Results 1 to 10 of about 2,059 (202)

Alpha Ketoglutarate Downregulates the Neutral Endopeptidase and Enhances the Growth Inhibitory Activity of Thiorphan in Highly Aggressive Osteosarcoma Cells [PDF]

open access: goldMolecules, 2022
Since natural substances are widely explored as epigenetic modulators of gene expression and epigenetic abnormalities are important causes of cancerogenesis, factors with pro-tumor activities subjected to epigenetic control, e.g., neutral endopeptidase ...
Magdalena Mizerska-Kowalska   +4 more
doaj   +4 more sources

Evaluation of In-Batch and In-Flow Synthetic Strategies towards the Stereoselective Synthesis of a Fluorinated Analogue of Retro-Thiorphan [PDF]

open access: goldMolecules, 2019
A stereoselective synthetic strategy for the preparation of trifluoromethylamine mimics of retro-thiorphan, involving a diastereoselective, metal-free catalytic step, has been studied in batch and afforded the target molecule in good yields and high ...
Margherita Pirola   +4 more
doaj   +4 more sources

Integrating metabolomics, bionics, and culturomics to study probiotics-driven drug metabolism [PDF]

open access: yesFrontiers in Pharmacology, 2023
Many drugs have been shown to be metabolized by the human gut microbiome, but probiotic-driven drug-metabolizing capacity is rarely explored. Here, we developed an integrated metabolomics, culturomics, and bionics framework for systematically studying ...
Bohai Li   +17 more
doaj   +2 more sources

CRISPR/Cas9-engineering of Kell null erythrocytes to unveil host targeted irresistible antimalarial [PDF]

open access: yesCommunications Biology
Malaria 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]

open access: yesBiomedicines, 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]

open access: yesCommunications Biology
Angiotensin 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

A comprehensive review of the pharmacodynamics, pharmacokinetics and clinical effects of the neutral endopeptidase inhibitor racecadotril [PDF]

open access: yesFrontiers 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]

open access: yesJournal 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

Significance of CD10 for Mucosal Immunomodulation by β-Casomorphin-7 in Exacerbation of Ulcerative Colitis [PDF]

open access: yesCurrent Issues in Molecular Biology
β-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]

open access: yesJ 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

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