Results 71 to 80 of about 109,018 (245)

ZW4864‐mediated inhibition of the β‐catenin/BCL9/BCL9L complex reveals therapeutic potential in bladder cancer

Molecular Oncology, EarlyView.
BCL9 and BCL9L drive bladder cancer progression by enhancing β‐catenin signaling, promoting proliferation, migration, invasion, and organoid growth. Genetic depletion of BCL9(L) suppresses malignant phenotypes, while pharmacological disruption of the β‐catenin/BCL9(L) complex with ZW4864 inhibits canonical Wnt signaling and tumor‐associated cellular ...
Roland Kotolloshi, Mandy Berndt‐Paetz, Eileen Lerner, Gregoire Najjar, Anca Azoitei, Krishna Pal Singh, Shailendra Kumar Gupta, Olaf Wolkenhauer, Cagatay Günes, Otmar Huber, Marc‐Oliver Grimm, Daniel Steinbach   +11 more
wiley   +1 more source

Adhirons are efficient tools to guide antiviral ligand discovery

Communications Biology
Adhirons are small, antibody-like proteins expressed in bacteria that bind to biological targets with high affinity. Since their discovery, Adhirons have been isolated against over 350 targets, and they can be used for many research applications. However,
Alex J. Flynn, Alex Derry, Oliver Debski-Antoniak, Stephen P. Muench, Juan Fontana, Katie J. Simmons   +5 more
doaj   +1 more source

The selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Lens-epithelium-derived growth-factor (LEDGF/p75)-binding site on HIV-1 integrase (IN), is an attractive target for antiviral chemotherapy. Small-molecule compounds binding to this site are referred as LEDGF-IN inhibitors (LEDGINs).
Da-Wei Zhang, Hao-Li Yan, Xiao-Shuang Xu, Lei Xu, Zhi-Hui Yin, Shan Chang, Heng Luo   +6 more
doaj   +1 more source

Single‐cell DNA methylation profiling: Technologies, computation, and applications in precision oncology

Molecular Oncology, EarlyView.
Single‐cell DNA methylation (scDNAme) profiling maps epimutational clonal evolution, revealing mechanisms of malignancy and therapeutic resistance across diverse cancer types. By providing a high‐resolution landscape of intratumoral heterogeneity, these technologies empower precise patient stratification, guide the development of enhanced ...
Ik Soo Kim
wiley   +1 more source

Preparation of Multiplexed Small RNA Libraries from Plants

Bio-Protocol, 2014
High-throughput sequencing is a powerful tool for exploring small RNA populations in plants. The ever-increasing output from an Illumina Sequencing System allows for multiplexing multiple samples while still obtaining sufficient data for small RNA ...
Kerrigan Gilbert, Noah Fahlgren, Kristin Kasschau, Elisabeth Chapman, James Carrington, Alberto Carbonell   +5 more
doaj   +1 more source

New classes of potent heparanase inhibitors from ligand-based virtual screening

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Heparanase is a validated target in cancer therapy and a potential target for several inflammatory pathologies. A ligand-based virtual screening of commercial libraries was performed to expand the chemical space of small-molecule inhibitors.
Daniele Pala, Laura Scalvini, Gian Marco Elisi, Alessio Lodola, Marco Mor, Gilberto Spadoni, Fabiana F. Ferrara, Emiliano Pavoni, Giuseppe Roscilli, Ferdinando M. Milazzo, Gianfranco Battistuzzi, Silvia Rivara, Giuseppe Giannini   +12 more
doaj   +1 more source

Targeting transcription factors associated with hemoglobinopathies: Lessons from successful interventions and implications for cancer

Molecular Oncology, EarlyView.
This review summarizes the transcription factors, repressive chromatin‐modifying complexes, and epigenetic mechanisms that control fetal hemoglobin repression. Notably, many regulators of γ‐globin silencing also function in transcriptional and epigenetic networks that drive cancer, highlighting opportunities to translate advances in hemoglobinopathy ...
Meigen Yu, Puspa Das, Xing Zhang, Xiaodong Cheng   +3 more
wiley   +1 more source

Docking of virtual libraries identifies small-molecule agonists of neurotensin receptors with analgesic activity

Nature Communications
Peptide-activated G protein-coupled receptors (GPCRs) play crucial roles in numerous diseases, but remain difficult therapeutic targets due to the challenges in developing small-molecule drugs.
Nicolas Panel, Duy Duc Vo, Harald Hübner, Mattia Deluigi, Szymon Pach, Félix Bélair, Dorothee Weikert, Christoph Klenk, Mark Hilge, Niharika Shiva, Isabelle Brochu, Jean-Michel Longpré, Frida Bällgren, Aljona Saleh, Huabin Hu, Jon Kapla, Stefanie Kampen, Israel Cabeza de Vaca, Jan Kihlberg, Nina Wettschureck, Philippe Sarret, Andreas Plückthun, Peter Gmeiner, Jens Carlsson   +23 more
doaj   +1 more source

Design, synthesis, and screening of an RNA optimized fluorinated fragment library

SLAS Discovery
Fragment-based screening is an efficient method for early-stage drug discovery. In this study, we aimed to create a fragment library optimized for producing high hit rates against RNA targets. RNA has historically been an underexplored target, but recent
Kasper P. Lundquist, Isabella Romeo, Raffaele B. Puglielli, Maëlle Pestalozzi, Marie L. Gram, Emily S. Hudson, Ofri Levi, Yoav S. Arava, Charlotte H. Gotfredsen, Mads H. Clausen   +9 more
doaj   +1 more source

Interferon beta drives therapy resistance in a patient‐derived model of high‐grade serous ovarian cancer

Molecular Oncology, EarlyView.
Interferon type 1 (IFN‐1) production and signaling is associated with the acquisition of therapy resistance, following chronic DNA damage, via Interferon‐related DNA damage resistance signature (IRDS) gene expression. An alternative, DNA damage‐independent role of sustained IFN‐1 mediated resistance was identified and characterized by the emergence of ...
Ashlyn Conant, Tise Suzuki, Kiera McGivney, V. S. S. Abhinav Ayyadevara, Sharon Asariah, Jay Deng, Ethan Nyein, Jacqueline Coats, Gary Yu, Yevgeniya J. Ioffe, Christian Hurtz, Juli J. Unternaehrer   +11 more
wiley   +1 more source