Results 21 to 30 of about 1,034 (134)

RhII‐Catalyzed De‐symmetrization of Ethane‐1,2‐dithiol and Propane‐1,3‐dithiol Yields Metallo‐β‐lactamase Inhibitors

open access: yesChemMedChem, Volume 16, Issue 22, Page 3410-3417, November 19, 2021., 2021
Thiols are potent inhibitors of metallo‐β‐lactamases, major resistance factors in Gram‐negative bacteria. Rh(II)‐based coupling procedure of dithiols to diazo building blocks was adopted for diversity‐oriented synthesis of a library of metallo‐β‐lactamase inhibitors.
Mikhail Krasavin   +13 more
wiley   +1 more source

A CD10‐OGP Membrane Peptolytic Signaling Axis in Fibroblasts Regulates Lipid Metabolism of Cancer Stem Cells via SCD1

open access: yesAdvanced Science, Volume 8, Issue 19, October 6, 2021., 2021
CD10, a transmembrane hydrolase expressed by a subset of carcinoma‐associated fibroblasts, drives tumor progression by degrading an anti‐tumoral peptide, osteogenic growth peptide (OGP). OGP impairs tumor lipid desaturation and consequently suppresses cancer stem cells (CSCs). This study sheds new light on a nexus between the niche and lipid metabolism
Shubin Yu   +18 more
wiley   +1 more source

The effect of neprilysin and renin inhibition on the renal dysfunction following ischemia‐reperfusion injury in the rat

open access: yesPhysiological Reports, Volume 9, Issue 6, March 2021., 2021
RAS blockade by a renin inhibitor (aliskiren) or neprilysin inhibition by sacubitril separately led to significant attenuation in the renal IRI‐induced renal dysfunction. The combination of aliskiren and sacubitril was more effective than either one alone. Abstract The natriuretic peptide (NP) system counter‐regulates the renin‐angiotensin system (RAS),
Fayez T. Hammad   +6 more
wiley   +1 more source

A Cell Cycle Progression‐Derived Gene Signature to Predict Prognosis and Therapeutic Response in Hepatocellular Carcinoma

open access: yesDisease Markers, Volume 2021, Issue 1, 2021., 2021
Objective. Dysregulation of cell cycle progression (CCP) is one of the hallmarks of cancer. Here, our study is aimed at developing a CCP‐derived gene signature for predicting high‐risk population of hepatocellular carcinoma (HCC). Methods. Our study retrospectively analyzed the transcriptome profiling and clinical information of HCC patients from The ...
Yongfeng Hui   +7 more
wiley   +1 more source

Substance P and thiorphan synergically enhance angiogenesis in wound healing [PDF]

open access: yesTissue 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
openaire   +2 more sources

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

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   +1 more source

Localization of the thiorphan‐sensitive endopeptidase, termed enkephalinase A, on glial cells [PDF]

open access: yesFEBS 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
openaire   +2 more sources

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

open access: yesMolecules, 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   +1 more source

Exogenous Angiotensin I Metabolism in Aorta Isolated from Streptozotocin Treated Diabetic Rats

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   +1 more source

Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice [PDF]

open access: yesBrain, 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
openaire   +3 more sources

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