Identifying Activity Cliff Generators of PPAR Ligands Using SAS Maps

2012 ◽  
Vol 31 (11-12) ◽  
pp. 837-846 ◽  
Author(s):  
Oscar Méndez-Lucio ◽  
Jaime Pérez-Villanueva ◽  
Rafael Castillo ◽  
José L. Medina-Franco
Keyword(s):  
Activity Cliff ◽  
Sas Maps ◽  
Ppar Ligands ◽  
Activity Cliff Generators

Activity cliffs and activity cliff generators based on chemotype-related activity landscapes

2015 ◽  
Vol 19 (4) ◽  
pp. 1021-1035 ◽  
Author(s):  
Jaime Pérez-Villanueva ◽  
Oscar Méndez-Lucio ◽  
Olivia Soria-Arteche ◽  
José L. Medina-Franco
Keyword(s):  
Related Activity ◽  
Activity Cliff ◽  
Activity Cliff Generators ◽  
Activity Cliffs

774: Improvement of Anti-Angiogenic and Anti-Tumorigenic Efficacy of Thrombospondin-1 by PPAR┌ Ligands in Bladder Cancer

2007 ◽  
Vol 177 (4S) ◽  
pp. 259-259
Author(s):  
Thomas Nelius ◽  
Hanua Huang ◽  
Stephanie Filleur ◽  
Steven C. Campbell ◽  
Werner de Riese ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Thrombospondin 1 ◽  
Ppar Ligands

PPAR ligands: Potential therapies for metabolic syndrome

2005 ◽  
Vol 5 (1) ◽  
pp. 45-52 ◽  
Author(s):  
Taro E. Akiyama ◽  
Peter T. Meinke ◽  
Joel P. Berger
Keyword(s):  
Metabolic Syndrome ◽  
Ppar Ligands

The effect of PPAR?? ligands on the proliferation and apoptosis of human melanoma cells

2003 ◽  
Vol 13 (5) ◽  
pp. 447-456 ◽  
Author(s):  
Wojciech Placha ◽  
Dorota Gil ◽  
Aldona Dembi??ska-Kie?? ◽  
Piotr Laidler
Keyword(s):  
Melanoma Cells ◽  
Human Melanoma ◽  
Human Melanoma Cells ◽  
Proliferation And Apoptosis ◽  
Ppar Ligands

Solution- and solid-phase synthesis of peptide-substituted thiazolidinediones as potential PPAR ligands

2000 ◽  
Vol 10 (20) ◽  
pp. 2239-2242 ◽  
Author(s):  
Debra L Mohler ◽  
Gang Shen ◽  
Anthony K Dotse
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Ppar Ligands

Ligand‐based Activity Cliff Prediction Models with Applicability Domain

2020 ◽  
Vol 39 (12) ◽  
pp. 2000103
Author(s):  
Shunsuke Tamura ◽  
Tomoyuki Miyao ◽  
Kimito Funatsu
Keyword(s):  
Prediction Models ◽  
Applicability Domain ◽  
Activity Cliff

scholarly journals Comparison of PPAR Ligands as Modulators of Resolution of Inflammation, via Their Influence on Cytokines and Oxylipins Release in Astrocytes

2020 ◽  
Vol 21 (24) ◽  
pp. 9577
Author(s):  
Dmitry V. Chistyakov ◽  
Alina A. Astakhova ◽  
Sergei V. Goriainov ◽  
Marina G. Sergeeva
Keyword(s):  
Interleukin 10 ◽  
Mitogen Activated Protein Kinase ◽  
Cytochrome P450 Monooxygenases ◽  
Peroxisome Proliferator ◽  
Peroxisome Proliferator Activated Receptor ◽  
P450 Monooxygenases ◽  
Pparγ Agonist ◽  
Inflammatory Stimuli ◽  
Anti Inflammatory ◽  
Ppar Ligands

Neuroinflammation is a key process of many neurodegenerative diseases and other brain disturbances, and astrocytes play an essential role in neuroinflammation. Therefore, the regulation of astrocyte responses for inflammatory stimuli, using small molecules, is a potential therapeutic strategy. We investigated the potency of peroxisome proliferator-activated receptor (PPAR) ligands to modulate the stimulating effect of lipopolysaccharide (LPS) in the primary rat astrocytes on (1) polyunsaturated fatty acid (PUFAs) derivative (oxylipins) synthesis; (2) cytokines TNFα and interleukin-10 (IL-10) release; (3) p38, JNK, ERK mitogen-activated protein kinase (MAPKs) phosphorylation. Astrocytes were exposed to LPS alone or in combination with the PPAR ligands: PPARα (fenofibrate, GW6471); PPARβ (GW501516, GSK0660); PPARγ (rosiglitazone, GW9662). We detected 28 oxylipins with mass spectrometry (UPLC-MS/MS), classified according to their metabolic pathways: cyclooxygenase (COX), cytochrome P450 monooxygenases (CYP), lipoxygenase (LOX) and PUFAs: arachidonic (AA), docosahexaenoic (DHA), eicosapentaenoic (EPA). All tested PPAR ligands decrease COX-derived oxylipins; both PPARβ ligands possessed the strongest effect. The PPARβ agonist, GW501516 is a strong inducer of pro-resolution substances, derivatives of DHA: 4-HDoHE, 11-HDoHE, 17-HDoHE. All tested PPAR ligands decreased the release of the proinflammatory cytokine, TNFα. The PPARβ agonist GW501516 and the PPARγ agonist, rosiglitazone induced the IL-10 release of the anti-inflammatory cytokine, IL-10; the cytokine index, (IL-10/TNFα) was more for GW501516. The PPARβ ligands, GW501516 and GSK0660, are also the strongest inhibitors of LPS-induced phosphorylation of p38, JNK, ERK MAPKs. Overall, our data revealed that the PPARβ ligands are a potential pro-resolution and anti-inflammatory drug for targeting glia-mediated neuroinflammation.

7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues

2018 ◽  
Vol 26 (14) ◽  
pp. 4254-4263 ◽  
Author(s):  
Hui-jiao Sun ◽  
Yu-hua Wang ◽  
Cong-min Yuan ◽  
Ling-hui Kong ◽  
Xue-jun Xu ◽  
...  
Keyword(s):  
Methyl Substituent ◽  
Structural Locus ◽  
Activity Cliff

scholarly journals Synergistic interaction between PPAR ligands and salbutamol on human bronchial smooth muscle cell proliferation

2012 ◽  
Vol 168 (1) ◽  
pp. 266-275 ◽  
Author(s):  
S Fogli ◽  
F Stefanelli ◽  
L Picchianti ◽  
M Del Re ◽  
V Mey ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Smooth Muscle ◽  
Smooth Muscle Cell ◽  
Muscle Cell ◽  
Synergistic Interaction ◽  
Smooth Muscle Cell Proliferation ◽  
Bronchial Smooth Muscle ◽  
Ppar Ligands
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