Epidermal Growth Factor Receptor (EGFR) Inhibitors for Tumor Anti-angiogenesis Activity

Abstract

The EGFR family plays an essential role in normal organ development by mediating morphogenesis and differentiation through effects on cell proliferation, differentiation, apoptosis, invasion, and angiogenesis. Unlike normal cells that have tight regulatory mechanisms controlling EGFR pathways, tumor cells often have dysregulated EGFR signaling, allowing them to proliferate under adverse conditions, invade surrounding tissues, and increase angiogenesis. Epidermal growth factor receptor (EGFR) is a transmembrane receptor tyrosine kinase that belongs to the Human epidermal receptor (HER) family of receptors. Receptor protein tyrosine kinases play a key role in signal transduction pathways that regulate cell division and differentiation. Among the growth factor receptor kinases that have been identified as being important in cancer is epidermal growth factor receptor (EGFR) kinase (also known as erb-B1 or HER-1) and the related human epidermal growth factor receptor HER-2 (also known as erbB-2). The quinazoline and other heterocyclic skeletons are of great importance to chemists as well as biologists as it is available in a large variety of naturally occurring compounds. In this article we are emphasizing on various heterocycles such as Quinazoline, pyrrolotriazines etc. as promising anticancer agents. These heterocycles showed the anticancer activity through the inhibition of EGFR enzyme. Attempt will be taken to provide details information on the said topic in the benefit of medicinal chemist.

Hydantoin derivatives: A review on their anticancer activities

“…The epidermal growth factor receptor (EGFR) family plays a crucial role in the normal development of organs by regulating processes such as cell proliferation, differentiation, apoptosis, invasion, and angiogenesis [65][66][67]. In tumor cells, EGFR signaling is often dysregulated, allowing them to proliferate in unfavorable conditions, invade neighboring tissues, and promote angiogenesis This contrasts with normal cells with strict regulatory systems that govern EGFR pathways [65,68]. Unfortunately, the overexpression of the EGFR gene leads to the activation of various downstream signaling pathways, contributing to cancer aggressiveness and invasiveness [69].…”