scholarly journals Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2Modified at the Para Position of the Benzyl Side Chain (DPhe): Importance for Mouse Melanocortin-3 Receptor Agonist versus Antagonist Activity

2008 ◽  
Vol 51 (18) ◽  
pp. 5585-5593 ◽  
Author(s):  
Bettina Proneth ◽  
Irina D. Pogozheva ◽  
Federico P. Portillo ◽  
Henry I. Mosberg ◽  
Carrie Haskell-Luevano
Keyword(s):  
Receptor Agonist ◽  
Para Position ◽  
Side Chain ◽  
Antagonist Activity

scholarly journals Cumyl‐CBMICA: A new synthetic cannabinoid receptor agonist containing a cyclobutyl methyl side chain

2020 ◽  
Author(s):  
Sebastian Halter ◽  
Benedikt Pulver ◽  
Maurice Wilde ◽  
Belal Haschimi ◽  
Folker Westphal ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Side Chain ◽  
Synthetic Cannabinoid Receptor Agonist

Modification in the side chain of solomonsterol A: discovery of cholestan disulfate as a potent pregnane-X-receptor agonist

2012 ◽  
Vol 10 (31) ◽  
pp. 6350 ◽  
Author(s):  
Valentina Sepe ◽  
Raffaella Ummarino ◽  
Maria Valeria D'Auria ◽  
Gianluigi Lauro ◽  
Giuseppe Bifulco ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Side Chain

scholarly journals Dual-acting peptide with prolonged glucagon-like peptide-1 receptor agonist and glucagon receptor antagonist activity for the treatment of type 2 diabetes

2007 ◽  
Vol 192 (2) ◽  
pp. 371-380 ◽  
Author(s):  
Thomas H Claus ◽  
Clark Q Pan ◽  
Joanne M Buxton ◽  
Ling Yang ◽  
Jennifer C Reynolds ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Insulin Secretion ◽  
Receptor Agonist ◽  
Antagonist Activity ◽  
Glucagon Receptor ◽  
Glucagon Receptor Antagonist ◽  
Glucagon Like Peptide ◽  
Glucagon Like Peptide 1

Type 2 diabetes is characterized by reduced insulin secretion from the pancreas and overproduction of glucose by the liver. Glucagon-like peptide-1 (GLP-1) promotes glucose-dependent insulin secretion from the pancreas, while glucagon promotes glucose output from the liver. Taking advantage of the homology between GLP-1 and glucagon, a GLP-1/glucagon hybrid peptide, dual-acting peptide for diabetes (DAPD), was identified with combined GLP-1 receptor agonist and glucagon receptor antagonist activity. To overcome its short plasma half-life DAPD was PEGylated, resulting in dramatically prolonged activity in vivo. PEGylated DAPD (PEG-DAPD) increases insulin and decreases glucose in a glucose tolerance test, evidence of GLP-1 receptor agonism. It also reduces blood glucose following a glucagon challenge and elevates fasting glucagon levels in mice, evidence of glucagon receptor antagonism. The PEG-DAPD effects on glucose tolerance are also observed in the presence of the GLP-1 antagonist peptide, exendin(9–39). An antidiabetic effect of PEG-DAPD is observed in db/db mice. Furthermore, PEGylation of DAPD eliminates the inhibition of gastrointestinal motility observed with GLP-1 and its analogues. Thus, PEG-DAPD has the potential to be developed as a novel dual-acting peptide to treat type 2 diabetes, with prolonged in vivo activity, and without the GI side-effects.

scholarly journals Carborane-based design of a potent vitamin D receptor agonist

2016 ◽  
Vol 7 (2) ◽  
pp. 1033-1037 ◽  
Author(s):  
Rocio Otero ◽  
Samuel Seoane ◽  
Rita Sigüeiro ◽  
Anna Y. Belorusova ◽  
Miguel A. Maestro ◽  
...  
Keyword(s):  
Vitamin D ◽  
Vitamin D Receptor ◽  
Receptor Agonist ◽  
Side Chain ◽  
Vitamin D Analog ◽  
Dihydrogen Bonding

The development of a promising clinical antitumor vitamin D analog possessing a side-chain o-carborane cluster that efficiently binds to VDR by unconventional dihydrogen bonding (BH⋯HN) is described.

Carbobenzoxy amino acids: structural requirements for cholecystokinin receptor antagonist activity

1985 ◽  
Vol 248 (4) ◽  
pp. G479-G484 ◽  
Author(s):  
P. N. Maton ◽  
V. E. Sutliff ◽  
R. T. Jensen ◽  
J. D. Gardner
Keyword(s):  
Amino Acids ◽  
Amino Acid ◽  
Receptor Antagonist ◽  
Amino Acid Derivative ◽  
Side Chain ◽  
Amylase Secretion ◽  
Amino Acid Side Chain ◽  
Antagonist Activity ◽  
Cholecystokinin Receptor ◽  
Stimulation Of

We used dispersed acini prepared from guinea pig pancreas to examine 28 carbobenzoxy (CBZ) amino acids for their abilities to function as cholecystokinin receptor antagonists. All amino acid derivatives tested, except for CBZ-alanine, CBZ-glycine, and N alpha-CBZ-lysine, were able to inhibit the stimulation of amylase secretion caused by the C-terminal octapeptide of cholecystokinin. In general, there was a good correlation between the ability of a carbobenzoxy amino acid to inhibit stimulated amylase secretion and the ability of the amino acid derivative to inhibit binding of 125I-cholecystokinin. The inhibition of cholecystokinin-stimulated amylase secretion was competitive, fully reversible, and specific for those secretagogues that interact with the cholecystokinin receptor. The potencies with which the various carbobenzoxy amino acids inhibited the action of cholecystokinin varied 100-fold and CBZ-cystine was the most potent cholecystokinin receptor antagonist. This variation in potency was primarily but not exclusively a function of the hydrophobicity of the amino acid side chain.

Subtle Side-Chain Modifications of the Hop Phytoestrogen 8-Prenylnaringenin Result in Distinct Agonist/Antagonist Activity Profiles for Estrogen Receptors α and β

2006 ◽  
Vol 49 (25) ◽  
pp. 7357-7365 ◽  
Author(s):  
Frederik Roelens ◽  
Nina Heldring ◽  
Willem Dhooge ◽  
Martin Bengtsson ◽  
Frank Comhaire ◽  
...  
Keyword(s):  
Estrogen Receptors ◽  
Side Chain ◽  
Antagonist Activity

Synthetic DAF-12 modulators with potential use in controlling the nematode life cycle

2014 ◽  
Vol 465 (1) ◽  
pp. 175-184 ◽  
Author(s):  
María V. Dansey ◽  
Lautaro D. Alvarez ◽  
Gisela Samaja ◽  
Daiana S. Escudero ◽  
Adriana S. Veleiro ◽  
...  
Keyword(s):  
Life Cycle ◽  
Double Bond ◽  
Side Chain ◽  
Antagonist Activity ◽  
Dafachronic Acid ◽  
Potential Use

Introduction of a 24,25-double bond into Δ4-dafachronic acid did not affect agonist DAF-12 activity. Shortening of the side chain resulted in antagonist activity, with 24-hydroxy-4-cholen-3-one being a pure antagonist in vitro and in vivo.

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