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Published on: August 6, 2020
Targeting CBP and p300: Emerging Anticancer Agents
Domiziana Masci1, Michela Puxeddu2, Romano Silvestri2
1Department of Basic Biotechnological Sciences, Intensivological and Perioperative Clinics, Catholic University of the Sacred Heart, Largo Francesco Vito 1, 00168 Rome, Italy.
Abstract:
CBP and p300 are versatile transcriptional co-activators that play essential roles in regulating a wide range of signaling pathways, including Wnt/β-catenin, p53, and HIF-1α. These co-activators influence various cellular processes such as proliferation, differentiation, apoptosis, and response to hypoxia, making them pivotal in normal physiology and disease progression. The Wnt/β-catenin signaling pathway, in particular, is crucial for cellular proliferation, differentiation, tissue homeostasis, and embryogenesis. Aberrant activation of this pathway is often associated with several types of cancer, such as colorectal tumor, prostate cancer, pancreatic and hepatocellular carcinomas. In recent years, significant efforts have been directed toward identifying and developing small molecules as novel anticancer agents capable of specifically inhibiting the interaction between β-catenin and the transcriptional co-activators CBP and p300, which are required for Wnt target gene expression and are consequently involved in the regulation of tumor cell proliferation, migration, and invasion. This review summarizes the most significant and original research articles published from 2010 to date, found by means of a PubMed search, highlighting recent advancements in developing both specific and non-specific inhibitors of CBP/β-catenin and p300/β-catenin interactions. For a more comprehensive view, we have also explored the therapeutic potential of CBP/p300 bromodomain and histone acetyltransferase inhibitors in disrupting the transcriptional activation of genes involved in various signaling pathways related to cancer progression. By focusing on these therapeutic strategies, this review aims to offer a detailed overview of recent approaches in cancer treatment that selectively target CBP and p300, with particular emphasis on their roles in Wnt/β-catenin-driven oncogenesis.
Insights
Researchers are developing small molecules to inhibit CBP and p300 co-activators, crucial for Wnt/β-catenin signaling, to treat cancers driven by this pathway.
Area of Science:
- Molecular Biology
- Cancer Research
- Drug Discovery
Background:
- CBP and p300 are key transcriptional co-activators regulating vital cellular processes and signaling pathways like Wnt/β-catenin.
- Dysregulated Wnt/β-catenin signaling is implicated in various cancers, driving tumor proliferation, migration, and invasion.
- Targeting the interaction between β-catenin and CBP/p300 presents a promising strategy for cancer therapy.
Purpose of the Study:
- To review recent advancements (2010-present) in developing small molecule inhibitors targeting CBP/β-catenin and p300/β-catenin interactions.
- To explore the therapeutic potential of CBP/p300 bromodomain and histone acetyltransferase inhibitors in cancer treatment.
- To provide an overview of strategies targeting CBP and p300 in Wnt/β-catenin-driven oncogenesis.
Main Methods:
- PubMed literature search for original research articles from 2010 to date.
- Focus on studies developing specific and non-specific inhibitors of CBP/β-catenin and p300/β-catenin interactions.
- Inclusion of research on CBP/p300 bromodomain and histone acetyltransferase inhibitors.
Main Results:
- Significant progress has been made in identifying small molecules that inhibit CBP/β-catenin and p300/β-catenin interactions.
- Various CBP/p300 inhibitors show therapeutic potential by disrupting oncogenic signaling pathways.
- Research highlights the role of these co-activators in Wnt/β-catenin-driven cancers.
Conclusions:
- Targeting CBP and p300 interactions with β-catenin offers a viable therapeutic approach for Wnt/β-catenin-driven cancers.
- CBP/p300 inhibitors, including bromodomain and HAT inhibitors, represent a promising avenue for novel cancer treatments.
- Further research into these targeted therapies is crucial for effective cancer intervention.
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