1,721,127 research outputs found
Homology model of the closed, functionally active, form of the amino terminal domain of mGlur1.
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Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis
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Farnesoid X receptor: from structure to potential clinical applications.
No full textThe farnesoid X receptor (FXR) is a well-characterized
member of the “metabolic” subfamily of NRs. In 1999
FXR was recognized to be a transcriptional sensor for
bile acids which are therefore witnessing their “renaissance”
as signaling molecules after more than 20 years
of research activity culminating with the clinical use of
chenodeoxycholic acid (CDCA) and ursodeoxycholic acid
(UDCA) in the treatment of gallbladder stones and
cholestatic liver diseases. Bile acids and oxysterols and
cholestanoic acids are distinct classes of steroidal molecules
derived from cholesterol. All of them
act as signaling molecules and participate in an intricate
network of interactions that ultimately govern lipid,
steroid, and cholesterol homeostasis and are involved
in processes such as glucose utilization, inflammation,
and cancer.
This Perspective will focus on the steps that led to
the discovery and deorphanization of FXR and to the
development of steroidal and nonsteroidal modulators,
with a special emphasis given to the increasing therapeutic
opportunities associated with FXR modulatio
Pharmacophore models of group I and group II metabotropic glutamate receptor agonists. Analysis of conformational, steric, and topological parameters affecting potency and selectivity
No full textModeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity
No full textExploring the Molecular Basis of Selectivity and Pharmacological Profile of Ligands with Metabotropic Glutamate Receptor
No full textLife or death decisions: the cast of poly(ADP-ribose)polymerase (PARP) as a therapeutic target for brain ischaemia.
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