Screening for EGFR and AKT dual-target inhibitors

Author:

Yang Han-Yu1,Zhang Zhi-Wei1,Yu Jie1,Liu Cong-Jin1,Lu Wen-Cai1

Affiliation:

1. Qingdao University

Abstract

Abstract Epidermal growth factor EGFR is an important target for non-small cell lung (NSCL) cancer, and inhibitors of AKT protein has been used in many cancer treatments including NSCL cancer. Therefore, screening small molecular inhibitors targeting both EGFR and AKT can help for cancer treatment. In this study, we screened Traditional Chinese Medicine on Immune-Oncology (TCMIO) database for potential natural product inhibitors that can target both EGFR and AKT using ligand-based pharmacophore model, molecular docking, and MD simulations methods. The human endogenous database HMDB was also screened. It was found that TCMIO89212, TCMIO90156 and TCMIO98874 from the TCMIO database had large binding free energies with EGFR and AKT. In the HMDB database, kinetin-7-N-glucoside was found to have ability to bind to EGFR and AKT. These results may provide valuable information for further experimental studies.

Publisher

Research Square Platform LLC

Reference57 articles.

1. Broekman, F. (2011). Tyrosine kinase inhibitors: multi-targeted or single-targeted? World journal of clinical oncology, 2(2), 80–93. Seshacharyulu P, Ponnusamy MP, Haridas D, Jain M, Ganti AK, Batra SK. Targeting the EGFR signaling pathway in cancer therapy. Expert Opin Ther Targets. 2012 Jan;16(1):15–31. doi: 10.1517/14728222.2011.648617. Epub 2012 Jan 12. PMID: 22239438; PMCID: PMC3291787.

2. Harari PM. Epidermal growth factor receptor inhibition strategies in oncology. Endocr Relat Cancer. 2004 Dec;11(4):689–708. doi: 10.1677/erc.1.00600. PMID: 15613446.

3. Targeting the EGFR signaling pathway in cancer therapy;Seshacharyulu P;Expert Opin Ther Targets.,2012

4. Epidermal growth factor receptor targeting in cancer: a review of trends and strategies;Yewale C;Biomaterials.,2013

5. Jin Zhang,Jin-Sen Tang.Ergosta-7,22-diene-2β,3α,9α-triol (EGDT) from Ganoderma lucidum inhibits nasopharyngeal carcinoma cells by blocking EGFR signaling pathway[J];Chinese Herbal Medicines,2018

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3