Feb 21, 2025 · Here we describe the evaluation of HER3-homing nanobiological particles (nanobioparticles (NBPs)) on such tumours in preclinical models and our discovery that systemic NBPs could be found in...

Oct 21, 2022 · Three mouse antibodies against HER3, HER3-3, HER3-8 and HER3-10, have been reported to be extremely potent in inhibiting basal proliferation and ligand-induced growth in breast cancer cell lines. HER3-8 and HER3-10 antibodies inhibited HER2-HER3 dimerization.

Mar 14, 2025 · Despite having only weak intrinsic kinase activity, HER3 can contribute to oncogenic signalling via ligand-induced heterodimerization with other HER family members. Evidence indicates that...

Sep 27, 2024 · HER3 can bind to the ligands heregulin and neuregulin 2 (NRG2). As shown in Figure 1, in the absence of a ligand, direct intramolecular interactions between subdomains II and IV keep HER3 in an inactive conformation.

Feb 8, 2023 · Given its ubiquitous expression across solid tumors, multiple efforts have been done to therapeutically target HER3 by blocking either the ligand binding domain or its dimerization with other receptors.

EGFR, HER3, HER4 have intact ligand binding sites. HER2 fails to bind any known ErbB ligands and HER3 has impaired catalytic activity. Two main strategies to target HER receptors for cancer treatment include monoclonal antibody (mAb) and tyrosine kinase inhibitor (TKI) approaches.

Oct 18, 2011 · A two-in-one antibody, MEHD7945A, binds to EGFR and HER3/ErbB3 and inhibits receptor function. Here, we demonstrate superiority of the dual-specific EGFR/HER3 antibody to monospecific HER antibodies.

Feb 1, 2022 · We report a structure-function study of constitutive HER2-HER3 signaling to identify opportunities for targeting. The allosteric activation of the HER2 kinase domain (KD) by the HER3 KD is required for tumorigenic signaling and can potentially be targeted by allosteric inhibitors.

Duligotumab is an antibody that targets both the human epidermal growth factor receptors 1 and 3. Heregulin is a human epidermal growth factor receptor 3 ligand that represents an encouraging candidate biomarker for the prediction of the efficacy of agents targeting this receptor.

Apr 5, 2016 · HER3 can be activated by its ligand (heregulin/HRG), which induces HER3 heterodimerization with EGFR, HER2, or other RTKs. Alternatively, HER3 can be activated in a ligand-independent manner through heterodimerization with HER2 in HER2-amplified cells.