Thomas P Burris

Thomas P Burris, Ph.D.

Director

Department: RE-GENETICS INSTITUTE-GENERAL
Business Phone: (352) 273-9893
Business Email: burris.thomas@ufl.edu

Teaching Profile

Courses Taught
2022-2023
PHA6512L Experiential Research Training in Pharmacodynamics
2022
PHA6521C Research Techniques in Pharmacodynamics

Research Profile

Open Researcher and Contributor ID (ORCID)

0000-0003-2922-4449

Publications

2022
Antihyperlipidemic Activity of Gut-Restricted LXR Inverse Agonists
ACS Chemical Biology. 17(5):1143-1154 [DOI] 10.1021/acschembio.2c00057.
2022
Emerging Role of Nuclear Receptors for the Treatment of NAFLD and NASH.
Metabolites. 12(3) [DOI] 10.3390/metabo12030238. [PMID] 35323681.
2022
Progress toward the De Novo Asymmetric Synthesis of Euphanes
Organic Letters. 24(20):3686-3690 [DOI] 10.1021/acs.orglett.2c01299. [PMID] 35584298.
2022
Structural basis of synthetic agonist activation of the nuclear receptor REV-ERB
Nature Communications. 13(1) [DOI] 10.1038/s41467-022-34892-4. [PMID] 36414641.
2022
The role of REV-ERB in NASH.
Acta pharmacologica Sinica. 43(5):1133-1140 [DOI] 10.1038/s41401-022-00883-w. [PMID] 35217816.
2021
A two-hit model of alcoholic liver disease that exhibits rapid, severe fibrosis.
PloS one. 16(3) [DOI] 10.1371/journal.pone.0249316. [PMID] 33770118.
2021
Fructose Promotes Cytoprotection in Melanoma Tumors and Resistance to Immunotherapy.
Cancer immunology research. 9(2):227-238 [DOI] 10.1158/2326-6066.CIR-20-0396. [PMID] 33023966.
2021
In Science Journals.
Science (New York, N.Y.). 374(6574):1458-1460 [DOI] 10.1126/science.acz9826. [PMID] 34914531.
2021
Naturally Occurring Genetic Variants in the Oxytocin Receptor Alter Receptor Signaling Profiles
ACS Pharmacology & Translational Science. 4(5):1543-1555 [DOI] 10.1021/acsptsci.1c00095. [PMID] 34661073.
2021
Restoration of the molecular clock is tumor suppressive in neuroblastoma
Nature Communications. 12(1) [DOI] 10.1038/s41467-021-24196-4. [PMID] 34183658.
2020
A Selective ERRα/γ Inverse Agonist, SLU-PP-1072, Inhibits the Warburg Effect and Induces Apoptosis in Prostate Cancer Cells
ACS Chemical Biology. 15(9):2338-2345 [DOI] 10.1021/acschembio.0c00670.
2020
Clock regulation of protein secretion
Nature Cell Biology. 22(1):1-3 [DOI] 10.1038/s41556-019-0449-4.
2020
Modulation of estrogen-related receptors subtype selectivity: Conversion of an ERRβ/γ selective agonist to ERRα/β/γ pan agonists.
Bioorganic chemistry. 102 [DOI] 10.1016/j.bioorg.2020.104079. [PMID] 32683181.
2020
REV-ERB agonism improves liver pathology in a mouse model of NASH.
PloS one. 15(10) [DOI] 10.1371/journal.pone.0236000. [PMID] 33002003.
2020
Rev-erbα heterozygosity produces a dose-dependent phenotypic advantage in mice.
PloS one. 15(5) [DOI] 10.1371/journal.pone.0227720. [PMID] 32407314.
2020
The Orphan Nuclear Receptor TLX Is a Receptor for Synthetic and Natural Retinoids
Cell Chemical Biology. 27(10):1272-1284.e4 [DOI] 10.1016/j.chembiol.2020.07.013.
2020
Weak Microbial Metabolites: a Treasure Trove for Using Biomimicry to Discover and Optimize Drugs.
Molecular pharmacology. 98(4):343-349 [DOI] 10.1124/molpharm.120.000035. [PMID] 32764096.
2019
A synthesis strategy for tetracyclic terpenoids leads to agonists of ERβ.
Nature communications. 10(1) [DOI] 10.1038/s41467-019-10415-6. [PMID] 31164645.
2019
Circadian clock protein Rev-erbα regulates neuroinflammation.
Proceedings of the National Academy of Sciences of the United States of America. 116(11):5102-5107 [DOI] 10.1073/pnas.1812405116. [PMID] 30792350.
2019
Circadian rhythm–dependent and circadian rhythm–independent impacts of the molecular clock on type 3 innate lymphoid cells
Science Immunology. 4(40) [DOI] 10.1126/sciimmunol.aay7501. [PMID] 31586012.
2019
Corrigendum to “Pharmacological targeting of the mammalian clock reveals a novel analgesic for osteoarthritis-induced pain” [GENE 655 (2018) 1-12].
Gene. 680 [DOI] 10.1016/j.gene.2018.06.013. [PMID] 29890121.
2019
Development of novel liver X receptor modulators based on a 1,2,4-triazole scaffold.
Bioorganic & medicinal chemistry letters. 29(3):449-453 [DOI] 10.1016/j.bmcl.2018.12.025. [PMID] 30587446.
2019
Doubled lifespan and patient-like pathologies in progeria mice fed high-fat diet.
Aging cell. 18(1) [DOI] 10.1111/acel.12852. [PMID] 30548460.
2019
Pharmacological activation of the nuclear receptor REV-ERB reverses cognitive deficits and reduces amyloid-β burden in a mouse model of Alzheimer’s disease
PLOS ONE. 14(4) [DOI] 10.1371/journal.pone.0215004. [PMID] 30973894.
2019
RORγ regulates the NLRP3 inflammasome.
The Journal of biological chemistry. 294(1):10-19 [DOI] 10.1074/jbc.AC118.002127. [PMID] 30455347.
2019
SR9009 administered for one day after myocardial ischemia-reperfusion prevents heart failure in mice by targeting the cardiac inflammasome.
Communications biology. 2 [DOI] 10.1038/s42003-019-0595-z. [PMID] 31602405.
2019
The nuclear receptor REV-ERBα modulates Th17 cell-mediated autoimmune disease.
Proceedings of the National Academy of Sciences of the United States of America. 116(37):18528-18536 [DOI] 10.1073/pnas.1907563116. [PMID] 31455731.
2018
Adropin: An endocrine link between the biological clock and cholesterol homeostasis.
Molecular metabolism. 8:51-64 [DOI] 10.1016/j.molmet.2017.12.002. [PMID] 29331507.
2018
Distinct roles for REV-ERBα and REV-ERBβ in oxidative capacity and mitochondrial biogenesis in skeletal muscle.
PloS one. 13(5) [DOI] 10.1371/journal.pone.0196787. [PMID] 29723273.
2018
Inhibition of Hepatotoxicity by a LXR Inverse Agonist in a Model of Alcoholic Liver Disease
ACS Pharmacology & Translational Science. 1(1):50-60 [DOI] 10.1021/acsptsci.8b00003. [PMID] 31696159.
2018
Nuclear Receptor Subfamily 1 Group D Member 1 Regulates Circadian Activity of NLRP3 Inflammasome to Reduce the Severity of Fulminant Hepatitis in Mice.
Gastroenterology. 154(5):1449-1464.e20 [DOI] 10.1053/j.gastro.2017.12.019. [PMID] 29277561.
2018
Pharmacological targeting of the mammalian clock reveals a novel analgesic for osteoarthritis-induced pain.
Gene. 655:1-12 [DOI] 10.1016/j.gene.2018.02.048. [PMID] 29474860.
2018
Recent Advances in the Medicinal Chemistry of Liver X Receptors
Journal of Medicinal Chemistry. 61(24):10935-10956 [DOI] 10.1021/acs.jmedchem.8b00045.
2018
REV-ERBβ is required to maintain normal wakefulness and the wake-inducing effect of dual REV-ERB agonist SR9009.
Biochemical pharmacology. 150:1-8 [DOI] 10.1016/j.bcp.2018.01.009. [PMID] 29355503.
2017
Disrupting the key circadian regulator CLOCK leads to age-dependent cardiovascular disease.
Journal of molecular and cellular cardiology. 105:24-37 [DOI] 10.1016/j.yjmcc.2017.01.008. [PMID] 28223222.
2017
Metabolic Characterization of a Novel RORα Knockout Mouse Model without Ataxia.
Frontiers in endocrinology. 8 [DOI] 10.3389/fendo.2017.00141. [PMID] 28744254.
2017
Oral IL-10 suppresses colon carcinogenesis via elimination of pathogenicCD4+ T-cells and induction of antitumor CD8+ T-cell activity.
Oncoimmunology. 6(6) [DOI] 10.1080/2162402X.2017.1319027. [PMID] 28680752.
2017
Pharmacological inhibition of REV-ERB stimulates differentiation, inhibits turnover and reduces fibrosis in dystrophic muscle.
Scientific reports. 7(1) [DOI] 10.1038/s41598-017-17496-7. [PMID] 29215066.
2017
Rev-Erb co-regulates muscle regeneration via tethered interaction with the NF-Y cistrome.
Molecular metabolism. 6(7):703-714 [DOI] 10.1016/j.molmet.2017.05.001. [PMID] 28702326.
2017
Rev-erb regulation of cholesterologenesis.
Biochemical pharmacology. 131:68-77 [DOI] 10.1016/j.bcp.2017.02.006. [PMID] 28213272.
2017
REV-ERBα ameliorates heart failure through transcription repression.
JCI insight. 2(17) [DOI] 10.1172/jci.insight.95177. [PMID] 28878135.
2017
Targeting Th17-IL-17 Pathway in Prevention of Micro-Invasive Prostate Cancer in a Mouse Model.
The Prostate. 77(8):888-899 [DOI] 10.1002/pros.23343. [PMID] 28240383.
2016
Correction: Pharmacological and Genetic Modulation of REV-ERB Activity and Expression Affects Orexigenic Gene Expression.
PloS one. 11(5) [DOI] 10.1371/journal.pone.0156367. [PMID] 27195801.
2016
Inhibition of RORα/γ suppresses atherosclerosis via inhibition of both cholesterol absorption and inflammation.
Molecular metabolism. 5(10):997-1005 [DOI] 10.1016/j.molmet.2016.07.001. [PMID] 27689012.
2016
Nuclear receptors: PPARα ligands make memories.
Nature chemical biology. 12(12):993-994 [DOI] 10.1038/nchembio.2241. [PMID] 27846207.
2016
Pharmacological and Genetic Modulation of REV-ERB Activity and Expression Affects Orexigenic Gene Expression.
PloS one. 11(3) [DOI] 10.1371/journal.pone.0151014. [PMID] 26963516.
2016
Pharmacological Targeting the REV-ERBs in Sleep/Wake Regulation.
PloS one. 11(9) [DOI] 10.1371/journal.pone.0162452. [PMID] 27603791.
2016
Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease.
Biochemical and biophysical research communications. 479(3):424-428 [DOI] 10.1016/j.bbrc.2016.09.036. [PMID] 27680310.
2016
Therapeutic Effect of a Synthetic RORα/γ Agonist in an Animal Model of Autism.
ACS chemical neuroscience. 7(2):143-8 [DOI] 10.1021/acschemneuro.5b00159. [PMID] 26625251.
2015
Anti-proliferative actions of a synthetic REV-ERBα/β agonist in breast cancer cells.
Biochemical pharmacology. 96(4):315-22 [DOI] 10.1016/j.bcp.2015.06.010. [PMID] 26074263.
2015
Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis.
Cancer cell. 28(1):42-56 [DOI] 10.1016/j.ccell.2015.05.007. [PMID] 26120082.
2015
Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists.
Bioorganic & medicinal chemistry letters. 25(7):1377-80 [DOI] 10.1016/j.bmcl.2015.02.062. [PMID] 25752984.
2015
ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes.
Endocrinology. 156(3):869-81 [DOI] 10.1210/en.2014-1677. [PMID] 25560829.
2015
Segregation of Clock and Non-Clock Regulatory Functions of REV-ERB.
Cell metabolism. 22(2):197-8 [DOI] 10.1016/j.cmet.2015.07.014. [PMID] 26244927.
2015
SIRT1 in the Ventromedial Hypothalamus: A Nutrient Sensor Input Into the Internal Timekeeper.
Endocrinology. 156(6):1936-8 [DOI] 10.1210/en.2015-1346. [PMID] 25978598.
2015
Suppression of atherosclerosis by synthetic REV-ERB agonist.
Biochemical and biophysical research communications. 460(3):566-71 [DOI] 10.1016/j.bbrc.2015.03.070. [PMID] 25800870.
2015
Th17 cells in Type 1 diabetes: a future perspective.
Diabetes management (London, England). 5(4):247-250 [PMID] 27708719.
2015
The LXR inverse agonist SR9238 suppresses fibrosis in a model of non-alcoholic steatohepatitis.
Molecular metabolism. 4(4):353-7 [DOI] 10.1016/j.molmet.2015.01.009. [PMID] 25830098.
2015
The optimal corepressor function of nuclear receptor corepressor (NCoR) for peroxisome proliferator-activated receptor γ requires G protein pathway suppressor 2.
The Journal of biological chemistry. 290(6):3666-79 [DOI] 10.1074/jbc.M114.598797. [PMID] 25519902.
2014
An alternate binding site for PPARγ ligands.
Nature communications. 5 [DOI] 10.1038/ncomms4571. [PMID] 24705063.
2014
Artemisia extracts activate PPARγ, promote adipogenesis, and enhance insulin sensitivity in adipose tissue of obese mice.
Nutrition (Burbank, Los Angeles County, Calif.). 30(7-8 Suppl):S31-6 [DOI] 10.1016/j.nut.2014.02.013. [PMID] 24985103.
2014
Artemisia scoparia enhances adipocyte development and endocrine function in vitro and enhances insulin action in vivo.
PloS one. 9(6) [DOI] 10.1371/journal.pone.0098897. [PMID] 24915004.
2014
Clock genes, pancreatic function, and diabetes.
Trends in molecular medicine. 20(12):685-93 [DOI] 10.1016/j.molmed.2014.10.007. [PMID] 25457619.
2014
International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands.
Pharmacological reviews. 66(4):918-47 [DOI] 10.1124/pr.114.008862. [PMID] 25026896.
2014
Pharmacological targeting of the mammalian clock regulates sleep architecture and emotional behaviour.
Nature communications. 5 [DOI] 10.1038/ncomms6759. [PMID] 25536025.
2014
REV-ERB and ROR nuclear receptors as drug targets.
Nature reviews. Drug discovery. 13(3):197-216 [DOI] 10.1038/nrd4100. [PMID] 24577401.
2014
Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist.
The Journal of biological chemistry. 289(29):20054-66 [DOI] 10.1074/jbc.M113.545111. [PMID] 24872411.
2013
A liver-selective LXR inverse agonist that suppresses hepatic steatosis.
ACS chemical biology. 8(3):559-67 [DOI] 10.1021/cb300541g. [PMID] 23237488.
2013
Involvement of the clock gene Rev-erb alpha in the regulation of glucagon secretion in pancreatic alpha-cells.
PloS one. 8(7) [DOI] 10.1371/journal.pone.0069939. [PMID] 23936124.
2013
Nuclear receptors and their selective pharmacologic modulators.
Pharmacological reviews. 65(2):710-78 [DOI] 10.1124/pr.112.006833. [PMID] 23457206.
2013
Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy.
Nature medicine. 19(8):1039-46 [DOI] 10.1038/nm.3213. [PMID] 23852339.
2013
Small molecule modulation of nuclear receptor conformational dynamics: implications for function and drug discovery.
Molecular pharmacology. 83(1):1-8 [DOI] 10.1124/mol.112.079285. [PMID] 22869589.
2013
The mammalian clock and chronopharmacology.
Bioorganic & medicinal chemistry letters. 23(7):1929-34 [DOI] 10.1016/j.bmcl.2013.02.015. [PMID] 23481644.
2012
Action of RORs and their ligands in (patho)physiology.
Trends in endocrinology and metabolism: TEM. 23(12):619-27 [DOI] 10.1016/j.tem.2012.05.012. [PMID] 22789990.
2012
Divergent transcriptional programming of class-specific B cell memory by T-bet and RORα.
Nature immunology. 13(6):604-11 [DOI] 10.1038/ni.2294. [PMID] 22561605.
2012
Identification of a selective RORγ ligand that suppresses T(H)17 cells and stimulates T regulatory cells.
ACS chemical biology. 7(9):1515-9 [PMID] 22769242.
2012
Identification of SR2211: a potent synthetic RORγ-selective modulator.
ACS chemical biology. 7(4):672-7 [DOI] 10.1021/cb200496y. [PMID] 22292739.
2012
Ligand and receptor dynamics contribute to the mechanism of graded PPARγ agonism.
Structure (London, England : 1993). 20(1):139-50 [DOI] 10.1016/j.str.2011.10.018. [PMID] 22244763.
2012
LXR-mediated inhibition of CD4+ T helper cells.
PloS one. 7(9) [DOI] 10.1371/journal.pone.0046615. [PMID] 23029557.
2012
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
Nature. 485(7396):62-8 [DOI] 10.1038/nature11030. [PMID] 22460951.
2012
Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα).
PloS one. 7(4) [DOI] 10.1371/journal.pone.0033804. [PMID] 22485150.
2012
Regulation of p53 stability and apoptosis by a ROR agonist.
PloS one. 7(4) [DOI] 10.1371/journal.pone.0034921. [PMID] 22509368.
2012
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
Bioorganic & medicinal chemistry letters. 22(13):4413-7 [DOI] 10.1016/j.bmcl.2012.04.126. [PMID] 22633688.
2012
Structural and biophysical insights into the ligand-free Pitx2 homeodomain and a ring dermoid of the cornea inducing homeodomain mutant.
Biochemistry. 51(2):665-76 [DOI] 10.1021/bi201639x. [PMID] 22224469.
2012
Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists.
Bioorganic & medicinal chemistry letters. 22(11):3739-42 [DOI] 10.1016/j.bmcl.2012.04.023. [PMID] 22560469.
2012
Targeting orphan nuclear receptors for treatment of metabolic diseases and autoimmunity.
Chemistry & biology. 19(1):51-9 [DOI] 10.1016/j.chembiol.2011.12.011. [PMID] 22284354.
2011
A role for rev-erbα ligands in regulation of adipogenesis.
Current pharmaceutical design. 17(4):320-4 [PMID] 21375499.
2011
Direct regulation of CLOCK expression by REV-ERB.
PloS one. 6(3) [DOI] 10.1371/journal.pone.0017290. [PMID] 21479263.
2011
DNA binding alters coactivator interaction surfaces of the intact VDR-RXR complex.
Nature structural & molecular biology. 18(5):556-63 [DOI] 10.1038/nsmb.2046. [PMID] 21478866.
2011
Genetic dissection of the functions of the melanocortin-3 receptor, a seven-transmembrane G-protein-coupled receptor, suggests roles for central and peripheral receptors in energy homeostasis.
The Journal of biological chemistry. 286(47):40771-81 [DOI] 10.1074/jbc.M111.278374. [PMID] 21984834.
2011
Identification of a novel non-retinoid pan inverse agonist of the retinoic acid receptors.
ACS chemical biology. 6(6):618-27 [DOI] 10.1021/cb100396s. [PMID] 21381756.
2011
Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist.
ACS chemical biology. 6(3):218-22 [DOI] 10.1021/cb1002762. [PMID] 21090593.
2011
Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.
ACS chemical biology. 6(2):131-4 [DOI] 10.1021/cb1002575. [PMID] 21043485.
2011
Liver X receptor-retinoid X receptor (LXR-RXR) heterodimer cistrome reveals coordination of LXR and AP1 signaling in keratinocytes.
The Journal of biological chemistry. 286(16):14554-63 [DOI] 10.1074/jbc.M110.165704. [PMID] 21349840.
2011
Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand.
Nature. 472(7344):491-4 [DOI] 10.1038/nature10075. [PMID] 21499262.
2011
The REV-ERBs and RORs: molecular links between circadian rhythms and lipid homeostasis.
Future medicinal chemistry. 3(5):623-38 [DOI] 10.4155/fmc.11.9. [PMID] 21526899.
2010
A second class of nuclear receptors for oxysterols: Regulation of RORalpha and RORgamma activity by 24S-hydroxycholesterol (cerebrosterol).
Biochimica et biophysica acta. 1801(8):917-23 [DOI] 10.1016/j.bbalip.2010.02.012. [PMID] 20211758.
2010
Characterization of the core mammalian clock component, NPAS2, as a REV-ERBalpha/RORalpha target gene.
The Journal of biological chemistry. 285(46):35386-92 [DOI] 10.1074/jbc.M110.129288. [PMID] 20817722.
2010
Hydrogen/deuterium exchange reveals distinct agonist/partial agonist receptor dynamics within vitamin D receptor/retinoid X receptor heterodimer.
Structure (London, England : 1993). 18(10):1332-41 [DOI] 10.1016/j.str.2010.07.007. [PMID] 20947021.
2010
Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ.
ACS chemical biology. 5(11):1029-34 [DOI] 10.1021/cb100223d. [PMID] 20735016.
2010
Ligand regulation of retinoic acid receptor-related orphan receptors: implications for development of novel therapeutics.
Current opinion in lipidology. 21(3):204-11 [DOI] 10.1097/MOL.0b013e328338ca18. [PMID] 20463469.
2010
Modulation of retinoic acid receptor-related orphan receptor alpha and gamma activity by 7-oxygenated sterol ligands.
The Journal of biological chemistry. 285(7):5013-25 [DOI] 10.1074/jbc.M109.080614. [PMID] 19965867.
2010
Regulation of adipogenesis by natural and synthetic REV-ERB ligands.
Endocrinology. 151(7):3015-25 [DOI] 10.1210/en.2009-0800. [PMID] 20427485.
2010
Regulation of FGF21 expression and secretion by retinoic acid receptor-related orphan receptor alpha.
The Journal of biological chemistry. 285(21):15668-73 [DOI] 10.1074/jbc.M110.102160. [PMID] 20332535.
2010
The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist.
Molecular pharmacology. 77(2):228-36 [DOI] 10.1124/mol.109.060905. [PMID] 19887649.
2009
Unique ligand binding patterns between estrogen receptor alpha and beta revealed by hydrogen-deuterium exchange.
Biochemistry. 48(40):9668-76 [DOI] 10.1021/bi901149t. [PMID] 19739677.
2008
Identification of adropin as a secreted factor linking dietary macronutrient intake with energy homeostasis and lipid metabolism.
Cell metabolism. 8(6):468-81 [DOI] 10.1016/j.cmet.2008.10.011. [PMID] 19041763.
2008
Implications of the binding of tamoxifen to the coactivator recognition site of the estrogen receptor.
Endocrine-related cancer. 15(4):851-70 [DOI] 10.1677/ERC-07-0281. [PMID] 18755852.
2008
Nuclear hormone receptors for heme: REV-ERBalpha and REV-ERBbeta are ligand-regulated components of the mammalian clock.
Molecular endocrinology (Baltimore, Md.). 22(7):1509-20 [DOI] 10.1210/me.2007-0519. [PMID] 18218725.
2008
Prediction of the tissue-specificity of selective estrogen receptor modulators by using a single biochemical method.
Proceedings of the National Academy of Sciences of the United States of America. 105(20):7171-6 [DOI] 10.1073/pnas.0710802105. [PMID] 18474858.
2008
Regulation of cholesterologenesis by the oxysterol receptor, LXRalpha.
The Journal of biological chemistry. 283(39):26332-9 [DOI] 10.1074/jbc.M804808200. [PMID] 18676367.
2008
Regulation of human 3 alpha-hydroxysteroid dehydrogenase (AKR1C4) expression by the liver X receptor alpha.
Molecular pharmacology. 73(2):607-12 [PMID] 18024509.
2008
Relationship between circadian oscillations of Rev-erbalpha expression and intracellular levels of its ligand, heme.
Biochemical and biophysical research communications. 368(4):955-8 [DOI] 10.1016/j.bbrc.2008.02.031. [PMID] 18280802.
2008
Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA.
Nature. 456(7220):350-6 [DOI] 10.1038/nature07413. [PMID] 19043829.
2008
The selective Alzheimer’s disease indicator-1 gene (Seladin-1/DHCR24) is a liver X receptor target gene.
Molecular pharmacology. 74(6):1716-21 [DOI] 10.1124/mol.108.048538. [PMID] 18815215.
2007
Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta.
Nature structural & molecular biology. 14(12):1207-13 [PMID] 18037887.
2007
Liver X receptor is a therapeutic target in collagen-induced arthritis.
Arthritis and rheumatism. 56(4):1365-7 [PMID] 17393442.
2007
Panning for SNuRMs: using cofactor profiling for the rational discovery of selective nuclear receptor modulators.
Drug discovery today. 12(19-20):860-9 [PMID] 17933688.
2006
A 15-ketosterol is a liver X receptor ligand that suppresses sterol-responsive element binding protein-2 activity.
Journal of lipid research. 47(5):1037-44 [PMID] 16415294.
2006
A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta.
Proceedings of the National Academy of Sciences of the United States of America. 103(26):9908-11 [PMID] 16782818.
2006
A selective estrogen receptor modulator for the treatment of hot flushes.
Journal of medicinal chemistry. 49(3):843-6 [PMID] 16451049.
2006
Identification and characterization of noncalcemic, tissue-selective, nonsecosteroidal vitamin D receptor modulators.
The Journal of clinical investigation. 116(4):892-904 [PMID] 16528410.
2005
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Distinct REV-ERBα Conformational State Predicted by GaMD Simulations Leads to the Structure-Based Discovery of Novel REV-ERBα Antagonist
. [DOI] 10.1101/2021.05.26.445894.

Grants

Dec 2021 – Sep 2022
Development of REV-ERB Antagonists to Accelerate Muscle Regeneration
Role: Principal Investigator
Funding: UNIV OF HLTH SCIENCES & PHARM ST LOUIS via *MALLINCKRODT PHARMACEUTICALS-Bankrupt
Sep 2021 ACTIVE
Pharmacological targeting of circadian clock components to treat glioblastoma
Role: Principal Investigator
Funding: SALK INSTITUTE via NATL INST OF HLTH NCI

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