Target intelligence / Profile preview

Epithelial splicing regulatory protein 1 (ESRP1)

Target
ESRP1
Molecular classification
RNA-binding protein, Splicing factor, Heterogeneous nuclear ribonucleoprotein (hnRNP) family
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Overview

Epithelial splicing regulatory protein 1 (ESRP1) is a cell-type specific RNA-binding protein characterized by three conserved RNA recognition motifs. It is expressed specifically in epithelial cells and orchestrates regulated alternative splicing events crucial for the maintenance of epithelial cell properties, including barrier function and cell-cell adhesion. ESRP1 and its closely related paralog ESRP2 manage the decision between epithelial and mesenchymal splicing programs, particularly during the EMT process, which is fundamental to development, wound healing, and cancer metastasis. Aberrant ESRP1 expression and activity are linked to the progression, invasion, and metastasis of multiple solid tumors. ESRP1's regulatory functions involve key cellular processes including proliferation, apoptosis, and migration, with specific influence on genes like CD44, FGFR2, ENAH, and CARM1. While not currently a direct pharmacological target, it is emerging as a putative biomarker and therapeutic target for cancer diagnosis, prognosis, and intervention.

Other names
ESRP1RBM35AFLJ20171RNA-binding motif protein 35ARNA-binding protein 35ADFNB109
02

Mechanism of action

Drugs modulating ESRP1 expression or activity could affect cancer cell sensitivity to chemotherapy (by altering alternative splicing of key resistance mediators such as CARM1)

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Biological functions

Alternative mRNA splicingRegulation of epithelial cell properties and EMTMaintenance of cell barrier functionRegulation of cell proliferation, apoptosis, migration
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Disease associations

Cancer (breast, colon, non-small cell lung, small cell lung, colorectal, head and neck, gastric)Drug resistance/chemoresistance in cancerTumor invasion and metastasis
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Safety considerations

Alterations in ESRP1 expression may affect normal epithelial tissue function, and therapeutic targeting could potentially disrupt normal splicing processes essential for homeostasis.Dual role in cancer—can be both tumor suppressor and pro-oncogenic depending on tissue and context.
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Interacting drugs

No direct drugs currently approved that target ESRP1, but its expression modulates sensitivity to chemotherapy agents such as those used in SCLC, and may become a future target for drug development
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Biomarkers

Tumor progression and prognosisChemoresistance/chemosensitivityEpithelial vs. mesenchymal cell state and EMTPatient stratification in cancer treatment

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