Transient Aggregation-Prone States in Disordered Proteins as Therapeutic Targets: The Amyloid-β Case

The amyloid-β (Aβ) peptide is an intrinsically disordered protein whose self-association into toxic oligomers underlies Alzheimer's disease. Because of its dynamic and heterogeneous nature, identifying the conformational states that nucleate aggregation remains a central challenge. In this work, we introduce a chemically interpretable descriptor of amyloidogenic propensity derived from self-docking analyses of conformational ensembles generated through temperature-replica exchange molecular dynamics (T-REMD) using different and complementary force fields. This descriptor classifies individual conformers within the generated ensembles according to their intrinsic aggregation tendency, enabling the identification of metastable, aggregation-prone states. The resulting ensembles reproduce experimental observables, and their classification based on amyloidogenic propensity provides a consistent structural basis for the rationalization and study of these metastable conformers. As a test, we demonstrate that the molecular chaperone DNAJB6, experimentally known to bind amyloidogenic conformations, preferentially interacts with aggregation-prone conformers, thus supporting both the proposed protocol and the consistency of the classification scheme. More broadly, this framework outlines a potentially generalizable strategy to identify metastable states in intrinsically disordered proteins as prospective pharmacological targets to help develop drugs or biomolecules capable of inhibiting the early stages of their aggregation.

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Publication Details

Journal
Journal of Chemical Information and Modeling
Published
2026-04-14
DOI
https://doi.org/10.1021/acs.jcim.6c00270
Primary Topic
Protein Structure and Dynamics
Type
article
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article

Transient Aggregation-Prone States in Disordered Proteins as Therapeutic Targets: The Amyloid-β Case

Valentina Tozzini, Luca Bellucci, Margherita Bini
Journal of Chemical Information and Modeling
Protein Structure and Dynamics
article

Transient Aggregation-Prone States in Disordered Proteins as Therapeutic Targets: The Amyloid-β Case

Valentina Tozzini, Luca Bellucci, Margherita Bini
article en

Abstract

The amyloid-β (Aβ) peptide is an intrinsically disordered protein whose self-association into toxic oligomers underlies Alzheimer's disease. Because of its dynamic and heterogeneous nature, identifying the conformational states that nucleate aggregation remains a central challenge. In this work, we introduce a chemically interpretable descriptor of amyloidogenic propensity derived from self-docking analyses of conformational ensembles generated through temperature-replica exchange molecular dynamics (T-REMD) using different and complementary force fields. This descriptor classifies individual conformers within the generated ensembles according to their intrinsic aggregation tendency, enabling the identification of metastable, aggregation-prone states. The resulting ensembles reproduce experimental observables, and their classification based on amyloidogenic propensity provides a consistent structural basis for the rationalization and study of these metastable conformers. As a test, we demonstrate that the molecular chaperone DNAJB6, experimentally known to bind amyloidogenic conformations, preferentially interacts with aggregation-prone conformers, thus supporting both the proposed protocol and the consistency of the classification scheme. More broadly, this framework outlines a potentially generalizable strategy to identify metastable states in intrinsically disordered proteins as prospective pharmacological targets to help develop drugs or biomolecules capable of inhibiting the early stages of their aggregation.

Journal of Chemical Information and Modeling
Scuola Normale Superiore (IT), Istituto Nanoscienze (IT), Istituto Nazionale di Fisica Nucleare, Sezione di Pisa (IT)
Openalex Percentile: Top 16%
Protein Structure and Dynamics
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Transient Aggregation-Prone States in Disordered Proteins as Therapeutic Targets: The Amyloid-β Case — Valentina Tozzini, Luca Bellucci, et al. · Journal of Chemical Information and Modeling (2026) | TGRS Research Map | TGRS