Conformational landscape of the epidermal growth factor receptor kinase reveals a mutant specific allosteric pocket-Reference-Cited by-同舟云学术

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Conformational landscape of the epidermal growth factor receptor kinase reveals a mutant specific allosteric pocket

Published:2018 Issue:23 Volume:9 Page:5212-5222
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Kannan Srinivasaraghavan¹²³^ORCID,Venkatachalam Gireedhar⁴²⁵,Lim Hong Hwa⁴²⁵⁶⁷,Surana Uttam⁴²⁵⁶⁷,Verma Chandra¹²³⁸⁹

Affiliation:

1. Bioinformatics Institute (BII)

2. A*STAR

3. Singapore 138671

4. Institute of Molecular and Cell Biology (IMCB)

5. Singapore 138673

6. Bioprocessing Technology Institute

7. Singapore 138668

8. School of Biological Sciences

9. Nanyang Technological University

Abstract

An oncogenic mutant-specific druggable allosteric pocket captured by MD simulations.

Funder

Agency for Science, Technology and Research

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2018/SC/C8SC01262H

Reference34 articles.

1. The International Association for the Study of Lung Cancer Consensus Statement on Optimizing Management of EGFR Mutation–Positive Non–Small Cell Lung Cancer: Status in 2016

2. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

3. Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor Sensitivity

4. Kinetic Analysis of Epidermal Growth Factor Receptor Somatic Mutant Proteins Shows Increased Sensitivity to the Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, Erlotinib

5. AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer

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4. Synthesis and preclinical evaluation of [11C]EAI045 as a PET tracer for imaging tumors expressing mutated epidermal growth factor receptor;EJNMMI Research;2024-02-16

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