Engineering an Enhanced EGFR Engager: Humanization of Cetuximab for Improved Developability.

ABSTRACT: The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase whose proliferative effects can contribute to the development of many types of solid tumors when overexpressed. For this reason, EGFR inhibitors such as cetuximab can play an important role in treating cancers such as colorectal cancer and head and neck cancer. Cetuximab is a chimeric monoclonal antibody containing mouse variable regions that bind to EGFR and prevent it from signaling. Although cetuximab has been used clinically since 2004 to successfully control solid tumors, advances in protein engineering have created the opportunity to address some of its shortcomings. In particular, the presence of mouse sequences could contribute to immunogenicity in the form of anti-cetuximab antibodies, and an occupied glycos

SUBMITTER: Goulet DR 

PROVIDER: S-EPMC8788544 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature