Vol.:(0123456789) 1 3
Biomolecular NMR Assignments
https://doi.org/10.1007/s12104-018-9819-2
ARTICLE
1
H,
13
C and
15
N resonance assignments for a chemokine receptor-
binding domain of FROUNT, a cytoplasmic regulator of chemotaxis
Sosuke Yoshinaga
1
· Norihito Ishida
1
· Tatsuichiro Tsuji
1
· Akihiro Sonoda
1
· Kaori Yunoki
1
· Mitsuhiro Takeda
1
·
Etsuko Toda
2
· Yuya Terashima
2
· Kouji Matsushima
2
· Hiroaki Terasawa
1
Received: 6 February 2018 / Accepted: 26 March 2018
© Springer Science+Business Media B.V., part of Springer Nature 2018
Abstract
FROUNT is a cytoplasmic protein that interacts with the membrane-proximal C-terminal regions (Pro-Cs) of the CCR2 and
CCR5 chemokine receptors. The interactions between FROUNT and the chemokine receptors play an important role in the
migration of infammatory immune cells. Therefore, FROUNT is a potential drug target for infammatory diseases. However,
the structural basis of the interactions between FROUNT and the chemokine receptors remains to be elucidated. We previ-
ously identifed the C-terminal region (residues 532–656) of FROUNT as the structural domain responsible for the Pro-C
binding, referred to as the chemokine receptor-binding domain (CRBD), and then constructed its mutant, bearing L538E/
P612S mutations, with improved NMR spectral quality, referred to as CRBD_LEPS. We now report the main-chain and
side-chain
1
H,
13
C, and
15
N resonance assignments of CRBD_LEPS. The NMR signals of CRBD_LEPS were well dispersed
and their intensities were uniform on the
1
H–
15
N HSQC spectrum, and thus almost all of the main-chain and side-chain
resonances were assigned. This assignment information provides the foundation for NMR studies of the three-dimensional
structure of CRBD_LEPS in solution and its interactions with chemokine receptors.
Keywords Infammation · Cell migration · Chemokine receptor-binding domain · CCR2 · CCR5 · GPCR
Biological context
Infammation is an initial biological defensive mechanism
against bacterial infection. Immune cells, such as mono-
cytes and macrophages, sense the concentration gradients of
chemokines and migrate to the infected site. This cell migra-
tion is triggered by chemokines, which bind to G protein-
coupled receptors (GPCRs) on the cell membrane.
We identifed FROUNT as a cytoplasmic protein that
binds to the C-terminal membrane proximal region (Pro-C)
of the chemokine receptor, CCR2. The interaction between
FROUNT and CCR2 regulates the migration of immune
cells (Terashima et al. 2005). FROUNT was also found
to bind CCR5, and thus it regulates CCR5-mediated cell
migration (Toda et al. 2009). The FROUNT protein pro-
duced by Escherichia coli naturally oligomerized (Esaki
et al. 2011). A 16 amino acid region on the side of CCR2
Pro-C was identifed as the FROUNT binding region (Toda
et al. 2014). The 16 amino acid peptide adopts an amphi-
pathic helical conformation upon binding to FROUNT
and interacts with FROUNT via its hydrophobic surface,
as revealed by NMR (Esaki et al. 2014). The C-terminal
region (residues 532–656) of FROUNT, named CRBD here,
was identifed as the structural domain responsible for bind-
ing to CCR2 Pro-C. However, the recombinant protein of
CRBD (14.5 kDa) exhibited signifcant aggregation pro-
pensity at a concentration of 100 µM (Sonoda et al. 2017).
We screened 1,6-hexanediol as a solubilizing compound for
the CRBD protein, using multiple terminal deletion mutants
(Yunoki et al. 2018). We assigned the main-chain resonances
of CRBD by deuteration and TROSY. However, the side-
chain resonance assignment of CRBD was difcult due to
its aggregation tendency. We also introduced L538E/P612S
mutations to the CRBD protein, referred to as CRBD_LEPS,
to mitigate its aggregation propensity and thereby improve
the quality of obtainable NMR spectra, with no infuence
* Hiroaki Terasawa
terasawa@structbiol.com
1
Department of Structural BioImaging, Faculty of Life
Sciences, Kumamoto University, Kumamoto, Japan
2
Department of Molecular Preventive Medicine, Graduate
School of Medicine, The University of Tokyo, Bunkyo-ku,
Tokyo, Japan