Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents

Eur J Med Chem. 2023 Jan 15:246:114971. doi: 10.1016/j.ejmech.2022.114971. Epub 2022 Nov 28.

Abstract

The biochemical role of the PI3K/PKB/mTOR signalling pathway in cell-cycle regulation is now well known. During the onset and development of different forms of cancer it becomes overactive reducing apoptosis and allowing cell proliferation. Therefore, this pathway has become an important target for the treatment of various forms of malignant tumors, including breast cancer and follicular lymphoma. Recently, several more or less selective inhibitors targeting these proteins have been identified. In general, drugs that act on multiple targets within the entire pathway are more efficient than single targeting inhibitors. Multiple inhibitors exhibit high potency and limited drug resistance, resulting in promising anticancer agents. In this context, the present survey focuses on small molecule drugs capable of modulating the PI3K/PKB/mTOR signalling pathway, thus representing drugs or drug candidates to be used in the pharmacological treatment of different forms of cancer.

Keywords: Cancer therapy; Dual inhibitors; Protein kinases; Rapamycin.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / chemistry
  • Breast Neoplasms* / drug therapy
  • Female
  • Humans
  • MTOR Inhibitors
  • Phosphatidylinositol 3-Kinases / metabolism
  • Proto-Oncogene Proteins c-akt / metabolism
  • TOR Serine-Threonine Kinases / metabolism

Substances

  • MTOR Inhibitors
  • Phosphatidylinositol 3-Kinases
  • TOR Serine-Threonine Kinases
  • Antineoplastic Agents
  • Proto-Oncogene Proteins c-akt
  • MTOR protein, human