Faculty, Staff and Student Publications

Publication Date

4-6-2026

Journal

Trends in Cancer

DOI

10.1016/j.trecan.2026.02.006

PMID

41942305

PMCID

PMC13060024

PubMedCentral® Posted Date

4-9-2026

PubMedCentral® Full Text Version

Author MSS

Abstract

Leucine-rich repeat-containing G protein-coupled receptor 5 (LGR5) is an established marker of normal and cancer stemlike cells. LGR5 has been implicated in promoting cancer cell plasticity that drives tumorigenesis, metastasis, and therapeutic resistance. LGR5 rapidly and constitutively internalizes and potentiates Wnt (Wingless/Int-1)/β-catenin and adhesion signaling pathways, though its precise mechanisms and interacting partners remain unresolved. An improved understanding of LGR5 signaling may provide invaluable insight into its intricate and important functions in cancer progression. Moreover, several LGR5-targeting therapies, including peptibody- and antibody-drug conjugates and bispecific antibodies, are showing promising efficacy and tolerability in colorectal cancer and other tumor types. This review discusses the cancer-related functions of LGR5 and explores the preclinical and clinical approaches to therapeutically target this enigmatic protein.

Keywords

LGR5, Wnt/β-catenin signaling, cancer cell plasticity, colorectal cancer, antibody-drug conjugate, bispecific antibody

Published Open-Access

yes

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