Douglas John Kojetin, Ph.D.

Associate Professor

douglas.kojetin@vanderbilt.edu
Faculty Appointments
Associate Professor of Biochemistry
Education
Ph.D., Biochemistry, North Carolina State University, Raleigh, North CarolinaB.S., Chemistry, emphasis in Biochemistry, Purdue University, West Lafayette, Indiana
Research Description
Nuclear receptors comprise a superfamily of transcription factors that evolved to bind endogenous small molecule cellular metabolites including lipids, steroid hormones, and vitamins—translating endocrine and metabolic signals into changes in gene expression. Nuclear receptors regulate many important physiological cellular functions and nuclear receptor dysfunction is linked to many different diseases including cancer, diabetes, inflammation, neurodegeneration, and others — as such, nuclear receptors are targets for ~15% of current FDA approved drugs.

My laboratory uses an integrative experimental approach to understand the molecular basis of nuclear receptor (dys)function. The methods we use spans the fields of structural biology (protein NMR spectroscopy, x-ray crystallography, mass spectrometry-based structural proteomics, and computation), biochemistry (protein-protein, protein-ligand, protein-nucleic acid interactions), molecular and cellular pharmacology (transcription and gene expression), development of high-throughput screening (HTS) assays (to discover new compounds), and collaboration with medicinal chemists (design drug-like molecules with improved properties, and complement mutagenesis using a chemical approach to test structure-function relationships).

I have a primary appointment in the Biochemistry department in the Vanderbilt School of Medicine. I am a member of several Centers and Institutes at Vanderbilt including the Vanderbilt Center for Structural Biology, Vanderbilt Institute of Chemical Biology, Vanderbilt-Ingram Cancer Center, and Vanderbilt Brain Institute.
Research in my lab has been funded by several NIH institutes (NIDDK, NIGMS, NIA, NIAID, NCI) including fellowships to trainees (NIH F31, NIH F32, NIH K99/R00, and AHA). My lab uses the bioR¿iv preprint server to communicate our research. I am a bioR¿iv affiliate member who provides feedback, acts as a preprint advocate, and screens preprints.

A major ongoing focus of my lab, funded by two NIH/NIDDK R01 awards, has advanced understanding of the structural mechanisms of ligand-dependent regulation of PPAR¿, a lipid-sensing NR that is the target for antidiabetic FDA-approved drugs and more recently a putative target for bladder cancer. My lab has filled several knowledge gaps over the past 10 years including the structural mechanisms driving partial/graded activation of PPAR¿; allosteric or alternate ligand binding sites; the structural basis of PPAR¿ transcriptional repression; and structural analysis of the ligand-free/apo-PPAR¿ LBD conformational ensemble.

Another focus of my lab, funded by NIH/NIGMS NIH/NIA R01 awards, has advanced understanding on the ligandability of the orphan NR Nurr1. Although Nurr1 has been thought to function independent of binding ligands, studies by my lab and others indicate that Nurr1 activity can be regulated by ligand binding directly to the Nurr1 LBD. We are currently exploring how endogenous ligands regulate Nurr1 structure and function, and as well as the structural mechanism of synthetic ligands that specifically target Nurr1-RXR heterodimers, which are also implicated as potential therapeutics in aging-associated neurodegenerative disorders including Parkinson's disease and Alzheimer's disease.

Finally, an emerging focus of my lab has advanced understanding on the mechanisms of transcriptional repression by the REV-ERB NRs. We defined the structural basis for heme-dependent corepressor recruitment to REV-ERBß, unifying more than a decade of contradictory published biochemical and cellular evidence on the role of heme in regulating REV-ERB function. Our findings should facilitate renewed efforts toward understanding the molecular basis of ligand-regulated REV-ERB function in health and disease.
Research Keywords
biochemistry, structural biology, biophysics, protein NMR spectroscopy, nuclear magnetic resonance, x-ray crystallography, computation, nuclear receptors, transcription factors, intrinsically disordered proteins, ligand binding, FDA-approved drugs, high-throughput screening, HTS, diabetes, cancer, neurodegeneration, Parkinson’s disease, Alzheimer’s disease, drug discovery, drug design, molecular pharmacology, cellular pharmacology, chemical biology, molecular biology
Publications
Yu X, Shang J, Kojetin DJ. Molecular basis of ligand-dependent Nurr1-RXRa activation. Elife. 2023 Apr 4/27/2023; 12: PMID: 37102494, PMCID: PMC10259986, PII: 85039, DOI: 10.7554/eLife.85039, ISSN: 2050-084X.

Gamage DG, Melikov K, Munoz-Tello P, Wherley TJ, Focke LC, Leikina E, Huffman E, Diao J, Kojetin DJ, Prasad V, Chernomordik LV, Millay DP. Phosphatidylserine orchestrates Myomerger membrane insertions to drive myoblast fusion. Proc Natl Acad Sci U S A [print-electronic]. 2022 Sep 9/20/2022; 119(38): e2202490119. PMID: 36095199, PMCID: PMC9499509, DOI: 10.1073/pnas.2202490119, ISSN: 1091-6490.

Shang J, Kojetin DJ. Structural mechanism underlying ligand binding and activation of PPAR¿. Structure [print-electronic]. 2021 Sep 9/2/2021; 29(9): 940-950.e4-950.e4. PMID: 33713599, PMCID: PMC8418994, PII: S0969-2126(21)00050-2, DOI: 10.1016/j.str.2021.02.006, ISSN: 1878-4186.

Chen ML, Huang X, Wang H, Hegner C, Liu Y, Shang J, Eliason A, Diao H, Park H, Frey B, Wang G, Mosure SA, Solt LA, Kojetin DJ, Rodriguez-Palacios A, Schady DA, Weaver CT, Pipkin ME, Moore DD, Sundrud MS. CAR directs T cell adaptation to bile acids in the small intestine. Nature [print-electronic]. 2021 May; 593(7857): 147-51. PMID: 33828301, PMCID: PMC8862117, PII: 10.1038/s41586-021-03421-6, DOI: 10.1038/s41586-021-03421-6, ISSN: 1476-4687.

Bruno NE, Nwachukwu JC, Srinivasan S, Nettles CC, Izard T, Jin Z, Nowak J, Cameron MD, Boregowda SV, Phinney DG, Elemento O, Liu X, Ortlund EA, Houtman R, Stavreva DA, Hager GL, Kamenecka TM, Kojetin DJ, Nettles KW. Chemical systems biology reveals mechanisms of glucocorticoid receptor signaling. Nat Chem Biol [print-electronic]. 2021 Mar; 17(3): 307-16. PMID: 33510451, PMCID: PMC8783757, PII: 10.1038/s41589-020-00719-w, DOI: 10.1038/s41589-020-00719-w, ISSN: 1552-4469.

Mosure SA, Strutzenberg TS, Shang J, Munoz-Tello P, Solt LA, Griffin PR, Kojetin DJ. Structural basis for heme-dependent NCoR binding to the transcriptional repressor REV-ERBß. Sci Adv [electronic-print]. 2021 Jan; 7(5): PMID: 33571111, PMCID: PMC7840129, PII: 7/5/eabc6479, DOI: 10.1126/sciadv.abc6479, ISSN: 2375-2548.

Munoz-Tello P, Lin H, Khan P, de Vera IMS, Kamenecka TM, Kojetin DJ. Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. J Med Chem [print-electronic]. 2020 Dec 12/24/2020; 63(24): 15639-54. PMID: 33289551, PMCID: PMC8006468, DOI: 10.1021/acs.jmedchem.0c00894, ISSN: 1520-4804.

Shang J, Mosure SA, Zheng J, Brust R, Bass J, Nichols A, Solt LA, Griffin PR, Kojetin DJ. A molecular switch regulating transcriptional repression and activation of PPAR¿. Nat Commun. 2020 Feb 2/19/2020; 11(1): 956. PMID: 32075969, PMCID: PMC7031403, PII: 10.1038/s41467-020-14750-x, DOI: 10.1038/s41467-020-14750-x, ISSN: 2041-1723.

Galmozzi A, Kok BP, Kim AS, Montenegro-Burke JR, Lee JY, Spreafico R, Mosure S, Albert V, Cintron-Colon R, Godio C, Webb WR, Conti B, Solt LA, Kojetin D, Parker CG, Peluso JJ, Pru JK, Siuzdak G, Cravatt BF, Saez E. PGRMC2 is an intracellular haem chaperone critical for adipocyte function. Nature [print-electronic]. 2019 Dec; 576(7785): 138-42. PMID: 31748741, PMCID: PMC6895438, PII: 10.1038/s41586-019-1774-2, DOI: 10.1038/s41586-019-1774-2, ISSN: 1476-4687.

Shang J, Brust R, Griffin PR, Kamenecka TM, Kojetin DJ. Quantitative structural assessment of graded receptor agonism. Proc Natl Acad Sci U S A [print-electronic]. 2019 Oct 10/29/2019; 116(44): 22179-88. PMID: 31611383, PMCID: PMC6825269, PII: 1909016116, DOI: 10.1073/pnas.1909016116, ISSN: 1091-6490.

Mediouni S, Kessing CF, Jablonski JA, Thenin-Houssier S, Clementz M, Kovach MD, Mousseau G, de Vera IMS, Li C, Kojetin DJ, Evans DT, Valente ST. The Tat inhibitor didehydro-cortistatin A suppresses SIV replication and reactivation. FASEB J [print-electronic]. 2019 Jul; 33(7): 8280-93. PMID: 31021670, PMCID: PMC6593873, DOI: 10.1096/fj.201801165R, ISSN: 1530-6860.

Mosure SA, Shang J, Eberhardt J, Brust R, Zheng J, Griffin PR, Forli S, Kojetin DJ. Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPAR¿ Drug Pioglitazone. J Med Chem [print-electronic]. 2019 Feb 2/28/2019; 62(4): 2008-23. PMID: 30676741, PMCID: PMC6898968, DOI: 10.1021/acs.jmedchem.8b01573, ISSN: 1520-4804.

Mediouni S, Chinthalapudi K, Ekka MK, Usui I, Jablonski JA, Clementz MA, Mousseau G, Nowak J, Macherla VR, Beverage JN, Esquenazi E, Baran P, de Vera IMS, Kojetin D, Loret EP, Nettles K, Maiti S, Izard T, Valente ST. Didehydro-Cortistatin A Inhibits HIV-1 by Specifically Binding to the Unstructured Basic Region of Tat. MBio. 2019 Feb 2/5/2019; 10(1): PMID: 30723126, PMCID: PMC6368365, PII: mBio.02662-18, DOI: 10.1128/mBio.02662-18, ISSN: 2150-7511.

de Vera IMS, Munoz-Tello P, Zheng J, Dharmarajan V, Marciano DP, Matta-Camacho E, Giri PK, Shang J, Hughes TS, Rance M, Griffin PR, Kojetin DJ. Defining a Canonical Ligand-Binding Pocket in the Orphan Nuclear Receptor Nurr1. Structure [print-electronic]. 2019 Jan 1/2/2019; 27(1): 66-77.e5-77.e5. PMID: 30416039, PMCID: PMC6318021, PII: S0969-2126(18)30363-0, DOI: 10.1016/j.str.2018.10.002, ISSN: 1878-4186.

Amir M, Chaudhari S, Wang R, Campbell S, Mosure SA, Chopp LB, Lu Q, Shang J, Pelletier OB, He Y, Doebelin C, Cameron MD, Kojetin DJ, Kamenecka TM, Solt LA. REV-ERBa Regulates TH17 Cell Development and Autoimmunity. Cell Rep. 2018 Dec 12/26/2018; 25(13): 3733-3749.e8-3749.e8. PMID: 30590045, PMCID: PMC6400287, PII: S2211-1247(18)31907-7, DOI: 10.1016/j.celrep.2018.11.101, ISSN: 2211-1247.

Shang J, Brust R, Mosure SA, Bass J, Munoz-Tello P, Lin H, Hughes TS, Tang M, Ge Q, Kamenekca TM, Kojetin DJ. Cooperative cobinding of synthetic and natural ligands to the nuclear receptor PPAR¿. Elife. 2018 Dec 12/21/2018; 7: PMID: 30575522, PMCID: PMC6317912, PII: 43320, DOI: 10.7554/eLife.43320, ISSN: 2050-084X.

Patil DN, Rangarajan ES, Novick SJ, Pascal BD, Kojetin DJ, Griffin PR, Izard T, Martemyanov KA. Structural organization of a major neuronal G protein regulator, the RGS7-Gß5-R7BP complex. Elife. 2018 Dec 12/12/2018; 7: PMID: 30540250, PMCID: PMC6310461, PII: 42150, DOI: 10.7554/eLife.42150, ISSN: 2050-084X.

Brust R, Shang J, Fuhrmann J, Mosure SA, Bass J, Cano A, Heidari Z, Chrisman IM, Nemetchek MD, Blayo AL, Griffin PR, Kamenecka TM, Hughes TS, Kojetin DJ. A structural mechanism for directing corepressor-selective inverse agonism of PPAR¿. Nat Commun. 2018 Nov 11/8/2018; 9(1): 4687. PMID: 30409975, PMCID: PMC6224492, PII: 10.1038/s41467-018-07133-w, DOI: 10.1038/s41467-018-07133-w, ISSN: 2041-1723.

Zheng J, Corzo C, Chang MR, Shang J, Lam VQ, Brust R, Blayo AL, Bruning JB, Kamenecka TM, Kojetin DJ, Griffin PR. Chemical Crosslinking Mass Spectrometry Reveals the Conformational Landscape of the Activation Helix of PPAR¿; a Model for Ligand-Dependent Antagonism. Structure [print-electronic]. 2018 Nov 11/6/2018; 26(11): 1431-1439.e6-1439.e6. PMID: 30146169, PMCID: PMC6221991, PII: S0969-2126(18)30253-3, DOI: 10.1016/j.str.2018.07.007, ISSN: 1878-4186.

Chrisman IM, Nemetchek MD, de Vera IMS, Shang J, Heidari Z, Long Y, Reyes-Caballero H, Galindo-Murillo R, Cheatham TE, Blayo AL, Shin Y, Fuhrmann J, Griffin PR, Kamenecka TM, Kojetin DJ, Hughes TS. Defining a conformational ensemble that directs activation of PPAR¿. Nat Commun. 2018 May 5/4/2018; 9(1): 1794. PMID: 29728618, PMCID: PMC5935666, PII: 10.1038/s41467-018-04176-x, DOI: 10.1038/s41467-018-04176-x, ISSN: 2041-1723.

Hudson WH, Vera IMS, Nwachukwu JC, Weikum ER, Herbst AG, Yang Q, Bain DL, Nettles KW, Kojetin DJ, Ortlund EA. Cryptic glucocorticoid receptor-binding sites pervade genomic NF-¿B response elements. Nat Commun. 2018 Apr 4/6/2018; 9(1): 1337. PMID: 29626214, PMCID: PMC5889392, PII: 10.1038/s41467-018-03780-1, DOI: 10.1038/s41467-018-03780-1, ISSN: 2041-1723.

de Vera IMS, Zheng J, Novick S, Shang J, Hughes TS, Brust R, Munoz-Tello P, Gardner WJ, Marciano DP, Kong X, Griffin PR, Kojetin DJ. Synergistic Regulation of Coregulator/Nuclear Receptor Interaction by Ligand and DNA. Structure [print-electronic]. 2017 Oct 10/3/2017; 25(10): 1506-1518.e4-1518.e4. PMID: 28890360, PMCID: PMC5653230, PII: S0969-2126(17)30253-8, DOI: 10.1016/j.str.2017.07.019, ISSN: 1878-4186.

Weikum ER, de Vera IMS, Nwachukwu JC, Hudson WH, Nettles KW, Kojetin DJ, Ortlund EA. Tethering not required: the glucocorticoid receptor binds directly to activator protein-1 recognition motifs to repress inflammatory genes. Nucleic Acids Res. 2017 Aug 8/21/2017; 45(14): 8596-608. PMID: 28591827, PMCID: PMC5737878, PII: 3862074, DOI: 10.1093/nar/gkx509, ISSN: 1362-4962.

Brust R, Lin H, Fuhrmann J, Asteian A, Kamenecka TM, Kojetin DJ. Modification of the Orthosteric PPAR¿ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor. ACS Chem Biol [print-electronic]. 2017 Apr 4/21/2017; 12(4): 969-78. PMID: 28165718, PMCID: PMC5652320, DOI: 10.1021/acschembio.6b01015, ISSN: 1554-8937.

Nwachukwu JC, Srinivasan S, Bruno NE, Nowak J, Wright NJ, Minutolo F, Rangarajan ES, Izard T, Yao XQ, Grant BJ, Kojetin DJ, Elemento O, Katzenellenbogen JA, Nettles KW. Systems Structural Biology Analysis of Ligand Effects on ERa Predicts Cellular Response to Environmental Estrogens and Anti-hormone Therapies. Cell Chem Biol [print-electronic]. 2017 Jan 1/19/2017; 24(1): 35-45. PMID: 28042045, PII: S2451-9456(16)30437-8, DOI: 10.1016/j.chembiol.2016.11.014, ISSN: 2451-9448.

Hughes TS, Shang J, Brust R, de Vera IMS, Fuhrmann J, Ruiz C, Cameron MD, Kamenecka TM, Kojetin DJ. Probing the Complex Binding Modes of the PPAR¿ Partial Agonist 2-Chloro-N-(3-chloro-4-((5-chlorobenzo[d]thiazol-2-yl)thio)phenyl)-4-(trifluoromethyl)benzenesulfonamide (T2384) to Orthosteric and Allosteric Sites with NMR Spectroscopy. J Med Chem [print-electronic]. 2016 Nov 11/23/2016; 59(22): 10335-41. PMID: 27783520, PMCID: PMC5179221, DOI: 10.1021/acs.jmedchem.6b01340, ISSN: 1520-4804.

Hepowit NL, de Vera IM, Cao S, Fu X, Wu Y, Uthandi S, Chavarria NE, Englert M, Su D, S¿ll D, Kojetin DJ, Maupin-Furlow JA. Mechanistic insight into protein modification and sulfur mobilization activities of noncanonical E1 and associated ubiquitin-like proteins of Archaea. FEBS J. 2016 Oct; 283(19): 3567-86. PMID: 27459543, PMCID: PMC5053900, DOI: 10.1111/febs.13819, ISSN: 1742-4658.

Fuhrmann J, Subramanian V, Kojetin DJ, Thompson PR. Activity-Based Profiling Reveals a Regulatory Link between Oxidative Stress and Protein Arginine Phosphorylation. Cell Chem Biol [print-electronic]. 2016 Aug 8/18/2016; 23(8): 967-77. PMID: 27524296, PMCID: PMC5157131, PII: S2451-9456(16)30237-9, DOI: 10.1016/j.chembiol.2016.07.008, ISSN: 2451-9448.

de Vera IM, Giri PK, Munoz-Tello P, Brust R, Fuhrmann J, Matta-Camacho E, Shang J, Campbell S, Wilson HD, Granados J, Gardner WJ, Creamer TP, Solt LA, Kojetin DJ. Identification of a Binding Site for Unsaturated Fatty Acids in the Orphan Nuclear Receptor Nurr1. ACS Chem Biol [print-electronic]. 2016 Jul 7/15/2016; 11(7): 1795-9. PMID: 27128111, PMCID: PMC4946999, DOI: 10.1021/acschembio.6b00037, ISSN: 1554-8937.

Thenin-Houssier S, de Vera IM, Pedro-Rosa L, Brady A, Richard A, Konnick B, Opp S, Buffone C, Fuhrmann J, Kota S, Billack B, Pietka-Ottlik M, Tellinghuisen T, Choe H, Spicer T, Scampavia L, Diaz-Griffero F, Kojetin DJ, Valente ST. Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication. Antimicrob Agents Chemother [electronic-print]. 2016 Apr; 60(4): 2195-208. PMID: 26810656, PMCID: PMC4808204, PII: AAC.02574-15, DOI: 10.1128/AAC.02574-15, ISSN: 1098-6596.

Hudson WH, Kossmann BR, de Vera IM, Chuo SW, Weikum ER, Eick GN, Thornton JW, Ivanov IN, Kojetin DJ, Ortlund EA. Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space. Proc Natl Acad Sci U S A [print-electronic]. 2016 Jan 1/12/2016; 113(2): 326-31. PMID: 26715749, PMCID: PMC4720311, PII: 1518960113, DOI: 10.1073/pnas.1518960113, ISSN: 1091-6490.

Kojetin DJ, Matta-Camacho E, Hughes TS, Srinivasan S, Nwachukwu JC, Cavett V, Nowak J, Chalmers MJ, Marciano DP, Kamenecka TM, Shulman AI, Rance M, Griffin PR, Bruning JB, Nettles KW. Structural mechanism for signal transduction in RXR nuclear receptor heterodimers. Nat Commun. 2015 Aug 8/20/2015; 6: 8013. PMID: 26289479, PMCID: PMC4547401, PII: ncomms9013, DOI: 10.1038/ncomms9013, ISSN: 2041-1723.

Wang Y, Kojetin D, Burris TP. Anti-proliferative actions of a synthetic REV-ERBa/ß agonist in breast cancer cells. Biochem Pharmacol [print-electronic]. 2015 Aug 8/15/2015; 96(4): 315-22. PMID: 26074263, PMCID: PMC4526361, PII: S0006-2952(15)00326-3, DOI: 10.1016/j.bcp.2015.06.010, ISSN: 1873-2968.

Marciano DP, Kuruvilla DS, Boregowda SV, Asteian A, Hughes TS, Garcia-Ordonez R, Corzo CA, Khan TM, Novick SJ, Park H, Kojetin DJ, Phinney DG, Bruning JB, Kamenecka TM, Griffin PR. Pharmacological repression of PPAR¿ promotes osteogenesis. Nat Commun. 2015 Jun 6/12/2015; 6: 7443. PMID: 26068133, PMCID: PMC4471882, PII: ncomms8443, DOI: 10.1038/ncomms8443, ISSN: 2041-1723.

Hughes TS, Wilson HD, de Vera IM, Kojetin DJ. Deconvolution of Complex 1D NMR Spectra Using Objective Model Selection. PLoS One. 2015; 10(8): e0134474. PMID: 26241959, PMCID: PMC4524620, PII: PONE-D-15-07562, DOI: 10.1371/journal.pone.0134474, ISSN: 1932-6203.

Hudson WH, Pickard MR, de Vera IM, Kuiper EG, Mourtada-Maarabouni M, Conn GL, Kojetin DJ, Williams GT, Ortlund EA. Conserved sequence-specific lincRNA-steroid receptor interactions drive transcriptional repression and direct cell fate. Nat Commun. 2014 Nov 11/7/2014; 5: 5395. PMID: 25377354, PMCID: PMC4280027, PII: ncomms6395, DOI: 10.1038/ncomms6395, ISSN: 2041-1723.

Matta-Camacho E, Banerjee S, Hughes TS, Solt LA, Wang Y, Burris TP, Kojetin DJ. Structure of REV-ERBß ligand-binding domain bound to a porphyrin antagonist. J Biol Chem [print-electronic]. 2014 Jul 7/18/2014; 289(29): 20054-66. PMID: 24872411, PMCID: PMC4106322, PII: S0021-9258(20)47655-0, DOI: 10.1074/jbc.M113.545111, ISSN: 1083-351X.

Nwachukwu JC, Srinivasan S, Bruno NE, Parent AA, Hughes TS, Pollock JA, Gjyshi O, Cavett V, Nowak J, Garcia-Ordonez RD, Houtman R, Griffin PR, Kojetin DJ, Katzenellenbogen JA, Conkright MD, Nettles KW. Resveratrol modulates the inflammatory response via an estrogen receptor-signal integration network. Elife. 2014 Apr 4/25/2014; 3: e02057. PMID: 24771768, PMCID: PMC4017646, PII: eLife.02057, DOI: 10.7554/eLife.02057, ISSN: 2050-084X.

Hughes TS, Giri PK, de Vera IM, Marciano DP, Kuruvilla DS, Shin Y, Blayo AL, Kamenecka TM, Burris TP, Griffin PR, Kojetin DJ. An alternate binding site for PPAR¿ ligands. Nat Commun. 2014 Apr 4/7/2014; 5: 3571. PMID: 24705063, PMCID: PMC4070320, PII: ncomms4571, DOI: 10.1038/ncomms4571, ISSN: 2041-1723.

Kojetin DJ, Burris TP. REV-ERB and ROR nuclear receptors as drug targets. Nat Rev Drug Discov. 2014 Mar; 13(3): 197-216. PMID: 24577401, PMCID: PMC4865262, PII: nrd4100, DOI: 10.1038/nrd4100, ISSN: 1474-1784.

Srinivasan S, Nwachukwu JC, Parent AA, Cavett V, Nowak J, Hughes TS, Kojetin DJ, Katzenellenbogen JA, Nettles KW. Ligand-binding dynamics rewire cellular signaling via estrogen receptor-a. Nat Chem Biol [print-electronic]. 2013 May; 9(5): 326-32. PMID: 23524984, PMCID: PMC3631275, PII: nchembio.1214, DOI: 10.1038/nchembio.1214, ISSN: 1552-4469.

Burris TP, Solt LA, Wang Y, Crumbley C, Banerjee S, Griffett K, Lundasen T, Hughes T, Kojetin DJ. Nuclear receptors and their selective pharmacologic modulators. Pharmacol Rev [electronic-print]. 2013 Apr; 65(2): 710-78. PMID: 23457206, PII: 65/2/710, DOI: 10.1124/pr.112.006833, ISSN: 1521-0081.

Kojetin DJ, Burris TP. Small molecule modulation of nuclear receptor conformational dynamics: implications for function and drug discovery. Mol Pharmacol [print-electronic]. 2013 Jan; 83(1): 1-8. PMID: 22869589, PMCID: PMC3533479, PII: mol.112.079285, DOI: 10.1124/mol.112.079285, ISSN: 1521-0111.

Shin Y, Noel R, Banerjee S, Kojetin D, Song X, He Y, Lin L, Cameron MD, Burris TP, Kamenecka TM. Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erba. Bioorg Med Chem Lett [print-electronic]. 2012 Jul 7/1/2012; 22(13): 4413-7. PMID: 22633688, PMCID: PMC3376186, PII: S0960-894X(12)00585-9, DOI: 10.1016/j.bmcl.2012.04.126, ISSN: 1464-3405.

Noel R, Song X, Shin Y, Banerjee S, Kojetin D, Lin L, Ruiz CH, Cameron MD, Burris TP, Kamenecka TM. Synthesis and SAR of tetrahydroisoquinolines as Rev-erba agonists. Bioorg Med Chem Lett [print-electronic]. 2012 Jun 6/1/2012; 22(11): 3739-42. PMID: 22560469, PMCID: PMC3488456, PII: S0960-894X(12)00462-3, DOI: 10.1016/j.bmcl.2012.04.023, ISSN: 1464-3405.

Doerdelmann T, Kojetin DJ, Baird-Titus JM, Rance M. ¹H, ¹³C and ¹5N chemical shift assignments for the human Pitx2 homeodomain in complex with a 22-base hairpin DNA. Biomol NMR Assign [print-electronic]. 2012 Apr; 6(1): 79-81. PMID: 21818549, PMCID: PMC3264750, DOI: 10.1007/s12104-011-9329-y, ISSN: 1874-270X.

Solt LA, Wang Y, Banerjee S, Hughes T, Kojetin DJ, Lundasen T, Shin Y, Liu J, Cameron MD, Noel R, Yoo SH, Takahashi JS, Butler AA, Kamenecka TM, Burris TP. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 3/29/2012; 485(7396): 62-8. PMID: 22460951, PMCID: PMC3343186, PII: nature11030, DOI: 10.1038/nature11030, ISSN: 1476-4687.

Doerdelmann T, Kojetin DJ, Baird-Titus JM, Solt LA, Burris TP, Rance M. Structural and biophysical insights into the ligand-free Pitx2 homeodomain and a ring dermoid of the cornea inducing homeodomain mutant. Biochemistry [print-electronic]. 2012 Jan 1/17/2012; 51(2): 665-76. PMID: 22224469, PMCID: PMC3264736, DOI: 10.1021/bi201639x, ISSN: 1520-4995.

Hughes TS, Chalmers MJ, Novick S, Kuruvilla DS, Chang MR, Kamenecka TM, Rance M, Johnson BA, Burris TP, Griffin PR, Kojetin DJ. Ligand and receptor dynamics contribute to the mechanism of graded PPAR¿ agonism. Structure. 2012 Jan 1/11/2012; 20(1): 139-50. PMID: 22244763, PMCID: PMC3278220, PII: S0969-2126(11)00407-2, DOI: 10.1016/j.str.2011.10.018, ISSN: 1878-4186.

Wang Y, Solt LA, Kojetin DJ, Burris TP. Regulation of p53 stability and apoptosis by a ROR agonist. PLoS One [print-electronic]. 2012; 7(4): e34921. PMID: 22509368, PMCID: PMC3324542, PII: PONE-D-11-05070, DOI: 10.1371/journal.pone.0034921, ISSN: 1932-6203.

Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Wang Y, Busby SA, Pascal BD, Garcia-Ordonez RD, Bruning JB, Istrate MA, Kojetin DJ, Dodge JA, Burris TP, Griffin PR. DNA binding alters coactivator interaction surfaces of the intact VDR-RXR complex. Nat Struct Mol Biol [print-electronic]. 2011 May; 18(5): 556-63. PMID: 21478866, PMCID: PMC3087838, PII: nsmb.2046, DOI: 10.1038/nsmb.2046, ISSN: 1545-9985.

Solt LA, Kojetin DJ, Burris TP. The REV-ERBs and RORs: molecular links between circadian rhythms and lipid homeostasis. Future Med Chem. 2011 Apr; 3(5): 623-38. PMID: 21526899, PMCID: PMC3134326, DOI: 10.4155/fmc.11.9, ISSN: 1756-8927.

Doerdelmann T, Kojetin DJ, Baird-Titus JM, Rance M. 1H, 13C and 15N chemical shift assignments for the human Pitx2 homeodomain and a R24H homeodomain mutant. Biomol NMR Assign [print-electronic]. 2011 Apr; 5(1): 105-7. PMID: 21052876, PMCID: PMC3111450, DOI: 10.1007/s12104-010-9278-x, ISSN: 1874-270X.

Kumar N, Kojetin DJ, Solt LA, Kumar KG, Nuhant P, Duckett DR, Cameron MD, Butler AA, Roush WR, Griffin PR, Burris TP. Identification of SR3335 (ML-176): a synthetic RORa selective inverse agonist. ACS Chem Biol [print-electronic]. 2011 Mar 3/18/2011; 6(3): 218-22. PMID: 21090593, PMCID: PMC3076127, DOI: 10.1021/cb1002762, ISSN: 1554-8937.

Kojetin D, Wang Y, Kamenecka TM, Burris TP. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB [letter]. ACS Chem Biol [print-electronic]. 2011 Feb 2/18/2011; 6(2): 131-4. PMID: 21043485, PMCID: PMC3042041, DOI: 10.1021/cb1002575, ISSN: 1554-8937.

Kojetin DJ, Burris TP. A role for rev-erba ligands in regulation of adipogenesis. Curr Pharm Des. 2011; 17(4): 320-4. PMID: 21375499, PII: BSP/CPD/E-Pub/000343, DOI: 10.2174/138161211795164211, ISSN: 1873-4286.

Refaei MA, Combs A, Kojetin DJ, Cavanagh J, Caperelli C, Rance M, Sapitro J, Tsang P. Observing selected domains in multi-domain proteins via sortase-mediated ligation and NMR spectroscopy. J Biomol NMR [print-electronic]. 2011 Jan; 49(1): 3-7. PMID: 21188472, PMCID: PMC3111449, DOI: 10.1007/s10858-010-9464-2, ISSN: 1573-5001.

Crumbley C, Wang Y, Kojetin DJ, Burris TP. Characterization of the core mammalian clock component, NPAS2, as a REV-ERBalpha/RORalpha target gene. J Biol Chem [print-electronic]. 2010 Nov 11/12/2010; 285(46): 35386-92. PMID: 20817722, PMCID: PMC2975162, PII: S0021-9258(20)46878-4, DOI: 10.1074/jbc.M110.129288, ISSN: 1083-351X.

Kojetin DJ, McLaughlin PD, Thompson RJ, Dubnau D, Prepiak P, Rance M, Cavanagh J. Structural and motional contributions of the Bacillus subtilis ClpC N-domain to adaptor protein interactions. J Mol Biol [print-electronic]. 2009 Apr 4/3/2009; 387(3): 639-52. PMID: 19361434, PMCID: PMC2692191, PII: S0022-2836(09)00096-5, DOI: 10.1016/j.jmb.2009.01.046, ISSN: 1089-8638.

Kojetin DJ, Burris TP, Jensen EV, Khan SA. Implications of the binding of tamoxifen to the coactivator recognition site of the estrogen receptor. Endocr Relat Cancer [print-electronic]. 2008 Dec; 15(4): 851-70. PMID: 18755852, PII: ERC-07-0281, DOI: 10.1677/ERC-07-0281, ISSN: 1351-0088.

Sullivan DM, Bobay BG, Kojetin DJ, Thompson RJ, Rance M, Strauch MA, Cavanagh J. Insights into the nature of DNA binding of AbrB-like transcription factors. Structure. 2008 Nov 11/12/2008; 16(11): 1702-13. PMID: 19000822, PMCID: PMC2606041, PII: S0969-2126(08)00370-5, DOI: 10.1016/j.str.2008.08.014, ISSN: 0969-2126.

Kojetin DJ, McLaughlin PD, Thompson RJ, Venters RA, Rance M, Cavanagh J. NMR assignment of the N-terminal repeat domain of Bacillus subtilis ClpC. Biomol NMR Assign [print-electronic]. 2007 Dec; 1(2): 163-5. PMID: 19636855, DOI: 10.1007/s12104-007-9046-8, ISSN: 1874-270X.

Kojetin DJ, Sullivan DM, Thompson RJ, Cavanagh J. Classification of response regulators based on their surface properties. Methods Enzymol. 2007; 422: 141-69. PMID: 17628138, PII: S0076-6879(06)22007-X, DOI: 10.1016/S0076-6879(06)22007-X, ISSN: 0076-6879.

Kojetin DJ, Venters RA, Kordys DR, Thompson RJ, Kumar R, Cavanagh J. Structure, binding interface and hydrophobic transitions of Ca2+-loaded calbindin-D(28K). Nat Struct Mol Biol [print-electronic]. 2006 Jul; 13(7): 641-7. PMID: 16799559, PII: nsmb1112, DOI: 10.1038/nsmb1112, ISSN: 1545-9993.

Kojetin DJ, Thompson RJ, Benson LM, Naylor S, Waterman J, Davies KG, Opperman CH, Stephenson K, Hoch JA, Cavanagh J. Structural analysis of divalent metals binding to the Bacillus subtilis response regulator Spo0F: the possibility for in vitro metalloregulation in the initiation of sporulation. Biometals. 2005 Oct; 18(5): 449-66. PMID: 16333746, DOI: 10.1007/s10534-005-4303-8, ISSN: 0966-0844.

Venters RA, Coggins BE, Kojetin D, Cavanagh J, Zhou P. (4,2)D Projection--reconstruction experiments for protein backbone assignment: application to human carbonic anhydrase II and calbindin D(28K). J Am Chem Soc. 2005 Jun 6/22/2005; 127(24): 8785-95. PMID: 15954785, DOI: 10.1021/ja0509580, ISSN: 0002-7863.

Ulrich DL, Kojetin D, Bassler BL, Cavanagh J, Loria JP. Solution structure and dynamics of LuxU from Vibrio harveyi, a phosphotransferase protein involved in bacterial quorum sensing. J Mol Biol. 2005 Mar 3/25/2005; 347(2): 297-307. PMID: 15740742, PII: S0022-2836(05)00072-0, DOI: 10.1016/j.jmb.2005.01.039, ISSN: 0022-2836.

Kojetin DJ, Thompson RJ, Cavanagh J. Sub-classification of response regulators using the surface characteristics of their receiver domains. FEBS Lett. 2003 Nov 11/20/2003; 554(3): 231-6. PMID: 14623071, PII: S0014579303011670, DOI: 10.1016/s0014-5793(03)01167-0, ISSN: 0014-5793.

Lutz W, Frank EM, Craig TA, Thompson R, Venters RA, Kojetin D, Cavanagh J, Kumar R. Calbindin D28K interacts with Ran-binding protein M: identification of interacting domains by NMR spectroscopy. Biochem Biophys Res Commun. 2003 Apr 4/18/2003; 303(4): 1186-92. PMID: 12684061, PII: S0006291X03004996, DOI: 10.1016/s0006-291x(03)00499-6, ISSN: 0006-291X.

Helton TD, Kojetin DJ, Cavanagh J, Horne WA. Alternative splicing of a beta4 subunit proline-rich motif regulates voltage-dependent gating and toxin block of Cav2.1 Ca2+ channels. J Neurosci. 2002 Nov 11/1/2002; 22(21): 9331-9. PMID: 12417658, PMCID: PMC6758066, PII: 22/21/9331, DOI: 10.1523/JNEUROSCI.22-21-09331.2002, ISSN: 1529-2401.

Phillips CL, Arend LJ, Filson AJ, Kojetin DJ, Clendenon JL, Fang S, Dunn KW. Three-dimensional imaging of embryonic mouse kidney by two-photon microscopy. Am J Pathol. 2001 Jan; 158(1): 49-55. PMID: 11141478, PMCID: PMC1850252, PII: S0002-9440(10)63943-0, DOI: 10.1016/S0002-9440(10)63943-0, ISSN: 0002-9440.