Results 21 to 30 of about 63,430 (242)

The anabolic steroid stanozolol is a potent inhibitor of human MutT homolog 1

open access: yesFEBS Letters, EarlyView.
MutT homolog 1 (MTH1) is a member of the NUDIX superfamily of enzymes and is an anticancer drug target. We show that stanozolol (Stz), an anabolic steroid, is an unexpected nanomolar inhibitor of MTH1. The X‐ray crystal structure of the human MTH1–Stz complex reveals a unique binding scaffold that could be utilized for future inhibitor development ...
Emma Scaletti Hutchinson   +7 more
wiley   +1 more source

The multifaceted allosteric regulation of Aurora kinase A [PDF]

open access: yesBiochemical Journal, 2018
The protein kinase Aurora A (AurA) is essential for the formation of bipolar mitotic spindles in all eukaryotic organisms. During spindle assembly, AurA is activated through two different pathways operating at centrosomes and on spindle microtubules.
openaire   +2 more sources

A nucleotide‐independent, pan‐RAS‐targeted DARPin elicits anti‐tumor activity in a multimodal manner

open access: yesMolecular Oncology, EarlyView.
We report a Designed Ankyrin Repeat Protein that binds and inhibits RAS proteins, which serve as central cell signaling hubs and are essential for the progression of many cancers. Its unique feature is that it does not discriminate between different RAS isoforms or mutations and is capable of binding to RAS in both its active (GTP‐bound) and inactive ...
Jonas N. Kapp   +13 more
wiley   +1 more source

YAP1::TFE3 mediates endothelial‐to‐mesenchymal plasticity in epithelioid hemangioendothelioma

open access: yesMolecular Oncology, EarlyView.
The YAP1::TFE3 fusion protein drives endothelial‐to‐mesenchymal transition (EndMT) plasticity, resulting in the loss of endothelial characteristics and gain of mesenchymal‐like properties, including resistance to anoikis, increased migratory capacity, and loss of contact growth inhibition in endothelial cells.
Ant Murphy   +9 more
wiley   +1 more source

Blocking the voltage‐gated sodium channel hNav1.5 as a novel pH‐dependent mechanism of action for tamoxifen

open access: yesFEBS Open Bio, EarlyView.
Patch‐clamp recordings revealed that tamoxifen inhibits voltage‐gated sodium channels, especially under acidic conditions, both common in metastatic cancer cells. These effects may explain certain antitumor properties of tamoxifen, highlighting a novel mechanism of action beyond its known endocrine effects.
Karl Josef Föhr   +5 more
wiley   +1 more source

Novel 3D‐Printed Biophotonic Scaffold Displaying Luminescence under Near‐Infrared Light for Photopharmacological Activation and Biological Signaling Compound Release

open access: yesAdvanced Healthcare Materials, EarlyView.
Despite significant efforts in developing novel biomaterials to regenerate tissue, only a few of them have successfully reached clinical use. It has become clear that the next generation of biomaterials must be multifunctional. Smart biomaterials can respond to environmental or external stimuli, interact in a spatial‐temporal manner, and trigger ...
Sonya Ghanavati   +12 more
wiley   +1 more source

DNA‑Directed Assembly of Photonic Nanomaterials for Diagnostic and Therapeutic Applications

open access: yesAdvanced Materials, EarlyView.
DNA‐directed assembly offers a powerful strategy for constructing structured photonic nanomaterials with precise spatial control. This review provides a comprehensive overview of recent advancements in DNA‐assembled photonic nanomaterials for diagnostics and therapeutics, highlighting key design principles, functionalization strategies, and optical ...
Longjiang Ding   +5 more
wiley   +1 more source

Doing justice to allosteric regulation

open access: yesComptes Rendus. Biologies, 2015
Jacques Monod gave us not only our first regulatory system, but also our first smart molecules - i.e., he gave us allosteric proteins. But both of these contributions hung in a certain tension with his primary commitments. In particular, I focus here on the ways in which his ontological commitments constrained his thinking about the power of allostery.
openaire   +3 more sources

Dual‐Selective Terahertz‐Nanodisc Metasurfaces for Exploring Neurotransmitter Dynamics beyond Spectral Limitations

open access: yesAdvanced Materials, EarlyView.
Observation and detection of neurotransmitter dynamics in aqueous system has been hurdle for analytical fields due to its weak and reversible nature. A terahertz‐nanodisc metasurface which implements comprehensive detection over conformational change and selective sensing is introduced. Utilizing the THz regime photonics and biomimetic environment with
Taeyeon Kim   +6 more
wiley   +1 more source

Stimuli‐Responsive Materials for Biomedical Applications

open access: yesAdvanced Materials, EarlyView.
Stimulus‐responsive materials (SRMs) hold great promise for use in a wide range of biomedical applications. This review covers four stimulus modalities, namely, electrical, optical, magnetic, and ultrasound, and their associated SRMs. It provides a summary of the materials in each modality, their development, and current research perspectives.
Adriana Teixeira do Nascimento   +8 more
wiley   +1 more source

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