Epidermal Growth Factor Receptor and its Trafficking Regulation by Acetylation: Implication in Resistance and Exploring the Newer Therapeutic Avenues in Cancer

Author(s): Manvendra Kumar, Gaurav Joshi, Joydeep Chatterjee, Raj Kumar*

Journal Name: Current Topics in Medicinal Chemistry

Volume 20 , Issue 12 , 2020

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Graphical Abstract:


Abstract:

Background: The EGFR is overexpressed in numerous cancers. So, it becomes one of the most favorable drug targets. Single-acting EGFR inhibitors on prolong use induce resistance and side effects. Inhibition of EGFR and/or its interacting proteins by dual/combined/multitargeted therapies can deliver more efficacious drugs with less or no resistance.

Objective: The review delves deeper to cover the aspects of EGFR mediated endocytosis, leading to its trafficking, internalization, and crosstalk(s) with HDACs.

Methods and Results: This review is put forth to congregate relevant literature evidenced on EGFR, its impact on cancer prognosis, inhibitors, and its trafficking regulation by acetylation along with the current strategies involved in targeting these proteins (EGFR and HDACs) successfully by involving dual/hybrid/combination chemotherapy.

Conclusion: The current information on cross-talk of EGFR and HDACs would likely assist researchers in designing and developing dual or multitargeted inhibitors through combining the required pharmacophores.

Keywords: Cancer, EGFR, HDAC, Drug resistance, Endocytosis, Dual/multi inhibitor, Chemotherapy.

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VOLUME: 20
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Year: 2020
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DOI: 10.2174/1568026620666200207100227
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