Results 251 to 260 of about 219,778 (281)

Progress in the Design and Development of Phosphoinositide-3-Kinase (PI3Kα) Inhibitors

Jordan Journal of Pharmaceutical Sciences, 2023
Background: The phosphatidylinositol 3-kinase (PI3Kα) has been spotlighted as a potential oncogene and therapeutic target for anticancer drug design. Objective: Target compounds were designed employing ligand- and structure-based drug design approaches to address the effect of the compounds’ backbones and functionalities on their biological ...
openaire   +1 more source

Preventive and Therapeutic Effects of Phosphoinositide 3-Kinase Inhibitors on Acute Lung Injury

Chest, 2011
Phosphoinositide 3-kinases (PI3Ks) are involved in a number of biologic responses. Recent preclinical studies demonstrated that the PI3K-dominant signal pathway could play an important role in the development of acute lung injury, although the mechanism remains unclear.CD-1 mice were administered different PI3K inhibitors either intranasally or ...
Chengshui, Chen, Xiaocong, Fang, Yaoli, Wang, Yuping, Li, Diane, Wang, Xia, Zhao, Chunxue, Bai, Xiangdong, Wang   +7 more
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Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases

Investigational New Drugs, 2012
Inhibitors of PI3K signaling are of great therapeutic interest in oncology. The phosphoinositide-3-kinase signaling pathway is activated in a variety of solid and non-solid tumors. We have identified an imidazopyrazine derivative, ETP-46321, as a potent inhibitor of PI3Kα [Formula: see text].
Teresa G, Granda, David, Cebrián, Sonia, Martínez, Patricia Villanueva, Anguita, Estela Casas, López, Wolfgang, Link, Teresa, Merino, Joaquín, Pastor, Beatriz G, Serelde, Sandra, Peregrina, Irene, Palacios, Maria Isabel, Albarran, Antonio, Cebriá, Milagros, Lorenzo, Patricia, Alonso, Jesús, Fominaya, Ana Rodríguez, López, James R, Bischoff   +17 more
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Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Bioorganic & Medicinal Chemistry, 2015
Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model.
Hatsuo, Kawada, Hirosato, Ebiike, Masao, Tsukazaki, Shun, Yamamoto, Kohei, Koyama, Mitsuaki, Nakamura, Kenji, Morikami, Kiyoshi, Yoshinari, Miyuki, Yoshida, Kotaro, Ogawa, Nobuo, Shinma, Takuo, Tsukuda, Jun, Ohwada   +12 more
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Inhibitors of phosphoinositide-3-kinase: a structure-based approach to understanding potency and selectivity

Organic & Biomolecular Chemistry, 2009
Phosphoinositide-3-kinase is a pivotal protein involved in a wide variety of signaling cascades and there has been a great deal of interest in the development of potent and selective inhibitors of this enzyme. In this review, the potency and selectivity of the known inhibitors is presented along with key structural information that helps rationalize ...
Teather J, Sundstrom, Amy C, Anderson, Dennis L, Wright   +2 more
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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
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Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.

Journal of Medicinal Chemistry, 2012
M. H. Norman, K. Andrews, Yunxin Y Bo, S. Booker, S. Caenepeel, V. Cee, Noel D'angelo, Daniel J. Freeman, B. Herberich, Fang-Tsao Hong, Claire L M Jackson, Jian Jiang, B. Lanman, Longbin Liu, J. McCarter, E. Mullady, N. Nishimura, L. Pettus, Anthony B. Reed, T. S. Miguel, A. Smith, Markian M Stec, S. Tadesse, A. Tasker, Divesh Aidasani, Xiaochun Zhu, R. Subramanian, N. Tamayo, Ling Wang, D. Whittington, Bin Wu, Tian Wu, Ryan P. Wurz, Kevin C Yang, Leeanne P Zalameda, Nancy Zhang, P. Hughes   +36 more
semanticscholar   +1 more source

The effect of phosphoinositide 3-kinase inhibitors on programmed nuclear degradation in Tetrahymena and fate of surviving nuclei

Cell Death and Differentiation, 2004
J. Yakisich, G. Kapler
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Pegylated wortmannin and 17-hydroxywortmannin conjugates as phosphoinositide 3-kinase inhibitors active in human tumor xenograft models.

Journal of Medicinal Chemistry, 2006
T. Zhu, J. Gu, Ker Yu, J. Lucas, P. Cai, R. Tsao, Yumin Gong, Fangbiao Li, Inder Chaudhary, Parimal Desai, M. Ruppen, M. Fawzi, J. Gibbons, S. Ayral-Kaloustian, J. Skotnicki, T. Mansour, A. Zask   +16 more
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A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma.

European Urology, 2017
Liqin Wang, Tonći Šuštić, R. Leite de Oliveira, C. Lieftink, P. Halonen, M. van de Ven, R. Beijersbergen, Michel M van den Heuvel, R. Bernards, M. S. van der Heijden   +9 more
semanticscholar   +1 more source