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PDBsum entry 2f1u
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Signaling protein receptor
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PDB id
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2f1u
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Contents |
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30 a.a.
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30 a.a.
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33 a.a.
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23 a.a.
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26 a.a.
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31 a.a.
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21 a.a.
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Theoretical model |
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PDB id:
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Signaling protein receptor
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Title:
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A homology-based 3d model of the human neuropeptide y receptor y1
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Structure:
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Neuropeptide y receptor type 1. Chain: a. Synonym: npy1-r. Neuropeptide y receptor type 1. Chain: b. Synonym: npy1-r. Neuropeptide y receptor type 1. Chain: c. Synonym: npy1-r.
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Source:
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Homo sapiens. Human. Human
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Authors:
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P.Sjodin,H.Akerberg,D.Larhammar
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Key ref:
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P.Sjödin
et al.
(2006).
Re-evaluation of receptor-ligand interactions of the human neuropeptide Y receptor Y1: a site-directed mutagenesis study.
Biochem J,
393,
161-169.
PubMed id:
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Date:
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15-Nov-05
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Release date:
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04-Jul-06
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PROCHECK
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Headers
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References
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P25929
(NPY1R_HUMAN) -
Neuropeptide Y receptor type 1
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Seq:
Struc:
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384 a.a.
30 a.a.
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P25929
(NPY1R_HUMAN) -
Neuropeptide Y receptor type 1
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Seq:
Struc:
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384 a.a.
30 a.a.
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P25929
(NPY1R_HUMAN) -
Neuropeptide Y receptor type 1
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Seq:
Struc:
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384 a.a.
33 a.a.
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P25929
(NPY1R_HUMAN) -
Neuropeptide Y receptor type 1
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Seq:
Struc:
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384 a.a.
23 a.a.
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P25929
(NPY1R_HUMAN) -
Neuropeptide Y receptor type 1
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Seq:
Struc:
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384 a.a.
26 a.a.
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Biochem J
393:161-169
(2006)
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PubMed id:
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Re-evaluation of receptor-ligand interactions of the human neuropeptide Y receptor Y1: a site-directed mutagenesis study.
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P.Sjödin,
S.K.Holmberg,
H.Akerberg,
M.M.Berglund,
N.Mohell,
D.Larhammar.
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ABSTRACT
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Interactions of the human NPY (neuropeptide Y) receptor Y1 with the two
endogenous agonists NPY and peptide YY and two non-peptide antagonists were
investigated using site-directed mutagenesis at 17 positions. The present study
was triggered by contradictions among previously published reports and
conclusions that seemed inconsistent with sequence comparisons across species
and receptor subtypes. Our results show that Asp287, at the border between TM
(transmembrane) region 6 and EL3 (extracellular loop 3) influences peptide
binding, while two aspartic residues in EL2 do not, in agreement with some
previous studies but in disagreement with others. A hydrophobic pocket of the Y1
receptor consisting of Tyr100 (TM2), Phe286 (TM6) and His298 (EL3) has been
proposed to interact with the amidated C-terminus of NPY, a theory that is
unsupported by sequence comparisons between Y1, Y2 and Y5. Nevertheless, our
results confirm that these amino acid residues are critical for peptide binding,
but probably interact with NPY differently than proposed previously. Studies
with the Y1-selective antagonist SR120819A identified a new site of interaction
at Asn116 in TM3. Position Phe173 in TM4 is also important for binding of this
antagonist. In contrast with previous reports, we found that Phe173 is not
crucial for the binding of BIBP3226, another selective Y1 receptor antagonist.
Also, we found that position Thr212 (TM5) is important for binding of both
antagonists. Our mutagenesis results and our three-dimensional model of the
receptor based on the high-resolution structure of bovine rhodopsin suggest new
interactions for agonist as well as antagonist binding to the Y1 receptor.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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L.E.Kilpatrick,
S.J.Briddon,
S.J.Hill,
and
N.D.Holliday
(2010).
Quantitative analysis of neuropeptide Y receptor association with beta-arrestin2 measured by bimolecular fluorescence complementation.
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Br J Pharmacol,
160,
892-906.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
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