TY - JOUR
T1 - Nuclear magnetic resonance (NMR) analysis of ligand receptor interactions
T2 - The cholinergic system - A model
AU - Fraenkel, Yigal
AU - Shalev, Deborah E.
AU - Gershoni, Jonathan M.
AU - Navon, Gil
PY - 1996
Y1 - 1996
N2 - Elucidation of the molecular mechanisms that govern ligand-receptor recognition is essential to the rational design of specific pharmacological reagents. Whereas often the receptor and its binding site are the target of investigation, study of the ligand in its free and bound state can also reveal important information regarding this recognition process. Nuclear magnetic resonance (NMR) spectroscopy can be extremely useful for such studies. In this review, we discuss the attributes of NMR in the study of ligand receptor interactions. The cholinergic receptor and its binding to the neurotransmitter, acetylcholine, and cholinergic antagonists serve as a model system, illustrating the power of ligand analysis by NMR. The results discussed prove that the region of residues α 180-205 of the nicotinic actylcholine receptor are an essential component of the cholinergic binding site and that ligand binding involves a positively charged hydrophobic motif.
AB - Elucidation of the molecular mechanisms that govern ligand-receptor recognition is essential to the rational design of specific pharmacological reagents. Whereas often the receptor and its binding site are the target of investigation, study of the ligand in its free and bound state can also reveal important information regarding this recognition process. Nuclear magnetic resonance (NMR) spectroscopy can be extremely useful for such studies. In this review, we discuss the attributes of NMR in the study of ligand receptor interactions. The cholinergic receptor and its binding to the neurotransmitter, acetylcholine, and cholinergic antagonists serve as a model system, illustrating the power of ligand analysis by NMR. The results discussed prove that the region of residues α 180-205 of the nicotinic actylcholine receptor are an essential component of the cholinergic binding site and that ligand binding involves a positively charged hydrophobic motif.
KW - cholinergic system
KW - ligand receptor interactions
KW - nuclear magnetic resonance
KW - pharmacological reagents
UR - http://www.scopus.com/inward/record.url?scp=0029742248&partnerID=8YFLogxK
U2 - 10.3109/10409239609106586
DO - 10.3109/10409239609106586
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C2 - 8877268
AN - SCOPUS:0029742248
SN - 1040-9238
VL - 31
SP - 273
EP - 301
JO - Critical Reviews in Biochemistry and Molecular Biology
JF - Critical Reviews in Biochemistry and Molecular Biology
IS - 4
ER -