Nature reviews. Drug discovery, 2021-10, Vol.20 (10), p.741-769
2021
Details
- Autor(en) / Beteiligte
- Titel
- PI3K inhibitors are finally coming of age
- Ist Teil von
- Nature reviews. Drug discovery, 2021-10, Vol.20 (10), p.741-769
- Ort / Verlag
- England: Nature Publishing Group
- Erscheinungsjahr
- 2021
- Link zum Volltext
- Beschreibungen/Notizen
- Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has been hampered by issues such as poor drug tolerance and drug resistance, several PI3K inhibitors have now received regulatory approval - the PI3Kα isoform-selective inhibitor alpelisib for the treatment of breast cancer and inhibitors mainly aimed at the leukocyte-enriched PI3Kδ in B cell malignancies. In addition to targeting cancer cell-intrinsic PI3K activity, emerging evidence highlights the potential of PI3K inhibitors in cancer immunotherapy. This Review summarizes key discoveries that aid the clinical translation of PI3Kα and PI3Kδ inhibitors, highlighting lessons learnt and future opportunities.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1474-1776eISSN: 1474-1784DOI: 10.1038/s41573-021-00209-1Titel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_9297732
- Format
- –
- Schlagworte
- Animals, Antimitotic agents, Antineoplastic agents, Breast cancer, Cancer, Cancer cells, Cellular signal transduction, Control, Drug resistance, Forecasts and trends, Growth, Health aspects, Humans, Immune System Diseases - drug therapy, Immune System Diseases - genetics, Immunotherapy, Inhibitor drugs, Neoplasms - drug therapy, Neoplasms - genetics, Phosphatidylinositol 3-Kinases - drug effects, Phosphatidylinositol 3-Kinases - metabolism, Phosphoinositide-3 Kinase Inhibitors - pharmacology, Phosphoinositide-3 Kinase Inhibitors - therapeutic use, Phosphoinositides, Physiological aspects, Regulatory approval