4.5 Review

An updated patent review of Akt inhibitors (2016-present)

期刊

EXPERT OPINION ON THERAPEUTIC PATENTS
卷 31, 期 9, 页码 837-849

出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2021.1915291

关键词

Akt; inhibitors; patents; cancer; clinical trial; new strategies; indications

资金

  1. National Natural Science Foundation of China [81973172, 82003579]
  2. Natural Science Foundation of Zhejiang Province [LR21H300003]
  3. National Major Scientific and Technological Special Project for 'Significant New Drugs Development' [2018ZX09711002-007, 2018ZX09711002-011-023]

向作者/读者索取更多资源

This review focuses on the patent literature covering small-molecule inhibitors of Akt kinase and their applications from 2016-present, indicating that although progress with Akt inhibitors has been slow, new strategies provide new opportunities for development. The combination of Akt inhibitors and immunotherapy may become a research hotspot in the future.
Introduction: Akt is a widely known serine threonine kinase involved in a series of critical cellular pathways like cell survival and proliferation. With the development of small-molecule Akt inhibitors, new strategies such as covalent, peptide-based, and PROTAC (Proteolysis Targeting Chimera) strategies have also been used the design of Akt inhibitors. On the other hand, due to the specificity of the Akt pathway, the use of Akt modulators in combination therapy and immunotherapy has been disclosed in the past 5 years. Areas covered: This review focuses on the patent literature covering small-molecule inhibitors of Akt kinase and their applications from 2016-present. Expert opinion: Although Akt inhibitors' progress has been somewhat slow over the past five years, new strategies still provide new opportunities for the development of Akt inhibitors. Combination with Akt pathway inhibitors for tumor therapy has also been widely disclosed in patents in the last 5 years. Notably, combination strategies of Akt inhibitors and immunotherapy have started to emerge in recent years. While the clinical indications of Akt modulators should not be limited to anti-cancer, it is still worth trying the treatment of other diseases. Within the next years, current drug development around Akt inhibitors should be fascinating.

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