Results 91 to 100 of about 27,094 (219)

BRD9 inhibition as potential treatment option for testicular germ cell tumors

Andrology, EarlyView.
Abstract Background Testicular germ cell tumors (TGCT) are the predominant tumor in younger males. Usually, 5‐year survival rates are quite high, but 15–20% of patients with metastatic non‐seminomas are resistant to standard cisplatin‐based therapy.
Aylin Hansen, Christine Sanders, Florian Fronhoffs, Kai Funke, Glen Kristiansen, Hubert Schorle   +5 more
wiley   +1 more source

Bromodomains on the brain [PDF]

Science-Business eXchange, 2013
A Dana-Farber–led team has found that MYCN amplification provides a marker for sensitivity to BET bromodomain inhibition in neuroblastomas. GSK is using the marker as one criterion to select patients for a Phase I trial of its BET bromodomain inhibitor in cancer.
openaire   +1 more source

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

, 2013
The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET ...
Knapp, Stefan, Olcina, MM, Gill, A, Sheppard, DW, Wells, C, Tumber, A, Ritchie, AJ, Freeman, K, Brennan, Paul, Filippakopoulos, Panagis, Picaud, S, Conway, Stuart, Fedorov, O, Hammond, Ester, Hewings, DS, Martin, S, Russell, Angela   +16 more
core   +1 more source

A Spotlight on Yolk‐sac Tumors: Molecular Pathology, Current Diagnostics, and Novel Therapeutics

Andrology, EarlyView.
ABSTRACT Background Yolk‐sac tumors are an aggressive subtype of testicular cancer that significantly contribute to disease progression and therapy resistance, especially in adults. While testicular cancer generally has high cure rates with cisplatin‐based treatment, adult yolk‐sac tumors often appear as components of mixed tumors with poor response to
Evangelos Prokakis, Lisa Schneider, Felix Bremmer, Daniel Nettersheim   +3 more
wiley   +1 more source

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition [PDF]

, 2013
Bromodomain inhibition comprises a promising therapeutic strategy in cancer, particularly for hematologic malignancies. To date, however, genomic biomarkers to direct clinical translation have been lacking. We conducted a cell-based screen of genetically
Bassil, Christopher F, Gustafson, William Clay, Nekritz, Erin A, Kung, Andrew L, Weiss, William A, Garnett, Matthew J, Puissant, Alexandre, Frumm, Stacey M, Chanthery, Yvan H, Benes, Cyril H, Zeid, Rhamy, Qi, Jun, Stegmaier, Kimberly, McDermott, Ultan, Bradner, James E, Greninger, Patricia, Alexe, Gabriela   +16 more
core   +1 more source

Integrating novel therapeutic strategies in myeloproliferative neoplasms: Driving disease‐directed progress

British Journal of Haematology, EarlyView.
Summary Over the past decade, there has been a substantial increase in the diversity and number of therapeutic options for myeloproliferative neoplasms (MPNs). While many remain within the clinical trial arena, the clinician and patient community have seen more approvals reaching the clinic and a rethink on how best we should be approaching these ...
Trung Q. Ngo, Maria Georgiou, Donal P. McLornan, Claire N. Harrison   +3 more
wiley   +1 more source

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

, 2015
The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET ...
Stuart J. Conway (1280553), Oleg Fedorov (244326), Stefan Knapp (244328), Sarah Picaud (1280562), Andrew Gill (1295037), Angela J. Russell (106482), Monica M. Olcina (1295040), Christopher Wells (1295034), David S. Hewings (1295028), David W. Sheppard (1295046), Ester M. Hammond (233098), Anthony Tumber (765317), Paul E. Brennan (1290474), Alison J. Ritchie (1295043), Katherine Freeman (239943), Panagis Filippakopoulos (1280556), Sarah Martin (1295031)   +16 more
core   +1 more source

Bromodomain Protein Inhibition Protects β-Cells from Cytokine-Induced Death and Dysfunction via Antagonism of NF-κB Pathway

Cells
Cytokine-induced β-cell apoptosis is a major pathogenic mechanism in type 1 diabetes (T1D). Despite significant advances in understanding its underlying mechanisms, few drugs have been translated to protect β-cells in T1D.
Vinny Negi, Jeongkyung Lee, Varun Mandi, Joseph Danvers, Ruya Liu, Eliana M. Perez-Garcia, Feng Li, Rajaganapati Jagannathan, Ping Yang, Domenic Filingeri, Amit Kumar, Ke Ma, Mousumi Moulik, Vijay K. Yechoor   +13 more
doaj   +1 more source

Histone deacetylase inhibitors as venetoclax‐sensitising partners in acute myeloid leukaemia: Mechanisms, pharmacology and translational perspectives

British Journal of Pharmacology, EarlyView.
Abstract Venetoclax combined with hypomethylating agents has improved treatment for older or unfit patients with acute myeloid leukaemia (AML), but resistance and relapse remain common. This review analyses the rationale for combining venetoclax with inhibitors of histone deacetylase (HDAC).
Jaebok Lee, Marc Diederich
wiley   +1 more source

Bromodomain-containing protein 4 knockdown promotes neuronal ferroptosis in a mouse model of subarachnoid hemorrhage

Neural Regeneration Research
Neuronal cell death is a common outcome of multiple pathophysiological processes and a key factor in neurological dysfunction after subarachnoid hemorrhage. Neuronal ferroptosis in particular plays an important role in early brain injury.
Peng Lu, Fan Zhang, Lei Yang, Yijing He, Xi Kong, Kecheng Guo, Yuke Xie, Huangfan Xie, Bingqing Xie, Yong Jiang, Jianhua Peng   +10 more
doaj   +1 more source