing clinical evaluation.
Copyright © 2020 American Chemical Society.

Entities:  

Year:  2020        PMID： 32292556      PMCID： PMC7153033          DOI： 10.1021/acsmedchemlett.9b00615

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  14 in total

1.  Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.

Authors:  Dennis Plenker; Maximilian Riedel; Johannes Brägelmann; Marcel A Dammert; Rakhee Chauhan; Phillip P Knowles; Carina Lorenz; Marina Keul; Mike Bührmann; Oliver Pagel; Verena Tischler; Andreas H Scheel; Daniel Schütte; Yanrui Song; Justina Stark; Florian Mrugalla; Yannic Alber; André Richters; Julian Engel; Frauke Leenders; Johannes M Heuckmann; Jürgen Wolf; Joachim Diebold; Georg Pall; Martin Peifer; Maarten Aerts; Kris Gevaert; René P Zahedi; Reinhard Buettner; Kevan M Shokat; Neil Q McDonald; Stefan M Kast; Oliver Gautschi; Roman K Thomas; Martin L Sos
Journal:  Sci Transl Med       Date:  2017-06-14       Impact factor: 17.956

2.  Precision Targeted Therapy with BLU-667 for RET-Driven Cancers.

Authors:  Vivek Subbiah; Justin F Gainor; Rami Rahal; Jason D Brubaker; Joseph L Kim; Michelle Maynard; Wei Hu; Qiongfang Cao; Michael P Sheets; Douglas Wilson; Kevin J Wilson; Lucian DiPietro; Paul Fleming; Michael Palmer; Mimi I Hu; Lori Wirth; Marcia S Brose; Sai-Hong Ignatius Ou; Matthew Taylor; Elena Garralda; Stephen Miller; Beni Wolf; Christoph Lengauer; Timothy Guzi; Erica K Evans
Journal:  Cancer Discov       Date:  2018-04-15       Impact factor: 39.397

3.  Identification of new ALK and RET gene fusions from colorectal and lung cancer biopsies.

Authors:  Doron Lipson; Marzia Capelletti; Roman Yelensky; Geoff Otto; Alex Parker; Mirna Jarosz; John A Curran; Sohail Balasubramanian; Troy Bloom; Kristina W Brennan; Amy Donahue; Sean R Downing; Garrett M Frampton; Lazaro Garcia; Frank Juhn; Kathy C Mitchell; Emily White; Jared White; Zac Zwirko; Tamar Peretz; Hovav Nechushtan; Lior Soussan-Gutman; Jhingook Kim; Hidefumi Sasaki; Hyeong Ryul Kim; Seung-il Park; Dalia Ercan; Christine E Sheehan; Jeffrey S Ross; Maureen T Cronin; Pasi A Jänne; Philip J Stephens
Journal:  Nat Med       Date:  2012-02-12       Impact factor: 53.440

4.  RET, ROS1 and ALK fusions in lung cancer.

Authors:  Kengo Takeuchi; Manabu Soda; Yuki Togashi; Ritsuro Suzuki; Seiji Sakata; Satoko Hatano; Reimi Asaka; Wakako Hamanaka; Hironori Ninomiya; Hirofumi Uehara; Young Lim Choi; Yukitoshi Satoh; Sakae Okumura; Ken Nakagawa; Hiroyuki Mano; Yuichi Ishikawa
Journal:  Nat Med       Date:  2012-02-12       Impact factor: 53.440

Review 5.  Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer.

Authors:  Chee-Seng Tan; David Gilligan; Simon Pacey
Journal:  Lancet Oncol       Date:  2015-09       Impact factor: 41.316

6.  A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.

Authors:  Hojong Yoon; Yeonui Kwak; Seunghye Choi; Hanna Cho; Nam Doo Kim; Taebo Sim
Journal:  J Med Chem       Date:  2015-12-22       Impact factor: 7.446

7.  Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial.

Authors:  Alexander Drilon; Natasha Rekhtman; Maria Arcila; Lu Wang; Andy Ni; Melanie Albano; Martine Van Voorthuysen; Romel Somwar; Roger S Smith; Joseph Montecalvo; Andrew Plodkowski; Michelle S Ginsberg; Gregory J Riely; Charles M Rudin; Marc Ladanyi; Mark G Kris
Journal:  Lancet Oncol       Date:  2016-11-04       Impact factor: 41.316

8.  Selective RET kinase inhibition for patients with RET-altered cancers.

Authors:  V Subbiah; V Velcheti; B B Tuch; K Ebata; N L Busaidy; M E Cabanillas; L J Wirth; S Stock; S Smith; V Lauriault; S Corsi-Travali; D Henry; M Burkard; R Hamor; K Bouhana; S Winski; R D Wallace; D Hartley; S Rhodes; M Reddy; B J Brandhuber; S Andrews; S M Rothenberg; A Drilon
Journal:  Ann Oncol       Date:  2018-08-01       Impact factor: 32.976

9.  Disease associated mutations at valine 804 in the RET receptor tyrosine kinase confer resistance to selective kinase inhibitors.

Authors:  Francesca Carlomagno; Teresa Guida; Suresh Anaganti; Giancarlo Vecchio; Alfredo Fusco; Anderson J Ryan; Marc Billaud; Massimo Santoro
Journal:  Oncogene       Date:  2004-08-12       Impact factor: 9.867

10.  Vandetanib in patients with previously treated RET-rearranged advanced non-small-cell lung cancer (LURET): an open-label, multicentre phase 2 trial.

Authors:  Kiyotaka Yoh; Takashi Seto; Miyako Satouchi; Makoto Nishio; Noboru Yamamoto; Haruyasu Murakami; Naoyuki Nogami; Shingo Matsumoto; Takashi Kohno; Koji Tsuta; Katsuya Tsuchihara; Genichiro Ishii; Shogo Nomura; Akihiro Sato; Atsushi Ohtsu; Yuichiro Ohe; Koichi Goto
Journal:  Lancet Respir Med       Date:  2016-11-04       Impact factor: 30.700
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  1 in total

Review 1.  Precision oncology for RET-related tumors.

Authors:  Antonella Verrienti; Giorgio Grani; Marialuisa Sponziello; Valeria Pecce; Giuseppe Damante; Cosimo Durante; Diego Russo; Sebastiano Filetti
Journal:  Front Oncol       Date:  2022-08-24       Impact factor: 5.738
  1 in total

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