Design of novel lipidated peptidomimetic conjugates for targeting EGFR heterodimerization in HER2 + cancer.

ABSTRACT: The human epidermal growth factor receptor (EGFR) family is known to be involved in cell signaling pathways. The extracellular domain of EGFR consists of four domains, of which domain II and domain IV are known to be involved in the dimerization process. Overexpression of these receptors is known to play a significant role in heterodimerization of these receptors leading to the development of cancer. We have designed peptidomimetic molecules to inhibit the EGFR heterodimerization interaction that have shown antiproliferative activity and specificity for HER2-positive cancer cell lines. Among these, a peptidomimetic, compound 5, exhibited antiproliferative activity at low nanomolar concentrations in HER2-overexpressing cancer cell lines. To improve the stability of this peptidomimetic, we h

SUBMITTER: Naik H 

PROVIDER: S-EPMC6283100 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature