Results 91 to 100 of about 342,422 (269)
Development of novel ligands influencing neurotransmission in the central nervous system
, 2007 The development of novel drugs targeting GPCRs is of particular interest since modulation of subfamilies of this receptor class highly influences neurotransmission in the central nervous system.
Sasse, Britta Caroline
core
Synthesis and evaluation of glycomimetic antagonists for the lectins DC-SIGN and FimH [PDF]
, 2014 Lectins are carbohydrate-binding proteins that are widely spread in nature and crucially involved in a multitude of biological processes. This thesis addresses the design of glycomimetic antagonists for the human lectin DC-SIGN (chapter 2) and the ...
Mayer, Katharina
core +1 more source
FEBS Open Bio, EarlyView.In a murine model of myocardial ischemia and reperfusion (MI/R), the CD36 azapeptide ligand MPE‐298 reduces cardiac injury and transiently lowers left ventricular long‐chain fatty acids (LCFAs) accumulation 3 h after reperfusion, accompanied by a decrease of oxidative stress and inflammation‐associated genes' expression in the heart and adipose tissue.
Jade Gauvin +12 more
wiley +1 more source
Halogen Bond: Its Role beyond Drug–Target Binding Affinity for Drug Discovery and Development
, 2015 Halogen bond has attracted a great deal of attention in the past years for hit-to-lead-to-candidate optimization aiming at improving drug-target binding affinity. In general, heavy organohalogens (i.e., organochlorines, organobromines, and organoiodines)
Yunxiang Lu (1305909) +5 more
core +1 more source
FEBS Open Bio, EarlyView.UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová +2 more
wiley +1 more source
FEBS Open Bio, EarlyView.IGFBP4 knockdown (KD) impairs preadipocyte proliferation and is associated with IGF1R protein downregulation and attenuated AKT phosphorylation. The mechanisms by which IGFBP4 KD influences the IGF1R/AKT signaling pathway involve newly synthesized proteins and lysosomal degradation pathways. Created in BioRender.
Yujia Guo +6 more
wiley +1 more source
Probing the druggability of the Notch1 ankyrin domain using a fragment-based approach
, 2011 Notch signalling is a highly conserved pathway that is important in the developmental processes that control cell differentiation and cell fates. This canonical pathway involves binding of a transmembrane ligand in one cell to the extraceullular domain ...
core +1 more source
Mutant NPM1 in Acute Myeloid Leukemia Initiation and Maintenance
Aging and Cancer, EarlyView.NPM1 mutations drive acute myeloid leukemia by acting as neomorphic transcriptional regulators that cooperate with Menin–MLL and XPO1 to sustain HOX/MEIS1 expression and block differentiation. Targeting these mutant‐specific transcriptional dependencies provides a rational therapeutic strategy for NPM1‐mutated AML.
Yanan Jiang +3 more
wiley +1 more source
Enabling target-aware molecule generation to follow multi objectives with Pareto MCTS
Communications BiologyTarget-aware drug discovery has greatly accelerated the drug discovery process to design small-molecule ligands with high binding affinity to disease-related protein targets.
Yaodong Yang +9 more
doaj +1 more source
Journal of Pharmaceutical AnalysisThe characterization of drug-target interactions is a key component of drug discovery, testing, and development. Affinity chromatography is one approach that can be used for this type of analysis.
David S. Hage +7 more
doaj +1 more source