Results 241 to 250 of about 193,906 (268)

AEs of phosphoinositide 3 kinase Inhibitors in patients with lymphoma

Reactions Weekly, 2022

semanticscholar   +2 more sources

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

Journal of Medicinal Chemistry, 2012
Inhibition of phosphoinositide 3-kinase (PI3K) signaling through PI3Kα has received significant attention for its potential in cancer therapy. While the PI3K pathway is a well-established and widely pursued target for the treatment of many cancer types due to the high frequency of abnormal PI3K signaling, glioblastoma multiforme (GBM) is particularly ...
Timothy Heffron, L. Salphati, B. Alicke, J. Cheong, Jennafer Dotson, K. Edgar, R. Goldsmith, S. Gould, Leslie B. Lee, J. Lesnick, C. Lewis, Chudi O. Ndubaku, J. Nonomiya, A. Olivero, Jodie Pang, E. Plise, S. Sideris, S. Trapp, J. Wallin, Lan Wang, Xiaolin Zhang   +20 more
semanticscholar   +3 more sources

Duvelisib: A New Phosphoinositide-3-Kinase Inhibitor in Chronic Lymphocytic Leukemia

Future Oncology, 2019
P110-γ and -δ act in lymphocytes chemotaxis, presenting distinct, nonredundant roles in B- and T-cell migration and adhesion to stromal cells. Moreover, phosphoinositide-3-kinase-γ inhibition contributes to regulate macrophage polarization inhibiting cancer growth.
Anna M Frustaci, Alessandra Tedeschi, Marina Deodato, Giulia Zamprogna, Cairoli Roberto, Marco Montillo   +5 more
openaire   +3 more sources

Post-Wortmannin Era: Novel Phosphoinositide 3-Kinase Inhibitors with Potential Therapeutic Applications [PDF]

Current Enzyme Inhibition, 2009
Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes extensively involved in cell signalling, acting downstream of tyrosine kinase and G-protein coupled receptors. Based on structural and substrate specificity, mammalian PI3Ks include class I (A, B), class II and class III enzymes.
Braccini, Laura, Morello, Fulvio, Perino, Alessia, Hirsch, Emilio   +3 more
openaire   +1 more source

Phosphoinositide 3-kinase α inhibitors: a patent review

Expert Opinion on Therapeutic Patents, 2013
The alpha isoform of the class 1A family of phosphatidylinositol 3-kinases (PI3Kα) has been extensively studied and exploited as a target for cancer drugs. A large number of compounds, from a wide variety of structural scaffolds, are in development. There is an ongoing debate about the desirability for selectivity between PI3Kα and the other isoforms ...
openaire   +2 more sources

Fluorescent phosphoinositide 3-kinase inhibitors suitable for monitoring of intracellular distribution

Bioorganic & Medicinal Chemistry, 2011
The monitoring of the drug behavior and distribution in biological system can provide information whether drug reaches its desired target, and a biological rationale for the design of new therapeutics. We have developed a family of potent fluorescent PI3Kα inhibitors in which part of the fluorophore was engineered to be a pharmacophore capable of ...
Donghee, Kim, Hyunseung, Lee, Hwiseok, Jun, Soon-Sun, Hong, Sungwoo, Hong   +4 more
openaire   +2 more sources

Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors

Current Topics in Medicinal Chemistry, 2016
The PI3K signaling cascade is the key moderator of cell proliferation, survival, motility, and apoptosis. Class I PI3K proteins are well characterized and linked to thrombosis (PI3Kβ), rheumatoid arthritis (PI3Kδ), and cancer (PI3Kα). In this review, we explore the latest progress in the design and development of selective Class I PI3K inhibitors from ...
Dima A, Sabbah, Jian, Hu, Haizhen A, Zhong   +2 more
openaire   +2 more sources

Phosphoinositide 3‐kinase δ inhibitor as a novel therapeutic agent in asthma

Respirology, 2008
Abstract:  Multiple signal transduction pathways are involved in airway inflammation with one of the key signalling pathways being phosphoinositide 3‐kinase (PI3K). Numerous components of the PI3K pathway play an important role in the expression and activation of inflammatory mediators, inflammatory cell recruitment, immune cell function, airway ...
Seoung J, Park, Kyung H, Min, Yong C, Lee   +2 more
openaire   +2 more sources

Pharmacophore modeling and 3D-QSAR analysis of phosphoinositide 3-kinase p110α inhibitors

Journal of Molecular Modeling, 2010
Pharmacophore modeling studies were undertaken for a series of compounds belonging several groups of phosphoinositide 3-kinase (PI3K) p110alpha inhibitors: 4-morpholino-2-phenylquinazolines derivatives, pyrido[3',2':4,5]furo-[3,2-d]pyrimidine derivatives, imidazo[1,2-a]pyridine derivatives, sulfonylhydrazone substituted imidazo[1,2-a]pyridines, and ...
Yiping, Li, Yawen, Wang, Fuqiang, Zhang
openaire   +2 more sources

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ

Journal of Medicinal Chemistry, 2015
A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase structure. Optimization of the alkylimidazole group led to inhibitors with higher levels of PI3Kγ selectivity.
Philip N, Collier, David, Messersmith, Arnaud, Le Tiran, Upul K, Bandarage, Christina, Boucher, Jon, Come, Kevin M, Cottrell, Veronique, Damagnez, John D, Doran, James P, Griffith, Suvarna, Khare-Pandit, Elaine B, Krueger, Mark W, Ledeboer, Brian, Ledford, Yusheng, Liao, Sudipta, Mahajan, Cameron S, Moody, Setu, Roday, Tiansheng, Wang, Jinwang, Xu, Alex M, Aronov   +20 more
openaire   +2 more sources