Results 121 to 130 of about 101,624 (260)

Pathological Signal‐Responsive Nanoplatforms for Sepsis: Integrating Biomarker Sensing With Spatiotemporal Drug Delivery and Immunomodulation

open access: yesAdvanced Science, EarlyView.
Biomarker‐triggered nanoplatforms transform sepsis therapy by coupling pathological sensing with precision drug release. This review reveals how microenvironment‐responsive nanomedicines enable stage‐specific intervention, improve therapeutic efficacy, and minimize systemic toxicity, while highlighting emerging opportunities for AI‐assisted and ...
Yukun Liu   +7 more
wiley   +1 more source

Evaluation of an in vivo pulmonary aspergillosis model for triazole susceptibility breakpoint development

open access: yesAntimicrobial Agents and Chemotherapy
Use of mouse infection models for antimicrobial pharmacokinetic/pharmacodynamic (PK/PD) analysis can assist in dosing regimen design and susceptibility breakpoint development.
Alex Lepak   +9 more
doaj   +1 more source

Isocyanate‐Modified Melatplatin(IV) Enhances Antitumor Efficacy via TCF4/COL6A3‐Mediated Extracellular Matrix Remodeling and cGAS‐STING Pathway Activation in Bladder Cancer

open access: yesAdvanced Science, EarlyView.
A series of melatonin‐conjugated platinum(IV) prodrugs was functionalized with isocyanate chains (compounds 5‒12). MP‐12C (compound 11) was identified as the lead candidate, with optimal potency and safety. MP‐12C exhibited greater efficacy than cisplatin by increasing intracellular uptake, reshaping the extracellular matrix, activating the cGAS‐STING ...
Linhui Wang   +18 more
wiley   +1 more source

Multi‐Layer Transcriptomic Comparison Across Human, Pig, and Mouse Informs Tissue‐ and Trait‐Specific Animal Model Selection

open access: yesAdvanced Science, EarlyView.
We integrated RNA‐seq data from humans, pigs, and mice across 15 matched tissues based on 14 910 one‐to‐one orthologous genes. Cross‐species similarity was systematically evaluated across multiple regulatory layers, including global co‐expression conservation, co‐expression networks, tissue‐specific programs, and 3D genome architecture.
Jingwen Dou   +21 more
wiley   +1 more source

Beyond Nature's Blueprint: Macrocyclic Peptides Containing Unnatural Amino Acids in Therapeutic Development

open access: yesAngewandte Chemie, EarlyView.
Strategic incorporation of unnatural amino acids transforms macrocyclic peptides into drug‐like molecules capable of engaging challenging targets. These building blocks enhance stability, permeability, and bioavailability, accelerating the development of next‐generation peptide therapeutics.
Krishna K. Sharma   +5 more
wiley   +2 more sources

Restores Aβ Clearance by Overcoming PCSK9–LRP1 Dysregulation and TRIB3‐Mediated Autophagy Blockade in Alzheimer's Disease

open access: yesAdvanced Science, EarlyView.
PCSK9 upregulation in cerebrovascular endothelial cells and microglia destabilizes the Aβ transporter LRP1, while TRIB3‐associated autophagy blockade further limits intracellular Aβ degradation. A RAP‐modified tea‐polyphenol nanoparticle co‐delivers siPCSK9 and siTRIB3 to restore LRP1‐mediated Aβ efflux and autophagy‐dependent degradation, reducing Aβ ...
Jie Miao   +8 more
wiley   +1 more source

Molecular Basis for Activation to Inhibition Switching in Kv7.2 Channel Modulators

open access: yesAngewandte Chemie, EarlyView.
The paper describes the serendipitous discovery of chemical manipulation allowing the activator‐to‐inhibitor switching in Kv7.2 channel modulators. The molecular determinants driving this switch have been rationalized by multidisciplinary investigation encompassing synthetic and analytical chemistry, in silico methods, cryo‐EM analysis ...
Tania Ciaglia   +20 more
wiley   +2 more sources

Engineered Peptide Self‐Assembled Nanofibers for Enhanced STING Activation: A Promising Nanodelivery Platform for Immunotherapy of Pediatric Solid Tumors

open access: yesAdvanced Science, EarlyView.
An engineered peptide self‐assembled nanofiber platform, designed to replicate STING–cGAMP binding motifs, facilitates pH‐responsive cytosolic delivery of cGAMP, enhances the endoplasmic reticulum with high efficiency, and robustly activates the STING pathway.
Yubin He   +6 more
wiley   +1 more source

A Modular Synthesis of C5‐Sulfenyl Thiazoles via an Intermolecular Pummerer Rearrangement: An Underexplored Scaffold for Medicinal Chemistry

open access: yesAngewandte Chemie, EarlyView.
Modular access to underexplored C5‐sulfenyl thiazoles via an intermolecular Pummerer rearrangement is reported. The methodology exhibits a broad functional group tolerance enabling the seamless design of trisubstituted thiazole cores bearing a sulfur handle for further elaboration.
Joe L. Smy   +5 more
wiley   +2 more sources

Investigating the hypothermic effects of fluoroquinolone antimicrobials on non-bacterial fever model mice

open access: yesJournal of Pharmaceutical Health Care and Sciences
Background Fluoroquinolone (FQ) antimicrobials have antipyretic effects during the treatment of bacterial infections; however, it is not clear whether these are due to their antimicrobial activities or their hypothermic effects.
Ryohei Hara   +7 more
doaj   +1 more source

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