Targeting PI3K/Akt signal transduction for cancer therapy

Y He, MM Sun, GG Zhang, J Yang, KS Chen… - Signal transduction and …, 2021 - nature.com
Abstract The phosphatidylinositol 3-kinase (PI3K)/Akt pathway plays a crucial role in various
cellular processes and is aberrantly activated in cancers, contributing to the occurrence and …

PI3K inhibitors are finally coming of age

B Vanhaesebroeck, MWD Perry, JR Brown… - Nature reviews Drug …, 2021 - nature.com
Abstract Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation
has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has …

[HTML][HTML] PIK3CA inhibition in models of proliferative glomerulonephritis and lupus nephritis

J Yamaguchi, P Isnard, N Robil, P de la Grange… - The Journal of Clinical …, 2024 - jci.org
Proliferative glomerulonephritis is a severe condition that often leads to kidney failure. There
is a significant lack of effective treatment for these disorders. Here, following the …

Application and synthesis of thiazole ring in clinically approved drugs

ZX Niu, YT Wang, SN Zhang, Y Li, XB Chen… - European Journal of …, 2023 - Elsevier
The development of heterocyclic derivatives has progressed considerably over the past few
decades, and many new agents of synthetic and natural origin have been produced. Among …

Alpelisib plus fulvestrant in PIK3CA-mutated, hormone receptor-positive advanced breast cancer after a CDK4/6 inhibitor (BYLieve): one cohort of a phase 2 …

HS Rugo, F Lerebours, E Ciruelos, P Drullinsky… - The Lancet …, 2021 - thelancet.com
Summary Background Alpelisib, a PI3Kα-selective inhibitor and degrader, plus fulvestrant
showed efficacy in hormone receptor-positive, HER2-negative, PIK3CA-mutated advanced …

Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

Alpelisib for PIK3CA-Mutated, Hormone Receptor–Positive Advanced Breast Cancer

F André, E Ciruelos, G Rubovszky… - … England Journal of …, 2019 - Mass Medical Soc
Background PIK3CA mutations occur in approximately 40% of patients with hormone
receptor (HR)–positive, human epidermal growth factor receptor 2 (HER2)–negative breast …

Targeting PI3K in cancer: mechanisms and advances in clinical trials

J Yang, J Nie, X Ma, Y Wei, Y Peng, X Wei - Molecular cancer, 2019 - Springer
Abstract Phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR)
signaling is one of the most important intracellular pathways, which can be considered as a …

[HTML][HTML] Alpelisib plus fulvestrant for PIK3CA-mutated, hormone receptor-positive, human epidermal growth factor receptor-2–negative advanced breast cancer: final …

F André, EM Ciruelos, D Juric, S Loibl, M Campone… - Annals of …, 2021 - Elsevier
Background Activation of the phosphatidylinositol-3-kinase (PI3K) pathway via PIK3CA
mutations occurs in 28%-46% of hormone receptor-positive (HR+), human epidermal growth …

[HTML][HTML] PI3K inhibitors in cancer: clinical implications and adverse effects

R Mishra, H Patel, S Alanazi, MK Kilroy… - International journal of …, 2021 - mdpi.com
The phospatidylinositol-3 kinase (PI3K) pathway is a crucial intracellular signaling pathway
which is mutated or amplified in a wide variety of cancers including breast, gastric, ovarian …