journal article·2026

Modeling β-sheet breaker peptides across multiple resolutions: from neurological targets to liposomal membranes

Gulsah Gul

Nanoscale· Volume 18· Issue 11
Publisher page

Abstract

β-Sheet-breaker peptides can destabilize protein aggregates associated with neurological disorders, thereby interfering with fibril formation. Given the pivotal role of misfolded protein oligomers such as amyloid-β and α-synuclein in Alzheimer's and Parkinson's diseases, respectively, strategies that block β-sheet formation or perturb β-sheet-rich interactions are promising therapeutic approaches to mitigate neurotoxicity and slow disease progression. However, cross-applicability of inhibitor peptides between these diseases remains largely unexplored. Moreover, the clinical potential of β-sheet-breaker peptides is often limited by enzymatic degradation and restricted blood-brain barrier permeability, necessitating effective delivery systems. To address these challenges, lipid-based nanocarriers offer versatile platforms for peptide encapsulation and controlled release. Therefore, in this study, we collected 50 experimentally validated β-sheet-breaker peptides and examined their binding to amyloid-β and α-synuclein fibrils using molecular docking and molecular dynamics simulations. The selected peptide was further evaluated via atomistic and coarse-grained simulations within PEGylated phosphatidylcholine bilayers at varying cholesterol concentrations to assess peptide-lipid interactions and encapsulation potential. Our results indicate that certain peptides may target multiple misfolded proteins, supporting their potential for cross-disease repurposing. Among the candidates, KR peptides exhibited the highest binding free energy toward both targets, while RR peptides demonstrated robust binding with comparable affinity. Multiscale simulations revealed that RR peptides predominantly localize within PEG corona regions and interact with lipid phosphate headgroups, suggesting preferential surface adsorption on pre-formed liposomal fragments. Peptide insertion was more pronounced in unsaturated membranes, whereas cholesterol-rich, saturated membranes hindered permeation and bilayer-to-vesicle transition. Overall, this study provides the first molecular-level insight into the potential of experimentally validated peptides against different neurodegenerative targets and presents a lipid-based delivery strategy to enhance their bioavailability by elucidating the underlying molecular interactions.
Source: europepmc · Quality: candidate unverified · Source record ↗

Research context

OpenAlex topics: Alzheimer's disease research and treatments · Supramolecular Self-Assembly in Materials · Advanced Glycation End Products research

SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.

Affiliations

Department of Chemical and Biological Engineering, Koç University, İstanbul, Turkey

Funding

Türkiye Bilimsel ve Teknolojik Araştırma Kurumu

References (100+)

Show source-provided references
1. Poewe · Nat. Rev. Dis. Primers · 2017 · 3 · 110.1038/nrdp.2017.13 ↗
2. Knopman · Nat. Rev. Dis. Primers · 2021 · 7 · 110.1038/s41572-021-00269-y ↗
3. Wang · Aging Dis. · 2024 · 16 · 293710.14336/ad.2024.1071 ↗
4. Irvine · Mol. Med. · 2008 · 14 · 45110.2119/2007-00100.Irvine ↗
5. Kurosinski · Trends Mol. Med. · 2002 · 8 · 310.1016/S1471-4914(01)02246-8 ↗
6. Xie · BioMed Res. Int. · 2014 · 2014 · 64874010.1155/2014/648740 ↗
7. Caligiore · IBRO Neurosci. Rep. · 2022 · 13 · 33010.1016/j.ibneur.2022.09.007 ↗
8. Serpell · Biochim. Biophys. Acta, Mol. Basis Dis. · 2000 · 1502 · 1610.1016/S0925-4439(00)00029-6 ↗
9. Burré · J. Neurosci. · 2015 · 35 · 522110.1523/JNEUROSCI.4650-14.2015 ↗
10. Du · Int. J. Mol. Sci. · 2020 · 21 · 110.3390/ijms21228645 ↗
11. Bruinsma · MedChemComm · 2011 · 2 · 6010.1039/c0md00213e ↗
12. Mullin · Vib. Spectrosc. · 2020 · 111 · 10316810.1016/j.vibspec.2020.103168 ↗
13. Soto · Biochem. Biophys. Res. Commun. · 1996 · 226 · 67210.1006/bbrc.1996.1413 ↗
14. Soto · Nat. Med. · 1998 · 4 · 82210.1038/nm0798-822 ↗
15. Tjernberg · J. Biol. Chem. · 1996 · 271 · 854510.1074/jbc.271.15.8545 ↗
16. Cheruvara · J. Biol. Chem. · 2015 · 290 · 742610.1074/jbc.M114.620484 ↗
17. Liu · Front. Pharmacol. · 2018 · 8 · 110.3389/fphar.2017.00969 ↗
18. Horsley · Biochem. J. · 2020 · 477 · 154110.1042/BCJ20200290 ↗
19. Popova · Front. Mol. Neurosci. · 2021 · 14 · 110.3389/fnmol.2021.659926 ↗
20. Muttenthaler · Nat. Rev. Drug Discovery · 2021 · 20 · 30910.1038/s41573-020-00135-8 ↗
21. Wang · Signal Transduction Targeted Ther. · 2022 · 7 · 4810.1038/s41392-022-00904-4 ↗
22. Maio · Acta Med. Mediterr. · 2020 · 36 · 228710.19193/0393-6384_2020_4_356 ↗
23. Seo · Biomed. Eng. Lett. · 2021 · 11 · 21110.1007/s13534-021-00198-5 ↗
24. Rezaei · Colloids Surf., B · 2020 · 185 · 11055210.1016/j.colsurfb.2019.110552 ↗
25. Sela · Adv. Mater. · 2023 · 35 · 110.1002/adma.202304654 ↗
26. Shan · Chem. Eng. J. · 2024 · 494 · 15321010.1016/j.cej.2024.153210 ↗
27. Zheng · Pharm. Res. · 2015 · 32 · 383710.1007/s11095-015-1744-9 ↗
28. Hetényi · Biochem. Biophys. Res. Commun. · 2002 · 292 · 93110.1006/bbrc.2002.6745 ↗
29. Viet · J. Phys. Chem. B · 2011 · 115 · 743310.1021/jp1116728 ↗
30. Gul · J. Mol. Graphics Modell. · 2025 · 139 · 10907910.1016/j.jmgm.2025.109079 ↗
31. Abe · BMC Bioinformatics · 2007 · 8 · 110.1186/1471-2105-8-451 ↗
32. Kundal · Curr. Comput.-Aided Drug Des. · 2023 · 19 · 28810.2174/1573409919666230112170012 ↗
33. Xiong · ACS Appl. Mater. Interfaces · 2015 · 7 · 565010.1021/acsami.5b00915 ↗
34. Hughes · Proc. Natl. Acad. Sci. U. S. A. · 1996 · 93 · 206510.1073/pnas.93.5.2065 ↗
35. Poduslo · J. Neurobiol. · 1999 · 39 · 37110.1002/(SICI)1097-4695(19990605)39:3<371::AID-NEU4>3.0.CO;2-E ↗
36. Chalifour · J. Biol. Chem. · 2003 · 278 · 3487410.1074/jbc.M212694200 ↗
37. El-Agnaf · FASEB J. · 2004 · 18 · 131510.1096/fj.03-1346fje ↗
38. Datki · Neurobiol. Dis. · 2004 · 17 · 50710.1016/j.nbd.2004.08.007 ↗
39. Austen · Biochemistry · 2008 · 47 · 198410.1021/bi701415b ↗
40. Wiesehan · Protein Eng., Des. Sel. · 2008 · 21 · 24110.1093/protein/gzm054 ↗
41. Van Groen · ChemMedChem · 2008 · 3 · 184810.1002/cmdc.200800273 ↗
42. Kim · Biochem. Biophys. Res. Commun. · 2009 · 387 · 68210.1016/j.bbrc.2009.07.083 ↗
43. Shaltiel-Karyo · PLoS One · 2010 · 5 · e1386310.1371/journal.pone.0013863 ↗
44. Jagota · Int. J. Pept. Res. Ther. · 2012 · 18 · 5310.1007/s10989-011-9278-4 ↗
45. Liu · Biomacromolecules · 2014 · 15 · 93110.1021/bm401795e ↗
46. Minicozzi · J. Biol. Chem. · 2014 · 289 · 1124210.1074/jbc.M113.537472 ↗
47. Lin · PLoS One · 2014 · 9 · 110.1371/journal.pone.0112052 ↗
48. Bansal · ACS Chem. Neurosci. · 2016 · 7 · 61510.1021/acschemneuro.6b00006 ↗
49. Klein · PLoS One · 2016 · 11 · e015303510.1371/journal.pone.0153035 ↗
50. Rezaeian · Arch. Biochem. Biophys. · 2017 · 634 · 9610.1016/j.abb.2017.09.015 ↗
51. Liu · Front. Pharmacol. · 2018 · 8 · 110.3389/fphar.2017.00969 ↗
52. Meade · J. Mol. Biol. · 2021 · 433 · 16732310.1016/j.jmb.2021.167323 ↗
53. Nim · Nat. Commun. · 2023 · 14 · 215010.1038/s41467-023-37464-2 ↗
54. Tien · PeerJ · 2013 · 2013 · 110.7717/peerj.80 ↗
55. Olsson · J. Chem. Theory Comput. · 2011 · 7 · 52510.1021/ct100578z ↗
56. Hsieh · ACS Chem. Neurosci. · 2018 · 9 · 252110.1021/acschemneuro.8b00177 ↗
57. Cornejo · J. Enzyme Inhib. Med. Chem. · 2021 · 36 · 15410.1080/14756366.2020.1851216 ↗
58. Marondedze · Biophys. Chem. · 2020 · 256 · 10628110.1016/j.bpc.2019.106281 ↗
59. Zhang · Bioinformatics · 2019 · 35 · 512110.1093/bioinformatics/btz459 ↗
60. Zhou · Nucleic Acids Res. · 2018 · 46 · W44310.1093/nar/gky357 ↗
61. Jo · J. Comput. Chem. · 2008 · 29 · 185910.1002/jcc.20945 ↗
62. Park · J. Chem. Inf. Model. · 2021 · 61 · 519210.1021/acs.jcim.1c00770 ↗
63. Huang · Nat. Methods · 2017 · 14 · 7110.1038/nmeth.4067 ↗
64. Darden · J. Chem. Phys. · 1993 · 98 · 1008910.1063/1.464397 ↗
65. Hess · J. Comput. Chem. · 1997 · 18 · 146310.1002/(SICI)1096-987X(199709)18:12<1463::AID-JCC4>3.0.CO;2-H ↗
66. Bussi · J. Chem. Phys. · 2007 · 126 · 01410110.1063/1.2408420 ↗
67. Parrinello · J. Appl. Phys. · 1981 · 52 · 718210.1063/1.328693 ↗
68. Valdés-Tresanco · J. Chem. Theory Comput. · 2021 · 17 · 628110.1021/acs.jctc.1c00645 ↗
69. Humphrey · J. Mol. Graphics · 1996 · 14 · 3310.1016/0263-7855(96)00018-5 ↗
70. Wallace · Protein Eng., Des. Sel. · 1995 · 8 · 12710.1093/protein/8.2.127 ↗
71. Róg · Biochim. Biophys. Acta, Biomembr. · 2009 · 1788 · 9710.1016/j.bbamem.2008.08.022 ↗
72. Magarkar · J. Phys. Chem. C · 2014 · 118 · 1554110.1021/jp504962m ↗
73. Piggot · J. Chem. Theory Comput. · 2017 · 13 · 568310.1021/acs.jctc.7b00643 ↗
74. Souza · Nat. Methods · 2021 · 18 · 38210.1038/s41592-021-01098-3 ↗
75. Grünewald · Nat. Commun. · 2022 · 13 · 110.1038/s41467-021-27627-4 ↗
76. Berendsen · J. Chem. Phys. · 1984 · 81 · 368410.1063/1.448118 ↗
77. Tironi · J. Chem. Phys. · 1995 · 102 · 545110.1063/1.469273 ↗
78. Kogkos · Biomolecules · 2022 · 12 · 136210.3390/biom12101362 ↗
79. Vitali · Pharmaceutics · 2024 · 16 · 21910.3390/pharmaceutics16020219 ↗
80. Okumura · Molecules · 2022 · 27 · 248310.3390/molecules27082483 ↗
81. Chen · Protein Sci. · 2013 · 22 · 51010.1002/pro.2230 ↗
82. Radwan · PLoS One · 2023 · 18 · 110.1371/journal.pone.0286195 ↗
83. Jakubowski · J. Chem. Inf. Model. · 2020 · 60 · 28910.1021/acs.jcim.9b00561 ↗
84. Buratti · Protein Sci. · 2022 · 31 · 110.1002/pro.4360 ↗
85. O'Shea · Cells · 2025 · 14 · 410.3390/cells14181477 ↗
86. Capponi · Biochim. Biophys. Acta, Biomembr. · 2016 · 1858 · 35410.1016/j.bbamem.2015.11.024 ↗
87. Olsen · Biophys. J. · 2013 · 105 · 183810.1016/j.bpj.2013.08.042 ↗
88. Gul · Biophys. J. · 2022 · 121 · 427110.1016/j.bpj.2022.10.014 ↗
89. Gul · Biophys. J. · 2023 · 122 · 110.1016/j.bpj.2023.04.005 ↗
90. Filippov · Biophys. J. · 2003 · 84 · 307910.1016/S0006-3495(03)70033-2 ↗
91. Nanda · Soft Matter · 2018 · 14 · 611910.1039/c7sm01720k ↗
92. Singh · Biomacromolecules · 2014 · 15 · 133710.1021/bm401884e ↗
93. Nielsen · RSC Adv. · 2020 · 10 · 3532910.1039/d0ra07679a ↗
94. Deng · Soft Matter · 2020 · 16 · 349810.1039/d0sm00046a ↗
95. Schmidt · FEBS Lett. · 2010 · 584 · 180610.1016/j.febslet.2009.11.046 ↗
96. Mohan · LWT–Food Sci. Technol. · 2018 · 87 · 4010.1016/j.lwt.2017.08.072 ↗
97. Ingólfsson · Wiley Interdiscip. Rev.: Comput. Mol. Sci. · 2014 · 4 · 22510.1002/wcms.1169 ↗
98. Doole · J. Membr. Biol. · 2022 · 255 · 38510.1007/s00232-022-00263-9 ↗
99. Chen · Biophys. J. · 1997 · 73 · 26710.1016/S0006-3495(97)78067-6 ↗
100. Gubernator · Expert Opin. Drug Delivery · 2011 · 8 · 56510.1517/17425247.2011.566552 ↗