G protein-coupled receptors (GPCRs) can be used to shuttle peptide-drug conjugates into cells. But, for efficient therapy, a high concentration of cargo needs to be delivered. To explore this, we studied the pharmacologically interesting neuropeptide Y receptor (Y R) in one recombinant and three oncogenic cell systems that endogenously express the receptor. We demonstrate that recycled receptors behave identically to newly synthesized receptors with respect to ligand binding and internalization pathways. Depending on the cell system, biosynthesis, recycling efficiency, and peptide uptake differ partially, but shuttling was efficient in all systems. However, by comparing continuous application of the ligand for four hours to four cycles of internalization and recycling in between, a significantly higher amount of peptide uptake was achieved in the pulsed application (150-250 % to 300-400 %). Accordingly, in this well-suited drug shuttle system pulsed application is superior under all investigated conditions and should be considered for innovative, targeted drug delivery in general.
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http://dx.doi.org/10.1002/cmdc.202000490 | DOI Listing |
Front Physiol
January 2025
Susan Samueli Integrative Health Institute and Department of Medicine, University of California, Irvine, Irvine, CA, United States.
Stellate ganglion blockade (SGB) is a practical approach to managing many clinical disorders. Ultrasound-guided SGB is currently adopted as a more effective and safer method in humans. Developing this technique in rats would facilitate further study of SGB application.
View Article and Find Full Text PDFRev Cardiovasc Med
January 2025
Cardiac Surgery, Lausanne University Hospital CHUV Lausanne, 1011 Lausanne, Switzerland.
Background: Currently, there are no standardized guidelines for graft allocation in heart transplants (HTxs), particularly when considering organs from marginal donors and donors after cardiocirculatory arrest. This complexity highlights the need for an effective risk analysis tool for primary graft dysfunction (PGD), a severe complication in HTx. Existing score systems for predicting PGD lack superior predictive capability and are often too complex for routine clinical use.
View Article and Find Full Text PDFInt J Clin Pediatr Dent
December 2024
Department of Pedodontics, Government Dental College, Alappuzha, Kerala, India.
Background: Pain management in pediatric patients during dental procedures is very important. Here, the traditional method of behavior management is compared with novel methods.
Aim: To compare and determine the effectiveness of an external cooling and vibrating device vs counterstimulation with the conventional technique in reducing the fear and discomfort of pediatric dental patients aged 5-7 years during inferior alveolar nerve block (IANB).
J Med Imaging (Bellingham)
January 2025
U.S. Food and Drug Administration, Office of Science and Engineering Labs, Division of Imaging, Diagnostics, and Software Reliability, Silver Spring, Maryland, United States.
Purpose: We evaluate the impact of charge summing correction on a cadmium telluride (CdTe)-based photon-counting detector in breast computed tomography (CT).
Approach: We employ a custom-built laboratory benchtop system using the X-THOR FX30 0.75-mm CdTe detector (Varex Imaging, Salt Lake City, Utah, United States) with a pixel pitch of 0.
NMR Biomed
March 2025
Centre for Advanced Imaging, The University of Queensland, St Lucia, Queensland, Australia.
In this work, we introduce spatial and chemical saturation options for artefact reduction in magnetic resonance fingerprinting (MRF) and assess their impact on T and T mapping accuracy. An existing radial MRF pulse sequence was modified to enable spatial and chemical saturation. Phantom experiments were performed to demonstrate flow artefact reduction and evaluate the accuracy of the T and T maps.
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