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http://dx.doi.org/10.1016/j.mvr.2024.104709 | DOI Listing |
Bioorg Chem
August 2025
Guangxi Key Laboratory for Polysaccharide Materials and Modifications, School of Chemistry and Chemical Engineering, Guangxi Minzu University, Nanning 530006, China. Electronic address:
Investigating the molecular interaction mechanisms of angiotensin-converting enzyme (ACE) inhibitory peptides is valuable in antihypertensive drug development. In this study, we designed two novel peptide variants, Leu-Leu-Phe (LLF) and Leu-Leu-Pro (LLP), by substituting the C-terminal tyrosine (Tyr) in casein-derived Leu-Leu-Tyr (LLY) with phenylalanine (Phe) and proline (Pro), respectively, to investigate the impact of C-terminal amino acid properties of peptide on ACE inhibition. The ACE inhibitory activity, inhibition kinetics, peptides-ACE binding mechanisms, and LLF and LLP conformational relationship were systematically investigated with comparative assessment against the LLY.
View Article and Find Full Text PDFInt J Mol Sci
August 2025
Laboratory of Centre for Preclinical Research, Department of Experimental and Clinical Physiology, Medical University of Warsaw, 02-097 Warsaw, Poland.
Thirst is usually characterized as an unpleasant sensation provoking drinking of water. The purpose of the present review is to draw attention to the importance of thirst in overall regulation of body fluid homeostasis in health and pathology. Intensity of thirst is determined by signals generated in multiple groups of osmosensitive neurons engaged in dipsogenic and antidipsogenic activities, which are located in the brain cortex, the insula, the amygdala, the median preoptic area, the hypothalamic nuclei and the organum vasculosum laminae terminalis.
View Article and Find Full Text PDFLife (Basel)
August 2025
Institute of Microbiology Heilongjiang Academy of Sciences, Harbin 150010, China.
Hypertension is a major pathogenic contributor to cardiovascular diseases, primarily mediated through activation of the angiotensin-converting enzyme (ACE) system. Food-derived ACE-inhibitory peptides represent a promising alternative to synthetic drugs due to their favorable safety profile and minimal side effects. ACE-inhibitory peptides have been extensively identified from various foods, with their antihypertensive activity and molecular mechanisms comprehensively characterized through in vitro and in vivo studies.
View Article and Find Full Text PDFBiomedicines
July 2025
Department of Pharmacy Practice, Retzky College of Pharmacy, University of Illinois Chicago, Chicago, IL 60612, USA.
: Perioperative hypotension during kidney transplantation poses a risk to graft function and survival. Angiotensin II (AngII) is an endogenous vasoconstrictor targeting the renin-angiotensin-aldosterone system (RAAS) to increase blood pressure. Black patients may have a different response to synthetic angiotensin II (AT2S) compared to non-Black patients, given differential expressions in renin profiles.
View Article and Find Full Text PDFRSC Med Chem
August 2025
Department of Medicinal Chemistry, BMC Uppsala University P.O. Box 574 SE-751 23 Uppsala Sweden
Inhibition of the insulin-regulated aminopeptidase (IRAP) is a promising therapeutic strategy for neurodegenerative disorders such as Alzheimer's disease, due to its role in cognitive processes. HA08, a macrocyclic peptidomimetic derived from angiotensin IV, is among the most potent known IRAP inhibitors (IC = 18 nM). However, detailed structure-activity relationship (SAR) studies at its C-terminus have been limited by synthetic constraints.
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