PMID- 29234489
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20201001
IS  - 1947-6019 (Print)
IS  - 1947-6027 (Electronic)
IS  - 1947-6019 (Linking)
VI  - 8
IP  - 9-10
DP  - 2017 Sep
TI  - Molecular insights: Suppression of EGFR and AKT activation by a small molecule in 
      non-small cell lung cancer.
PG  - 713-724
LID - 10.18632/genesandcancer.154 [doi]
AB  - Epidermal growth factor receptor (EGFR) activation events and the mammalian 
      target of rampamycin (mTOR) are considered important therapeutic targets in 
      alleviating cancer conditions. The current treatment paradigm has shifted to 
      personalized treatment strategies with tyrosine kinase inhibitors (TKIs) or 
      anaplastic lymphoma kinase (ALK) inhibitors, due to low survival rates in 
      non-small cell lung cancer (NSCLC) in terms of the prevailing platinum-based 
      therapy. In the present study, we examined the anticancer potential of Verrucarin 
      J (VJ), a small molecule, in NSCLC cell lines (H460 and A549). The small molecule 
      significantly inhibited cell growth, proliferation, colony forming ability, and 
      induced apoptosis in both lung cancer cell lines. The inhibitory effects on EGFR 
      (pEGFR -tyr1173) and AKT (pAKT Serine473) signaling, downregulates downstream 
      pro-survival signaling (mTOR and NF-kappaB) in cancer cell lines. In addition, VJ 
      abrogated invasive and migratory potential of A549 and H460 cells. We also 
      observed a downregulation of mesenchymal markers such as N-cadherin, Slug, 
      beta-catenin, and vimentin expression in both cell lines. Our results suggest that 
      VJ inhibited cancer cell growth and could be a potent molecule to inhibit EGFR 
      and AKT signaling in NSCLC.
FAU - Chandrasekaran, Balaji
AU  - Chandrasekaran B
AD  - Department of Urology, University of Louisville, Louisville, KY, USA.
FAU - Tyagi, Ashish
AU  - Tyagi A
AD  - Department of Urology, University of Louisville, Louisville, KY, USA.
FAU - Sharma, Arun K
AU  - Sharma AK
AD  - Department of Pharmacology, Penn State University, Hershey, PA, USA.
FAU - Cai, Lu
AU  - Cai L
AD  - Pediatrics Research Institute, The Department of Pediatrics of the University of 
      Louisville, Louisville, USA.
FAU - Ankem, Murali
AU  - Ankem M
AD  - Department of Urology, University of Louisville, Louisville, KY, USA.
FAU - Damodaran, Chendil
AU  - Damodaran C
AD  - Department of Urology, University of Louisville, Louisville, KY, USA.
LA  - eng
PT  - Journal Article
PL  - United States
TA  - Genes Cancer
JT  - Genes & cancer
JID - 101516546
PMC - PMC5724805
OTO - NOTNLM
OT  - AKT
OT  - EGFR
OT  - growth inhibition
OT  - lung cancer
COIS- CONFLICTS OF INTEREST The authors have no conflicts of interest to declare.
EDAT- 2017/12/14 06:00
MHDA- 2017/12/14 06:01
PMCR- 2017/09/01
CRDT- 2017/12/14 06:00
PHST- 2017/12/14 06:00 [entrez]
PHST- 2017/12/14 06:00 [pubmed]
PHST- 2017/12/14 06:01 [medline]
PHST- 2017/09/01 00:00 [pmc-release]
AID - 154 [pii]
AID - 10.18632/genesandcancer.154 [doi]
PST - ppublish
SO  - Genes Cancer. 2017 Sep;8(9-10):713-724. doi: 10.18632/genesandcancer.154.