Results 171 to 180 of about 5,309,323 (231)

Parallelized 61‐Sample Inhibition Screening Accelerated by 19F‐MRI Compressed Sensing

open access: yesSmall Methods, EarlyView.
One scan, swift answers: a 19F‐MRI honeycomb captures reporter ligand displacement across dozens of non‐fluorinated drug candidates in parallel. Miniaturized arrays with compressed sensing speed up acquisition, delivering rapid, quantitative readouts for ligand screening.
Dilara Faderl   +3 more
wiley   +1 more source

Nanobodies as next‐generation targeting platforms: From discovery technologies to translational biomedicine

open access: yesVIEW, EarlyView.
Nanobodies, derived from the variable domains of camelid heavy‐chain‐only antibodies, have emerged as transformative biomedical tools due to their nanoscale size, exceptional stability, and unique capacity to recognize cryptic epitopes. This review provides a comprehensive overview of the field, outlining the structural and biochemical features of ...
Zhenrui Ye, Xianyang Li, Meixiao Zhan
wiley   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Notoginsenoside‐Fa mitigates vascular endothelial permeability via targeting SUGT1 to stabilize NLRP3 in a resting state

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Notoginsenoside‐Fa (Noto‐Fa) is an emerging active compound derived from notoginseng with promise in treating cardiovascular diseases. The development of cardiovascular diseases is intricately linked to the damage of vascular endothelium and it is widely acknowledged that numerous chronic inflammation pathways, especially the ...
Xiao‐Ying Yu   +9 more
wiley   +1 more source

The Role of IGF2BP3‐Mediated Immune Response Activation in Enhancing Immunotherapy of Koumine for Gastric Cancer

open access: yesCancer Science, EarlyView.
Koumine binds IGF2BP3 and promotes its proteasomal degradation, reducing m6A on EED mRNA, accelerating EED decay, lowering H3K27me3, and promoting IRF transcription, thereby restoring MHC‐I and enhancing CD8+ T cell killing. ABSTRACT Resistance to immune checkpoint blockade in gastric cancer often arises from defective antigen presentation due to MHC‐I
Qiu Hongqiang   +10 more
wiley   +1 more source

Surface plasmon resonance (SPR) - applications in carbohydrate analysis

open access: yesActa Biochimica Polonica, 2008
Krotkiewski, Hubert   +1 more
openaire  

Iloperidone treatment mitigates the Juvenile Huntington's Disease phenotype possibly via Sigma‐1 Receptor Modulation

open access: yesThe FEBS Journal, EarlyView.
We investigated the potential of iloperidone as an activator of Sigma‐1 receptor (S1R) neuroprotective function in juvenile Huntington's disease (jHD). We tested iloperidone on cortical neurons differentiated from patient‐derived iPSCs, demonstrating that it acts as a S1R agonist, decreasing apoptosis, huntingtin aggregation, and oxidative stress ...
Ersilia Fornetti   +11 more
wiley   +1 more source

Long‐read sequencing‐based atlas of tissue‐specific expression of DNM1L transcript variants

open access: yesThe FEBS Journal, EarlyView.
Targeted long‐read sequencing resolves full‐length DNM1L (Drp1) isoforms and reveals conserved, tissue‐specific expression patterns across human and mouse tissues. Functional assays show that Drp1 isoforms differ in their ability to drive mitochondrial fission, independent of abundance, with specific exons modulating activity.
Feng Yan   +19 more
wiley   +1 more source

Defining the role of αC helix interactions in the activation of the integrin αI domain

open access: yesThe FEBS Journal, EarlyView.
The α2I domain of the α2β1 integrin contains a distinctive αC helix and a conserved Arg288‐Glu318 ion pair that stabilizes the closed state of the domain. Disruption of this ion pair in the activated α2I variant unwinds the αC helix, which allows interaction with additional collagen‐binding sites increasing collagen binding.
Liisa Pösö   +7 more
wiley   +1 more source

Ion binding sites and intermediate domain closure induced by D‐serine in the GluD1 ligand‐binding domain

open access: yesThe FEBS Journal, EarlyView.
GluD1 belongs to the ionotropic glutamate receptors and has important functions in the brain and brain diseases. We report the crystal structure of the GluD1 ligand‐binding domain with D‐serine and zinc ions. MD simulations supported promiscuous binding of cations and that chloride ions play a stabilizing role. Pro725 seems to hinder interlobe closure,
Flemming Steen Jørgensen   +4 more
wiley   +1 more source

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