What question did this study set out to answer?

Determine whether recombinant neutral endopeptidase (rNEP) functions as an endothelin-converting enzyme by processing big endothelin-1 (BET-1) into mature endothelin-1 (ET-1).

August 1, 1993British Journal of PharmacologyOpen Access

Metabolism of endothelin‐1 and big endothelin‐1 by recombinant neutral endopeptidase EC.3.4.24.11

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Determine whether recombinant neutral endopeptidase (rNEP) functions as an endothelin-converting enzyme by processing big endothelin-1 (BET-1) into mature endothelin-1 (ET-1).
Incubated radiolabeled [125I]-ET-1 and [125I]-BET-1 in vitro with recombinant neutral endopeptidase (rNEP) at concentrations of 1 µg/ml and 10 µg/ml.
Assessed enzyme inhibition and peptide protection using phosphoramidon (10 µM) and SQ-28,603 (100 µM).
Incubation with rNEP degraded [125I]-ET-1 within minutes at 1 µg/ml and caused complete cleavage within seconds at 10 µg/ml, which was fully blocked by phosphoramidon and SQ-28,603.
Degradation of [125I]-BET-1 occurred substantially slower than that of [125I]-ET-1, and no intact [125I]-ET-1 was detected following incubation with rNEP.

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Implication

In vitro assay demonstrates rapid cleavage of endothelin-1 by neutral endopeptidase, indicating the enzyme degrades rather than activates the peptide.

Cite This Study

Abassi et al. (1993) studied this question.

synapsesocial.com/papers/6a7c55518ded3476ac0857ce https://doi.org/10.1111/j.1476-5381.1993.tb13724.x

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Implication

In vitro assay demonstrates rapid cleavage of endothelin-1 by neutral endopeptidase, indicating the enzyme degrades rather than activates the peptide.

Metabolism of endothelin‐1 and big endothelin‐1 by recombinant neutral endopeptidase EC.3.4.24.11

Key Points

Discussion

Implication

Cite This Study

Metabolism of endothelin‐1 and big endothelin‐1 by recombinant neutral endopeptidase EC.3.4.24.11

Key Points

Discussion

Implication

Cite This Study

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