amyloid β

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Ligands
amyloid β (Human)

GtoPdb Ligand ID: 4865

Synonyms: amyloid β-peptide | beta-amyloid protein

Compound class: Endogenous peptide in human, mouse or rat

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

View interactive charts of activity data across species

References
1. Bardroff M, Bohrmann B, Brockhaus M, Huber W, Kretzschmar T, Loetscher H, Löhning C, Nordstedt C, Rothe C. (2010) variable regions peptides for immunizing against amyloid plaque formation; biodrug for dementia, Alzheimer's disease, neuropathy, Down's syndrome, Creutzfeld Jacob disease, Parkinson's disease, amyotropic lateral sclerosis; neuroprotectants; hemostatic agent. Patent number: US7794719. Assignee: Hoffmann-La Roche Ag, Morphosys Ag. Priority date: 20/02/2002. Publication date: 14/09/2010.
2. Bussiere T, Weinreb PH, Engber T, Rhodes K, Arndt J, Qian F, Dunstan RW, Patel S. (2014) A METHOD OF REDUCING BRAIN AMYLOID PLAQUES USING ANTI-Aß ANTIBODIES. Patent number: WO2014089500. Assignee: Biogen Idec International Neuroscience Gmbh. Priority date: 07/12/2012. Publication date: 12/06/2014.
3. Choi SR, Golding G, Zhuang Z, Zhang W, Lim N, Hefti F, Benedum TE, Kilbourn MR, Skovronsky D, Kung HF. (2009) Preclinical properties of 18F-AV-45: a PET agent for Abeta plaques in the brain. J Nucl Med, 50 (11): 1887-94. [PMID:19837759]
4. Dewji NN, Singer SJ, Masliah E, Rockenstein E, Kim M, Harber M, Horwood T. (2015) Peptides of Presenilin-1 Bind the Amyloid Precursor Protein Ectodomain and Offer a Novel and Specific Therapeutic Approach to Reduce ß-Amyloid in Alzheimer's Disease. PLoS ONE, 10 (4): e0122451. [PMID:25923432]
5. Garber K. (2012) Genentech's Alzheimer's antibody trial to study disease prevention. Nat Biotechnol, 30 (8): 731-2. [PMID:22871696]
6. Gellerfors P, Lannfelt L, Sehlin D, Pettersson FE, Englund H. (2011) Protofibril selective antibodies and the use thereof. Patent number: US8025878B2. Assignee: Bioarctic Neuroscience AB. Priority date: 23/03/2006. Publication date: 27/09/2011.
7. Holtzman DM, DeMattos R, Bales KR, Paul SM, Tsurushita N, Vasquez M. (2007) Humanized antibodies that sequester abeta peptide. Patent number: US7195761. Assignee: Eli Lilly And Company, Washington University. Priority date: 24/02/2002. Publication date: 27/03/2007.
8. Le Y, Gong W, Tiffany HL, Tumanov A, Nedospasov S, Shen W, Dunlop NM, Gao JL, Murphy PM, Oppenheim JJ et al.. (2001) Amyloid (beta)42 activates a G-protein-coupled chemoattractant receptor, FPR-like-1. J Neurosci, 21 (2): RC123. [PMID:11160457]
9. Miles LA, Crespi GA, Doughty L, Parker MW. (2013) Bapineuzumab captures the N-terminus of the Alzheimer's disease amyloid-beta peptide in a helical conformation. Sci Rep, 3: 1302. [PMID:23416764]
10. Pfeifer A, Pihlgren M, Muhs A, Watts R. (2011) Humanized anti-beta-amyloid antibody. Patent number: US7892544. Assignee: Ac Immune Sa, Genentech, Inc.. Priority date: 14/07/2006. Publication date: 22/10/2012.
11. Roher AE, Cribbs DH, Kim RC, Maarouf CL, Whiteside CM, Kokjohn TA, Daugs ID, Head E, Liebsack C, Serrano G et al.. (2013) Bapineuzumab alters aβ composition: implications for the amyloid cascade hypothesis and anti-amyloid immunotherapy. PLoS ONE, 8 (3): e59735. [PMID:23555764]
12. Rozema NB, Procissi D, Bertolino N, Viola KL, Nandwana V, Abdul N, Pribus S, Dravid V, Klein WL, Disterhoft JF et al.. (2020) Aβ oligomer induced cognitive impairment and evaluation of ACU193-MNS-based MRI in rabbit. Alzheimers Dement (N Y), 6 (1): e12087. [PMID:33072847]
13. Tiffany HL, Lavigne MC, Cui YH, Wang JM, Leto TL, Gao JL, Murphy PM. (2001) Amyloid-beta induces chemotaxis and oxidant stress by acting at formylpeptide receptor 2, a G protein-coupled receptor expressed in phagocytes and brain. J Biol Chem, 276 (26): 23645-52. [PMID:11316806]
14. Tucker S, Möller C, Tegerstedt K, Lord A, Laudon H, Sjödahl J, Söderberg L, Spens E, Sahlin C, Waara ER et al.. (2015) The murine version of BAN2401 (mAb158) selectively reduces amyloid-β protofibrils in brain and cerebrospinal fluid of tg-ArcSwe mice. J Alzheimers Dis, 43 (2): 575-88. [PMID:25096615]
15. Yu P, Cui M, Wang X, Zhang X, Li Z, Yang Y, Jia J, Zhang J, Ono M, Saji H et al.. (2012) ¹⁸F-labeled 2-phenylquinoxaline derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques. Eur J Med Chem, 57: 51-8. [PMID:23047223]
16. Zha Z, Choi SR, Ploessl K, Lieberman BP, Qu W, Hefti F, Mintun M, Skovronsky D, Kung HF. (2011) Multidentate (18)F-polypegylated styrylpyridines as imaging agents for Aβ plaques in cerebral amyloid angiopathy (CAA). J Med Chem, 54 (23): 8085-98. [PMID:22011144]

References

1. Bardroff M, Bohrmann B, Brockhaus M, Huber W, Kretzschmar T, Loetscher H, Löhning C, Nordstedt C, Rothe C. (2010)
variable regions peptides for immunizing against amyloid plaque formation; biodrug for dementia, Alzheimer's disease, neuropathy, Down's syndrome, Creutzfeld Jacob disease, Parkinson's disease, amyotropic lateral sclerosis; neuroprotectants; hemostatic agent.
Patent number: US7794719. Assignee: Hoffmann-La Roche Ag, Morphosys Ag. Priority date: 20/02/2002. Publication date: 14/09/2010.

2. Bussiere T, Weinreb PH, Engber T, Rhodes K, Arndt J, Qian F, Dunstan RW, Patel S. (2014)
A METHOD OF REDUCING BRAIN AMYLOID PLAQUES USING ANTI-Aß ANTIBODIES.
Patent number: WO2014089500. Assignee: Biogen Idec International Neuroscience Gmbh. Priority date: 07/12/2012. Publication date: 12/06/2014.

3. Choi SR, Golding G, Zhuang Z, Zhang W, Lim N, Hefti F, Benedum TE, Kilbourn MR, Skovronsky D, Kung HF. (2009)
Preclinical properties of 18F-AV-45: a PET agent for Abeta plaques in the brain.
J Nucl Med, 50 (11): 1887-94. [PMID:19837759]

4. Dewji NN, Singer SJ, Masliah E, Rockenstein E, Kim M, Harber M, Horwood T. (2015)
Peptides of Presenilin-1 Bind the Amyloid Precursor Protein Ectodomain and Offer a Novel and Specific Therapeutic Approach to Reduce ß-Amyloid in Alzheimer's Disease.
PLoS ONE, 10 (4): e0122451. [PMID:25923432]

5. Garber K. (2012)
Genentech's Alzheimer's antibody trial to study disease prevention.
Nat Biotechnol, 30 (8): 731-2. [PMID:22871696]

6. Gellerfors P, Lannfelt L, Sehlin D, Pettersson FE, Englund H. (2011)
Protofibril selective antibodies and the use thereof.
Patent number: US8025878B2. Assignee: Bioarctic Neuroscience AB. Priority date: 23/03/2006. Publication date: 27/09/2011.

7. Holtzman DM, DeMattos R, Bales KR, Paul SM, Tsurushita N, Vasquez M. (2007)
Humanized antibodies that sequester abeta peptide.
Patent number: US7195761. Assignee: Eli Lilly And Company, Washington University. Priority date: 24/02/2002. Publication date: 27/03/2007.

8. Le Y, Gong W, Tiffany HL, Tumanov A, Nedospasov S, Shen W, Dunlop NM, Gao JL, Murphy PM, Oppenheim JJ et al.. (2001)
Amyloid (beta)42 activates a G-protein-coupled chemoattractant receptor, FPR-like-1.
J Neurosci, 21 (2): RC123. [PMID:11160457]

9. Miles LA, Crespi GA, Doughty L, Parker MW. (2013)
Bapineuzumab captures the N-terminus of the Alzheimer's disease amyloid-beta peptide in a helical conformation.
Sci Rep, 3: 1302. [PMID:23416764]

10. Pfeifer A, Pihlgren M, Muhs A, Watts R. (2011)
Humanized anti-beta-amyloid antibody.
Patent number: US7892544. Assignee: Ac Immune Sa, Genentech, Inc.. Priority date: 14/07/2006. Publication date: 22/10/2012.

11. Roher AE, Cribbs DH, Kim RC, Maarouf CL, Whiteside CM, Kokjohn TA, Daugs ID, Head E, Liebsack C, Serrano G et al.. (2013)
Bapineuzumab alters aβ composition: implications for the amyloid cascade hypothesis and anti-amyloid immunotherapy.
PLoS ONE, 8 (3): e59735. [PMID:23555764]

12. Rozema NB, Procissi D, Bertolino N, Viola KL, Nandwana V, Abdul N, Pribus S, Dravid V, Klein WL, Disterhoft JF et al.. (2020)
Aβ oligomer induced cognitive impairment and evaluation of ACU193-MNS-based MRI in rabbit.
Alzheimers Dement (N Y), 6 (1): e12087. [PMID:33072847]

13. Tiffany HL, Lavigne MC, Cui YH, Wang JM, Leto TL, Gao JL, Murphy PM. (2001)
Amyloid-beta induces chemotaxis and oxidant stress by acting at formylpeptide receptor 2, a G protein-coupled receptor expressed in phagocytes and brain.
J Biol Chem, 276 (26): 23645-52. [PMID:11316806]

14. Tucker S, Möller C, Tegerstedt K, Lord A, Laudon H, Sjödahl J, Söderberg L, Spens E, Sahlin C, Waara ER et al.. (2015)
The murine version of BAN2401 (mAb158) selectively reduces amyloid-β protofibrils in brain and cerebrospinal fluid of tg-ArcSwe mice.
J Alzheimers Dis, 43 (2): 575-88. [PMID:25096615]

15. Yu P, Cui M, Wang X, Zhang X, Li Z, Yang Y, Jia J, Zhang J, Ono M, Saji H et al.. (2012)
¹⁸F-labeled 2-phenylquinoxaline derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques.
Eur J Med Chem, 57: 51-8. [PMID:23047223]

16. Zha Z, Choi SR, Ploessl K, Lieberman BP, Qu W, Hefti F, Mintun M, Skovronsky D, Kung HF. (2011)
Multidentate (18)F-polypegylated styrylpyridines as imaging agents for Aβ plaques in cerebral amyloid angiopathy (CAA).
J Med Chem, 54 (23): 8085-98. [PMID:22011144]

amyloid β

GtoPdb Ligand ID: 4865

Ligand Activity Visualisation Charts