Transition Metal Ion FRET-Based Probe to Study Cu(II)-Mediated Amyloid-β Ligand Binding


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Date

2024-01-24

Publication Type

Journal Article

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Abstract

Recent therapeutic strategies suggest that small peptides can act as aggregation inhibitors of monomeric amyloid-beta (Alpha beta) by inducing structural rearrangements upon complexation. However, characterizing the binding events in such dynamic and transient noncovalent complexes, especially in the presence of natively occurring metal ions, remains a challenge. Here, we deploy a combined transition metal ion Forster resonance energy transfer (tmFRET) and native ion mobility-mass spectrometry (IM-MS) approach to characterize the structure of mass- and charge-selected A beta complexes with Cu(II) ions (a quencher) and a potential aggregation inhibitor, a small neuropeptide named leucine enkephalin (LE). We show conformational changes of monomeric Alpha beta species upon Cu(II)-binding, indicating an uncoiled N-terminus and a close interaction between the C-terminus and the central hydrophobic region. Furthermore, we introduce LE labeled at the N-terminus with a metal-chelating agent, nitrilotriacetic acid (NTA). This allows us to employ tmFRET to probe the binding even in low-abundance and transient A beta-inhibitor-metal ion complexes. Complementary intramolecular distance and global shape information from tmFRET and native IM-MS, respectively, confirmed Cu(II) displacement toward the N-terminus of Alpha beta, which discloses the binding region and the inhibitor's orientation.

Publication status

published

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Volume

146 (3)

Pages / Article No.

2102 - 2112

Publisher

American Chemical Society

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Organisational unit

03430 - Zenobi, Renato / Zenobi, Renato check_circle

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Funding

178765 - Soft ionization mass spectrometry for studying noncovalent interactions (SNF)
ETH-07 15-1 - Native Biomolecular Ions in the Gas Physe? A Functional and Structural Approach (ETHZ)

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