Results 231 to 240 of about 38,654,738 (261)

A Yeast-Based In Vivo Bioassay to Screen for Class I Phosphatidylinositol 3-Kinase Specific Inhibitors [PDF]

SLAS Discovery, 2012
The phosphatidylinositol 3-kinase (PI3K) pathway couples receptor-mediated signaling to essential cellular functions by generating the lipid second messenger phosphatidylinositol-3,4,5-trisphosphate. This pathway is implicated in multiple aspects of oncogenesis. A low-cost bioassay that readily measures PI3K inhibition in vivo would serve as a valuable
Teresa Fernández-Acero, José R Tormo, Isabel Rodríguez-Escudero   +2 more
exaly   +3 more sources

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Inhibition of Human Class I vs Class III Phosphatidylinositol 3′-Kinases

Biochemistry, 2017
Most investigations of phosphatidylinositol 3'-kinase (PI3K) drug inhibition have been via assays based on ADP appearance or ATP consumption (e.g., Liu, Q., et al. ( 2011 ) J. Med. Chem. 54 , 1473 - 1480 ). However, at least some PI3K isoforms show basal ATPase activity in the absence of PI lipid substrate(s), which may complicate quantification of ...
Matthew R. Hassett, Anna R. Sternberg, Paul D. Roepe   +2 more
openaire   +2 more sources

Structure-Based Design of a Novel Series of Potent, Selective Inhibitors of the Class I Phosphatidylinositol 3-Kinases

Journal of Medicinal Chemistry, 2012
A highly selective series of inhibitors of the class I phosphatidylinositol 3-kinases (PI3Ks) has been designed and synthesized. Starting from the dual PI3K/mTOR inhibitor 5, a structure-based approach was used to improve potency and selectivity, resulting in the identification of 54 as a potent inhibitor of the class I PI3Ks with excellent selectivity
Adrian L, Smith, Noel D, D'Angelo, Yunxin Y, Bo, Shon K, Booker, Victor J, Cee, Brad, Herberich, Fang-Tsao, Hong, Claire L M, Jackson, Brian A, Lanman, Longbin, Liu, Nobuko, Nishimura, Liping H, Pettus, Anthony B, Reed, Seifu, Tadesse, Nuria A, Tamayo, Ryan P, Wurz, Kevin, Yang, Kristin L, Andrews, Douglas A, Whittington, John D, McCarter, Tisha San, Miguel, Leeanne, Zalameda, Jian, Jiang, Raju, Subramanian, Erin L, Mullady, Sean, Caenepeel, Daniel J, Freeman, Ling, Wang, Nancy, Zhang, Tian, Wu, Paul E, Hughes, Mark H, Norman   +31 more
openaire   +2 more sources

Synthesis and Evaluation of Imidazo[1,2‐a]pyridine Analogues of the ZSTK474 Class of Phosphatidylinositol 3‐Kinase Inhibitors

Chemistry – An Asian Journal, 2019
AbstractUsing a scaffold‐hopping approach, imidazo[1,2‐a]pyridine analogues of the ZSTK474 (benzimidazole) class of phosphatidylinositol 3‐kinase (PI3K) inhibitors have been synthesized for biological evaluation. Compounds were prepared using a heteroaryl Heck reaction procedure, involving the palladium‐catalysed coupling of 2‐(difluoromethyl)imidazo[1,
Swarna A. Gamage, Julie A. Spicer, Kit Y. Tsang, Patrick D. O'Connor, Jack U. Flanagan, Woo‐Jeong Lee, James M. J. Dickson, Peter R. Shepherd, William A. Denny, Gordon W. Rewcastle   +9 more
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The Phosphatidylinositol 3‐kinase Class III Complex Containing TcVps15 and TcVps34 Participates in Autophagy in Trypanosoma cruzi

Journal of Eukaryotic Microbiology, 2016
AbstractAutophagy is a degradative process by which eukaryotic cells digest their own components to provide aminoacids that may function as energy source under nutritional stress conditions. There is experimental evidence for autophagy in parasitic protists belonging to the family Trypanosomatidae.
Alejandra C, Schoijet, Tamara, Sternlieb, Guillermo D, Alonso   +2 more
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IL-10 inhibits the starvation induced autophagy in macrophages via class I phosphatidylinositol 3-kinase (PI3K) pathway

Molecular Immunology, 2011
Autophagy is an important process which maintains cellular homeostasis under stressful conditions such as starvation and pathogenic invasion. Previous observations have indicated that several cytokines are important regulators of the autophagic process.
Hun-Jung, Park, Suk Jun, Lee, Sang-Hoon, Kim, Jihye, Han, Joonbeom, Bae, Sang Joon, Kim, Chung-Gyu, Park, Taehoon, Chun   +7 more
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Is stimulation of class-I phosphatidylinositol 3-kinase activity by insulin sufficient to activate pathways involved in glucose metabolism

Biochemical Society Transactions, 1997
In summary, it is still unclear which type of PI 3-kinase is involved in the activation of glycogen synthase. However, there is a strong body of evidence to suggest class-1 PI 3-kinase activity is necessary for insulin stimulation of glucose transport and a growing body of evidence to suggest that insulin stimulation of this class of PI 3-kinase is ...
P. R. Shepherd, K. Siddle, B. T. Navé
openaire   +1 more source

Expression pattern of class I phosphoinositide 3-kinase and distribution of its product, phosphatidylinositol-3,4,5-trisphosphate, during Drosophila embryogenesis

Gene Expression Patterns, 2014
The class I phosphoinositide 3-kinase (PI3K) can be activated by a large variety of extracellular stimuli and is responsible for generating phosphatidylinositol-3,4,5-trisphosphate (PI(3,4,5)P(3)) from phosphatidylinositol-4,5-bisphosphate at the plasma membrane.
Xin Xi, Kazuaki Tatei, Yumiko Kihara, Takashi Izumi   +3 more
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Girdin: A Class I Phosphatidylinositol 3-Kinase-Binding Protein in the Retina

Girdin is a nonreceptor guanine nucleotide exchange factor but functions as a guanine nucleotide exchange factor for the G protein Gαi. It plays a crucial role in regulating cell migration and adhesion, as well as protecting cells from apoptosis.
Raju V S, Rajala, Ammaji, Rajala
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Effects of rifampin on the pharmacokinetics of copanlisib, a novel pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor in cancer patients.

Journal of Clinical Oncology, 2018
e14559Background: Copanlisib, an iv pan-PI3K inhibitor recently approved for treatment of relapsed follicular lymphoma, is metabolized by CYP3A4 ( > 90%) in vitro.
Anna Spreafico, Michael B. Sawyer, Lillian L. Siu, Funan Huang, Susanne Reschke, Chenghua Xia, Zhaoping Yan, Isabelle Genvresse, Galia Cisternas, Andrea Kelly, Fatima Khan, Stefanie Reif, Camille Granvil   +12 more
openaire   +1 more source