Results 261 to 270 of about 112,243 (300)

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Journal of Medicinal Chemistry, 2011
Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3Kα has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve PI3Kα vs PI3Kβ selectivity for two chemical series.
Timothy P, Heffron, Binqing, Wei, Alan, Olivero, Steven T, Staben, Vickie, Tsui, Steven, Do, Jennafer, Dotson, Adrian J, Folkes, Paul, Goldsmith, Richard, Goldsmith, Janet, Gunzner, John, Lesnick, Cristina, Lewis, Simon, Mathieu, Jim, Nonomiya, Stephen, Shuttleworth, Daniel P, Sutherlin, Nan Chi, Wan, Shumei, Wang, Christian, Wiesmann, Bing-Yan, Zhu   +20 more
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Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold

Bioorganic & Medicinal Chemistry, 2004
Phosphoinositide 3-kinases (PI3-Ks) are an ubiquitous class of signaling enzymes that regulate diverse cellular processes including growth, differentiation, and motility. Physiological roles of PI3-Ks have traditionally been assigned using two pharmacological inhibitors, LY294002 and wortmannin. Although these compounds are broadly specific for the PI3-
Zachary A, Knight, Gary G, Chiang, Peter J, Alaimo, Denise M, Kenski, Caroline B, Ho, Kristin, Coan, Robert T, Abraham, Kevan M, Shokat   +7 more
openaire   +2 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

Development of First Lead Structures for Phosphoinositide 3-Kinase-C2γ Inhibitors

Journal of Medicinal Chemistry, 2014
The importance of complete elucidation of the biological functions of phosphoinositide 3-kinases (PI3K) was realized years ago. They generate 3-phosphoinositides, which are known to function as important second messengers in many inter- and intracellular signaling pathways. However, the functional role of class II PI3Ks is still unclear.
Anne, Freitag, Prajwal, Prajwal, Aliaksei, Shymanets, Christian, Harteneck, Bernd, Nürnberg, Christoph, Schächtele, Michael, Kubbutat, Frank, Totzke, Stefan A, Laufer   +8 more
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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
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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
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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