Results 121 to 130 of about 4,906,436 (344)

PARP inhibition and pharmacological ascorbate demonstrate synergy in castration‐resistant prostate cancer

Molecular Oncology, EarlyView.
Pharmacologic ascorbate (vitamin C) increases ROS, disrupts cellular metabolism, and induces DNA damage in CRPC cells. These effects sensitize tumors to PARP inhibition, producing synergistic growth suppression with olaparib in vitro and significantly delayed tumor progression in vivo. Pyruvate rescue confirms ROS‐dependent activity.
Nicolas Gordon, Peter T. Gallagher, Orly I. Richter, Neermala Poudel Neupane, Amy C. Mandigo, Jennifer J. McCann, Emanuela Dylgjeri, Irina Vasilevskaya, Christopher McNair, Channing J. Paller, Wm. Kevin Kelly, Karen E. Knudsen, Matthew J. Schiewer, Ayesha A. Shafi   +13 more
wiley   +1 more source

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. [PDF]

, 2010
Deregulation of the phosphoinositide-3-OH kinase (PI(3)K) pathway has been implicated in numerous pathologies including cancer, diabetes, thrombosis, rheumatoid arthritis and asthma.
Alex Berndt, Benjamin T Houseman, Christian Rommel, Daniel D Le, Fabrice Gorrec, Jeffrey P Shaw, Joseph I Pacold, Kevan M Shokat, Matthias K Schwarz, Olusegun Williams, Pascale Gaillard, Pingda Ren, Roger L Williams, Simon Miller, Thomas Rückle, Wai-Ching Hon, Yi Liu   +16 more
core   +2 more sources

The Future of Janus Kinase Inhibitors in Inflammatory Bowel Disease

Journal of Crohn's & Colitis, 2017
Inflammatory bowel diseases, such as ulcerative colitis and Crohn’s disease, are disabling conditions characterised by chronic, relapsing inflammation of the gastrointestinal tract.
L. D. Vries, M. Wildenberg, W. Jonge, G. D'Haens   +3 more
semanticscholar   +1 more source

Dammarenediol II enhances etoposide‐induced apoptosis by targeting O‐GlcNAc transferase and Akt/GSK3β/mTOR signaling in liver cancer

Molecular Oncology, EarlyView.
Etoposide induces DNA damage, activating p53‐dependent apoptosis via caspase‐3/7, which cleaves PARP1. Dammarenediol II enhances this apoptotic pathway by suppressing O‐GlcNAc transferase activity, further decreasing O‐GlcNAcylation. The reduction in O‐GlcNAc levels boosts p53‐driven apoptosis and influences the Akt/GSK3β/mTOR signaling pathway ...
Jaehoon Lee, Byung‐Cheol Han, Gi‐Bang Koo, Jihye Park, Mijin Kwon, Young Bin Park, Jae‐Mun Choi, Seung‐Ho Lee, Sangho Roh   +8 more
wiley   +1 more source

The Emerging World of JAK Inhibitors

Nepal Journal of Dermatology, Venereology & Leprology
The Janus Kinase inhibitors are a new emerging class of small molecules. These target the Janus Kinase proteins located on the cell membrane. Janus Kinase proteins regulate the cellular transcription of several proteins and act as mediators in several ...
Shraddha Uprety
doaj   +3 more sources

The PI3Kδ inhibitor roginolisib (IOA‐244) preserves T‐cell function and activity

Molecular Oncology, EarlyView.
Identification of novel PI3K inhibitors with limited immune‐related adverse effects is highly sought after. We found that roginolisib and idelalisib inhibit chronic lymphocytic leukemia (CLL) cells and Treg suppressive functions to similar extents, but roginolisib affects cytotoxic T‐cell function and promotion of pro‐inflammatory T helper subsets to a
Elise Solli, Alessio Bevilacqua, Mathias Wenes, Denis Migliorini, Lars van der Veen, Sigrid S Skånland, Giusy Di Conza, Kjetil Taskén   +7 more
wiley   +1 more source

Targeting Brutons Tyrosine Kinase in Chronic Lymphocytic Leukemia at the Crossroad between Intrinsic and Extrinsic Pro-survival Signals [PDF]

, 2016
Chemo immunotherapies for chronic lymphocytic leukemia (CLL) showed a positive impact on clinical outcome, but many patients relapsed or become refractory to the available treatments.
Facco, Monica, Frezzato, Federica, Martini, Veronica, Semenzato, Gianpietro, Severin, Filippo, Trentin, Livio, Trimarco, Valentina, Visentin, Andrea   +7 more
core   +1 more source

Medicinal chemistry breakthroughs on ATM, ATR, and DNA-PK inhibitors as prospective cancer therapeutics

Journal of Enzyme Inhibition and Medicinal Chemistry
This review discusses the critical roles of Ataxia Telangiectasia Mutated Kinase (ATM), ATM and Rad3-related Kinase (ATR), and DNA-dependent protein kinase (DNA-PK) in the DNA damage response (DDR) and their implications in cancer.
Ram Sharma, Anshul Mishra, Monika Bhardwaj, Gurpreet Singh, Larasati Vanya Indira Harahap, Sakshi Vanjani, Chun Hsu Pan, Kunal Nepali   +7 more
doaj   +1 more source

Kinase inhibitors in cancer therapy [PDF]

Veterinary and Comparative Oncology, 2004
AbstractOver the past few years, protein kinases have arisen as promising targets for therapeutic intervention in cancer therapy. This is due to a combination of several key events, including the identification of common kinase dysfunction in particular tumours and the recent success of such targeted kinase inhibitors as Gleevec (imatinib mesylate) and
openaire   +2 more sources

Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment

Molecular Oncology, EarlyView.
This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley   +1 more source