Results 121 to 130 of about 63,359 (335)

Posttranscriptional Upregulation of IDH1 by HuR Establishes a Powerful Survival Phenotype in Pancreatic Cancer Cells. [PDF]

, 2017
Cancer aggressiveness may result from the selective pressure of a harsh nutrient-deprived microenvironment. Here we illustrate how such conditions promote chemotherapy resistance in pancreatic ductal adenocarcinoma (PDAC). Glucose or glutamine withdrawal
Blanco, Fernando F, Brody, Jonathan R., Chand, Saswati N., Cozzitorto, Joseph A., Dukleska, Katerina, Jiang, Wei, Jimbo, Masaya, Lal, Shruti, Londin, Eric R., Mambelli-Lisboa, Nicole C., Metallo, Christian M., Moffat, Cynthia, Nevler, Avinoam, Parker, Seth J., Seifert, Erin L., Vaziri-Gohar, Ali, Winter, Jordan M., Yeo, Charles J., Zarei, Mahsa   +18 more
core   +1 more source

Optimizing survival outcomes with post-remission therapy in acute myeloid leukemia. [PDF]

, 2019
Optimization of post-remission therapies to maintain complete remission and prevent relapse is a major challenge in treating patients with acute myeloid leukemia (AML).
Chan, Steven M, Daver, Naval G, Jonas, Brian A, Medeiros, Bruno C, Pollyea, Daniel A   +4 more
core   +1 more source

Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor.

Journal of Medicinal Chemistry, 2020
Inhibition of mutant IDH1 is being evaluated clinically as a treatment option for oncology. Here we describe structure-based design and optimization of quinoline lead compounds to identify FT-2102, a potent, orally bioavailable, brain pene-trant and ...
Justin A. Caravella, Jian Lin, R. B. Diebold, A. Campbell, Anna M. Ericsson, G. Gustafson, Zhongguo Wang, Jennifer Castro, A. Clarke, D. Gotur, H. R. Josephine, M. Katz, Mark T. Kershaw, Lili Yao, A. Toms, K. Barr, C. Dinsmore, D. Walker, S. Ashwell, Wei-Yu Lu   +19 more
semanticscholar   +1 more source

Novel IDH1-Targeted Glioma Therapies

CNS Drugs, 2019
Mutations in the isocitrate dehydrogenase (IDH) 1 gene are commonly found in human glioma, with the majority of low-grade gliomas harboring a recurrent point mutation (IDH1 R132H). Mutant IDH reveals an altered enzymatic activity leading to the synthesis of 2-hydroxyglutarate, which has been implicated in epigenetic mechanisms of oncogenesis ...
Trang T. T. Nguyen, Markus D. Siegelin, Enyuan Shang, Georg Karpel-Massler   +3 more
openaire   +3 more sources

Therapeutic targeting of chromatin alterations in leukemia and solid tumors

International Journal of Cancer, EarlyView.
Abstract Alterations in chromatin conformation and post‐translational modification of histones have become increasingly recognized as critical drivers of cancer development, progression, and therapy resistance. Recent advances in drug development have led to the establishment of several highly selective small molecule inhibitors, several of which are ...
Florian Perner, Tobias Berg, Daniel Sasca, Sophie‐Luise Mersiowsky, Jayant Y. Gadrey, Johanna Thomas, Michael W. M. Kühn, Michael Lübbert   +7 more
wiley   +1 more source

Correlation of microRNAs-10b/21/34a expression levels with IDH1-mutation status in patients with glioblastoma [PDF]

Srpski Arhiv za Celokupno Lekarstvo
Introduction/Objective. Isocitrate dehydrogenase (IDH) mutations play a significant role in gliomagenesis. Specific microRNAs, such as microRNA-10b and microRNA-21, act as oncogenic microRNAs, whereas microRNA-34a acts as a tumor suppressor in ...
Stepanović Aleksandar, Petrović Nina, Arsenijević Tatjana, Nikitović Marina   +3 more
doaj   +1 more source

Metabolic Dependencies in Pancreatic Cancer. [PDF]

, 2018
Pancreatic ductal adenocarcinoma (PDA) is a highly lethal cancer with a long-term survival rate under 10%. Available cytotoxic chemotherapies have significant side effects, and only marginal therapeutic efficacy. FDA approved drugs currently used against
Brody, Jonathan R., Vaziri-Gohar, Ali, Winter, Jordan M., Zarei, Mahsa   +3 more
core   +1 more source

Triptolide suppresses IDH1-mutated malignancy via Nrf2-driven glutathione metabolism

Proceedings of the National Academy of Sciences of the United States of America, 2020
Significance IDH1 mutation is a common genetic abnormality in human malignancies, whereas selective therapeutics for IDH1-mutated malignancies remain unavailable. Our present study reveals that IDH1-mutated cancer cells exhibit addiction to Nrf2-governed
Di Yu, Yang Liu, Yiqiang Zhou, V. Ruiz-Rodado, Mioara Larion, Guowang Xu, Chunzhang Yang   +6 more
semanticscholar   +1 more source

Epigenetic reprogramming in multiple myeloma—Challenges and opportunities

International Journal of Cancer, EarlyView.
Abstract In cancer, mutational processes act in concert with epigenetic reprogramming to endow malignant cells with hallmark properties that underpin tumorigenesis. Compared with the relatively rigid and slow processes of genetic evolution, the plastic nature of chromatin enables cells to adapt to a changing environment more rapidly.
Subhasree Kumar, Lev M. Kats, Emily Gruber   +2 more
wiley   +1 more source

Treatment with a Small Molecule Mutant IDH1 Inhibitor Suppresses Tumorigenic Activity and Decreases Production of the Oncometabolite 2-Hydroxyglutarate in Human Chondrosarcoma Cells. [PDF]

PLoS ONE, 2015
Chondrosarcomas are malignant bone tumors that produce cartilaginous matrix. Mutations in isocitrate dehydrogenase enzymes (IDH1/2) were recently described in several cancers including chondrosarcomas. The IDH1 inhibitor AGI-5198 abrogates the ability of
Luyuan Li, Ana C Paz, Breelyn A Wilky, Britt Johnson, Karina Galoian, Andrew Rosenberg, Guozhi Hu, Gabriel Tinoco, Olaf Bodamer, Jonathan C Trent   +9 more
doaj   +1 more source