Analysis of Structure−Activity Relationships for MT2 Selective Antagonists by Melatonin MT1 and MT2 Receptor Models
Three-dimensional homology models of human MT1 and MT2 melatonin receptors were
built with the aim to investigate the structure− activity relationships (SARs) of MT2 selective …
built with the aim to investigate the structure− activity relationships (SARs) of MT2 selective …
MT1‐Selective Melatonin Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Dynamics Investigation of N‐{[(3‐O‐Substituted)anilino]alkyl} …
The design of compounds selective for the MT1 melatonin receptor is still a challenging task
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …
Three-Dimensional Quantitative Structure−Activity Relationship Studies on Selected MT1 and MT2 Melatonin Receptor Ligands: Requirements for Subtype …
The three-dimensional quantitative structure− activity relationship comparative molecular
field analysis (3D-QSAR CoMFA) approach was applied to some classes of melatonin (MLT) …
field analysis (3D-QSAR CoMFA) approach was applied to some classes of melatonin (MLT) …
Synthesis and Structure−Affinity−Activity Relationships of Novel Benzofuran Derivatives as MT2 Melatonin Receptor Selective Ligands
V Wallez, S Durieux-Poissonnier… - Journal of medicinal …, 2002 - ACS Publications
A series of N-(2-phenylbenzofuran-3-yl) ethyl amide and N-(2-arylalkylbenzofuran-3-yl) ethyl
amide derivatives were synthesized and evaluated as melatonin receptor ligands. The …
amide derivatives were synthesized and evaluated as melatonin receptor ligands. The …
Bivalent ligand approach on N-{2-[(3-methoxyphenyl) methylamino] ethyl} acetamide: Synthesis, binding affinity and intrinsic activity for MT1 and MT2 melatonin …
We report the synthesis, binding properties and intrinsic activity at MT1 and MT2 melatonin
receptors of new dimeric melatonin receptor ligands in which two units of the monomeric …
receptors of new dimeric melatonin receptor ligands in which two units of the monomeric …
Highly Potent and Selective MT2 Melatonin Receptor Full Agonists from Conformational Analysis of 1-Benzyl-2-acylaminomethyl-tetrahydroquinolines
Molecular superposition models guided the design of novel melatonin receptor ligands
characterized by a 2-acylaminomethyltetrahydroquinoline scaffold. Starting from the …
characterized by a 2-acylaminomethyltetrahydroquinoline scaffold. Starting from the …
Molecular modeling of human MT2 melatonin receptor: the role of Val204, Leu272 and Tyr298 in ligand binding
P Mazna, V Obsilova, I Jelinkova, A Balik… - Journal of …, 2004 - Wiley Online Library
A model of the helical part of the human MT2 melatonin (hMT2) receptor, a member of the G
protein‐coupled receptors superfamily has been generated, based on the structure of …
protein‐coupled receptors superfamily has been generated, based on the structure of …
Design and Synthesis of N-(3,3-Diphenylpropenyl)alkanamides as a Novel Class of High-Affinity MT2-Selective Melatonin Receptor Ligands
A novel series of melatonin receptor ligands was discovered by opening the cyclic scaffolds
of known classes of high affinity melatonin receptor antagonists, while retaining the …
of known classes of high affinity melatonin receptor antagonists, while retaining the …
Synthesis of substituted N-[3-(3-methoxyphenyl) propyl] amides as highly potent MT2-selective melatonin ligands
Y Hu, MKC Ho, KH Chan, DC New, YH Wong - Bioorganic & Medicinal …, 2010 - Elsevier
A series of substituted N-[3-(3-methoxyphenyl) propyl] amides were synthesized and their
binding affinities towards human melatonin MT1 and MT2 receptors were evaluated. It was …
binding affinities towards human melatonin MT1 and MT2 receptors were evaluated. It was …
Ligand binding to the human MT2 melatonin receptor: the role of residues in transmembrane domains 3, 6, and 7
P Mazna, K Berka, I Jelinkova, A Balik… - Biochemical and …, 2005 - Elsevier
To better understand the mechanism of interactions between G-protein-coupled melatonin
receptors and their ligands, our previously reported homology model of human MT2 receptor …
receptors and their ligands, our previously reported homology model of human MT2 receptor …