Draining the FEN1s for cancer therapy

Rossetti, Giacomo G.; Sotiriou, Sotirios K.; Halazonetis, Thanos D.

doi:10.1073/pnas.2014862117

Cited by 1 publication

(1 citation statement)

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“…Its expression is frequently altered by disharmony or mutation in cancer, and these changes contribute to genomic instability and cancer progression [ 11 ]. FEN1 is highly expressed in a variety of tumors, including prostate cancer, neuroblastoma, pancreatic and breast cancer, lung cancer, testicular cancer, glioblastoma, and astrocytoma and so on [ 51 , 52 , 53 , 54 , 55 ]. The expression of FEN1 in different tumors and healthy tissues obtained from the TGCA database is shown in Figure 4 .…”

Section: The Role Of Fen1 In Diseasesmentioning

confidence: 99%

Small-Molecule Inhibitors Targeting FEN1 for Cancer Therapy

Yang

Guo

2022

Biomolecules

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DNA damage repair plays a key role in maintaining genomic stability and integrity. Flap endonuclease 1 (FEN1) is a core protein in the base excision repair (BER) pathway and participates in Okazaki fragment maturation during DNA replication. Several studies have implicated FEN1 in the regulation of other DNA repair pathways, including homologous recombination repair (HRR) and non-homologous end joining (NHEJ). Abnormal expression or mutation of FEN1 in cells can cause a series of pathological responses, leading to various diseases, including cancers. Moreover, overexpression of FEN1 contributes to drug resistance in several types of cancers. All this supports the hypothesis that FEN1 could be a therapeutic target for cancer treatment. Targeting FEN1 has been verified as an effective strategy in mono or combined treatment of cancer. Small-molecule compounds targeting FEN1 have also been developed and detected in cancer regression. In this review, we summarize the recent development of small-molecule inhibitors targeting FEN1 in recent years, thereby expanding their therapeutic potential and application.

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