Target intelligence / Profile preview

Epidermal growth factor receptor and beta-tubulin (EGFR/Tubulin)

Target
EGFR/Tubulin
Molecular classification
Receptor tyrosine kinase, Cytoskeletal protein, Enzyme, Receptor
01

Overview

The dual target comprising the Epidermal Growth Factor Receptor (EGFR) and beta-tubulin represents a strategic approach in cancer therapy designed to simultaneously inhibit cell signaling and mitosis [1, 2]. EGFR is a transmembrane receptor tyrosine kinase that plays a critical role in cell growth, survival, and differentiation, and its dysregulation is a hallmark of various malignancies, particularly non-small cell lung cancer [7, 9]. Beta-tubulin is a core structural component of microtubules, which are essential for the formation of the mitotic spindle during cell division and for maintaining cellular architecture [1, 5]. Drugs targeting this dual entity, often referred to as dual EGFR/tubulin inhibitors, aim to achieve synergistic antitumor effects by blocking the phosphorylation-dependent signaling pathways of EGFR while concurrently disrupting microtubule dynamics [2, 3]. This multi-targeted mechanism is particularly valuable for overcoming resistance to conventional EGFR tyrosine kinase inhibitors, which often arises from secondary mutations or the activation of alternative survival pathways [4, 6]. By inducing both G2/M phase arrest and apoptosis, these agents offer a potent therapeutic option for treating heterogeneous and drug-resistant tumors [3, 8].

Other names
EGFR/tubulin dual targetEGFR and microtubule dual targetEGFR-tubulinEpidermal growth factor receptor and tubulin
02

Mechanism of action

Dual inhibition of EGFR tyrosine kinase activity and tubulin polymerization, leading to disruption of oncogenic signaling and mitotic spindle formation.

03

Biological functions

Signal transductionCell divisionMitosisCell proliferationApoptosis
04

Disease associations

CancerNon-small cell lung cancerBreast cancerGlioblastoma
05

Safety considerations

Skin rashDiarrheaPeripheral neuropathyMyelosuppressionNeutropenia
06

Interacting drugs

LASSBio-2070

4 more in the full profile.

07

Biomarkers

EGFR mutation status (e.g., L858R, T790M, C797S)Beta-III tubulin (TUBB3) expressionPhospho-EGFR levels

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