Characterization of a specific binding site for angiotensin II in chicken liver

1997 ◽  
Vol 75 (6) ◽  
pp. 568-575 ◽  
Author(s):  
R Bouley ◽  
M Gosselin ◽  
H Plante ◽  
G Servant ◽  
J Pérodin ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Binding Site ◽  
Specific Binding ◽  
Chicken Liver

scholarly journals Characterization of a high-affinity and specific binding site for Gas6

FEBS Letters ◽  
1996 ◽  
Vol 387 (1) ◽  
pp. 75-77 ◽  
Author(s):  
Toru Nakano ◽  
Junji Kishino ◽  
Hitoshi Arita
Keyword(s):  
Binding Site ◽  
Specific Binding ◽  
High Affinity

scholarly journals Identification and Mechanistic Characterization of a Peptide Inhibitor of Glycogen Synthase Kinase (GSK3β) Derived from the Disrupted in Schizophrenia 1 (DISC1) Protein

2020 ◽  
Author(s):  
Stephanie Saundh ◽  
Debasis Patnaik ◽  
Steve Gagné ◽  
Josh Bishop ◽  
Sean Lipsit ◽  
...  
Keyword(s):  
Binding Site ◽  
Glycogen Synthase ◽  
Specific Binding ◽  
Direct Interaction ◽  
Glycogen Synthase Kinase ◽  
Atp Binding Site ◽  
Inhibitory Region ◽  
Competitive Inhibitors ◽  
Cellular Pathways

ABSTRACTGlycogen Synthase Kinase 3-beta (GSK3β) is a critical regulator of several cellular pathways involved in neuroplasticity and is a potential target for neurotherapeutic development in the treatment of neuropsychiatric and neurodegenerative diseases. The majority of efforts to develop inhibitors of GSK3β have been focused on developing small molecule inhibitors that compete with ATP through direct interaction with the ATP binding site. This strategy has presented selectivity challenges due to the evolutionary conservation of this domain within the kinome. The Disrupted in Schizophrenia (DISC1) protein, has previously been shown to bind and inhibit GSK3β activity. Here, we report the characterization of a 44-mer peptide derived from human DISC1 (hDISCtide) that is sufficient to both bind and inhibit GSK3β in a non-competitive mode that is distinct from classical ATP competitive inhibitors. Based on multiple independent biochemical and biophysical assays, we propose that hDISCtide interacts at two distinct regions of GSK3β: an inhibitory region that partially overlaps with the binding site of FRATide, a well-known GSK3β binding peptide, and a specific binding region that is unique to hDISCtide. Taken together, our findings present a novel avenue for developing a peptide-based selective inhibitor of GSK3β.

Preparation and characterization of adrenocortical plasma membrane angiotensin II receptors

1976 ◽  
Vol 54 (5) ◽  
pp. 698-707 ◽  
Author(s):  
Gilles Forget ◽  
Seymour Heisler
Keyword(s):  
Angiotensin Ii ◽  
Sucrose Gradient ◽  
Binding Capacity ◽  
Specific Binding ◽  
High Affinity ◽  
Specific Effects ◽  
Highly Sensitive ◽  
High Affinity Binding Site ◽  
Gradient Bound

A bovine adrenocortical particulate fraction prepared by zonal ultracentrifugation and banding between ρ20 1.08 and 1.101 in a linear sucrose gradient bound 7.3 times more [3H]angiotensin II (ATII) per milligram protein than the original homogenate. Enzyme marker and electron microscope studies indicated that this fraction was largely devoid of mitochondria while being enriched in smooth membranes of predominantly plasmalemmal origin. The binding of labeled ATII was maximal after 10 min incubation (22 °C) and remained at equilibrium for at least 20 min thereafter. [3H]ATII binding was completely inhibited by saturating concentrations of nonradioactive ATII. The high-affinity binding site in the preparation had a specific binding capacity of 2.38 pmol∙mg−1, with an equilibrium constant of 2.36 × 108 M−1. Inhibition–displacement studies with unlabeled ATI, ATII, ATII fragments, analogs, and antagonists show that the receptor fraction has the highest affinity for the intact native octapeptide. ACTH and bradykinin had no specific effects on [3H]ATII binding. The current study suggests that the receptor fraction may be of use in a highly sensitive ATII radioligand assay.

A specific binding site recognizing a fragment of angiotensin II in bovine adrenal cortex membranes

1994 ◽  
Vol 271 (1) ◽  
pp. 55-63 ◽  
Author(s):  
Sylvie G. Bernier ◽  
Alain Fournier ◽  
Gaétan Guillemette
Keyword(s):  
Angiotensin Ii ◽  
Binding Site ◽  
Adrenal Cortex ◽  
Specific Binding
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