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 …

Targeting the PI3K/AKT/mTOR signaling pathway in the treatment of human diseases: Current status, trends, and solutions

J Huang, L Chen, J Wu, D Ai, JQ Zhang… - Journal of medicinal …, 2022 - ACS Publications
The phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of
rapamycin (mTOR) pathway is one of the most important intracellular pathways involved in …

Modulating tumor-associated macrophages to enhance the efficacy of immune checkpoint inhibitors: A TAM-pting approach

AN Chamseddine, T Assi, O Mir, S Chouaib - Pharmacology & therapeutics, 2022 - Elsevier
Tumor-associated macrophages (TAM) plasticity and diversity are both essential hallmarks
of the monocyte-macrophage lineage and the tumor-derived inflammation. TAM exemplify …

Class 1 PI3K clinical candidates and recent inhibitor design strategies: a medicinal chemistry perspective

AE Garces, MJ Stocks - Journal of medicinal chemistry, 2018 - ACS Publications
Phosphatidylinositol 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylate the 3-
OH of the inositol ring of phosphoinositides, and deregulation of this pathway has …

Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer

FM Elmenier, DS Lasheen, KAM Abouzid - European journal of medicinal …, 2019 - Elsevier
Abstract Phosphatidylinositol-3 kinase (PI3K) pathway is one of the most frequently activated
pathogenic signaling cascades in human malignancies. PI3K is genetically mutated or …

The role of PI3Kγ in the immune system: new insights and translational implications

SM Lanahan, MP Wymann, CL Lucas - Nature Reviews Immunology, 2022 - nature.com
Over the past two decades, new insights have positioned phosphoinositide 3-kinase-γ
(PI3Kγ) as a context-dependent modulator of immunity and inflammation. Recent advances …

The remarkable plasticity of macrophages: a chance to fight cancer

N Bercovici, MV Guérin, A Trautmann… - Frontiers in …, 2019 - frontiersin.org
It is well established that tumor-associated macrophages (TAM) found in most advanced
tumors have a pro-tumoral role. In this context, TAM limit the activity of tumor-infiltrating …

Structural determinants of isoform selectivity in PI3K inhibitors

MS Miller, PE Thompson, SB Gabelli - Biomolecules, 2019 - mdpi.com
Phosphatidylinositol 3-kinases (PI3Ks) are important therapeutic targets for the treatment of
cancer, thrombosis, and inflammatory and immune diseases. The four highly homologous …

Evolution of PI3Kγ and δ inhibitors for inflammatory and autoimmune diseases

MWD Perry, R Abdulai, M Mogemark… - Journal of Medicinal …, 2018 - ACS Publications
Phosphoinositol 3-kinases (PI3Ks) γ and δ are key enzymes in hematopoietic cells and have
been seen as high-value targets for the treatment of diseases with inflammatory and …

Targeting phosphatidylinositol 3‐kinase gamma (PI3Kγ): Discovery and development of its selective inhibitors

J Zhu, K Li, L Yu, Y Chen, Y Cai, J Jin… - Medicinal research …, 2021 - Wiley Online Library
Abstract Phosphatidylinositol 3‐kinase gamma (PI3Kγ) has been regarded as a promising
drug target for the treatment of advanced solid tumors, leukemia, lymphoma, and …