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Published on: January 22, 2019
CDC25 phosphatase inhibitors: an update
A Lavecchia1, C Di Giovanni, E Novellino
1Dipartimento di Chimica Farmaceutica e Tossicologica, "Drug Discovery" Laboratory, Universita di Napoli "Federico II", Napoli, Italy. lavecchi@unina.it
Abstract:
The cell division cycle 25 (CDC25) family of proteins is a group of highly conserved dual-specificity phosphatases. They are key regulators of normal cell division and the cell response to DNA damage, and play a fundamental role in transitions between cell cycle phases during normal cell division, via the activation of CdK/cyclin complexes. Their abnormal expression, detected in a number of tumors, often correlated with a poor clinical prognosis, implies that their dysregulation is involved in malignant transformation. Thus, inhibition of these proteins represents an attractive therapeutic target in oncology, as evidenced from many patents and papers published on the subject in recent years. Hence, this review aims to provide an overview of recent developments in the field of CDC25 phosphatase inhibitor design since 2008.
Insights
The cell division cycle 25 (CDC25) protein family regulates cell division and DNA damage response. Inhibiting CDC25 phosphatases is a promising cancer therapy strategy, with recent advancements in inhibitor design.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- The cell division cycle 25 (CDC25) family are conserved dual-specificity phosphatases.
- They are critical regulators of cell cycle progression and DNA damage response.
- CDC25 dysregulation is implicated in various cancers, correlating with poor prognosis.
Purpose of the Study:
- To review recent developments in CDC25 phosphatase inhibitor design.
- To highlight CDC25 proteins as attractive therapeutic targets in oncology.
Main Methods:
- Literature review of patents and publications since 2008.
- Analysis of recent advancements in the design of CDC25 inhibitors.
Main Results:
- CDC25 phosphatases are key regulators of cell cycle transitions via CdK/cyclin activation.
- Abnormal CDC25 expression is linked to malignant transformation and poor clinical outcomes.
- Inhibition of CDC25 proteins is a validated therapeutic strategy in oncology.
Conclusions:
- CDC25 phosphatase inhibitors represent a significant area of research in cancer therapy.
- Continued development in inhibitor design is crucial for effective oncology treatments.
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