Targeting Trop2 by Bruceine D suppresses breast cancer metastasis by blocking Trop2/β-catenin positive feedback loop.

ABSTRACT:

Introduction

Tumor-associated calcium signal transducer 2 (Trop2) has been used as a transport gate for cytotoxic agents into cells in antibody-drug conjugate designs because of its expression in a wide range of solid tumors. However, the specific role of Trop2 itself in breast cancer progression remains unclear and small molecules targeting Trop2 have not yet been reported.

Objectives

To screen small molecules targeting Trop2, and to reveal its pharmacological effects and the molecular mechanisms of action.

Methods

Small molecule targeting Trop2 was identified by cell membrane chromatography, and validated by cellular thermal shift assay and point mutation analyses. We investigated the pharmacological effects of Trop2 inhibitor using RNA-seq, human foreskin fibroblas

SUBMITTER: Tang W 

PROVIDER: S-EPMC10982870 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature