Results 91 to 100 of about 4,932,082 (261)
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka +9 more
wiley +1 more source
DrugForm-DTA: Towards real-world drug-target binding affinity model
Drug-target affinity (DTA) prediction is a fundamental challenge in drug discovery. Computational methods for predicting DTA can greatly assist drug design by narrowing the search space and reducing the number of protein-ligand complexes with low ...
Ivan Khokhlov +8 more
doaj +1 more source
Breast cancer remains a major cause of cancer death in women, frequently developing endocrine therapy resistance. This study demonstrates that upregulated p21‐activated kinase 1 (PAK1) activity drives resistance to tamoxifen and long‐term estrogen deprivation in ER+ breast cancer models.
Luisa Schwarzmüller +10 more
wiley +1 more source
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
ADP‐ribosylation: An emerging regulator of the epigenome
ADP‐ribosylation has emerged as a dynamic epigenetic signaling mechanism that modifies histones and chromatin‐associated proteins. Through coordinated PARylation and MARylation, it integrates with other histone modifications to regulate chromatin structure, transcription factor activity, and gene expression, influencing genome function and disease ...
Cristel V. Camacho +2 more
wiley +1 more source
Target‐mediated drug disposition (TMDD) is often associated with high‐affinity binding to a target resulting in nonlinear pharmacokinetics. For large molecules, such as monoclonal antibodies, this can lead to increased clearance at sub‐saturating ...
Ronny Straube
doaj +1 more source
Partial inhibition of focal adhesion kinase (FAK) can paradoxically promote tumor growth, rather than simply producing a weaker antitumor effect than that observed with strong FAK suppression. In breast cancer and melanoma models, targeting p110δ PI3K, particularly in macrophages, counteracted these tumor‐promoting effects, highlighting the importance ...
Lydia Xenou +4 more
wiley +1 more source
The immune system as drug target [PDF]
The immune system is perhaps the largest yet most diffuse and distributed somatic system in vertebrates. It plays vital roles in fighting infection and in the homeostatic control of chronic disease.
Flower, Darren R.
core +1 more source
GraphPrint: Extracting Features from 3D Protein Structure for Drug Target Affinity Prediction [PDF]
Accurate drug target affinity prediction can improve drug candidate selection, accelerate the drug discovery process, and reduce drug production costs. Previous work focused on traditional fingerprints or used features extracted based on the amino acid ...
Singh, Amritpal
core +1 more source
DTA Atlas: A massive-scale drug repurposing database
The drug development process is costly and time-consuming. Repurposing existing approved drugs, an efficient and cost-effective strategy, involves assessing numerous drug-protein pairs to uncover new interactions.
Madina Sultanova +4 more
doaj +1 more source

