Publications by authors named "X Iturrioz"

Background: To protect patients after myocardial infarction (MI) and preserve cardiac function, the development of new therapeutics remains an important issue. Apelin, a neuro-vasoactive peptide, increases aqueous diuresis and cardiac contractility while reducing vascular resistance. However, its in vivo half-life is very short.

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  • Researchers have developed a new fluorescent unnatural amino acid called Alared, designed for environmental sensitivity and efficient operation in the red part of the light spectrum.
  • Alared can be incorporated into bioactive peptides and exhibits varying fluorescence properties based on its surrounding environment, making it useful for studying biomolecular interactions.
  • The ability to track Alared-labeled peptides in live cells with minimal interference allows for better understanding of receptor activation and peptide binding behavior in cellular contexts.
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  • The renin-angiotensin system (RAS) is crucial for regulating heart and blood vessel functions, involving key components like ACE and the AT1 and AT2 receptors.
  • While ACE and AT1 are targets for hypertension treatments, the AT2 receptor's role remains less understood and underutilized.
  • Researchers discovered a new toxin called A-CTX-cMila from Brazilian viper venom, showing strong selectivity for the AT1 receptor and blocking various cellular pathways, marking it as the first animal toxin known to impact angiotensin II receptors.
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Herein, we describe a catalyst-free thia-Diels-Alder cycloaddition for the chemoselective labeling of fully deprotected phosphonodithioester-peptides in solution with fluorophores functionalized with an exocyclic diene. The reaction was optimized on the model tripeptide containing a lysine residue, which enabled its rapid and straightforward labeling with three different fluorophores (fluorescein, lissamine rhodamine B, and squaraine) in very mild conditions (HO/PrOH, 37 °C, 1 h). The reaction was then successfully applied to the chemoselective labeling of fully deprotected apelin-13 with squaraine dye.

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High blood pressure and consequential cardiovascular diseases are among the top causes of death worldwide. The apelinergic (APJ) system has emerged as a promising target for the treatment of cardiovascular issues, especially prevention of ischemia reperfusion (IR) injury after a heart attack or stroke. However, rapid degradation of the endogenous apelin peptides limits their use as therapeutic agents.

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