Literature DB >> 26819655

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer.

Julian Engel1, Jonas Lategahn1, Daniel Rauh1.   

Abstract

In the last five years, the detailed understanding of how to overcome T790M drug resistance in non-small cell lung cancer (NSCLC) has culminated in the development of a third-generation of covalent EGFR inhibitors with excellent clinical outcomes. However, the emergence of a newly discovered acquired drug resistance challenges the concept of small molecule targeted cancer therapy in NSCLC.

Entities:  

Year:  2015        PMID: 26819655      PMCID: PMC4716607          DOI: 10.1021/acsmedchemlett.5b00475

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


  11 in total

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3.  Rociletinib in EGFR-mutated non-small-cell lung cancer.

Authors:  Lecia V Sequist; Jean-Charles Soria; Jonathan W Goldman; Heather A Wakelee; Shirish M Gadgeel; Andrea Varga; Vassiliki Papadimitrakopoulou; Benjamin J Solomon; Geoffrey R Oxnard; Rafal Dziadziuszko; Dara L Aisner; Robert C Doebele; Cathy Galasso; Edward B Garon; Rebecca S Heist; Jennifer Logan; Joel W Neal; Melody A Mendenhall; Suzanne Nichols; Zofia Piotrowska; Antoinette J Wozniak; Mitch Raponi; Chris A Karlovich; Sarah Jaw-Tsai; Jeffrey Isaacson; Darrin Despain; Shannon L Matheny; Lindsey Rolfe; Andrew R Allen; D Ross Camidge
Journal:  N Engl J Med       Date:  2015-04-30       Impact factor: 91.245

4.  Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial.

Authors:  Vincent A Miller; Vera Hirsh; Jacques Cadranel; Yuh-Min Chen; Keunchil Park; Sang-We Kim; Caicun Zhou; Wu-Chou Su; Mengzhao Wang; Yan Sun; Dae Seog Heo; Lucio Crino; Eng-Huat Tan; Tsu-Yi Chao; Mehdi Shahidi; Xiuyu Julie Cong; Robert M Lorence; James Chih-Hsin Yang
Journal:  Lancet Oncol       Date:  2012-03-26       Impact factor: 41.316

Review 5.  Epidermal growth factor receptor mutations in lung cancer.

Authors:  Sreenath V Sharma; Daphne W Bell; Jeffrey Settleman; Daniel A Haber
Journal:  Nat Rev Cancer       Date:  2007-03       Impact factor: 60.716

6.  EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib.

Authors:  William Pao; Vincent Miller; Maureen Zakowski; Jennifer Doherty; Katerina Politi; Inderpal Sarkaria; Bhuvanesh Singh; Robert Heelan; Valerie Rusch; Lucinda Fulton; Elaine Mardis; Doris Kupfer; Richard Wilson; Mark Kris; Harold Varmus
Journal:  Proc Natl Acad Sci U S A       Date:  2004-08-25       Impact factor: 11.205

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Authors:  Helena A Yu; Maria E Arcila; Natasha Rekhtman; Camelia S Sima; Maureen F Zakowski; William Pao; Mark G Kris; Vincent A Miller; Marc Ladanyi; Gregory J Riely
Journal:  Clin Cancer Res       Date:  2013-03-07       Impact factor: 12.531

8.  BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.

Authors:  D Li; L Ambrogio; T Shimamura; S Kubo; M Takahashi; L R Chirieac; R F Padera; G I Shapiro; A Baum; F Himmelsbach; W J Rettig; M Meyerson; F Solca; H Greulich; K-K Wong
Journal:  Oncogene       Date:  2008-04-14       Impact factor: 9.867

9.  Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.

Authors:  Anja Michalczyk; Sabine Klüter; Haridas B Rode; Jeffrey R Simard; Christian Grütter; Matthias Rabiller; Daniel Rauh
Journal:  Bioorg Med Chem       Date:  2008-02-20       Impact factor: 3.641

10.  AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer.

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Journal:  N Engl J Med       Date:  2015-04-30       Impact factor: 91.245

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  17 in total

1.  A Near-IR Fluorescent Dasatinib Derivative That Localizes in Cancer Cells.

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3.  Capilliposide from Lysimachia capillipes inhibits AKT activation and restores gefitinib sensitivity in human non-small cell lung cancer cells with acquired gefitinib resistance.

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4.  Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.

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5.  Meeting Proceedings ICBS2016-Translating the Power of Chemical Biology to Clinical Advances.

Authors:  Yugo Kuriki; Toru Komatsu; Peter D Ycas; Sara K Coulup; Erick J Carlson; William C K Pomerantz
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Review 6.  Targeted protein degradation: A promise for undruggable proteins.

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7.  Development of Erasin: a chromone-based STAT3 inhibitor which induces apoptosis in Erlotinib-resistant lung cancer cells.

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Review 8.  Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology.

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Review 9.  Advanced new strategies for metastatic cancer treatment by therapeutic stem cells and oncolytic virotherapy.

Authors:  Geon-Tae Park; Kyung-Chul Choi
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10.  Partial response to carboplatin in an RRx-001 pretreated patient with EGFR-inhibitor-resistance and T790M-negative NSCLC.

Authors:  Corey A Carter; Bryan Oronsky; Scott Caroen; Jan Scicinski; Pedro Cabrales; Aiste Degesys; Christina Brzezniak
Journal:  Respir Med Case Rep       Date:  2016-04-24
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