AI Article Synopsis
- The human Peptide Transporter 1 (hPepT1) effectively transports a variety of (pro-)drugs, making it a key player in drug absorption.
- Through solid supported membrane-based electrophysiology (SSME), researchers found that steady-state currents were recorded without peptide-induced pre-steady-state currents.
- The study identified the electrogenic co-transport of H+ and glycylglycine (GlyGly) across different pH levels, and determined specific inhibitor effects, helping advance the development of pharmacologically relevant drugs.
Article Abstract
The human Peptide Transporter 1 (hPepT1) is known for its broad substrate specificity and its ability to transport (pro-)drugs. Here, we present an in-depth comprehensive study of hPepT1 and its interactions with various substrates via solid supported membrane-based electrophysiology (SSME). Using hPepT1-containing vesicles, we could not identify any peptide induced pre-steady-state currents, indicating that the recorded peak currents reflect steady-state transport. Electrogenic co-transport of H/glycylglycine (GlyGly) was observed across a pH range of 5.0 to 9.0. The pH dependence is described by a bell-shaped activity curve and two pK values. K and relative V values of various canonical and non-canonical peptide substrates were contextualized with current mechanistic understandings of hPepT1. Finally, specific inhibition was observed for various inhibitors in a high throughput format, and IC50 values are reported. Taken together, these findings contribute to promoting the design and analysis of pharmacologically relevant substances.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bioelechem.2023.108573 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Investigating the LiO-AlO-BO matrix: A promising approach for immobilizing radioactive waste.
Appl Radiat Isot
January 2025
Department of Physics, Faculty of Science, Universiti Teknologi Malaysia, 81300, Skudai, Johor, Malaysia.
Dealing with radioactive waste, particularly from various industrial processes, poses significant challenges. This paper explores the use of lithium aluminate borate (Li-Al-B) glass matrix as an alternative method for immobilizing radioactive waste, focusing specifically on waste generated in tin smelting industries, known as tin slag. The study primarily concentrates on transforming tin slag, a byproduct abundant in Natural Occurring Radioactive Material (NORM), into a stable and safe form for disposal.
View Article and Find Full Text PDFNew Layered Boride NiPtB ( = 0.5) with a Ternary Derivative Structure of MoB.
Inorg Chem
January 2025
Institute of Solid State Physics, TU Wien, A-1040 Vienna, Austria.
A novel ternary boride, NiPtB ( = 0.5), was obtained by argon-arc melting of the elements followed by annealing at 750 °C. It exhibits a new structure type with the space group ( = 2.
View Article and Find Full Text PDFVAX014 Activates Tumor-Intrinsic STING and RIG-I to Promote the Development of Antitumor Immunity.
Mol Cancer Ther
January 2025
Vaxiion Therapeutics (United States), San Diego, California, United States.
In situ immunization (ISI) has emerged as a promising approach to bolster early phases of the cancer immunity cycle through improved T cell priming. One class of ISI agents, oncolytic viruses (OVs), has demonstrated clinical activity, but overall benefit remains limited. Mounting evidence suggests that due to their inherent vulnerability to antiviral effects of type I interferon (IFN), OVs have limited activity in solid tumors expressing stimulator of interferon genes (STING) and/or retinoic acid-inducible gene I (RIG-I).
View Article and Find Full Text PDFSelf-sovereign management scheme of personal health record with personal data store and decentralized identifier.
Comput Struct Biotechnol J
November 2024
Intellicode Cooperation, Republic of Korea.
Conventional personal health record (PHR) management systems are centralized, making them vulnerable to privacy breaches and single points of failure. Despite progress in standardizing healthcare data with the FHIR format, hospitals often lack efficient platforms for transferring PHRs, leading to redundant tests and delayed treatments. To address these challenges, we propose a decentralized PHR management system leveraging Personal Data Stores (PDS) and Decentralized Identifiers (DIDs) in line with the Web 3.
View Article and Find Full Text PDFA Database on Antibiotics and Antibiotic Resistance in Wastewater and Solid Waste from Pharmaceutical Industry Based on a Systematic Review.
China CDC Wkly
January 2025
State Key Laboratory of Environmental Aquatic Chemistry, Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing, China.
Residual antimicrobial agents in wastewater and solid waste from antimicrobial manufacturing facilities can potentially contaminate environments. The World Health Organization has established technical guidelines for managing antimicrobial resistance (AMR) in pharmaceutical wastewater and solid waste. However, the scarcity of publicly available data on antimicrobial manufacturing processes impedes the development of effective mitigation strategies.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!