amyloid β   Click here for help

GtoPdb Ligand ID: 4865

Synonyms: amyloid β-peptide | beta-amyloid protein
Comment: We give the sequence for the 42 amino acid peptide here, but note that use of the name β-amyloid generally refers to the ensemble of peptides of 40 to 43 residues excised from the precursor APP protein by the combined action of β- and γ-secretases. These peptides may be soluble monomers or oligomers and contribute to the formation of fibrils and plaques that are associated with Alzheimer's disease.

The amino acid sequences of alternative forms are;
1-40 DAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVV
1-42 DAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIA
1-43 DAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIAT

So far we have annotated three types of target relationships for β-amyloid:
1) antibodies directed against the peptide forms for depletion
2) aggregation antagonists
3) imaging reagents for detection
Species: Human
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Bioactivity Comments
Acumen Pharmaceuticals are developing the affinity matured, humanized, IgG2 monoclonal antibody ACU193 which binds to soluble amyloid-β oligomers rather than amyloid plaques [11]. As of July 2021, ACU193 was entering Phase 1 evaluation in trial NCT04931459, which will recruit participants who have been diagnosed with mild cognitive impairment or mild dementia due to Alzheimer's disease.
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
FPR2/ALX Hs Agonist Full agonist 7.0 pEC50 - 7,12
pEC50 7.0 [7,12]
Other ligands which bind to or alter the activity of this ligand
Key to terms and symbols Click column headers to sort
Ligand Sp. Type Action Value Parameter Concentration range (M) Reference
solanezumab Peptide Primary target of this compound Hs Antibody Binding 10.4 pKd - 6
pKd 10.4 (Kd 4x10-11 M) [6]
Description: Binding affinity for Aβ1-42 measured using proprietary BIAcore technology
gantenerumab Peptide Primary target of this compound Hs Antibody Binding 9.1 – 9.6 pKd - 1
pKd 9.1 – 9.6 (Kd 7x10-10 – 2.4x10-10 M) [1]
Description: Binding to Aβ40 and Aβ42
P8 [PMID: 25923432] Peptide Primary target of this compound Hs Inhibitor Binding 8.5 pKd - 4
pKd 8.5 (Kd 3.45x10-9 M) [4]
Description: Assessed using biolayer interferometry measuring the binding of the test peptide to the soluble ectodomain of APP.
P4 [PMID: 25923432] Peptide Primary target of this compound Hs Inhibitor Binding 7.8 pKd - 4
pKd 7.8 (Kd 1.61x10-8 M) [4]
Description: Assessed using biolayer interferometry measuring the binding of the test peptide to the soluble ectodomain of APP.
crenezumab Peptide Primary target of this compound Hs Antibody Binding >7.7 pKd - 5,9
pKd >7.7 (Kd <2x10-8 M) [5,9]
Description: Binding affinity to Aβ monomer
bapineuzumab Peptide Primary target of this compound Hs Antibody Binding:
Binding of soluble amyloid β(1-40)
7.1 pKd - 8,10
pKd 7.1 (Kd 8.9x10-8 M) Binding of soluble amyloid β(1-40) [8,10]
flutemetamol Small molecule or natural product Approved drug Primary target of this compound Ligand is labelled Ligand is radioactive Hs None Binding:
PET imaging agent for Aβ plaques in brain
9.1 pKi - 14
pKi 9.1 (Ki 7.4x10-10 M) PET imaging agent for Aβ plaques in brain [14]
florbetaben Small molecule or natural product Approved drug Primary target of this compound Ligand is labelled Ligand is radioactive Hs None Binding:
PET imaging agent for Aβ plaques in brain
8.6 pKi - 3
pKi 8.6 (Ki 2.22x10-9 M) PET imaging agent for Aβ plaques in brain [3]
Description: Inhibition of 18F-AV-45 binding to Aβ plaques in postmortem AD brain homogenates.
florbetapir Small molecule or natural product Approved drug Primary target of this compound Ligand is labelled Ligand is radioactive Hs None Binding:
PET imaging agent for Aβ plaques in brain
8.5 pKi - 13
pKi 8.5 (Ki 2.87x10-9 M) PET imaging agent for Aβ plaques in brain [13]
aducanumab Peptide Approved drug Primary target of this compound Hs Antibody Binding 9.4 pEC50 - 2
pEC50 9.4 (EC50 4x10-10 M) [2]
Description: Binding to recombinamt human Aβ 1-42
Ligand mentioned in the following text fields