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 …

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 …

Wnt and PI3K/Akt/mTOR survival pathways as therapeutic targets in glioblastoma

A Barzegar Behrooz, Z Talaie, F Jusheghani… - International journal of …, 2022 - mdpi.com
Glioblastoma (GBM) is a devastating type of brain tumor, and current therapeutic treatments,
including surgery, chemotherapy, and radiation, are palliative at best. The design of effective …

[HTML][HTML] Role and regulation of autophagy in cancer

R Rakesh, LC PriyaDharshini, KM Sakthivel… - … et Biophysica Acta (BBA …, 2022 - Elsevier
Autophagy is an intracellular self-degradative mechanism which responds to cellular
conditions like stress or starvation and plays a key role in regulating cell metabolism, energy …

[HTML][HTML] Targeting the PI3K/AKT/mTOR signaling pathway in lung cancer: an update regarding potential drugs and natural products

Iksen, S Pothongsrisit, V Pongrakhananon - Molecules, 2021 - mdpi.com
Lung cancer is one of the most common cancers and has a high mortality rate. Due to its
high incidence, the clinical management of the disease remains a major challenge. Several …

Atropisomerism in drug discovery: a medicinal chemistry perspective inspired by atropisomeric class I PI3K inhibitors

S Perreault, J Chandrasekhar… - Accounts of Chemical …, 2022 - ACS Publications
Conspectus Atropisomerism is a type of axial chirality resulting from hindered rotation about
a σ bond that gives rise to nonsuperimposable stereoisomers (termed “atropisomers”). The …

Is target-based drug discovery efficient? Discovery and “off-target” mechanisms of all drugs

A Sadri - Journal of medicinal chemistry, 2023 - ACS Publications
Target-based drug discovery is the dominant paradigm of drug discovery; however, a
comprehensive evaluation of its real-world efficiency is lacking. Here, a manual systematic …

Targeting the PI3K/AKT/mTOR pathway in triple-negative breast cancer: a review

RLB Costa, HS Han, WJ Gradishar - Breast cancer research and treatment, 2018 - Springer
Purpose Triple-negative breast cancer (TNBC) accounts for approximately 20% of breast
cancer cases. Although there have been advances in the treatment of hormone receptor …

Targeting B cell receptor signalling in cancer: preclinical and clinical advances

JA Burger, A Wiestner - Nature Reviews Cancer, 2018 - nature.com
B cell receptor (BCR) signalling is crucial for normal B cell development and adaptive
immunity. BCR signalling also supports the survival and growth of malignant B cells in …

Idelalisib and rituximab in relapsed chronic lymphocytic leukemia

RR Furman, JP Sharman, SE Coutre… - … England Journal of …, 2014 - Mass Medical Soc
Background Patients with relapsed chronic lymphocytic leukemia (CLL) who have clinically
significant coexisting medical conditions are less able to undergo standard chemotherapy …