The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27994765 |
95 |
Discovery of Highly Potent Liver X Receptorß Agonists. |
Bristol-Myers Squibb |
27815118 |
112 |
Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists. |
Galderma R & D |
27599745 |
106 |
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core. |
Vitae Pharmaceuticals |
27326332 |
66 |
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist. |
Bristol-Myers Squibb |
27283790 |
33 |
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency andß-selectivity of liver X receptor agonist. |
Kowa |
26990539 |
79 |
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist. |
Vitae Pharmaceuticals |
27011007 |
17 |
Identification and in Vivo Evaluation of Liver X Receptorß-Selective Agonists for the Potential Treatment of Alzheimer's Disease. |
Wuxi Apptec |
26905831 |
11 |
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317. |
The University of Tokyo |
26288691 |
54 |
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators. |
The University of Tokyo |
26321361 |
56 |
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists. |
Genentech |
26238323 |
12 |
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists. |
Daiichi Sankyo Rd Novare |
26048793 |
91 |
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists. |
Genentech |
25998501 |
79 |
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptorß-selective agonists. |
Kowa |
25677664 |
30 |
Design and discovery of 2-oxochromene derivatives as liver X receptorß-selective agonists. |
Kowa |
25017032 |
62 |
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists. |
Genentech |
24502334 |
123 |
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc). |
Genentech |
25453817 |
130 |
A reversed sulfonamide series of selective RORc inverse agonists. |
Argenta Discovery |
25435151 |
34 |
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRß. |
Bristol-Myers Squibb |
25408828 |
4 |
Liver x receptor agonists for the treatment of coronary heart disease and other disorders. |
Therachem Research Medilab (India) |
25305688 |
41 |
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t. |
Phenex Pharmaceuticals |
24702856 |
84 |
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (ROR¿)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand. |
The University of Tokyo |
24685544 |
75 |
Identification of tertiary sulfonamides as RORc inverse agonists. |
Genentech |
24239186 |
84 |
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc. |
Genentech |
23769638 |
9 |
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes. |
Korea University |
23246324 |
2 |
Induction of ABCA1 and ABCG1 expression by the liver X receptor modulator cineole in macrophages. |
Korea University |
20345102 |
34 |
Discovery of tertiary sulfonamides as potent liver X receptor antagonists. |
Glaxosmithkline |
22579484 |
6 |
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells. |
Korea University |
22873709 |
45 |
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton. |
The University of Tokyo |
22901900 |
92 |
Discovery and optimization of a series of liver X receptor antagonists. |
Amgen |
22406115 |
18 |
Discovery of a new binding mode for a series of liver X receptor agonists. |
Amgen |
21218783 |
117 |
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents. |
Johnson & Johnson Pharmaceutical Research and Development |
20005711 |
102 |
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists. |
Wyeth Pharmaceuticals |
15911262 |
38 |
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters. |
Merck Research Laboratories |
20638278 |
145 |
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. |
Phenex Pharmaceuticals |
20382019 |
51 |
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists. |
Wyeth Pharmaceuticals |
20350005 |
45 |
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
Wyeth Pharmaceuticals |
20006495 |
62 |
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists. |
Wyeth Pharmaceuticals |
19962892 |
48 |
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
Wyeth Pharmaceuticals |
19932617 |
46 |
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists. |
Wyeth Pharmaceuticals |
19717304 |
29 |
The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
Glaxosmithkline |
19539483 |
78 |
Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists. |
The University of Tokyo |
19394832 |
74 |
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta. |
Wyeth Research |
19264481 |
58 |
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides. |
Astrazeneca R&D SöDertäLje |
18800767 |
45 |
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
Glaxosmithkline |
16180833 |
4 |
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents. |
Merck Research Laboratories |
16124770 |
26 |
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources. |
Merck Research Laboratories |
15844964 |
2 |
Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand. |
Merck Research Laboratories |
18023179 |
58 |
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity. |
Wyeth Pharmaceuticals |
17498949 |
4 |
Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors. |
University of Tokyo |
16876993 |
192 |
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta. |
F. Hoffmann-La Roche |
16529931 |
139 |
SAR studies: designing potent and selective LXR agonists. |
Merck Research Laboratories |
16125384 |
109 |
Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis. |
Merck Research Laboratories |
32551004 |
32 |
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist. |
Bristol Myers Squibb |
30702885 |
256 |
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation. |
Goethe University Frankfurt |
31257087 |
243 |
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists. |
Bristol-Myers Squibb |
30587446 |
46 |
Development of novel liver?X?receptor modulators based on a 1,2,4-triazole scaffold. |
Benha University |
31202993 |
37 |
Identify liver X receptor ? modulator building blocks by developing a fluorescence polarization-based competition assay. |
Sun Yat-Sen University |
30891142 |
121 |
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists. |
Bristol-Myers Squibb |
31638797 |
193 |
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy. |
Bristol-Myers Squibb |
30301676 |
91 |
Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (ROR?t) inhibitor, S18-000003. |
Shionogi |
30004226 |
9 |
Recent Advances in the Medicinal Chemistry of Liver X Receptors. |
Saint Louis University School of Medicine |
29571573 |
34 |
Sulfoximines as potent ROR? inverse agonists. |
Nestle Skin Health |
29398545 |
20 |
Structural development of tetrachlorophthalimides as liver X receptor ? (LXR?)-selective agonists with improved aqueous solubility. |
The University of Tokyo |
29233651 |
121 |
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR?/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity. |
Bristol-Myers Squibb |
30034593 |
58 |
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton. |
The University of Tokyo |
28735214 |
54 |
Indazole-based ligands for estrogen-related receptor ? as potential anti-diabetic agents. |
Janssen Research and Development |
28169169 |
8 |
DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators. |
Goethe-University Frankfurt |
28741954 |
22 |
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists. |
Universit£ |
24936059 |
26 |
The role of a novel auxiliary pocket in bacterial phenylalanyl-tRNA synthetase druggability. |
Astrazeneca R&D Boston |
24917667 |
36 |
Digoxin derivatives with enhanced selectivity for the a2 isoform of Na,K-ATPase: effects on intraocular pressure in rabbits. |
Weizmann Institute of Science |
24891505 |
6 |
Two amino acid residues confer different binding affinities of Abelson family kinase SRC homology 2 domains for phosphorylated cortactin. |
Yale University |
11438309 |
51 |
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. |
Janssen Research Foundation |
11408607 |
25 |
The peptide YY-preferring receptor mediating inhibition of small intestinal secretion is a peripheral Y(2) receptor: pharmacological evidence and molecular cloning. |
U410 |
15368579 |
20 |
Bisubstrate inhibitors of the enzyme catechol O-methyltransferase (COMT): efficient inhibition despite the lack of a nitro group. |
Laboratorium FÜR Organische Chemie |
7984267 |
675 |
Molecular biology of 5-HT receptors. |
University of Alberta |
7965790 |
38 |
Species orthologs of the alpha-2A adrenergic receptor: the pharmacological properties of the bovine and rat receptors differ from the human and porcine receptors. |
University of Nebraska |
7910212 |
34 |
Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo. |
Yamanouchi Pharmaceutical |
2958621 |
15 |
Characterization of D-2 dopamine receptors in a tumor of the rat anterior pituitary gland. |
University of Pennsylvania |
15489168 |
31 |
Disruption of protein-membrane binding and identification of small-molecule inhibitors of coagulation factor VIII. |
University of Washington |
15123286 |
131 |
Synthesis and target identification of hymenialdisine analogs. |
Genomics Institute of The Novartis Research Foundation |
18311908 |
42 |
Characterization of Type II Ligands in CYP2C9 and CYP3A4. |
Astrazeneca |