Thomas P Burris, Ph.D.
Director And Chair Of The Department Of Pharmacodynamics
Department:
RE-GENETICS INSTITUTE-GENERAL
Business Phone:
(352) 273-9893
Business Email:
burris.thomas@ufl.edu
Teaching Profile
Courses Taught
2022-2024
PHA6512L Experiential Research Training in Pharmacodynamics
2022
PHA6521C Research Techniques in Pharmacodynamics
2023-2024
PHA4911 Undergraduate Research in Pharmacodynamics
Research Profile
Open Researcher and Contributor ID (ORCID)
0000-0003-2922-4449
Publications
2024
A Synthetic ERR Agonist Alleviates Metabolic Syndrome.
The Journal of pharmacology and experimental therapeutics.
388(2):232-240
[DOI] 10.1124/jpet.123.001733.
[PMID] 37739806.
2024
From Functional Fatty Acids to Potent and Selective Natural-Product-Inspired Mimetics via Conformational Profiling
ACS Central Science.
10(2):477-486
[DOI] 10.1021/acscentsci.3c01155.
[PMID] 38435518.
2024
How to Make Glucocorticoids Safer.
The Journal of pharmacology and experimental therapeutics.
388(3):748-750
[DOI] 10.1124/jpet.123.001931.
[PMID] 38360801.
2023
Assigning pathogenicity for TAB2 variants using a novel scalable functional assay and expanding TAB2 disease spectrum.
Human molecular genetics.
32(6):959-970
[DOI] 10.1093/hmg/ddac252.
[PMID] 36229919.
2023
Development and pharmacological evaluation of a new chemical series of potent pan-ERR agonists, identification of SLU-PP-915.
European journal of medicinal chemistry.
258
[DOI] 10.1016/j.ejmech.2023.115582.
[PMID] 37421886.
2023
Development of LXR inverse agonists to treat MAFLD, NASH, and other metabolic diseases.
Frontiers in medicine.
10
[DOI] 10.3389/fmed.2023.1102469.
[PMID] 36817797.
2023
International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023.
Pharmacological reviews.
75(6):1233-1318
[DOI] 10.1124/pharmrev.121.000436.
[PMID] 37586884.
2023
REV-ERB activation as a novel pharmacological approach for treating inflammatory pain.
Frontiers in pharmacology.
14
[DOI] 10.3389/fphar.2023.1171931.
[PMID] 37153791.
2023
Rev-erbα agonists suppresses TGFβ1-induced fibroblast-to-myofibroblast transition and pro-fibrotic phenotype in human lung fibroblasts.
Biochemical and biophysical research communications.
669:120-127
[DOI] 10.1016/j.bbrc.2023.05.092.
[PMID] 37269594.
2023
Synthetic ERRα/β/γ Agonist Induces an ERRα-Dependent Acute Aerobic Exercise Response and Enhances Exercise Capacity
ACS Chemical Biology.
18(4):756-771
[DOI] 10.1021/acschembio.2c00720.
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
REV-ERB is essential in cardiac fibroblasts homeostasis.
Frontiers in pharmacology.
13
[DOI] 10.3389/fphar.2022.899628.
[PMID] 36386186.
2022
SR9009 improves heart function after pressure overload independent of cardiac REV-ERB.
Frontiers in cardiovascular medicine.
9
[DOI] 10.3389/fcvm.2022.952114.
[PMID] 35911512.
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
Coactivation of the human vitamin D receptor by the peroxisome proliferator-activated receptor gamma coactivator-1 alpha.
Molecular pharmacology.
68(2):511-7
[PMID] 15908514.
2005
Estrogen: a mitochondrial energizer that keeps on going.
Molecular pharmacology.
68(4):956-8
[PMID] 16051746.
2005
Ligand-dependent coactivation of the human bile acid receptor FXR by the peroxisome proliferator-activated receptor gamma coactivator-1alpha.
The Journal of pharmacology and experimental therapeutics.
312(1):170-8
[PMID] 15329387.
2005
Potent inhibitors of LXXLL-based protein-protein interactions.
Chembiochem : a European journal of chemical biology.
6(11):1991-8
[PMID] 16222726.
2005
Reconstitution of functional nuclear receptor proteins using high pressure refolding.
Molecular genetics and metabolism.
85(4):318-22
[PMID] 15946878.
2005
Regulation of carbohydrate metabolism by the farnesoid X receptor.
Endocrinology.
146(3):984-91
[PMID] 15564327.
2005
Regulation of pyruvate dehydrogenase kinase expression by the farnesoid X receptor.
Biochemical and biophysical research communications.
329(1):391-6
[PMID] 15721319.
2005
The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand.
Molecular pharmacology.
67(3):948-54
[PMID] 15602004.
2005
The pharmacology of LXR.
Mini reviews in medicinal chemistry.
5(8):729-40
[PMID] 16101409.
2004
Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.
Journal of medicinal chemistry.
47(1):196-209
[PMID] 14695833.
2004
Pharmacology of nuclear receptor-coregulator recognition.
Vitamins and hormones.
68:145-83
[PMID] 15193454.
2004
T0901317 is a dual LXR/FXR agonist.
Molecular genetics and metabolism.
83(1-2):184-7
[PMID] 15464433.
2004
The coactivator LXXLL nuclear receptor recognition motif.
The journal of peptide research : official journal of the American Peptide Society.
63(3):207-12
[PMID] 15049832.
2004
Thioether side chain cyclization for helical peptide formation: inhibitors of estrogen receptor-coactivator interactions.
The journal of peptide research : official journal of the American Peptide Society.
63(3):297-302
[PMID] 15049842.
2003
A natural product ligand of the oxysterol receptor, liver X receptor.
The Journal of pharmacology and experimental therapeutics.
307(1):291-6
[PMID] 12893846.
2003
Alternative splicing within the ligand binding domain of the human constitutive androstane receptor.
Molecular genetics and metabolism.
80(1-2):216-26
[PMID] 14567971.
2003
Benzoxazinones as PPARgamma agonists. part 1: SAR of three aromatic regions.
Bioorganic & medicinal chemistry letters.
13(14):2359-62
[PMID] 12824034.
2003
Helix-stabilized cyclic peptides as selective inhibitors of steroid receptor-coactivator interactions.
Proceedings of the National Academy of Sciences of the United States of America.
100(20):11273-8
[PMID] 13679575.
2003
Ligand and coactivator identity determines the requirement of the charge clamp for coactivation of the peroxisome proliferator-activated receptor gamma.
The Journal of biological chemistry.
278(10):8637-44
[PMID] 12502716.
2003
Molecular determinants of LXRalpha agonism.
Journal of molecular graphics & modelling.
22(2):173-81
[PMID] 12932788.
2003
Retinoid X receptor is a nonsilent major contributor to vitamin D receptor-mediated transcriptional activation.
Molecular endocrinology (Baltimore, Md.).
17(11):2320-8
[PMID] 12893883.
2003
Target specificity of selective estrogen receptor modulators within human endometrial cancer cells.
The Journal of steroid biochemistry and molecular biology.
86(1):27-34
[PMID] 12943742.
2002
Effects of selective estrogen receptor modulators (SERMs) on coactivator nuclear receptor (NR) box binding to estrogen receptors.
Molecular genetics and metabolism.
76(3):225-33
[PMID] 12126937.
2002
PGC-1 functions as a transcriptional coactivator for the retinoid X receptors.
The Journal of biological chemistry.
277(6):3913-7
[PMID] 11714715.
2002
Requirement of helix 1 and the AF-2 domain of the thyroid hormone receptor for coactivation by PGC-1.
The Journal of biological chemistry.
277(11):8898-905
[PMID] 11751919.
2002
Ser-884 adjacent to the LXXLL motif of coactivator TRBP defines selectivity for ERs and TRs.
Molecular endocrinology (Baltimore, Md.).
16(1):128-40
[PMID] 11773444.
2001
Ligands specify coactivator nuclear receptor (NR) box affinity for estrogen receptor subtypes.
Molecular endocrinology (Baltimore, Md.).
15(6):909-22
[PMID] 11376110.
2000
A dominant-negative peroxisome proliferator-activated receptor gamma (PPARgamma) mutant is a constitutive repressor and inhibits PPARgamma-mediated adipogenesis.
The Journal of biological chemistry.
275(8):5754-9
[PMID] 10681562.
2000
Correlation of farnesoid X receptor coactivator recruitment and cholesterol 7alpha-hydroxylase gene repression by bile acids.
Molecular genetics and metabolism.
71(4):609-15
[PMID] 11136553.
2000
HIV protease inhibitors block human preadipocyte differentiation, but not via the PPARgamma/RXR heterodimer.
The Journal of endocrinology.
164(2):R7-R10
[PMID] 10657860.
1999
8th Annual International Conference on Obesity and Non-Insulin Dependent Diabetes Mellitus: novel drug developments.
Expert opinion on investigational drugs.
8(7):1117-25
[PMID] 15992112.
1999
A novel method for analysis of nuclear receptor function at natural promoters: peroxisome proliferator-activated receptor gamma agonist actions on aP2 gene expression detected using branched DNA messenger RNA quantitation.
Molecular endocrinology (Baltimore, Md.).
13(3):410-7
[PMID] 10076998.
1999
PPARgamma activation induces the expression of the adipocyte fatty acid binding protein gene in human monocytes.
Biochemical and biophysical research communications.
261(2):456-8
[PMID] 10425206.
1998
DAX1 mutations map to putative structural domains in a deduced three-dimensional model.
American journal of human genetics.
62(4):855-64
[PMID] 9529340.
1997
Betidamino acid scan of the GnRH antagonist acyline.
Journal of medicinal chemistry.
40(23):3739-48
[PMID] 9371239.
1996
Ahch, the mouse homologue of DAX1: cloning, characterization and synteny with GyK, the glycerol kinase locus.
Gene.
178(1-2):31-4
[PMID] 8921887.
1996
Genomic sequence of the DAX1 gene: an orphan nuclear receptor responsible for X-linked adrenal hypoplasia congenita and hypogonadotropic hypogonadism.
The Journal of clinical endocrinology and metabolism.
81(7):2481-6
[PMID] 8675564.
1996
The gene responsible for adrenal hypoplasia congenita, DAX-1, encodes a nuclear hormone receptor that defines a new class within the superfamily.
Recent progress in hormone research.
51:241-59; discussion 259
[PMID] 8701082.
1995
A nuclear hormone receptor-associated protein that inhibits transactivation by the thyroid hormone and retinoic acid receptors.
Proceedings of the National Academy of Sciences of the United States of America.
92(21):9525-9
[PMID] 7568167.
1995
Expression of DAX-1, the gene responsible for X-linked adrenal hypoplasia congenita and hypogonadotropic hypogonadism, in the hypothalamic-pituitary-adrenal/gonadal axis.
Biochemical and molecular medicine.
56(1):8-13
[PMID] 8593542.
1995
Identification of a putative steroidogenic factor-1 response element in the DAX-1 promoter.
Biochemical and biophysical research communications.
214(2):576-81
[PMID] 7677767.
1995
The tau 4 activation domain of the thyroid hormone receptor is required for release of a putative corepressor(s) necessary for transcriptional silencing.
Molecular and cellular biology.
15(1):76-86
[PMID] 7799971.
1994
Comparison of the forms of the dopamine D2 receptor expressed in GH4C1 cells.
Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.).
205(3):226-35
[PMID] 8171043.
1994
The yeast SIN3 gene product negatively regulates the activity of the human progesterone receptor and positively regulates the activities of GAL4 and the HAP1 activator.
Molecular & general genetics : MGG.
245(6):724-33
[PMID] 7830720.
1993
Infusion of dopamine at low concentrations stimulates the release of prolactin from alpha-methyl-p-tyrosine-treated rats.
Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.).
203(1):60-3
[PMID] 8097329.
1993
Low concentrations of dopamine increase cytosolic calcium in lactotrophs.
Endocrinology.
133(1):63-8
[PMID] 8391429.
1992
The stimulatory and inhibitory effects of dopamine on prolactin secretion involve different G-proteins.
Endocrinology.
130(2):926-32
[PMID] 1733734.
1991
Endothelin-3 inhibits prolactin and stimulates LH, FSH and TSH secretion from pituitary cell culture.
Biochemical and biophysical research communications.
174(1):338-43
[PMID] 1899191.
1991
Inhibition of prolactin secretion by endothelin-3 is pertussis toxin-sensitive.
European journal of pharmacology.
198(2-3):223-5
[PMID] 1907563.
1991
Pharmacologic evidence that a D2 receptor subtype mediates dopaminergic stimulation of prolactin secretion from the anterior pituitary gland.
Neuroendocrinology.
54(2):175-83
[PMID] 1685014.
1991
The effects of endothelins on the secretion of prolactin, luteinizing hormone, and follicle-stimulating hormone are mediated by different guanine nucleotide-binding proteins.
Endocrinology.
129(5):2607-13
[PMID] 1935791.
Grants
Aug 2023
– Oct 2023
ASTEROID THERAPEUTICS
Role: Principal Investigator
Funding: ASTEROID THERAPEUTICS
Jun 2023
– Oct 2023
Pelagos Chemical Series Evaluation
Role: Principal Investigator
Funding: PELAGOS PHARMACEUTICALS
Feb 2023
ACTIVE
Exercise Mimetics for Dementia and Alzheimer's Disease
Role: Principal Investigator
Funding: NATL INST OF HLTH NIA
Feb 2023
ACTIVE
Targeting REV-ERB to treat Alzheimer's disease
Role: Principal Investigator
Funding: NATL INST OF HLTH NIA
Jul 2022
ACTIVE
Nuclear Receptor REV-ERB alpha Role in the Pathophysiology of Allergic Asthma
Role: Principal Investigator
Funding: UNIV OF KANSAS MEDICAL CTR
via NATL INST OF HLTH NHLBI
Jan 2022
– Aug 2023
REV-ERB Antagonists for Treatment of Muscle Injuries
Role: Principal Investigator
Funding: US ARMY MED RES ACQUISITION
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
Oct 2021
ACTIVE
Transcriptional regulation of cardiac pathological remodeling by REV-ERBa
Role: Principal Investigator
Funding: BAYLOR COLLEGE OF MEDICINE
via NATL INST OF HLTH NHLBI
Sep 2021
ACTIVE
Pharmacological targeting of circadian clock components to treat glioblastoma
Role: Principal Investigator
Funding: SALK INSTITUTE
via NATL INST OF HLTH NCI
Jul 2015
ACTIVE
UF component for SRI program
Role: Project Manager
Funding: UNIV OF CENTRAL FLORIDA SPACE INST
via FL LEGISLATURE
Contact Details
Phones:
- Business:
- (352) 273-9893
Emails:
- Business:
- burris.thomas@ufl.edu
Addresses:
- Business Mailing:
-
PO Box 103610
2033 MOWRY RD
GAINESVILLE FL 32610 - Business Street:
-
2033 MOWRY RD
GAINESVILLE FL 32611