CRISPR/Cas9-engineering of Kell null erythrocytes to unveil host targeted irresistible antimalarial [PDF]
Communications BiologyMalaria elimination faces challenges from drug resistance, stemming from mutations within the parasite’s genetic makeup. Genetic adaptations in key erythrocyte proteins offer malaria protection in endemic regions.
Geeta Kumari +15 more
doaj +2 more sources
Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity [PDF]
Biomedicines, 2021 Background: Alzheimer’s disease (AD) involves impairment of Aβ clearance. Neprilysin (NEP) is the most efficient Aβ peptidase. Enhancement of the activity or expression of NEP may provide a prominent therapeutic strategy against AD.
Dimitris Matiadis +7 more
doaj +2 more sources
Exploiting the angiotensin-converting enzyme pathway to augment endogenous opioid signaling [PDF]
Communications BiologyAngiotensin Converting Enzyme (ACE) impacts hemodynamics by regulating the conversion of angiotensin I to the vasoconstricting angiotensin II. We recently identified a non-canonical central role of ACE in the degradation of enkephalin heptapeptide, Met ...
Prakashkumar Dobariya +4 more
doaj +2 more sources
Neprilysin Degrades Both Amyloid β Peptides 1–40 and 1–42 Most Rapidly and Efficiently among Thiorphan- and Phosphoramidon-sensitive Endopeptidases* [PDF]
Journal of Biological Chemistry, 2001 To identify the amyloid β peptide (Aβ) 1–42-degrading enzyme whose activity is inhibited by thiorphan and phosphoramidon in vivo, we searched for neprilysin (NEP) homologues and cloned neprilysin-likepeptidase (NEPLP) α, NEPLP β, and NEPLP γ cDNAs.
K. Shirotani +11 more
semanticscholar +2 more sources
Thiorphan enhances bradykinin-induced vascular relaxation in hypoxic/hyperkalaemic porcine coronary artery [PDF]
Journal of Pharmacy and Pharmacology, 2003 Abstract Relaxation induced by bradykinin is diminished by hypoxia in epicardial coronary arteries. The bradykinin-degrading enzyme, neutral endopeptidase (NEP, EC.3.4.24.11), is a potential target for coronary artery vasodilators. In this study, we examined the effect of thiorphan, an inhibitor of NEP, on the tone of porcine isolated ...
Irén Krassói +2 more
openalex +3 more sources
A comprehensive review of the pharmacodynamics, pharmacokinetics and clinical effects of the neutral endopeptidase inhibitor racecadotril [PDF]
Frontiers in Pharmacology, 2012 Racecadotril, via its active metabolite thiorphan, is an inhibitor of the enzyme neutral endopeptidase (NEP, EC 3.4.24.11), thereby increasing exposure to NEP including enkephalins and atrial natriuretic peptide.
Marion eEberlin +2 more
doaj +5 more sources
Exogenous Angiotensin I Metabolism in Aorta Isolated from Streptozotocin Treated Diabetic Rats [PDF]
Journal of Diabetes Research, 2016 Purpose. Products of angiotensin (ANG) I metabolism may predispose to vascular complications of diabetes mellitus. Methods. Diabetes was induced with streptozotocin (75 mg/kg i.p.).
P. P. Wołkow +6 more
doaj +2 more sources
Japanese Journal of Pharmacology, 1986 The contents of [Met5]-enkephalin and its four hydrolysis products, Tyr, Tyr-Gly, Tyr-Gly-Gly, and Tyr-Gly-Gly-Phe, in the sample obtained after enkephalin was incubated with tissues in either the absence or the presence of the peptidase inhibitor were ...
T. Hiranuma, T. Oka
semanticscholar +2 more sources
Significance of CD10 for Mucosal Immunomodulation by β-Casomorphin-7 in Exacerbation of Ulcerative Colitis [PDF]
Current Issues in Molecular Biologyβ-Casomorphin-7 (BCM), a breakdown product of milk β-casein, exhibits opioid activity. Opioids are known to affect the immune system, but the effects of BCM on ulcerative colitis (UC) are not clear.
Yoshihiro Miyagawa +9 more
doaj +2 more sources
Opioid Withdrawal Abruptly Disrupts Amygdala Circuit Function by Reducing Peptide Actions. [PDF]
J Neurosci, 2023 While the physical signs of opioid withdrawal are most readily observable, withdrawal insidiously drives relapse and contributes to compulsive drug use, by disrupting emotional learning circuits.
Gregoriou GC +4 more
europepmc +3 more sources