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@ARTICLE{Huck:476472,
author = {Huck, Volker and Chen, Po-Chia and Xu, Emma-Ruoqi and
Tischer, Alexander and Klemm, Ulrike and Aponte-Santamaría,
Camilo and Mess, Christian and Obser, Tobias and Kutzki,
Fabian and König, Gesa and Denis, Cécile V. and Gräter,
Frauke and Wilmanns, Matthias and Auton, Matthew and
Schneider, Stefan W. and Schneppenheim, Reinhard and Hennig,
Janosch and Brehm, Maria A.},
title = {{G}ain-of-{F}unction {V}ariant p.{P}ro2555{A}rg of von
{W}illebrand {F}actor {I}ncreases {A}ggregate {S}ize through
{A}ltering {S}tem {D}ynamics},
journal = {Thrombosis and haemostasis},
volume = {122},
number = {02},
issn = {0340-6245},
address = {Stuttgart},
publisher = {Thieme},
reportid = {PUBDB-2022-01749},
pages = {226 - 239},
year = {2022},
abstract = {The multimeric plasma glycoprotein (GP) von Willebrand
factor (VWF) is best known for recruiting platelets to sites
of injury during primary hemostasis. Generally, mutations in
the VWF gene lead to loss of hemostatic activity and thus
the bleeding disorder von Willebrand disease. By employing
cone and platelet aggregometry and microfluidic assays, we
uncovered a platelet GPIIb/IIIa-dependent prothrombotic gain
of function (GOF) for variant p.Pro2555Arg, located in the
C4 domain, leading to an increase in platelet aggregate
size. We performed complementary biophysical and structural
investigations using circular dichroism spectra, small-angle
X-ray scattering, nuclear magnetic resonance spectroscopy,
molecular dynamics simulations on the single C4 domain, and
dimeric wild-type and p.Pro2555Arg constructs.
C4-p.Pro2555Arg retained the overall structural conformation
with minor populations of alternative conformations
exhibiting increased hinge flexibility and slow
conformational exchange. The dimeric protein becomes
disordered and more flexible. Our data suggest that the GOF
does not affect the binding affinity of the C4 domain for
GPIIb/IIIa. Instead, the increased VWF dimer flexibility
enhances temporal accessibility of platelet-binding sites.
Using an interdisciplinary approach, we revealed that
p.Pro2555Arg is the first VWF variant, which increases
platelet aggregate size and shows a shear-dependent function
of the VWF stem region, which can become hyperactive through
mutations. Prothrombotic GOF variants of VWF are a novel
concept of a VWF-associated pathomechanism of thromboembolic
events, which is of general interest to vascular health but
not yet considered in diagnostics. Thus, awareness should be
raised for the risk they pose. Furthermore, our data
implicate the C4 domain as a novel antithrombotic drug
target.},
cin = {EMBL-User / EMBL},
ddc = {610},
cid = {I:(DE-H253)EMBL-User-20120814 / I:(DE-H253)EMBL-20120731},
pnm = {6G3 - PETRA III (DESY) (POF4-6G3)},
pid = {G:(DE-HGF)POF4-6G3},
experiment = {EXP:(DE-H253)P-P12-20150101},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:33385180},
UT = {WOS:000640018900001},
doi = {10.1055/a-1344-4405},
url = {https://bib-pubdb1.desy.de/record/476472},
}