Structural determinants for selective recognition of peptide ligands for endothelin receptor subtypes ETA and ETB

2009 ◽  
Vol 15 (7) ◽  
pp. 479-491 ◽  
Author(s):  
Jens Lättig ◽  
Alexander Oksche ◽  
Michael Beyermann ◽  
Walter Rosenthal ◽  
Gerd Krause
Keyword(s):  
Peptide Ligands ◽  
Selective Recognition ◽  
Receptor Subtypes ◽  
Endothelin Receptor ◽  
Structural Determinants

scholarly journals Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Xuesong Wang ◽  
Willem Jespers ◽  
Rubén Prieto-Díaz ◽  
Maria Majellaro ◽  
Adriaan P. IJzerman ◽  
...  
Keyword(s):  
Radioligand Binding ◽  
Structural Data ◽  
Binding Mode ◽  
Selective Recognition ◽  
Chiral Hplc ◽  
Binding Assays ◽  
Structural Determinants ◽  
X Ray Crystallography ◽  
Adenosine Receptor Antagonist ◽  
Energy Perturbation

AbstractThe four adenosine receptors (ARs) A1AR, A2AAR, A2BAR, and A3AR are G protein-coupled receptors (GPCRs) for which an exceptional amount of experimental and structural data is available. Still, limited success has been achieved in getting new chemical modulators on the market. As such, there is a clear interest in the design of novel selective chemical entities for this family of receptors. In this work, we investigate the selective recognition of ISAM-140, a recently reported A2BAR reference antagonist. A combination of semipreparative chiral HPLC, circular dichroism and X-ray crystallography was used to separate and unequivocally assign the configuration of each enantiomer. Subsequently affinity evaluation for both A2A and A2B receptors demonstrate the stereospecific and selective recognition of (S)-ISAM140 to the A2BAR. The molecular modeling suggested that the structural determinants of this selectivity profile would be residue V2506.51 in A2BAR, which is a leucine in all other ARs including the closely related A2AAR. This was herein confirmed by radioligand binding assays and rigorous free energy perturbation (FEP) calculations performed on the L249V6.51 mutant A2AAR receptor. Taken together, this study provides further insights in the binding mode of these A2BAR antagonists, paving the way for future ligand optimization.

Significance of Endothelin Receptor Subtypes in the Kidneys of Spontaneously Hypertensive Rats

1995 ◽  
Vol 26 ◽  
pp. S470-472
Author(s):  
Berthold Hocher ◽  
Peter Rohmeiss ◽  
Rüdiger Zart ◽  
Fritz Diekmann ◽  
Volker Vogt ◽  
...  
Keyword(s):  
Spontaneously Hypertensive Rats ◽  
Receptor Subtypes ◽  
Endothelin Receptor ◽  
Hypertensive Rats ◽  
Spontaneously Hypertensive

Localization and Distribution of Endothelin Receptor Subtypes in Pulmonary Vasculature of Normal and Hypoxia-Exposed Rats

1999 ◽  
Vol 20 (4) ◽  
pp. 620-630 ◽  
Author(s):  
Sanae Soma ◽  
Hideki Takahashi ◽  
Masashi Muramatsu ◽  
Masahiko Oka ◽  
Yoshinosuke Fukuchi
Keyword(s):  
Pulmonary Vasculature ◽  
Receptor Subtypes ◽  
Endothelin Receptor

scholarly journals Structural determinants for the interaction of formyl peptide receptor 2 with peptide ligands.

2014 ◽  
Vol 289 (8) ◽  
pp. 4814-4814
Author(s):  
Hui-Qiong He ◽  
Erica L. Troksa ◽  
Gianluigi Caltabiano ◽  
Leonardo Pardo ◽  
Richard D. Ye
Keyword(s):  
Peptide Ligands ◽  
Formyl Peptide Receptor ◽  
Structural Determinants ◽  
Peptide Receptor ◽  
Formyl Peptide

CELLULAR LOCALIZATION OF ENDOTHELIN RECEPTOR SUBTYPES IN THE RAT KIDNEY FOLLOWING IN VITRO LABELLING

1996 ◽  
Vol 23 (6-7) ◽  
pp. 524-531 ◽  
Author(s):  
Rachael Dean ◽  
Jialong Zhuo ◽  
Daine Alcorn ◽  
David Casley ◽  
Frederick AO Mendelsohn
Keyword(s):  
Cellular Localization ◽  
Rat Kidney ◽  
Receptor Subtypes ◽  
Endothelin Receptor

Different distribution of endothelin receptor subtypes in pulmonary tissues revealed by the novel selective ligands BQ-123 and [Ala1,3,11,15]ET-1

1992 ◽  
Vol 182 (1) ◽  
pp. 144-150 ◽  
Author(s):  
Kyoko Nakamichi ◽  
Masaki Ihara ◽  
Masahiko Kobayashi ◽  
Toshihiko Saeki ◽  
Kiyofumi Ishikawa ◽  
...  
Keyword(s):  
Receptor Subtypes ◽  
The Novel ◽  
Endothelin Receptor ◽  
Selective Ligands
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