ArticleACS chemical neuroscience2013
Aβ42-binding peptoids as amyloid aggregation inhibitors and detection ligands.
Article in ACS chemical neuroscience, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers, 1 of them a synthesis that pooled it.
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Who cites it
12 citing papers in PubMed, 1 synthesis or guideline pooled it, 42 citations in OpenAlex.
- A Systematic Review of Antiamyloidogenic and Metal-Chelating Peptoids: Two Structural Motifs for the Treatment of Alzheimer's Disease.Molecules (Basel, Switzerland) · 2018Pooled it
- Neuroprotective efficiency of celecoxib vesicular bilosomes for the management of lipopolysaccharide-induced Alzheimer in mice employing 2Inflammopharmacology · 2024Article
- Targeting Protein-Protein Interfaces with Peptides: The Contribution of Chemical Combinatorial Peptide Library Approaches.International journal of molecular sciences · 2023Review
- Recent Advances in the Application Peptide and Peptoid in Diagnosis Biomarkers of Alzheimer's Disease in Blood.Frontiers in molecular neuroscience · 2021Review
- Galectin-3 promotes Aβ oligomerization and Aβ toxicity in a mouse model of Alzheimer's disease.Cell death and differentiation · 2020Article
- Chain-End Modifications and Sequence Arrangements of Antimicrobial Peptoids for Mediating Activity and Nano-Assembly.Frontiers in chemistry · 2020Article
- Therapy of Dredging the Bowels Enhanced the Neuroprotective Effect of Nourishing Kidney Herbs on Hippocampal Cholinergic System in Alzheimer's Disease Model Rat Induced by AEvidence-based complementary and alternative medicine : eCAM · 2018Article
- Towards vast libraries of scaffold-diverse, conformationally constrained oligomers.Chemical communications (Cambridge, England) · 2016Article
- Transthyretin-derived peptides as β-amyloid inhibitors.ACS chemical neuroscience · 2014Article
- Rationally designed peptoids modulate aggregation of amyloid-beta 40.ACS chemical neuroscience · 2014Article
- Roadblocks for integration of novel biomarker concepts into clinical routine: the peptoid approach.Alzheimer's research & therapy · 2014Review
- Protein folding and aggregation into amyloid: the interference by natural phenolic compounds.International journal of molecular sciences · 2013Review
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
Alzheimer's disease (AD) is the most common form of dementia and currently affects 5.4 million Americans. A number of anti-Aβ (beta amyloid) therapeutic agents have been developed for AD, but so far all of them failed in clinic. Here we used peptoid chemistry to develop ligands selective for Aβ42. Peptoids are N-substituted glycine oligomers, a class of peptidomimics. We synthesized an on-bead peptoid library consisting of 38,416 unique peptoids. The generated peptoid library was screened and arrays of Aβ42-selective peptoid ligands were identified. One of those peptoid ligands, IAM1 (inhibitor of amyloid), and the dimeric form (IAM1)2 were synthesized and evaluated in a variety of biochemical assays. We discovered that IAM1 selectively binds to Aβ42, while the dimeric derivative (IAM1)2 has a higher affinity for Aβ42. Furthermore, we demonstrated that IAM1 and (IAM1)2 were able to inhibit the aggregation of Aβ42 in a concentration-dependent manner, and that (IAM1)2 protected primary hippocampal neurons from the Aβ-induced toxicity in vitro. These results suggest that IAM1 and (IAM1)2 are specific Aβ42 ligands with antiaggregation and neuroprotective properties. IAM1, (IAM1)2, and their derivatives hold promise as Aβ42 detection agents and as lead compounds for the development of AD therapeutic agents.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.