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 …

For better or worse: the potential for dose limiting the on-target toxicity of PI 3-kinase inhibitors

CM Buchanan, KL Lee, PR Shepherd - Biomolecules, 2019 - mdpi.com
The hyper-activation of the phosphoinositide (PI) 3-kinase signaling pathway is a hallmark of
many cancers and overgrowth syndromes, and as a result, there has been intense interest in …

AutophagySMDB: a curated database of small molecules that modulate protein targets regulating autophagy

R Nanduri, R Kalra, E Bhagyaraj, AP Chacko, N Ahuja… - Autophagy, 2019 - Taylor & Francis
Macroautophagy/autophagy is a complex self-degradative mechanism responsible for
clearance of non functional organelles and proteins. A range of factors influences the …

Free–Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of N-Methylation for PI3Kδ Activity

L Barnes, H Blaber, DTK Brooks, L Byers… - Journal of Medicinal …, 2019 - ACS Publications
Phosphoinositide-3-kinase δ (PI3Kδ) is a critical regulator of cell growth and transformation
and has been explored as a therapeutic target for a range of diseases. Through the …

Discovery of 1, 3-dihydro-2H-imidazo [4, 5-c] quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors

R Bahekar, B Dave, S Soman, D Patel… - Bioorganic & Medicinal …, 2019 - Elsevier
PI3Kδ is implicated in various inflammatory and autoimmune diseases. For the effective
treatment of chronic immunological disorders such as rheumatoid arthritis, it is essential to …

Optimization of 5, 6, 7, 8-tetrahydropyrido [4, 3-d] pyrimidines to generate a highly selective PI3Kδ inhibitor

T Hamajima, F Takahashi, K Kato, Y Sugano… - Bioorganic & Medicinal …, 2019 - Elsevier
Abstract Chemical optimization of the 5, 6, 7, 8-tetrahydropyrido [4, 3-d] pyrimidine (THPP)
scaffold was conducted with a focus on cellular potency while maintaining high selectivity …