• Publications
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PPARs: therapeutic targets for metabolic disease.
Novel PPAR ligands are now being developed that possess broader efficacies and improved tolerability compared with currently available therapeutic agents. Expand
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase.
A novel fungal metabolite, apicidin, that exhibits potent, broad spectrum antiprotozoal activity in vitro against Apicomplexan parasites has been identified and is also orally and parenterally active in vivo against Plasmodium berghei malaria in mice. Expand
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Optimize SHI-1:2 structures exhibit enhanced intrinsic activity against HDAC1 and HDAC2, and are greater than 100-fold selective versus other HDACs, including HDAC3. Expand
Selective Small-Molecule Agonists of G Protein–Coupled Receptor 40 Promote Glucose-Dependent Insulin Secretion and Reduce Blood Glucose in Mice
GPR40 does not mediate the chronic toxic effects of FFAs on islet function, and pharmacological activation of GPR40 may potentiate GDIS in humans and be beneficial for overall glucose control in patients with type 2 diabetes. Expand
Guggulsterone Is a Farnesoid X Receptor Antagonist in Coactivator Association Assays but Acts to Enhance Transcription of Bile Salt Export Pump*
  • J. Cui, Li Huang, +7 authors S. Wright
  • Biology, Medicine
  • The Journal of Biological Chemistry
  • 21 March 2003
It is proposed that guggulipid is a selectivebile acid receptormodulator that regulates expression of a subset of FXR targets, and defines a novel class ofFXR ligands characterized by antagonist activities in coactivator association assays but with the ability to enhance the action of agonists onBSEP expression in vivo. Expand
Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the gamma-aminobutyric acid(A) receptor.
Avermectins, which were anticonvulsant, were also potent inhibitors of [(3)H]ivermectin binding in rat brain, and it is unlikely that these effects can be separated, which may contraindicate the potential use of avermECTins as anticonVulsants. Expand
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
The pyridone-containing tetracycle may be prepared from trisubstituted imidazole in high yield by irradiation with >350 nm light and inhibits the phosphorylation of STAT5 (an in vivo substrate of the Jak family) as measured by Western blotting. Expand
Lithocholic Acid Decreases Expression of Bile Salt Export Pump through Farnesoid X Receptor Antagonist Activity*
  • J. Yu, J. Lo, +6 authors J. Cui
  • Medicine, Biology
  • The Journal of Biological Chemistry
  • 30 August 2002
It is demonstrated that BSEP expression is dramatically regulated by ligands of the nuclear receptor farnesoid X receptor (FXR) and that FXR ligands may be potential therapeutic drugs for intrahepatic cholestasis. Expand
Discovery of a Pharmacologically Active Antagonist of the Two‐Pore‐Domain Potassium Channel K2P9.1 (TASK‐3)
The discovery and lead optimization efforts for a novel series of TASK‐3 channel antagonists based on a 5,6,7,8‐tetrahydropyrido[4,3‐d]pyrimidine high‐throughput screening lead from which a subseries of potent and selective inhibitors were identified were described. Expand
Discovery of MK‐8742: An HCV NS5A Inhibitor with Broad Genotype Activity
The research efforts that led to the discovery of MK‐8742, a tetracyclic indole‐based NS5A inhibitor, which is currently in phase 2b clinical trials as part of an all‐oral, interferon‐free regimen for the treatment of HCV infection is described. Expand