Probing the Capsid: pH-Driven Gating at the AAV 5-Fold Pore and Its Role in Peptide Ligand Binding
Background/Objectives: Adeno-associated virus (AAV) capsids undergo pH-dependent conformational gating at the 5-fold symmetry pore, but how these structural dynamics shape serotype-specific behavior and affinity-ligand recognition remains unclear, particularly for the clinically important serotypes AAV8 and AAV9. This study aimed to establish a pH-resolved structural framework linking 5-fold pore dynamics to peptide-ligand recognition and to translate this framework into sequence-based design principles for affinity capture of gene therapy vectors. Methods: AAV8 and AAV9 5-fold capsid assemblies were subjected to 500 ns molecular dynamics simulations under acidic (pH 5), neutral (pH 7), and basic (pH 9) conditions, with analysis of pore volume, inter-residue contact networks, electrostatic potential, and solvent-accessible surface area. In parallel, affinity chromatography using three mixed-mode peptide ligands (RVVAVYRI, TTFRAHHI, and TYHHHHII) was performed on clarified HEK293 lysates containing AAV8 or AAV9, with capsid yield, host-cell-protein clearance, and transduction activity assessed by ELISA, SEC-HPLC, and flow-cytometry-based transduction assays. Results: AAV8 displayed a heterogeneous, bimodal pore conformational landscape at pH 7, whereas AAV9 exhibited a discrete gate-like transition with maximal pore constriction at physiological pH; both serotypes showed pore-proximal contact remodeling with distinct network topologies. Experimentally, TYHHHHII achieved the highest selectivity for genome-containing capsids at pH 7, with transduction activity enrichment factors of 2.82 (AAV8) and 5.61 (AAV9), while TTFRAHHI provided the broadest operational pH range for bulk capsid recovery. Conclusions: These findings establish a structural framework linking pH-dependent pore dynamics to affinity ligand recognition and suggest practical sequence-design rules for ligand engineering: clustered histidines for neutral-pH selectivity, Arg-containing motifs for broad-pH robustness, and aromatic or hydrophobic residues for reinforcement of capsid binding.
Authors
- Sushmita Koley (ORCID: https://orcid.org/0000-0001-5826-8307)
- Ciera Khuu
- Shriarjun Shastry (ORCID: https://orcid.org/0000-0001-9164-9398)
- Christopher Belisle
- Eduardo Barbieri (ORCID: https://orcid.org/0000-0002-4829-2087)
- Stefano Menegatti (ORCID: https://orcid.org/0000-0001-5633-434X)
- Benjamin G. Bobay (ORCID: https://orcid.org/0000-0003-4775-3686)
- Shizuo Kamita
- Arianna Minzoni (ORCID: https://orcid.org/0000-0002-4504-9567)
- Peyton Russelburg
- Michael Angelo-Anthony Daniele (ORCID: https://orcid.org/0000-0002-2016-4091)
- Joseph Siino
- Crystal Collazo
- Brandon Brino
- Alexander Polgar
- Danni Wang
- Mark Snyder
Institutions
- Michigan Technological University (US)
- Bio-Rad (United States) (US)
- North Carolina State University (US)
- Duke University (US)
- North Central State College (US)
- TiGenix (Spain) (ES)
- Duke Medical Center (US)
Publication Details
- Journal
- Pharmaceutics
- Published
- 2026-08-25
- DOI
- https://doi.org/10.3390/pharmaceutics18091053
- Primary Topic
- Virus-based gene therapy research
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Science Foundation
- U.S. Food and Drug Administration
- National Institute for Innovation in Manufacturing Biopharmaceuticals