[HTML][HTML] Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery
As a conserved protein interaction module that recognizes and binds to acetylated lysine,
bromodomain (BRD) contains a deep, largely hydrophobic acetyl lysine binding site …
bromodomain (BRD) contains a deep, largely hydrophobic acetyl lysine binding site …
The BET bromodomain inhibitor OTX015 affects pathogenetic pathways in preclinical B-cell tumor models and synergizes with targeted drugs
Purpose: In cancer cells, the epigenome is often deregulated, and inhibition of the
bromodomain and extra-terminal (BET) family of bromodomain-containing proteins is a …
bromodomain and extra-terminal (BET) family of bromodomain-containing proteins is a …
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses
A Hammitzsch, C Tallant, O Fedorov… - Proceedings of the …, 2015 - National Acad Sciences
Th17 responses are critical to a variety of human autoimmune diseases, and therapeutic
targeting with monoclonal antibodies against IL-17 and IL-23 has shown considerable …
targeting with monoclonal antibodies against IL-17 and IL-23 has shown considerable …
Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy
S Picaud, O Fedorov, A Thanasopoulou, K Leonards… - Cancer research, 2015 - AACR
The histone acetyltransferases CBP/p300 are involved in recurrent leukemia-associated
chromosomal translocations and are key regulators of cell growth. Therefore, efforts to …
chromosomal translocations and are key regulators of cell growth. Therefore, efforts to …
Novel drug targets for personalized precision medicine in relapsed/refractory diffuse large B-cell lymphoma: a comprehensive review
R Camicia, HC Winkler, PO Hassa - Molecular cancer, 2015 - Springer
Diffuse large B-cell lymphoma (DLBCL) is a clinically heterogeneous lymphoid malignancy
and the most common subtype of non-Hodgkin's lymphoma in adults, with one of the highest …
and the most common subtype of non-Hodgkin's lymphoma in adults, with one of the highest …
Discovery and development of the Polo-like kinase inhibitor volasertib in cancer therapy
BT Gjertsen, P Schöffski - Leukemia, 2015 - nature.com
Owing to their integral involvement in cell cycle regulation, the Polo-like kinase (Plk) family,
particularly Plk1, has emerged as an attractive therapeutic target in oncology. In recent …
particularly Plk1, has emerged as an attractive therapeutic target in oncology. In recent …
Beating the odds: BETs in disease
CY Wang, P Filippakopoulos - Trends in biochemical sciences, 2015 - cell.com
Bromodomains (BRDs) are evolutionarily conserved protein interaction modules that
specifically recognise acetyl-lysine on histones and other proteins, facilitating roles in …
specifically recognise acetyl-lysine on histones and other proteins, facilitating roles in …
ROR nuclear receptors: structures, related diseases, and drug discovery
Nuclear receptors (NRs) are ligand-regulated transcription factors that regulate metabolism,
development and immunity. The NR superfamily is one of the major classes of drug targets …
development and immunity. The NR superfamily is one of the major classes of drug targets …
Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance
O Fedorov, J Castex, C Tallant, DR Owen, S Martin… - Science …, 2015 - science.org
Mammalian SWI/SNF [also called Brg/Brahma-associated factors (BAFs)] are evolutionarily
conserved chromatin-remodeling complexes regulating gene transcription programs during …
conserved chromatin-remodeling complexes regulating gene transcription programs during …