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Breast cancer remains a significant global health challenge. In the pursuit of novel therapeutic approaches, the emerging role of bromodomain and extraterminal (BET) inhibitors has garnered increasing attention in the field of breast cancer research. At Alfa Cytology, we specialize in the preclinical discovery of BET inhibitors and promotes the development of new therapies for breast cancer.
BET proteins, a family of epigenetic regulators, have been identified as key players in the dysregulation of gene expression associated with cancer development. Interestingly, amplification or overexpression of BET proteins has been observed in breast tumors. This observation has prompted extensive research into the potential of BET inhibitors as a novel therapeutic strategy for breast cancer. BET inhibitors work by disrupting the binding of BET proteins to acetylated chromatin, effectively suppressing the transcription of genes involved in cancer progression in both estrogen receptor-positive (ER+) and triple-negative breast cancer (TNBC) subtypes.
Estrogen Receptor-positive (ER+) Breast Cancer
In ER+ breast cancer, BET inhibition has been shown to disrupt the intricate interplay between BET proteins and estrogen receptor signaling pathways, leading to suppression of tumor growth and enhanced sensitivity to endocrine therapies.
Triple-negative Breast Cancer (TNBC)
For the challenging TNBC subtype, BET inhibition has demonstrated the ability to downregulate the expression of key oncogenic drivers, such as MYC, offering a potential therapeutic strategy for this aggressive and often treatment-resistant form of the disease.
Fig.1 Mechanisms of BET inhibitor activity, resistance and combinatorial application. (Khandekar D., et al. 2020)
BET proteins act as epigenetic super-enhancer modulators with a unique structure consisting of two tandem bromodomains (BrD1 and BrD2), an extraterminal (ET) domain, and a C-terminal domain. Researchers have been able to develop more targeted and effective BET inhibitor therapies that aim to disrupt the interaction between BET proteins and acetylated histones. The development of these BET inhibitor therapies holds promise for breast cancer treatment.
| NCT number | AR agent | Phase |
| NCT02259114 | MK-8628/OTX105 | |
| NCT01587703 | GSK525762 | |
| NCT02698176 | MK-8628 | |
| NCT02431260 | INCB054329 |
As a leading preclinical CRO, Alfa Cytology is committed to advancing the development of innovative cancer therapies, including novel BET inhibitor for breast cancer. Our state-of-the-art facilities and multidisciplinary team of experts provide comprehensive services to support the entire drug development process, from target identification and validation to preclinical studies and biomarker development.
Pan BET Inhibitors Development
Bivalent BET Inhibitors Development
Selective BET Inhibitors Development
BET Dual-Targeting Inhibitors Development
Alfa Cytology provides development services for BET inhibitors, covering drug design, screening, and efficacy research to find ideal drug candidates for you and accelerate preclinical research on your breast cancer therapeutics. To learn more about our capabilities in BET inhibitors development for breast cancer or to discuss potential collaborative opportunities, please don't hesitate to contact us.
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