Nuclear Receptors: Recent Drug Discovery for Cancer Therapies

Area of Science:

• Molecular Biology
• Oncology
• Pharmacology

Background:

• Nuclear receptors (NRs) are crucial transcription factors regulating physiological processes and gene networks.
• NRs play significant roles in various cancers, leading to therapeutic targeting.
• Established NR-targeted therapies, like estrogen receptor (ER)α and androgen receptor (AR) blockers, have improved patient survival.

Purpose of the Study:

• To review NR-based drug discovery in cancer.
• To discuss resistance mechanisms to current NR-targeted therapies.
• To highlight novel strategies for targeting both established and emerging NRs in oncology.

Main Methods:

• Literature review of NR functions in cancer.
• Analysis of therapeutic strategies targeting NRs.
• Examination of resistance mechanisms to NR-targeted drugs.
• Exploration of novel NR targets in immuno-oncology.

Main Results:

• Drugs targeting ERα and AR have shown efficacy in breast and prostate cancers, respectively.
• Drug resistance necessitates the development of novel therapeutic approaches.
• Emerging NRs like liver X receptors, retinoic acid-related orphan receptors, and farnesoid X receptors show promise in immuno-oncology.

Conclusions:

• Targeting NRs remains a vital strategy in cancer drug discovery.
• Addressing resistance mechanisms is crucial for improving treatment outcomes.
• Exploring novel NRs offers new avenues for cancer therapy, particularly in immuno-oncology.