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- Publications
- Influence
LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse[S]
Liver X receptors (LXRs) are ligand-activated transcription factors that coordinate regulation of gene expression involved in several cellular functions but most notably cholesterol homeostasis… Expand
Differing pharmacological activities of thiazolidinone analogs at the FSH receptor.
- B. Arey, Stephen D. Yanofsky, +6 authors Richard C. Winneker
- Biology, Medicine
- Biochemical and biophysical research…
- 11 April 2008
The follicle-stimulating hormone is critical to reproductive success and is an important target for development of novel reproductive therapies. We have recently reported the development of… Expand
Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR).
- B. Flatt, R. Martin, +14 authors Raju Mohan
- Chemistry, Medicine
- Journal of medicinal chemistry
- 21 January 2009
Azepino[4,5-b]indoles have been identified as potent agonists of the farnesoid X receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m (XL335, WAY-362450) as a potent,… Expand
Identification and characterization of a selective, nonpeptide follicle-stimulating hormone receptor antagonist.
- B. Arey, D. Deecher, +5 authors F. López
- Biology, Medicine
- Endocrinology
- 1 October 2002
The glycoprotein hormones (LH, FSH, and TSH) are critical to the maintenance of physiological homeostasis and control of reproduction. However, despite an obvious utility for synthetic… Expand
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
- B. Hu, R. Unwalla, +9 authors J. Wrobel
- Chemistry, Medicine
- Journal of medicinal chemistry
- 30 March 2010
A series of phenyl sulfone substituted quinoxaline were prepared and the lead compound 13 (WYE-672) was shown to be a tissue selective LXR Agonist. Compound 13 demonstrated partial agonism for… Expand
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.
- J. Pelletier, J. Lundquist, +25 authors P. Bodine
- Medicine, Chemistry
- Journal of medicinal chemistry
- 26 October 2009
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… Expand
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.
- J. Wrobel, J. Sredy, +9 authors Z. Y. Zhang
- Chemistry, Medicine
- Journal of medicinal chemistry
- 10 August 1999
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal…
- A. Fensome, R. Bender, +16 authors J. Wrobel
- Chemistry, Medicine
- Journal of medicinal chemistry
- 12 July 2005
Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives.… Expand
In Vivo and In Vitro Characterization of a First-in-Class Novel Azole Analog That Targets Pregnane X Receptor Activation
- Madhukumar Venkatesh, H. Wang, +5 authors S. Mani
- Biology, Medicine
- Molecular Pharmacology
- 1 July 2011
The pregnane X receptor (PXR) is a master regulator of xenobiotic clearance and is implicated in deleterious drug interactions (e.g., acetaminophen hepatotoxicity) and cancer drug resistance.… Expand
Small-Molecule Probes Targeting the Viral PPxY-Host Nedd4 Interface Block Egress of a Broad Range of RNA Viruses
- Z. Han, Jianhong Lu, +9 authors R. N. Harty
- Biology, Medicine
- Journal of Virology
- 16 April 2014
ABSTRACT Budding of filoviruses, arenaviruses, and rhabdoviruses is facilitated by subversion of host proteins, such as Nedd4 E3 ubiquitin ligase, by viral PPxY late (L) budding domains expressed… Expand
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