نتایج جستجو برای: gdc

تعداد نتایج: 840  

2015
Dario Barbone Carlo Follo Nohemy Echeverry Victor H. Gerbaudo Astero Klabatsa Raphael Bueno Emanuela Felley-Bosco V. Courtney Broaddus Ying-Jan Wang

Malignant pleural mesothelioma is a highly chemoresistant solid tumor. We have studied this apoptotic resistance using in vitro and ex vivo three-dimensional models, which acquire a high level of chemoresistance that can be reduced by PI3K/mTOR inhibitors. Here, we investigate the activity of GDC-0980, a novel dual PI3K/mTOR inhibitor, which has been proposed to be effective in mesothelioma. In...

2016
James D Joseph Beatrice Darimont Wei Zhou Alfonso Arrazate Amy Young Ellen Ingalla Kimberly Walter Robert A Blake Jim Nonomiya Zhengyu Guan Lorna Kategaya Steven P Govek Andiliy G Lai Mehmet Kahraman Dan Brigham John Sensintaffar Nhin Lu Gang Shao Jing Qian Kate Grillot Michael Moon Rene Prudente Eric Bischoff Kyoung-Jin Lee Celine Bonnefous Karensa L Douglas Jackaline D Julien Johnny Y Nagasawa Anna Aparicio Josh Kaufman Benjamin Haley Jennifer M Giltnane Ingrid E Wertz Mark R Lackner Michelle A Nannini Deepak Sampath Luis Schwarz Henry Charles Manning Mohammed Noor Tantawy Carlos L Arteaga Richard A Heyman Peter J Rix Lori Friedman Nicholas D Smith Ciara Metcalfe Jeffrey H Hager

ER-targeted therapeutics provide valuable treatment options for patients with ER+ breast cancer, however, current relapse and mortality rates emphasize the need for improved therapeutic strategies. The recent discovery of prevalent ESR1 mutations in relapsed tumors underscores a sustained reliance of advanced tumors on ERα signaling, and provides a strong rationale for continued targeting of ER...

2016
Roxana Khoshravesh Corey R. Stinson Matt Stata Florian A. Busch Rowan F. Sage Martha Ludwig Tammy L. Sage

Photorespiratory glycine shuttling and decarboxylation in bundle sheath (BS) cells exhibited by C2 species is proposed to be the evolutionary bridge to C4 photosynthesis in eudicots. To evaluate this in grasses, we compare anatomy, cellular localization of glycine decarboxylase (GDC), and photosynthetic physiology of a suspected C2 grass, Homolepis aturensis, with these traits in known C2 grass...

Journal: :AJNR. American journal of neuroradiology 2002
Angelika Sorteberg Wilhelm Sorteberg Alan Rappe Charles M Strother

BACKGROUND AND PURPOSE Guglielmi detachable coils (GDCs) are effective in preventing rebleeding of ruptured aneurysms. To better understand the mechanism underlying this protective effect, we evaluated blood flow in aneurysms and their parent arteries before and after GDC coil placement. METHODS An 0.14-inch guidewire containing a combined pressure and thermistor sensor was inserted through a...

2018
John C. Byrd Stephen Smith Nina Wagner-Johnston Jeff Sharman Andy I. Chen Ranjana Advani Bradley Augustson Paula Marlton S. Renee Commerford Kwame Okrah Lichuan Liu Elaine Murray Elicia Penuel Ashley F. Ward Ian W. Flinn

GDC-0853 is a selective, reversible, and non-covalent inhibitor of Bruton's tyrosine kinase (BTK) that does not require interaction with the Cys481 residue for activity. In this first-in-human phase 1 study we evaluated safety, tolerability, pharmacokinetics, and activity of GDC-0853 in patients with relapsed or refractory non-Hodgkin lymphoma (NHL) or chronic lymphocytic leukemia (CLL). Twenty...

Journal: :Plant physiology 2007
Nadja Engel Kirsten van den Daele Uner Kolukisaoglu Katja Morgenthal Wolfram Weckwerth Tiit Pärnik Olav Keerberg Hermann Bauwe

The mitochondrial multienzyme glycine decarboxylase (GDC) catalyzes the tetrahydrofolate-dependent catabolism of glycine to 5,10-methylene-tetrahydrofolate and the side products NADH, CO(2), and NH(3). This reaction forms part of the photorespiratory cycle and contributes to one-carbon metabolism. While the important role of GDC for these two metabolic pathways is well established, the existenc...

2010

2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) is a novel small molecule inhibitor of the phosphatidylinositol 3-kinase (PI3K) pathway currently evaluated in the clinic as an anticancer agent. The objectives of this study were to determine in vitro whether GDC-0941 was a substrate of P-glycoprotein (P-gp) and breast cancer resis...

Journal: :Clinical cancer research : an official journal of the American Association for Cancer Research 2016
Wei Yang Sarah R Hosford Lloye M Dillon Kevin Shee Stephanie C Liu Jennifer R Bean Laurent Salphati Jodie Pang Xiaolin Zhang Michelle A Nannini Eugene Demidenko Darcy Bates Lionel D Lewis Jonathan D Marotti Alan R Eastman Todd W Miller

PURPOSE Phosphatidylinositol 3-kinase (PI3K) inhibitors are being developed for the treatment of estrogen receptor α (ER)-positive breast cancer in combination with antiestrogens. Understanding the temporal response and pharmacodynamic effects of PI3K inhibition in ER(+) breast cancer will provide a rationale for treatment scheduling to maximize therapeutic index. EXPERIMENTAL DESIGN Antiestr...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2012
Laurent Salphati Jodie Pang Emile G Plise Leslie B Lee Alan G Olivero Wei Wei Prior Deepak Sampath Susan Wong Xiaolin Zhang

(S)-1-{4-[2-(2-Amino-pyrimidin-5-yl)-7-methyl-4-morpholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl]-piperazin-1-yl}-2-hydroxy-propan-1-one (GDC-0980) is a potent and selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin, two key components of the PI3K pathway, the deregulation of which is associated with the development of many cancers. The objectives of th...

2010

2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) is a novel small molecule inhibitor of the phosphatidylinositol 3-kinase (PI3K) pathway currently evaluated in the clinic as an anticancer agent. The objectives of this study were to determine in vitro whether GDC-0941 was a substrate of P-glycoprotein (P-gp) and breast cancer resis...

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