Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015)

ABSTRACT

Introduction: Glycogen synthase kinase (GSK-3) is a serine/threonine kinase that phosphorylates more than one hundred different sequences within proteins in a variety of different pathways. It is a key component of a remarkably large number of cellular processes and diseases. Imbalance of GSK-3 activity is involved in various prevalent pathological diseases, such as diabetes, neurodegenerative diseases and cancer. Understanding its role in different disorders has been central in the last several decades and there has been a significantly large development of GSK-3 inhibitors, some of which, show promising results for the treatment of these devastating diseases.

Areas covered: This review covers patent literature on GSK-3 inhibitors and their applications published and/or granted between 2014 and 2015.

Expert opinion: GSK-3 inhibitors have gained a prominent role in regenerative medicine based in their ability to modulate stem cells. Moreover, some allosteric modulators of GSK-3 emerge as safe compounds for chronic treatments.

KEYWORDS:

• Alzheimer’s disease
• cancer
• GSK-3 inhibitors
• stem cells
• regenerative medicine

Article highlights

• GSK-3 inhibitors have gained a prominent role in regenerative medicine

• Allosteric modulators of GSK-3 emerge as safe compounds for chronic treatments.

• Contribution of GSK-3 inhibitors as coadjuvants in immunotherapy approaches is gaining relevance.

• GSK-3 inhibitors are showing promising results in different cancer combination therapies.

• New therapeutic uses for GSK-3 inhibitors are being discovered continuously

This box summarizes key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Additional information

Funding

This paper was funded by Ministerio de Economía y Competitividad, Secretaría de Estado de Investigación, Desarrollo e Innovación. Grant number: IJCI-2014-20767, Fellowship number: SAF2012-37979-CO3-01.