Splicing modulator FR901464 is a potential agent for colorectal cancer in combination therapy.

ABSTRACT: FR901464 (FR) was first described as an anticancer drug and later identified as a modulator of splicing factor 3B subunit 1 (SF3B1). Although the effectiveness of splicing modulators has been investigated in colorectal cancer (CRC) cells, their usefulness in animal experiments has not been confirmed. The association of SF3B1 with CRC progression and the influence of FR on transcriptional activity in CRC has not been fully elucidated. FR showed strong cytotoxicity against CRC cell lines, SF3B1-mutated cancer cell lines, and human fibroblasts with IC₅₀ values less than 1 ng/ml. FR-resistant clones derived from HCT116, DLD1, Lovo, and CT26 cells showed IC₅₀ values greater than 100 ng/ml. SF3B1 sequencing demonstrated low frequencies of SF3B1 m

SUBMITTER: Yamano T 

PROVIDER: S-EPMC6349454 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature