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 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

scholarly journals Solomonsterol A, a Marine Pregnane-X-Receptor Agonist, Attenuates Inflammation and Immune Dysfunction in a Mouse Model of Arthritis

Marine Drugs ◽  
2013 ◽  
Vol 12 (1) ◽  
pp. 36-53 ◽  
Author(s):  
Andrea Mencarelli ◽  
Claudio D'Amore ◽  
Barbara Renga ◽  
Sabrina Cipriani ◽  
Adriana Carino ◽  
...  
Keyword(s):  
Mouse Model ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Immune Dysfunction

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.

Pregnane X Receptor agonist Increases the Expression Levels of the Plasma Membrane Monoamine Transporter

2014 ◽  
Vol 22 (1) ◽  
pp. 19
Author(s):  
Sung Kweon Cho ◽  
Haejin Oh ◽  
Se Hyang Hong ◽  
Min Soo Park ◽  
Jae Yong Chung
Keyword(s):  
Plasma Membrane ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Monoamine Transporter ◽  
Expression Levels

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

Total Synthesis and Pharmacological Characterization of Solomonsterol A, a Potent Marine Pregnane-X-Receptor Agonist Endowed with Anti-Inflammatory Activity

2011 ◽  
Vol 54 (13) ◽  
pp. 4590-4599 ◽  
Author(s):  
Valentina Sepe ◽  
Raffaella Ummarino ◽  
Maria Valeria D’Auria ◽  
Andrea Mencarelli ◽  
Claudio D’Amore ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Inflammatory Activity ◽  
Pharmacological Characterization ◽  
Anti Inflammatory

A Pregnane X Receptor Agonist with Unique Species-Dependent Stereoselectivity and Its Implications in Drug Development

2005 ◽  
Vol 68 (2) ◽  
pp. 403-413 ◽  
Author(s):  
Ying Mu ◽  
Corey R. J. Stephenson ◽  
Christopher Kendall ◽  
Simrat P. S. Saini ◽  
David Toma ◽  
...  
Keyword(s):  
Drug Development ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Unique Species

scholarly journals Mangrove Tirucallane- and Apotirucallane-Type Triterpenoids: Structure Diversity of the C-17 Side-Chain and Natural Agonists of Human Farnesoid/Pregnane–X–Receptor

Marine Drugs ◽  
2018 ◽  
Vol 16 (12) ◽  
pp. 488 ◽  
Author(s):  
Zhong-Ping Jiang ◽  
Zhi-Lin Luan ◽  
Ruo-Xi Liu ◽  
Qun Zhang ◽  
Xiao-Chi Ma ◽  
...  
Keyword(s):  
Pregnane X Receptor ◽  
2D Nmr ◽  
Farnesoid X Receptor ◽  
Side Chain ◽  
X Ray Diffraction ◽  
One Dimensional ◽  
Excoecaria Agallocha ◽  
Xylocarpus Granatum ◽  
Modified Mosher’S Method ◽  
Structure Diversity

Ten new triterpenoid compounds with structure diversity of the C-17 side-chain, including nine tirucallanes, named xylocarpols A–E (1–5) and agallochols A–D (6–9), and an apotirucallane, named 25-dehydroxy protoxylogranatin B (10), were isolated from the mangrove plants Xylocarpus granatum, Xylocarpus moluccensis, and Excoecaria agallocha. The structures of these compounds were established by HR-ESIMS and extensive one-dimensional (1D) and two-dimensional (2D) NMR investigations. The absolute configurations of 1 and 2 were unequivocally determined by single-crystal X-ray diffraction analyses, conducted with Cu Kα radiation; whereas those of 4, 6–8 were assigned by a modified Mosher’s method and the comparison of experimental electronic circular dichroism (ECD) spectra. Most notably, 5, 6, 7, and 9 displayed potent activation effects on farnesoid–X–receptor (FXR) at the concentration of 10.0 μM; 10 exhibited very significant agonistic effects on pregnane–X–receptor (PXR) at the concentration of 10.0 nM.

The First Total Synthesis of Solomonsterol B, a Marine Pregnane X Receptor Agonist

2012 ◽  
Vol 2012 (27) ◽  
pp. 5187-5194 ◽  
Author(s):  
Valentina Sepe ◽  
Raffaella Ummarino ◽  
Maria Valeria D'Auria ◽  
Barbara Renga ◽  
Stefano Fiorucci ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Receptor Agonist ◽  
Pregnane X Receptor

scholarly journals High affinity rigidified AT2 receptor ligands with indane scaffolds

MedChemComm ◽  
2019 ◽  
Vol 10 (12) ◽  
pp. 2146-2160 ◽  
Author(s):  
Charlotta Wallinder ◽  
Christian Sköld ◽  
Sara Sundholm ◽  
Marie-Odile Guimond ◽  
Samir Yahiaoui ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Side Chain ◽  
At2 Receptor ◽  
Receptor Ligands ◽  
Receptor Agonists ◽  
High Affinity ◽  
Receptor Agonists And Antagonists

Rigidification of the isobutyl side chain of drug-like AT2 receptor agonists and antagonists that are structurally related to the first reported selective AT2 receptor agonist 1 (C21) delivered bioactive indane derivatives.

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