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@ARTICLE{Ahmad:902474,
author = {Ahmad, Sabahuddin and Strunk, Christoph Heinrich and
Schott, Stephan and Jaeger, Karl-Erich and Kovacic, Filip
and Gohlke, Holger},
title = {{S}ubstrate {A}ccess {M}echanism in a {N}ovel
{M}embrane-{B}ound {P}hospholipase {A} of {P}seudomonas
aeruginosa {C}oncordant with {S}pecificity and
{R}egioselectivity},
journal = {Journal of chemical information and modeling},
volume = {61},
number = {11},
issn = {0095-2338},
address = {Washington, DC},
publisher = {American Chemical Society},
reportid = {FZJ-2021-04293},
pages = {5626–5643},
year = {2021},
abstract = {PlaF is a cytoplasmic membrane-bound phospholipase A1 from
Pseudomonas aeruginosa that alters the membrane
glycerophospholipid (GPL) composition and fosters the
virulence of this human pathogen. PlaF activity is regulated
by a dimer-to-monomer transition followed by tilting of the
monomer in the membrane. However, how substrates reach the
active site and how the characteristics of the active site
tunnels determine the activity, specificity, and
regioselectivity of PlaF for natural GPL substrates have
remained elusive. Here, we combined unbiased and biased
all-atom molecular dynamics (MD) simulations and
configurational free-energy computations to identify access
pathways of GPL substrates to the catalytic center of PlaF.
Our results map out a distinct tunnel through which
substrates access the catalytic center. PlaF variants with
bulky tryptophan residues in this tunnel revealed decreased
catalysis rates due to tunnel blockage. The MD simulations
suggest that GPLs preferably enter the active site with the
sn-1 acyl chain first, which agrees with the experimentally
demonstrated PLA1 activity of PlaF. We propose that the acyl
chain-length specificity of PlaF is determined by the
structural features of the access tunnel, which results in
favorable free energy of binding of medium-chain GPLs. The
suggested egress route conveys fatty acid (FA) products to
the dimerization interface and, thus, contributes to
understanding the product feedback regulation of PlaF by
FA-triggered dimerization. These findings open up
opportunities for developing potential PlaF inhibitors,
which may act as antibiotics against P. aeruginosa.},
cin = {IBG-4 / JSC / NIC / IBI-7 / IMET},
ddc = {540},
cid = {I:(DE-Juel1)IBG-4-20200403 / I:(DE-Juel1)JSC-20090406 /
I:(DE-Juel1)NIC-20090406 / I:(DE-Juel1)IBI-7-20200312 /
I:(DE-Juel1)IMET-20090612},
pnm = {2171 - Biological and environmental resources for
sustainable use (POF4-217) / 5111 - Domain-Specific
Simulation $\&$ Data Life Cycle Labs (SDLs) and Research
Groups (POF4-511) / Forschergruppe Gohlke $(hkf7_20200501)$
/ DFG project 267205415 - SFB 1208: Identität und Dynamik
von Membransystemen - von Molekülen bis zu zellulären
Funktionen (267205415)},
pid = {G:(DE-HGF)POF4-2171 / G:(DE-HGF)POF4-5111 /
$G:(DE-Juel1)hkf7_20200501$ / G:(GEPRIS)267205415},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:34748335},
UT = {WOS:000757001900030},
doi = {10.1021/acs.jcim.1c00973},
url = {https://juser.fz-juelich.de/record/902474},
}