نتایج جستجو برای: nvp bez235

تعداد نتایج: 1391  

2018
Xiaoyu Chai Dan Sun Qian Han Liang Yi Yanping Wu Xinmin Liu

The present study was designed to examine whether hypoxia induces the proliferation, migration and differentiation of pulmonary arterial fibroblasts (PAFs) via the PI3K/Akt/p70S6K signaling pathway. PAFs were subjected to normoxia (21% O2) or hypoxia (1% O2). The proliferation, migration, differentiation and cellular p110α, p‑Akt, and p‑p70S6K expression levels of the PAFs were examined in vitr...

2014
João D. Seixas Sandra A. Luengo-Arratta Rosario Diaz Manuel Saldivia Domingo I. Rojas-Barros Pilar Manzano Silvia Gonzalez Manuela Berlanga Terry K. Smith Miguel Navarro Michael P. Pollastri

Compound NVP-BEZ235 (1) is a potent inhibitor of human phospoinositide-3-kinases and mammalian target of rapamycin (mTOR) that also showed high inhibitory potency against Trypanosoma brucei cultures. With an eye toward using 1 as a starting point for anti-trypanosomal drug discovery, we report efforts to reduce host cell toxicity, to improve the physicochemical properties, and to improve the se...

Journal: :Molecular cancer therapeutics 2012
Sauveur-Michel Maira Sabina Pecchi Alan Huang Matthew Burger Mark Knapp Dario Sterker Christian Schnell Daniel Guthy Tobi Nagel Marion Wiesmann Saskia Brachmann Christine Fritsch Marion Dorsch Patrick Chène Kevin Shoemaker Alain De Pover Daniel Menezes Georg Martiny-Baron Doriano Fabbro Christopher J Wilson Robert Schlegel Francesco Hofmann Carlos García-Echeverría William R Sellers Charles F Voliva

Following the discovery of NVP-BEZ235, our first dual pan-PI3K/mTOR clinical compound, we sought to identify additional phosphoinositide 3-kinase (PI3K) inhibitors from different chemical classes with a different selectivity profile. The key to achieve these objectives was to couple a structure-based design approach with intensive pharmacologic evaluation of selected compounds during the medici...

2012
Sauveur-Michel Maira Sabina Pecchi Alan Huang Matthew Burger Mark Knapp Dario Sterker Christian Schnell Daniel Guthy Tobi Nagel Marion Wiesmann Saskia Brachmann Christine Fritsch Doriano Fabbro Christopher J. Wilson Robert Schlegel Francesco Hofmann Charles F. Voliva

Following the discovery of NVP-BEZ235, our first dual pan-PI3K/mTOR clinical compound, we sought to identify additional phosphoinositide 3-kinase (PI3K) inhibitors fromdifferent chemical classeswith a different selectivity profile. The key to achieve these objectives was to couple a structure-based design approach with intensive pharmacologic evaluation of selected compounds during the medicina...

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