Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064
about
FXR signaling in the enterohepatic systemDiscovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasisFarnesoid X receptor: from medicinal chemistry to clinical applicationsExposure to the synthetic FXR agonist GW4064 causes alterations in gene expression and sublethal hepatotoxicity in eleutheroembryo medaka (Oryzias latipes)Two farnesoid X receptor alpha isoforms in Japanese medaka (Oryzias latipes) are differentially activated in vitro.Pharmacophore-based discovery of FXR agonists. Part I: Model development and experimental validation.Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone.Structure-function correlation of G6, a novel small molecule inhibitor of Jak2: indispensability of the stilbenoid core.Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discoveryHalogen-enriched fragment libraries as chemical probes for harnessing halogen bonding in fragment-based lead discovery.Farnesoid X Receptor Agonist Represses Cytochrome P450 2D6 Expression by Upregulating Small Heterodimer Partner.Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease.Farnesoid X receptor modulators: a patent review.Medicinal chemistry of farnesoid X receptor ligands: from agonists and antagonists to modulators.Characterizing ligands for farnesoid X receptor--available in vitro test systems for farnesoid X receptor modulator development.Role of farnesoid X receptor in inflammation and resolution.Combining self- and cross-docking as benchmark tools: the performance of DockBench in the D3R Grand Challenge 2.Performance of HADDOCK and a simple contact-based protein-ligand binding affinity predictor in the D3R Grand Challenge 2.SAR studies on FXR modulators led to the discovery of the first combined FXR antagonistic/TGR5 agonistic compound.Design, Synthesis, and Biological Evaluation of Novel Nonsteroidal Farnesoid X Receptor (FXR) Antagonists: Molecular Basis of FXR Antagonism.Antidiabetic sulfonylureas modulate farnesoid X receptor activation and target gene transcription.Simultaneous diastereo- and enantioseparation of farnesoid X receptor (FXR) agonists with a quinine carbamate-based chiral stationary phase.Lessons learned in induced fit docking and metadynamics in the Drug Design Data Resource Grand Challenge 2.CDOCKER and λ-dynamics for prospective prediction in D₃R Grand Challenge 2.Nonacidic Chemotype Possessing N-Acylated Piperidine Moiety as Potent Farnesoid X Receptor (FXR) Antagonists.Bile acids are important direct and indirect regulators of the secretion of appetite- and metabolism-regulating hormones from the gut and pancreas.Discovery of new FXR agonists based on 6-ECDCA binding properties by virtual screening and molecular docking
P2860
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P2860
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064
description
2008 nî lūn-bûn
@nan
2008 թուականի Օգոստոսին հրատարակուած գիտական յօդուած
@hyw
2008 թվականի օգոստոսին հրատարակված գիտական հոդված
@hy
2008年の論文
@ja
2008年論文
@yue
2008年論文
@zh-hant
2008年論文
@zh-hk
2008年論文
@zh-mo
2008年論文
@zh-tw
2008年论文
@wuu
name
Conformationally constrained f ...... acid-based analogs of GW 4064
@ast
Conformationally constrained f ...... acid-based analogs of GW 4064
@en
Conformationally constrained f ...... acid-based analogs of GW 4064
@nl
type
label
Conformationally constrained f ...... acid-based analogs of GW 4064
@ast
Conformationally constrained f ...... acid-based analogs of GW 4064
@en
Conformationally constrained f ...... acid-based analogs of GW 4064
@nl
prefLabel
Conformationally constrained f ...... acid-based analogs of GW 4064
@ast
Conformationally constrained f ...... acid-based analogs of GW 4064
@en
Conformationally constrained f ...... acid-based analogs of GW 4064
@nl
P2093
P1476
Conformationally constrained f ...... acid-based analogs of GW 4064
@en
P2093
Aaron B Miller
Adwoa Akwabi-Ameyaw
David N Deaton
Derek J Parks
Frank Navas
G Bruce Wisely
Harry B Marr
Istvan Kaldor
Jonathan Y Bass
P304
P356
10.1016/J.BMCL.2008.06.073
P407
P577
2008-06-28T00:00:00Z