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Advances in targeting EGFR allosteric site as anti-NSCLC therapy to overcome the drug resistance by Swastika Maity; K. Sreedhara Ranganath Pai; Yogendra Nayak is a Neuroscience article available to read on EtoBox.
What is Advances in targeting EGFR allosteric site as anti-NSCLC therapy to overcome the drug resistance about?
## Abstract ## Background The epidermal growth factor receptor (EGFR) inhibitors represent the first-line therapy regimen for non-small cell lung cancer (NSCLC). Most of these inhibitors target the ATP-site to stop the aggressive development of NSCLC. Stabilization of the ATP-binding on EGFR is difficult due to autophosphorylation of the EGFR domain. This leads to activation of nonintrinsic influence of the tumor microenvironment and expression of anti-apoptotic pathways and drug resistance. ## Methods The NSCLC related literature search was carried out using online databases such as Scopus, Web of Sciences, PubMed, Protein Data Bank and UniPort for the last ten years and selected articles are referred for discussion in this review. ## Results To overcome the problem of mutations in NSCLC, the allosteric site of EGFR was targeted, which shows significant therapeutic outcome without causing resistance. Compounds like EAI001, EAI045 JBJ-04-125-02, DDC4002 and a series of small molecules with an affinity towards the EGFR allosteric site are reported and are under the investigational stage. These compounds are categorized under fourth-generation anti-NSCLC agents. ## Conclusion Composi
Who reads Advances in targeting EGFR allosteric site as anti-NSCLC therapy to overcome the drug resistance?
It is typically read by researchers, students, and practitioners in Neuroscience.
- Author
- Swastika Maity; K. Sreedhara Ranganath Pai; Yogendra Nayak
- Publisher
- Springer Science and Business Media LLC
- Published
- 2020
- Language
- EN
- Field
- Neuroscience (Life Sciences)