Results 81 to 90 of about 128,101 (191)

Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition [PDF]

Clinical Cancer Research, 2016
Abstract Purpose: Targeting BET proteins was previously shown to have specific antitumoral efficacy against MYCN-amplified neuroblastoma. We here assess the therapeutic efficacy of the BET inhibitor, OTX015, in preclinical neuroblastoma models and extend the knowledge on the role of BRD4 in MYCN-driven neuroblastoma.
Henssen, Anton, Althoff, Kristina, Odersky, Andrea, Beckers, Anneleen, Koche, Richard, Speleman, Frank, Schäfers, Simon, Bell, Emma, Nortmeyer, Maike, Westermann, Frank, De Preter, Katleen, Florin, Alexandra, Heukamp, Lukas, Spruessel, Annika, Astrahanseff, Kathy, Lindner, Sven, Sadowski, Natalie, Schramm, Alexander, Astorgues-Xerri, Lucile, Riveiro, Maria E., Eggert, Angelika, Cvitkovic, Esteban, Schulte, Johannes   +22 more
openaire   +3 more sources

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

Erratum: BET bromodomain inhibitors synergize with ATR inhibitors in melanoma [PDF]

Cell Death & Disease, 2017
AbstractMetastatic malignant melanoma continues to be a challenging disease despite clinical translation of the comprehensive understanding of driver mutations and how melanoma cells evade immune attack. In Myc-driven lymphoma, efficacy of epigenetic inhibitors of the bromodomain and extra-terminal domain (BET) family of bromodomain proteins can be ...
Somsundar Veppil Muralidharan, Berglind Osk Einarsdottir, Joydeep Bhadury, Mattias F Lindberg, Jin Wu, Eric Campeau, Roger Olofsson Bagge, Ulrika Stierner, Lars Ny, Lisa M Nilsson, Jonas A Nilsson   +10 more
openaire   +4 more sources

BET degrader exhibits lower antiproliferative activity than its inhibitor via EGR1 recruiting septins to promote E2F1-3 transcription in triple-negative breast cancer

Pharmacological Research
The bromodomain and extraterminal domain (BET) family proteins serve as primary readers of acetylated lysine residues and play crucial roles in cell proliferation and differentiation.
Nan Liu, Shuai Wang, Munan Li, Nan Zhao, Deyu Wang, Rui Zhang, Mingxin Yu, Luoyi Zhao, Siwei Zhang, Fangbin Han, Ying Zhao, Quan Liu   +11 more
doaj   +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

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

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

, 2014
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional regulator, pharmacological inhibition of BET proteins shows therapeutic ...
Shi, J., Vakoc, C. R.
core   +1 more source

A guide to transcriptional cyclin‐dependent kinases in cancer

The FEBS Journal, EarlyView.
Transcriptional cyclin‐dependent‐kinases (tCDKs) facilitate gene expression by promoting RNA polymerase II (RNAPII) progression through discrete phases of the transcription cycle. Aberrant tCDK activity is detectable in different human cancers, thereby contributing to de‐regulated gene expression programs that drive oncogenic phenotypes.
Jennifer R. Devlin, Salla Kyheröinen, Ricky W. Johnstone   +2 more
wiley   +1 more source

Zebrafish and are paralogous members of the bromodomain-ET (BET) family of transcriptional coregulators that show structural and expression divergence-3

, 2011
Nio (chr16.1 or chr16.2 for simBrd2; and Brd2b), Onchorynchus (Oncho2L for Brd2L) and Oryzias (OryzUn for Brd), are shown below consensus sequences (top line of each section, in bold), for bromodomain 1 (Bromo 1; 60 amino acid core), bromodomain 2 (Bromo
Todd R Jackman (91591), Michael M Schmidt (91590), Katharine J Bee (91589), Jake B Guinto (91587), Angela J DiBenedetto (91586), Timothy D Ebert (91588)   +5 more
core   +1 more source

Genetic Architecture of Southern Stem Canker Resistance in Elite Southern Soybean (Glycine max [L.] Merr.) Germplasm

Plant Breeding, EarlyView.
ABSTRACT Southern stem canker (SSC), caused by the fungus Diaporthe aspalathi, is one of the major constraints to soybean (Glycine max [L.] Merr.) production in the southern United States and South America. Genetic resistance is the most effective strategy for managing SSC; however, the genetic architecture underlying resistance in elite southern ...
M. Habib Widyawan, James W. Buck, Qijian Song, Zenglu Li   +3 more
wiley   +1 more source