Alpha Ketoglutarate Downregulates the Neutral Endopeptidase and Enhances the Growth Inhibitory Activity of Thiorphan in Highly Aggressive Osteosarcoma Cells [PDF]
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 +2 more sources
Integrating metabolomics, bionics, and culturomics to study probiotics-driven drug metabolism [PDF]
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]
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
Exploiting the angiotensin-converting enzyme pathway to augment endogenous opioid signaling [PDF]
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
Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity [PDF]
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
Structures of soluble rabbit neprilysin complexed with phosphoramidon or thiorphan [PDF]
Neutral endopeptidase (neprilysin; NEP) is a proteinase that cleaves a wide variety of peptides and has been implicated in Alzheimer's disease, cardiovascular conditions, arthritis and other inflammatory diseases. The structure of the soluble extracellular domain (residues 55–750) of rabbit neprilysin was solved both in its native form at 2.1 Å ...
Jürgen Sygusch +2 more
exaly +3 more sources
Integrated network pharmacology and bioinformatics analysis reveals MME as key target of Notoginsenoside R1 in diabetic nephropathy [PDF]
Background Diabetic nephropathy (DN) is a major diabetes complication and a primary cause of end-stage renal failure. Notoginsenoside R1 (NGR1) is known to reduce proteinuria, exert hypoglycemic effects, and enhance renal function in DN patients. However,
Xinyu Gan +7 more
doaj +2 more sources
Significance of CD10 for Mucosal Immunomodulation by β-Casomorphin-7 in Exacerbation of Ulcerative Colitis [PDF]
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
Thiorphan reprograms neurons to promote functional recovery after spinal cord injury. [PDF]
Abstract We previously identified an embryonic shift in the corticospinal motor neuronal transcriptome after spinal cord injury associated with successful axonal regeneration 1 .
van Niekerk EA +17 more
europepmc +3 more sources
Background and purpose: Although pain is one of the most common symptoms of diseases, it is often mismanaged due to limited access to painkillers and ineffectiveness, unacceptable side effects, or the possibility of abuse.
Mehdi Asadi +5 more
doaj +1 more source

