Structural insights into the role and targeting of EGFRvIII
2024年9月5日 · We selected a nanobody with preferential binding to EGFRvIII relative to EGFR and structurally defined an epitope on domain IV that is occluded in the unliganded intact EGFR. These findings suggest new avenues for EGFRvIII targeting in GBM.
Epidermal growth factor receptor (EGFR) and EGFRvIII in …
EGFRvIII is with the deletion of almost the entire L1 and CR1 domains, resulting in deficiency in ligand binding. The transmembrane and intracellular regions of EGFR and EGFRvIII are identical.
表皮生长因子受体III 型突变体(epidermal growth factor receper variant III,EGFRvIII) 是EGFR的一种突变体,在胶质母细胞瘤中高表达。 它通过建立信号通路调控网,增强神经胶质母细胞瘤的细胞增殖能力和侵袭能力,并提高其对化疗药物的耐受能力。 ( 1. Xiangya School of Medicine, Central South University, Changsha 410013; 2. Department of Neurosurgery, Xiangya Hospital, Central South University, Changsha 410008, China )
2024年6月21日 · To shed light on the role of EGFRvIII and its potential as a therapeutic target, we determined X-ray crystal structures of a monomeric EGFRvIII extracellular region (ECR). The EGFRvIII ECR resembles the unliganded conformation of EGFR, including the orientation of the C-terminal region of domain II.
Structural insights into the role and targeting of EGFRvIII
2024年9月5日 · To shed light on the role of EGFRvIII and its potential as a therapeutic target, we determined X-ray crystal structures of a monomeric EGFRvIII extracellular region (ECR). The EGFRvIII ECR resembles the unliganded conformation of EGFR, including the orientation of the C-terminal region of domain II.
Monoclonal antibody cetuximab binds to and down-regulates ...
EGFR variant III (EGFRvIII) is a truncated form of EGFR that does not bind ligand, is constitutively active, and is reported to be coexpressed with EGFR in some human tumors including breast, glioblastoma, lung, and prostate.
Identification of a novel peptide ligand for the cancer-specific ...
2022年12月1日 · EGFRvIII is the most common EGFR mutation occurring in patients with glioblastoma, being expressed in 20–50% of glioblastomas 8, 9, 10. Prevalence is the highest in patients with tumors...
Structural insights into the role and targeting of EGFRvIII - Cell Press
We selected a nanobody with preferential binding to EGFRvIII relative to EGFR and structurally defined an epitope on domain IV that is occluded in the unliganded intact EGFR. These findings suggest new avenues for EGFRvIII targeting in GBM.
EGFR mutations and abnormal trafficking in cancers
2024年8月21日 · EGFRvIII is a mutated form of EGFR, that is found in 40–50% of EGFR-amplified glioblastomas. It arises from the deletion of exons 2–7, resulting in the absence of the extracellular ligand-binding domain and constitutive activity .
Epidermal growth factor receptor and EGFRvIII in glioblastoma ...
2018年1月11日 · In this review, we discuss signaling pathways mediated by EGFR and EGFRvIII, current therapeutics targeting EGFR and/or EGFRvIII, and future directions in treating EGFR/EGFRvIII-amplified GBM...