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Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR).
TLDR
6m (XL335, WAY-362450) as a potent, selective, and orally bioavailable FXR agonist (EC(50) = 4 nM, Eff = 149%).
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LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse[S]
TLDR
Way-252623 (LXR-623) is a highly selective and orally bioavailable synthetic modulator of LXR, which demonstrated efficacy for reducing lesion progression in the murine LDLR−/− atherosclerosis model with no associated increase in hepatic lipogenesis either in this model or Syrian hamsters.
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Differing pharmacological activities of thiazolidinone analogs at the FSH receptor.
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Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
TLDR
Results suggest quinoxaline 13 may have an improved biological profile for potential use as a therapeutic agent and reduction of aortic arch lesion progression and no plasma or hepatic triglyceride increase are suggested.
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Identification and characterization of a selective, nonpeptide follicle-stimulating hormone receptor antagonist.
TLDR
A novel synthetic molecule capable of inhibiting the action of FSH is identified and characterized, providing proof of concept that selective, small molecule antagonists can be designed for glycoprotein hormone receptors.
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(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted…
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PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes.
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In Vivo and In Vitro Characterization of a First-in-Class Novel Azole Analog That Targets Pregnane X Receptor Activation
TLDR
The development and characterization of a first-in-class novel azole analog that antagonizes the activated state of PXR with limited effects on other related nuclear receptors is reported, suitable for development as chemical probes of P XR function as well as potential PX R-directed therapeutics.
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Small-Molecule Probes Targeting the Viral PPxY-Host Nedd4 Interface Block Egress of a Broad Range of RNA Viruses
TLDR
It is suggested that inhibition of the PPxY-Nedd4 interaction can serve as the basis for the development of a novel class of broad-spectrum, host-oriented antivirals targeting viruses that depend on a functional PPxy L domain for efficient egress.
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Synthesis of (bis)sulfonic acid, (bis)benzamides as follicle-stimulating hormone (FSH) antagonists.
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