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Ruthenium-Mediated 18F-Fluorination and Preclinical Evaluation of a New CB1 Receptor Imaging Agent [18F]FPATPP
<p>Cannabinoid receptor 1 (CB1R) controls various physiological and pathological conditions, including memory, motivation, and inflammation, and is thus an interesting target for positron emission tomography (PET). Herein, ...
Dynamic covalent macrocycles co-delivering genes and drugs against drug-resistant cancer
<p>Polymeric carriers have dominated the development of delivering chemotherapeutic drugs and genes against drug-resistant cancer. However, the biocompatibility, loading, and release capabilities of polymers are unsatisfactory. Here, we have advanced the delivery system by developing dynamic covalent macrocycles using a dithiol monomer through a thiol/disulfide exchange reaction to co-deliver doxorubicin (DOX) and small interfering RNA (siRNA). Our thermodynamically based macrocycles achieve a drug-loading content of 30.2%, whereas a disulfide polymer prepared from the same monomer under kinetic control cannot load DOX. In combination with siRNA, the macrocycles exhibit excellent delivery efficiency and enhanced anti-tumor efficacy in vitro without systemic toxicity. Our findings suggest that dynamic covalent chemistry offers a powerful strategy for exploring macrocyclic carriers that could replace conventional polymers for co-delivery systems, paving the way to more efficient clinic therapies.<br></p>...
Effects of short-term sprint interval and moderate-intensity continuous training on liver fat content, lipoprotein profile, and substrate uptake: a randomized trial
<div>Type 2 diabetes (T2D) and increased liver fat content (LFC) alter lipoprotein profile and composition and impair liver substrate uptake. Exercise training mitigates T2D and reduces LFC, but the benefits of different ...
Application of the PET ligand [C-11]ORM-13070 to examine receptor occupancy by the alpha(2C)-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain
<b>Background</b><div>Availability of the α<sub>2C</sub>-adrenoceptor (α2C-AR) positron emission tomography (PET) tracer, [<sup>11</sup>C]ORM-13070, and the α2C-AR antagonist ORM-12741 allows probing of the roles of this ...
[F-18]FMPEP-d(2) PET imaging shows age- and genotype-dependent impairments in the availability of cannabinoid receptor 1 in a mouse model of Alzheimer's disease
Contradictory findings on the role of the type 1 cannabinoid receptor (CB1R) during the pathogenesis of Alzheimer's disease (AD) have been reported. Here, we evaluated the CB1R brain profile in an AD mouse model using ...
Comparison of Ga-68-DOTA-Siglec-9 and F-18-Fluorodeoxyribose-Siglec-9: Inflammation Imaging and Radiation Dosimetry
Sialic acid-binding immunoglobulin-like lectin 9 (Siglec-9) is a ligand of inflammation-inducible vascular adhesion protein-1 (VAP1). We compared Ga-68-DOTA-and F-18-fluorodeoxyribose-(FDR) labeled Siglec-9motif peptides ...