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@ARTICLE{Weil:284347,
author = {Weil, Tatjana and Lawrenz, Jan and Taghuo Kaptouom, Estelle
and Mieres-Perez, Joel and Hunszinger, Victoria and Sparrer,
Konstantin M J and Almeida-Hernandez, Yasser and Schrader,
Thomas and Sanchez-Garcia, Elsa and Münch, Jan},
title = {{A}dvanced {M}olecular {T}weezers {E}ffectively {T}arget
{M}embranes {L}acking {C}holine {H}eadgroups for
{B}road-{S}pectrum {A}ntiviral {E}fficacy.},
journal = {Journal of the American Chemical Society},
volume = {148},
number = {3},
issn = {0002-7863},
address = {Washington, DC},
publisher = {ACS Publications},
reportid = {DZNE-2026-00118},
pages = {3626 - 3637},
year = {2026},
abstract = {Broad-spectrum antivirals are urgently required to counter
present and emerging viral threats. It has previously been
shown that the parental molecular tweezers CLR01 and CLR05
disrupt viral envelopes by complexing choline headgroups and
that ester-functionalized 'advanced' tweezers display
markedly enhanced antiviral potency. Here, we determine the
molecular basis of this improved activity. Using liposome
leakage assays, giant unilamellar vesicles, NMR, Langmuir
film balance experiments, and atomistic simulations, we
demonstrate that advanced tweezers not only encapsulate
choline-containing lipids but also engage lipids lacking
choline headgroups via transient and conserved hydrophobic
insertion events. These interactions preferentially
destabilize membranes enriched in sphingomyelin, unsaturated
acyl chains, or inverted cone-shaped lipids and are
especially effective against small, highly curved particles
resembling viral particles, explaining their broad antiviral
activity for enveloped viruses. Our findings reveal a dual
mechanism of action, choline binding and hydrophobic
insertion, that underpins the broad-spectrum antiviral
activity of advanced molecular tweezers and establish them
as a promising new class of membrane-targeting antivirals
for prophylactic and therapeutic use.},
cin = {AG Sparrer},
ddc = {540},
cid = {I:(DE-2719)1910003},
pnm = {351 - Brain Function (POF4-351)},
pid = {G:(DE-HGF)POF4-351},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:41552975},
doi = {10.1021/jacs.5c19450},
url = {https://pub.dzne.de/record/284347},
}