Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2
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Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2. / Jensen, P.C.; Thiele, S; Steen, A; Elder, A; Kolbeck, R; Ghosh, Sudip; Frimurer, T M; Rosenkilde, Mette Marie.
In: British Journal of Pharmacology, Vol. 166, No. 1, 05.2012, p. 258-75.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2
AU - Jensen, P.C.
AU - Thiele, S
AU - Steen, A
AU - Elder, A
AU - Kolbeck, R
AU - Ghosh, Sudip
AU - Frimurer, T M
AU - Rosenkilde, Mette Marie
N1 - © 2011 The Authors. British Journal of Pharmacology © 2011 The British Pharmacological Society.
PY - 2012/5
Y1 - 2012/5
N2 - The majority of small molecule compounds targeting chemokine receptors share a similar pharmacophore with a centrally located aliphatic positive charge and flanking aromatic moieties. Here we describe a novel piperidine-based compound with structural similarity to previously described CCR8-specific agonists, but containing a unique phenyl-tetrazol moiety which, in addition to activity at CCR8 was also active at CCR1.
AB - The majority of small molecule compounds targeting chemokine receptors share a similar pharmacophore with a centrally located aliphatic positive charge and flanking aromatic moieties. Here we describe a novel piperidine-based compound with structural similarity to previously described CCR8-specific agonists, but containing a unique phenyl-tetrazol moiety which, in addition to activity at CCR8 was also active at CCR1.
KW - Animals
KW - Binding Sites
KW - COS Cells
KW - Cercopithecus aethiops
KW - Glutamic Acid
KW - Humans
KW - Inositol 1,4,5-Trisphosphate
KW - Ligands
KW - Models, Molecular
KW - Piperidines
KW - Point Mutation
KW - Receptors, CCR1
KW - Receptors, CCR8
KW - Tetrazoles
U2 - 10.1111/j.1476-5381.2011.01771.x
DO - 10.1111/j.1476-5381.2011.01771.x
M3 - Journal article
C2 - 22050085
VL - 166
SP - 258
EP - 275
JO - British Journal of Pharmacology
JF - British Journal of Pharmacology
SN - 0007-1188
IS - 1
ER -
ID: 48972161