Development of Cyclic Tetrapeptide as an EGFR Tyrosine Kinase Inhibitor Assayed by ELISA Experiment and Docking Study: A Novel Approach| Chapter 10 | Challenges and Advances in Pharmaceutical Research Vol. 2

The first objective of this project is to synthesize innovative cyclic peptides and test them as

Epidermal Growth Factor Tyrosine Kinase Inhibitor (EGFR-TKI) by Enzyme-Linked Immuno Sorbent

Assay (ELISA) experiment. The Cyclic Phe-Phe-Phe-Gly Tetrapeptide (CPTP) exhibited a strong IC50

of 55.6 nM while cyclic heptapeptides, μM level. The second objective is to compare by AutoDock

experiment the effectiveness between our most potent CPTP and US Food Drug Administration (FDA)

approved erlotinib. The result of a docking study of the CPTP showed a fairy strong inhibition free

energy of -7.74 kcal/mol. The two hydrogen bonds were observed between the donor hydrogen of

CPTP and the acceptor oxygen of the EGFR residue PHE771, confirming the strong affinity between

CPTP and EGFR protein. Cancer reveals the major mortality world-wide. The comprehensive

understanding and strategy of cancer is inevitable for the diagnosis, treatment, and prevention of

cancer. Various therapeutic techniques aimed at overcoming the resistance to currently available

EGFR inhibitors and preventing its onset failed. Our honest goal is that our novel tetracyclic peptide

will be a safe and effective treatment for non-small-cell lung cancer without causing resistance. We

hope that the future clinical research will elucidate the fact that our novel CPTP is a resistant free and

effective drug for the treatment of Non-Small-Cell (NCS) lung cancer.

 

Author(s) Details:

E. Akaho,
Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Kobe, Japan.

Please see the link here: https://stm.bookpi.org/CAPR-V2/article/view/6582