Alpha Ketoglutarate Downregulates the Neutral Endopeptidase and Enhances the Growth Inhibitory Activity of Thiorphan in Highly Aggressive Osteosarcoma Cells [PDF]
Molecules, 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 +5 more sources
Evaluation of In-Batch and In-Flow Synthetic Strategies towards the Stereoselective Synthesis of a Fluorinated Analogue of Retro-Thiorphan [PDF]
Molecules, 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 +5 more sources
Thiorphan reprograms neurons to promote functional recovery after spinal cord injury. [PDF]
NatureWe previously identified an embryonic shift in the corticospinal motor neuronal transcriptome after spinal cord injury associated with successful axonal regeneration1.
van Niekerk EA +17 more
europepmc +5 more sources
Structures of soluble rabbit neprilysin complexed with phosphoramidon or thiorphan. [PDF]
Acta Crystallographica Section F Structural Biology Communications, 2019 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.
S. Labiuk, J. Sygusch, P. Grochulski
semanticscholar +5 more sources
Substance P and thiorphan synergically enhance angiogenesis in wound healing [PDF]
Tissue Engineering and Regenerative Medicine, 2016 Impaired angiogenesis is a common pathological characteristic of chronic wounds. Therefore, the regulation of angiogenesis is important for proper tissue repair. It was reported that substance P (SP) accelerates wound healing in a skin injury model. SP is degraded by neutral endopeptidase (NEP).
Jihyun Um +3 more
semanticscholar +5 more sources
Telmisartan and thiorphan combination treatment attenuates fibrosis and apoptosis in preventing diabetic cardiomyopathy [PDF]
Cardiovascular Research, 2018 Aims LCZ696, a first-generation dual angiotensin receptor-neprilysin inhibitor (ARNi), is effective in treating heart failure patients. However, the role of ARNis in treating diabetic cardiomyopathy is poorly understood. This study evaluates the efficacy
V. Malek, A. Gaikwad
semanticscholar +4 more sources
Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice. [PDF]
Brain, 2006 Excitotoxic damage appears to be a critical factor in the formation of perinatal brain lesions associated with cerebral palsy (CP). When injected into newborn mice, the glutamatergic analogue, ibotenate, produces cortical lesions and white matter cysts that mimic human perinatal brain lesions.
F. Medja +9 more
semanticscholar +5 more sources
Localization of the thiorphan‐sensitive endopeptidase, termed enkephalinase A, on glial cells [PDF]
FEBS Letters, 1983 Degradation of tritiated Leu‐enkephalin was studied in cultures of primary astrocytes from rat brain. The incubation experiments with a cell suspension revealed Tyr as the main tritiated metabolite; however, Tyr—Gly—Gly and Tyr—Gly were detectable as well.
Lentzen Hans, J. Palenker
semanticscholar +4 more sources
Complete differentiation between enkephalinase and angiotensin-converting enzyme inhibition by retro-thiorphan. [PDF]
Proceedings of the National Academy of Sciences, 1983 Thiorphan, N-[(R,S)-3-mercapto-2-benzylpropanoyl]glycine is a highly potent inhibitor (Ki = 3.5 nM) of "enkephalinase," a metalloendopeptidase cleaving the Gly-Phe bond (positions 3 and 4) of enkephalins in brain tissue. In accordance with this property, thiorphan displays antinociceptive activity after systemic administration.
B. Roques +4 more
semanticscholar +5 more sources
Integrating metabolomics, bionics, and culturomics to study probiotics-driven drug metabolism [PDF]
Frontiers 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