Sakthivel, K M (2018) Targeting apoptosis by 1,2-diazole through regulation of EGFR, Bcl-2 and CDK-2 mediated signaling pathway in human non-small cell lung carcinoma A549 cells. Gene, 679. pp. 352-359.

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Abstract

Lung cancer is the leading cause of cancer deaths worldwide and non-small cell lung carcinoma (NSCLC), a
heterogeneous class of tumors, represents approximately 85% of all new lung cancer diagnosis. Conventional
treatment options have limited efficacy because most cases are in the advanced stage at the time of diagnosis.
The present study evaluates the anti-cancer activity of 1,2-diazole (pyrazole), a natural compound from mangrove plant Rhizophora apiculata (R.apiculata) on A549 lung carcinoma cells. In the present study the anti-cancer
mechanism of pyrazole, was examined by the expression level of proteins Epidermal growth factor receptor
(EGFR), Bcl-2-associated X protein (Bax), B-cell lymphoma-2 (Bcl-2) and Cyclin-dependent kinase-2 (CDK-2)
which are commonly associated with the cell signaling pathways that control cell survival and apoptosis, that
could facilitate to develop a novel target and effective treatment approach for patients with NSCLC. Pyrazole
significantly induced cell cycle arrest and initiated apoptosis through inhibition of downstream components of
EGFR tyrosine kinase pathway. Pyrazole disrupts the mitochondrial membrane potential and modulated the
protein levels of Bax and Bcl-2 which could probably lead to caspase-3 activation. Furthermore, Pyrazole suppresses the expression of CDK-2 resulting in cell cycle arrest at G1 phase and in the G1-S phase transition. Taken
together, the current study provides new insight in to the precise molecular mechanisms responsible for the anticancer activity of pyrazole in NSCLC, A549 cells. The study opens an avenue for development of a natural
compound as a potential therapeutic agent which could target cell signaling pathways to combat human NSCLC

Item Type: Article
Uncontrolled Keywords: 1,2-diazole Pyrazole Lung cancer Apoptosis Epidermal growth factor receptor Targeted gene therapy Non-small cell lung carcinoma
Depositing User: Mr Team Mosys
Date Deposited: 21 Jul 2022 04:18
Last Modified: 21 Jul 2022 04:18
URI: http://ir.psgcas.ac.in/id/eprint/1326

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