scholarly journals Structure‐based survey of ligand binding in the human insulin receptor

2021 ◽  
Author(s):  
Lokender Kumar ◽  
Whitney Vizgaudis ◽  
Judith Klein‐Seetharaman
Keyword(s):  
Ligand Binding ◽  
Insulin Receptor ◽  
Human Insulin ◽  
Human Insulin Receptor

The ligand binding characteristics of a kinase-defective A/K1018 human insulin receptor expressed in Rat 1 fibroblasts

1990 ◽  
Vol 1053 (2-3) ◽  
pp. 185-188 ◽  
Author(s):  
Hiroshi Maegawa ◽  
Masashi Kobayashi ◽  
Katsuya Egawa ◽  
Donald A. McClain ◽  
Jerrold M. Olefsky ◽  
...  
Keyword(s):  
Ligand Binding ◽  
Insulin Receptor ◽  
Human Insulin ◽  
Binding Characteristics ◽  
Human Insulin Receptor

Ligand-binding properties of the two isoforms of the human insulin receptor.

Endocrinology ◽  
1993 ◽  
Vol 132 (3) ◽  
pp. 1132-1138 ◽  
Author(s):  
Y Yamaguchi ◽  
J S Flier ◽  
H Benecke ◽  
B J Ransil ◽  
D E Moller
Keyword(s):  
Ligand Binding ◽  
Insulin Receptor ◽  
Human Insulin ◽  
Binding Properties ◽  
Human Insulin Receptor

scholarly journals Structure-based survey of ligand binding in the human insulin receptor

2021 ◽  
Author(s):  
Judith Klein-Seetharaman ◽  
Whitney Vizgaudis ◽  
Lokender Kumar
Keyword(s):  
Ligand Binding ◽  
Insulin Receptor ◽  
Human Insulin ◽  
Nutrient Balance ◽  
Docking Study ◽  
Human Insulin Receptor ◽  
Receptor Pharmacology ◽  
Entire Sequence ◽  
Treatment Of Diabetes ◽  
Structural Insights

The insulin receptor is a membrane protein responsible for regulation of nutrient balance and therefore an attractive target in the treatment of diabetes and metabolic syndrome. Pharmacology of the insulin receptor involves two distinct mechanisms, (1) activation of the receptor by insulin mimetics that bind in the extracellular domain and (2) inhibition of the receptor tyrosine kinase enzymatic activity in the cytoplasmic domain. While a complete structural picture of the full-length receptor comprising the entire sequence covering extracellular, transmembrane, juxtamembrane and cytoplasmic domains is still elusive, recent progress through cryoelectron microscopy has made it possible to describe the initial insulin ligand binding events at atomistic detail. We utilize this opportunity to obtain structural insights into the pharmacology of the insulin receptor. To this end, we conducted a comprehensive docking study of known ligands to the new structures of the receptor. Through this approach, we provide an in-depth, structure-based review of human insulin receptor pharmacology in light of the new structures.

scholarly journals Identification of a Ligand-Binding Region of the Human Insulin Receptor Encoded by the Second Exon of the Gene

1990 ◽  
Vol 4 (3) ◽  
pp. 409-416 ◽  
Author(s):  
Pierre De Meyts ◽  
Jia-Li Gu ◽  
Ronald M. Shymko ◽  
Bruce E. Kaplan ◽  
Graeme I. Bell ◽  
...  
Keyword(s):  
Ligand Binding ◽  
Insulin Receptor ◽  
Human Insulin ◽  
Binding Region ◽  
Human Insulin Receptor
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