[HTML][HTML] Site-directed Mutagenesis Identifies Residues Involved in Ligand Recognition in the Human A2a Adenosine Receptor∗
J Kim, J Wess, AM van Rhee, T Schöneberg… - Journal of Biological …, 1995 - ASBMB
The A 2a adenosine receptor is a member of the G-protein coupled receptor family, and its
activation stimulates cyclic AMP production. To determine the residues which are involved in …
activation stimulates cyclic AMP production. To determine the residues which are involved in …
Molecular architecture of G protein‐coupled receptors
AM van Rhee, KA Jacobson - Drug development research, 1996 - Wiley Online Library
This review of the current literature on mutations in G protein‐coupled receptors (GPCRs) of
the rhodopsin‐related family intends to draw inferences from amino acid sequences for …
the rhodopsin‐related family intends to draw inferences from amino acid sequences for …
Interaction of 1,4-Dihydropyridine and Pyridine Derivatives with Adenosine Receptors: Selectivity for A3 Receptors
AM van Rhee, J Jiang, N Melman… - Journal of medicinal …, 1996 - ACS Publications
1,4-Dihydropyridine and pyridine derivatives bound to three subtypes of adenosine receptors
in the micromolar range. Affinity was determined in radioligand binding assays at rat brain …
in the micromolar range. Affinity was determined in radioligand binding assays at rat brain …
A mutational analysis of residues essential for ligand recognition at the human P2Y1 receptor
Q Jiang, D Guo, BX Lee, AM Van Rhee, YC Kim… - Molecular …, 1997 - ASPET
We conducted a mutational analysis of residues potentially involved in the adenine nucleotide
binding pocket of the human P2Y 1 receptor. Mutated receptors were expressed in COS-7 …
binding pocket of the human P2Y 1 receptor. Mutated receptors were expressed in COS-7 …
[HTML][HTML] Hydrophilic side chains in the third and seventh transmembrane helical domains of human A2A adenosine receptors are required for ligand recognition
Q Jiang, AM VAN RHEE, J Kim, S Yehle… - Molecular …, 1996 - ncbi.nlm.nih.gov
Hydrophilic residues of the G protein-coupled human A 2A adenosine receptor that are
potentially involved in the binding of the ribose moiety of adenosine were targeted for …
potentially involved in the binding of the ribose moiety of adenosine were targeted for …
6-Phenyl-1,4-dihydropyridine Derivatives as Potent and Selective A3 Adenosine Receptor Antagonists
J Jiang, AM van Rhee, N Melman, X Ji… - Journal of medicinal …, 1996 - ACS Publications
An approach to designing dihydropyridines that bind to adenosine receptors without binding
to L-type calcium channels has been described. 1,4-Dihydropyridine derivatives substituted …
to L-type calcium channels has been described. 1,4-Dihydropyridine derivatives substituted …
Structure−Activity Relationships of 4-(Phenylethynyl)-6-phenyl-1,4- dihydropyridines as Highly Selective A3 Adenosine Receptor Antagonists
J Jiang, AM Van Rhee, L Chang… - Journal of medicinal …, 1997 - ACS Publications
4-(Phenylethynyl)-6-phenyl-1,4-dihydropyridine derivatives are selective antagonists at
human A 3 adenosine receptors, with K i values in a radioligand binding assay vs [ 125 I]AB-…
human A 3 adenosine receptors, with K i values in a radioligand binding assay vs [ 125 I]AB-…
Mutagenesis Reveals Structure−Activity Parallels between Human A2A Adenosine Receptors and Biogenic Amine G Protein-Coupled Receptors
…, BX Lee, M Glashofer, AM van Rhee… - Journal of medicinal …, 1997 - ACS Publications
Structure−affinity relationships for ligand binding at the human A 2A adenosine receptor
have been probed using site-directed mutagenesis in the transmembrane helical domains (TMs)…
have been probed using site-directed mutagenesis in the transmembrane helical domains (TMs)…
[HTML][HTML] Modelling the P2Y purinoceptor using rhodopsin as template
AM Van Rhee, B Fischer, PJM Van Galen… - Drug design and …, 1995 - ncbi.nlm.nih.gov
The P2Y 1 purinoceptor cloned from chick brain (Webb, T. et al.(1993) FEBS Lett., 324, 219–225)
is a 362 amino acid, 41 kDa protein. To locate residues tentatively involved in ligand …
is a 362 amino acid, 41 kDa protein. To locate residues tentatively involved in ligand …
Flavonoid derivatives as adenosine receptor antagonists: a comparison of the hypothetical receptor binding site based on a comparative molecular field analysis …
S Moro, AM van Rhee, LH Sanders… - Journal of medicinal …, 1998 - ACS Publications
Flavonoid derivatives have been optimized as relatively rigid antagonists of adenosine
receptors with particular selectivity for the A 3 receptor subtype. A quantitative study of the …
receptors with particular selectivity for the A 3 receptor subtype. A quantitative study of the …