scholarly journals Identification of essential residues for binding and activation in the human 5-HT7(a) serotonin receptor by molecular modeling and site-directed mutagenesis

2015 ◽  
Vol 9 ◽  
Author(s):  
Agata Antonina Rita Impellizzeri ◽  
Matteo Pappalardo ◽  
Livia Basile ◽  
Ornella Manfra ◽  
Kjetil Wessel Andressen ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Serotonin Receptor ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis

Combination of Molecular Modeling, Site-Directed Mutagenesis, and SAR Studies To Delineate the Binding Site of Pyridopyrimidine Antagonists on the Human CCK1 Receptor

2005 ◽  
Vol 48 (15) ◽  
pp. 4842-4850 ◽  
Author(s):  
Mercedes Martín-Martínez ◽  
Anne Marty ◽  
Maud Jourdan ◽  
Chantal Escrieut ◽  
Elodie Archer ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Binding Site ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Sar Studies ◽  
Cck1 Receptor

ATP-Binding Site of Human Brain Hexokinase As Studied by Molecular Modeling and Site-Directed Mutagenesis†

Biochemistry ◽  
1996 ◽  
Vol 35 (40) ◽  
pp. 13157-13164 ◽  
Author(s):  
Chenbo Zeng ◽  
Alexander E. Aleshin ◽  
Jason B. Hardie ◽  
Robert W. Harrison ◽  
Herbert J. Fromm
Keyword(s):  
Molecular Modeling ◽  
Human Brain ◽  
Binding Site ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Atp Binding ◽  
Atp Binding Site

scholarly journals Identification of Residues within Human Glycoprotein VI Involved in the Binding to Collagen

2004 ◽  
Vol 279 (50) ◽  
pp. 52293-52299 ◽  
Author(s):  
Christelle Lecut ◽  
Véronique Arocas ◽  
Hans Ulrichts ◽  
Anthony Elbaz ◽  
Jean-Luc Villeval ◽  
...  
Keyword(s):  
Monoclonal Antibody ◽  
Monoclonal Antibodies ◽  
Molecular Modeling ◽  
Binding Sites ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Binding Assays ◽  
Glycoprotein Vi ◽  
Ligand Binding Sites ◽  
Human Receptor

Glycoprotein VI (GPVI) has a crucial role in platelet responses to collagen. Still, little is known about its interaction with its ligands. In binding assays using soluble or cell-expressed human GPVI, we observed that (i) collagen, and the GPVI-specific ligands collagen-related peptides (CRP) and convulxin, competed with one another for the binding to GPVI and (ii) monoclonal antibodies directed against the extracellular part of the human receptor displayed selective inhibitory properties on GPVI interaction with its ligands. Monoclonal antibody 9E18 strongly reduced the binding of GPVI to collagen/CRP, 3F8 inhibited its interaction with convulxin, whereas 9O12 prevented all three interactions. These observations suggest that ligand-binding sites are distinct, exhibiting specific features but at the same time also sharing some common residues participating in the recognition of these ligands. The epitope of 9O12 was mapped by phage display, along with molecular modeling of human GPVI, which allowed the identification of residues within GPVI potentially involved in ligand recognition. Site-directed mutagenesis revealed that valine 34 and leucine 36 are critical for GPVI interaction with collagen and CRP. The loop might thus be part of a collagen/CRP-binding site.

scholarly journals Human P2Y1Receptor:  Molecular Modeling and Site-Directed Mutagenesis as Tools To Identify Agonist and Antagonist Recognition Sites

1998 ◽  
Vol 41 (9) ◽  
pp. 1456-1466 ◽  
Author(s):  
Stefano Moro ◽  
Danping Guo ◽  
Emidio Camaioni ◽  
José L. Boyer ◽  
T. Kendall Harden ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Recognition Sites ◽  
Agonist And Antagonist

Molecular Modeling-Guided Site-Directed Mutagenesis of Cytochrome P450 2D6

2007 ◽  
Vol 8 (1) ◽  
pp. 59-77 ◽  
Author(s):  
Chris de Graaf ◽  
Chris Oostenbrink ◽  
Peter J. Keizers ◽  
Barbara A. van Vugt-Lussenburg ◽  
Robert B. van Waterschoot ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Molecular Modeling ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Cytochrome P450 2D6 ◽  
P450 2D6
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