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. The structure of the soluble extracellular domain (residues 55–750) of rabbit neprilysin was solved both in its native form at 2.1 Å ...
Shaunivan L, Labiuk +2 more
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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
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Thiorphan reprograms neurons to promote functional recovery after spinal cord injury. [PDF]
NatureAbstract 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
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Thiorphan and retro-thiorphan display equivalent interactions when bound to crystalline thermolysin [PDF]
Biochemistry, 1989 The three-dimensional structures of (S)-thiorphan and (R)-retro-thiorphan bound to thermolysin have been determined crystallographically and refined to residuals of 0.183 and 0.187 at 1.7-A resolution. Thiorphan [N-[(S)-2-(mercaptomethyl)-1-oxo-3-phenylpropyl]glycine] [HSCH2CH(CH2C6H5)CONHC-H2COOH] and retro-thiorphan [[[(R)-1-(mercaptomethyl)-2 ...
S L, Roderick +3 more
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Telmisartan and thiorphan combination treatment attenuates fibrosis and apoptosis in preventing diabetic cardiomyopathy [PDF]
Cardiovascular Research, 2018 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 of a novel combination of telmisartan [angiotensin receptor blocker (ARB)] and thiorphan [neprilysin ...
Vajir, Malek, Anil Bhanudas, Gaikwad
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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
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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.
Medja, Fadia +9 more
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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.
Hans, Lentzen, Palenker, Jochen
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Thiorphan, tiopronin, and related analogs as substrates and inhibitors of peptidylglycine α‐amidating monooxygenase (PAM) [PDF]
FEBS Letters, 2005 Peptidyglycine α‐amidating monooxygenase is a copper‐ and zinc‐dependent, bifunctional enzyme that catalyzes the cleavage of glycine‐extended peptides or N‐acylglycines to the corresponding amides and glyoxylate. This reaction is a key step in the biosynthesis of bioactive α‐amidated peptides and, perhaps, the primary fatty acids amides also.
McIntyre, Neil R. +4 more
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Pharmacophore-Based Identification and Molecular Characterization of Potent Neprilysin Inhibitors: Biochemical and Therapeutic Implications for Cardiovascular Diseases. [PDF]
Chem Biol Drug DesPharmacophore‐based virtual screening and molecular dynamics identified pentagalloylglucose and tannic acid as potent, non‐toxic neprilysin inhibitors. These natural compounds demonstrated strong binding affinity and stable interactions with the catalytic Zn2+ site, offering promising leads for cardiovascular drug development. ABSTRACT Neprilysin (NEP),
Kuo CT, Wu YC, Li JM, Ju TC, Tseng TS.
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