What is the clinical evidence from this study?

Intervention: furylacryloyl (fa)-amino acid derivatives. Primary outcome: Binding affinity and active site mapping of ACE.

What does this research mean for the field?

Transferred NOE spectroscopy enables active site mapping and rapid mixture-based screening of ligand binding specificity for angiotensin-converting enzyme, demonstrating selective binding of fa-Phe to the S1 and S2 subsites. Novelty: ClaimNovelty.METHODOLOGICAL. Consensus alignment: ConsensusAlignment.NEUTRAL.

May 16, 2000Journal of Medicinal Chemistry

Mapping the Active Site of Angiotensin-Converting Enzyme by Transferred NOE Spectroscopy

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Key result

Transferred NOESY experiments identify strong ACE binders to enable rapid active site mapping.

Population

Angiotensin-converting enzyme and five furylacryloyl-amino acid derivatives (fa-Phe, fa-Phe-Phe…

Design

Preclinical

Authors

MMMoriz MayerBoehringer Ingelheim (Austria)BMBernd MeyerMonash University

Discussion

Member takes

Implication

May aid in vitro ACE ligand screening; leaves open clinical translation from this Level 5 animal study.

Structured PICO

Population

Angiotensin-converting enzyme (ACE) (MW = 130 kDa) and five furylacryloyl (fa)-amino acid derivatives (fa-Phe, fa-Phe-Phe, fa-Gly-Leu-NH(2), fa-Ala-Lys, and fa-Trp)

Intervention

Transferred NOESY experiments to study binding interactions

Outcome

Binding affinities and mapping of the active site of ACEsurrogate

Transferred NOE spectroscopy allows for rapid screening of binding specificity and mapping of the active site of ACE from mixtures of ligands.

Cite This Study

Mayer et al. (2000) studied this question. furylacryloyl (fa)-amino acid derivatives was evaluated on Binding affinity and active site mapping of ACE. Transferred NOESY experiments identified that fa-Phe, fa-Trp, and fa-Gly-Leu-NH(2) bind strongly to ACE, allowing rapid screening of binding specificity and mapping of the active site.

synapsesocial.com/papers/6aa5bc5227cf4f5fd98e3278 https://doi.org/10.1021/jm990194x

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Mapping the Active Site of Angiotensin-Converting Enzyme by Transferred NOE Spectroscopy

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Mapping the Active Site of Angiotensin-Converting Enzyme by Transferred NOE Spectroscopy

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Also Consider