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Bushweller, John

John Bushweller

Primary Appointment

Molecular Physiology and Biological Physics

Contact Information

Telephone: 434-243-6409
Email: jhb4v@virginia.edu
Website: http://www.bushwellerlab.org/

Research Interests

Drug Development Targeting Transcription Drivers in Cancer; Structure/Function Studies of Transcription Factor Drivers in Cancer; Structural Studies of Membrane Proteins

Research Description

Drug Development Targeting Transcription Drivers in Cancer Dysregulation of gene expression is a hallmark of all cancers. It is critical for self-renewal and chemo-resistance of cancer cells which contributes to the inability to completely eradicate cancer cells, thereby leading to relapse. The specific gene expression program that confers these properties derives from the aberrant activity of specific transcription factors which are drivers of disease. Clearly, the most direct and effective approach to alter this gene expression program is to directly target the activity of the transcription factors driving the disease. There are numerous examples of such transcription factor drivers in cancer such as fusion proteins of RUNX1 and CBF? in leukemia, fusion proteins of ERG in prostate cancer and Ewing?s sarcoma, ETV-1 in melanoma, other members of the Ets family of transcription factors in a variety of different cancers, etc. Transcription factors have traditionally been viewed as ?undruggable? due to the need to target more challenging protein-protein or protein nucleic acid interactions through which these proteins act. There are still relatively few examples of such agents for cancer treatment, with the MDM2-p53 inhibitors being one example of such an agent that has progressed to the clinic. We are exploring several unique approaches to target this important class of proteins for drug development. Illendula A, Pulikkan JA, Zong H, Grembecka J, Xue L, Sen S, Zhou Y, Boulton A, Kuntimaddi A, Gao Y, Rajewski RA, Guzman ML, Castilla LH, Bushweller JH. Chemical biology. A small-molecule inhibitor of the aberrant transcription factor CBF?-SMMHC delays leukemia in mice. Science. 2015 Feb 13;347(6223):779-84. PubMed PMID: 25678665; PubMed Central PMCID: PMC4423805. Illendula A, Gilmour J, Grembecka J, Tirumala VSS, Boulton A, Kuntimaddi A, Schmidt C, , Wang L, John A. Pulikkan, Hongliang Zong, Mahmut Parlak, Cem Kuscu, Anna Pickin, Yunpeng Zhou, Yan Gao Y, Mishra L, Adli M, Castilla LH, Rajewski RA, Janes KA, Guzman ML, Bonifer C, and Bushweller JH. Small Molecule Inhibitor of CBFB-RUNX Binding for RUNX Transcription Factor Driven Cancers. EBioMedicine. 2016 8: 117-131. Pubmed PMID: 27428424; PubMed Central PMCID: PMC4919611. Pulikkan JA, Hegde M, Belaghzal H, Illendula A, Yu J, Ahmed H, O?Hagan K, Ou J, Muller-Tidow C, Wolfe SA, Zhu LJ, Dekker J, Bushweller JH, Castilla LH. CBF?-SMMHC inhibition leads to alteration of chromatin dynamics at MYC distal enhancers and abrogation of inv(16) leukemia. Cell. 2018 174(1):172-186.e21. Pubmed PMID: 29958106. Structure/Function Studies of Transcription Factor Drivers in Cancer Our lab is fundamentally interested in understanding, from a structural and biophysical perspective, the functioning of proteins involved in regulating transcription, particularly those involved in the dysregulation associated with the development of cancer. Structural and functional characterization of the native forms of these proteins and their relevant complexes via NMR spectroscopy, X-ray crystallography, and a variety of other techniques provides a baseline of understanding. Subsequent characterization of the oncoprotein forms then provides a detailed understanding of the molecular mechanism of oncogenesis associated with altered forms of these proteins. Such knowledge leads to novel avenues for the design of therapeutic agents to treat the cancers associated with these particular oncoproteins. A long-term focus has been structural studies of a novel transcription factor referred to as the core-binding factor (CBF). This heterodimeric protein is essential for hematopoietic development. Gene translocations associated with the genes coding for the two subunits of CBF produce novel fusion proteins which have been implicated as playing a role in more than 30% of acute leukemias. We have carried out extensive structural and functional studies of the oncoprotein forms of the two subunits of CBF that are associated with leukemia. We have extended these studies to the MLL protein, a key epigenetic regulator that is the target of chromosomal translocations in leukemia which are particularly poor prognosis. Cierpicki T, Risner LE, Grembecka J, Lukasik SM, Popovic R, Omonkowska M, Shultis DD, Zeleznik-Le NJ, Bushweller JH. Structure of the MLL CXXC domain-DNA complex and its functional role in MLL-AF9 leukemia. Nat Struct Mol Biol. 2010 Jan;17(1):62-8. PubMed PMID: 20010842; PubMed Central PMCID: PMC2908503. Kuntimaddi A, Achille NJ, Thorpe J, Lokken AA, Singh R, Hemenway CS, Adli M, Zeleznik-Le NJ, Bushweller JH. Degree of recruitment of DOT1L to MLL-AF9 defines level of H3K79 Di- and tri-methylation on target genes and transformation potential. Cell Rep. 2015 May 5;11(5):808-20. PubMed PMID: 25921540; PubMed Central PMCID: PMC4426023. Structural Studies of Membrane Proteins. A third focus for the lab is the application of solution NMR methods to the structure determination of membrane proteins. The vast majority of drug targets are membrane-embedded proteins. This class of proteins has presented significant challenges for structure determination by any method. We determined the structure of the 4 TM enzyme DsbB by solution NMR which established a paradigm for tackling this class of proteins by NMR. We recently completed the structure determination and mechanistic studies of the 6 TM membrane transporter CcdA. Zhou Y, Cierpicki T, Jimenez RH, Lukasik SM, Ellena JF, Cafiso DS, Kadokura H, Beckwith J, Bushweller JH. NMR solution structure of the integral membrane enzyme DsbB: functional insights into DsbB-catalyzed disulfide bond formation. Mol Cell. 2008 Sep 26;31(6):896-908. PubMed PMID: 18922471; PubMed Central PMCID: PMC2622435. Zhou Y and Bushweller JH. Solution Structure and Elevator Mechanism of the Membrane Electron Transporter CcdA. Nat Struct Mol Biol. 2018 25(2):163-169. Pubmed PMID: 29379172. List of Publications in Pubmed

Selected Publications

Zhou N, Gutierrez-Uzquiza A, Zheng XY, Chang R, Vogl DT, Garfall AL, Bernabei L, Saraf A, Florens L, Washburn MP, Illendula A, Bushweller JH, Busino L, RUNX proteins desensitize multiple myeloma to lenalidomide via protecting IKZFs from degradation., 2019; Leukemia. () PMID: 30760870 |

Mill CP, Fiskus W, DiNardo CD, Qian Y, Raina K, Rajapakshe K, Perera D, Coarfa C, Kadia TM, Khoury JD, Saenz DT, Saenz DN, Illendula A, Takahashi K, Kornblau SM, Green MR, Futreal AP, Bushweller JH, Crews CM, Bhalla KN, RUNX1 targeted therapy for AML expressing somatic or germline mutation in RUNX1., 2019; Blood. () PMID: 31023702 |

Zhou Y, Bushweller JH, Solution structure and elevator mechanism of the membrane electron transporter CcdA., 2018; Nature structural & molecular biology. 25(2) 163-169 PMID: 29379172 | PMCID: PMC5805637

Carlton AL, Illendula A, Gao Y, Llaneza DC, Boulton A, Shah A, Rajewski RA, Landen CN, Wotton D, Bushweller JH, Small molecule inhibition of the CBF?/RUNX interaction decreases ovarian cancer growth and migration through alterations in genes related to epithelial-to-mesenchymal transition., 2018; Gynecologic oncology. 149(2) 350-360 PMID: 29551565 | PMCID: PMC5915923

Pulikkan JA, Hegde M, Ahmad HM, Belaghzal H, Illendula A, Yu J, O'Hagan K, Ou J, Muller-Tidow C, Wolfe SA, Zhu LJ, Dekker J, Bushweller JH, Castilla LH, CBF?-SMMHC Inhibition Triggers Apoptosis by Disrupting MYC Chromatin Dynamics in Acute Myeloid Leukemia., 2018; Cell. 174(1) 172-186.e21 PMID: 29958106 | PMCID: PMC6211564

Tahirov TH, Bushweller J, Structure and Biophysics of CBF?/RUNX and Its Translocation Products., 2017; Advances in experimental medicine and biology. 962() 21-31 PMID: 28299648 |

Oo ZM, Illendula A, Grembecka J, Schmidt C, Zhou Y, Esain V, Kwan W, Frost I, North TE, Rajewski RA, Speck NA, Bushweller JH, A tool compound targeting the core binding factor Runt domain to disrupt binding to CBF? in leukemic cells., 2017; Leukemia & lymphoma. 59(9) 2188-2200 PMID: 29249175 | PMCID: PMC6005736

Margulieux KR, Liebov BK, Tirumala VSK, Singh A, Bushweller JH, Nakamoto RK, Hughes MA, Bacillus anthracis Peptidoglycan Integrity Is Disrupted by the Chemokine CXCL10 through the FtsE/X Complex., 2017; Frontiers in microbiology. 8() 740 PMID: 28496437 | PMCID: PMC5406473

Choi A, Illendula A, Pulikkan JA, Roderick JE, Tesell J, Yu J, Hermance N, Zhu LJ, Castilla LH, Bushweller JH, Kelliher MA, RUNX1 is required for oncogenic Myb and Myc enhancer activity in T cell acute lymphoblastic leukemia., 2017; Blood. () PMID: 28790107 |

Castilla LH, Bushweller JH, Molecular Basis and Targeted Inhibition of CBF?-SMMHC Acute Myeloid Leukemia., 2017; Advances in experimental medicine and biology. 962() 229-244 PMID: 28299661 |

Illendula A, Gilmour J, Grembecka J, Tirumala VS, Boulton A, Kuntimaddi A, Schmidt C, Wang L, Pulikkan JA, Zong H, Parlak M, Kuscu C, Pickin A, Zhou Y, Gao Y, Mishra L, Adli M, Castilla LH, Rajewski RA, Janes KA, Guzman ML, Bonifer C, Bushweller JH, Small Molecule Inhibitor of CBF?-RUNX Binding for RUNX Transcription Factor Driven Cancers., 2016; EBioMedicine. 8() 117-31 PMID: 27428424 | PMCID: PMC4919611

Huang Y, Thoms JA, Tursky ML, Knezevic K, Beck D, Chandrakanthan V, Suryani S, Olivier J, Boulton A, Glaros EN, Thomas SR, Lock RB, MacKenzie KL, Bushweller JH, Wong JW, Pimanda JE, MAPK/ERK2 phosphorylates ERG at serine 283 in leukemic cells and promotes stem cell signatures and cell proliferation., 2016; Leukemia. 30(7) 1552-61 PMID: 27055868 |

Xiao S, Brannon MK, Zhao X, Fread KI, Ellena JF, Bushweller JH, Finkielstein CV, Armstrong GS, Capelluto DG, Tom1 Modulates Binding of Tollip to Phosphatidylinositol 3-Phosphate via a Coupled Folding and Binding Mechanism., 2015; Structure (London, England : 1993). 23(10) 1910-20 PMID: 26320582 |

Kuntimaddi A, Achille NJ, Thorpe J, Lokken AA, Singh R, Hemenway CS, Adli M, Zeleznik-Le NJ, Bushweller JH, Degree of recruitment of DOT1L to MLL-AF9 defines level of H3K79 Di- and tri-methylation on target genes and transformation potential., 2015; Cell reports. 11(5) 808-20 PMID: 25921540 | PMCID: PMC4426023

Illendula A, Pulikkan JA, Zong H, Grembecka J, Xue L, Sen S, Zhou Y, Boulton A, Kuntimaddi A, Gao Y, Rajewski RA, Guzman ML, Castilla LH, Bushweller JH, Chemical biology. A small-molecule inhibitor of the aberrant transcription factor CBF?-SMMHC delays leukemia in mice., 2015; Science (New York, N.Y.). 347(6223) 779-84 PMID: 25678665 | PMCID: PMC4423805

Lokken AA, Achille NJ, Chang MJ, Lin JJ, Kuntimaddi A, Leach BI, Malik B, Nesbit JB, Zhang S, Bushweller JH, Zeleznik-Le NJ, Hemenway CS, Importance of a specific amino acid pairing for murine MLL leukemias driven by MLLT1/3 or AFF1/4., 2014; Leukemia research. 38(11) 1309-15 PMID: 25282333 | PMCID: PMC4253547

Risner LE, Kuntimaddi A, Lokken AA, Achille NJ, Birch NW, Schoenfelt K, Bushweller JH, Zeleznik-Le NJ, Functional specificity of CpG DNA-binding CXXC domains in mixed lineage leukemia., 2013; The Journal of biological chemistry. 288(41) 29901-10 PMID: 23990460 | PMCID: PMC3795288

Regan MC, Horanyi PS, Pryor EE, Sarver JL, Cafiso DS, Bushweller JH, Structural and dynamic studies of the transcription factor ERG reveal DNA binding is allosterically autoinhibited., 2013; Proceedings of the National Academy of Sciences of the United States of America. 110(33) 13374-9 PMID: 23898196 | PMCID: PMC3746864

Leach BI, Kuntimaddi A, Schmidt CR, Cierpicki T, Johnson SA, Bushweller JH, Leukemia fusion target AF9 is an intrinsically disordered transcriptional regulator that recruits multiple partners via coupled folding and binding., 2012; Structure (London, England : 1993). 21(1) 176-83 PMID: 23260655 | PMCID: PMC3545106

Chen H, Ji F, Olman V, Mobley CK, Liu Y, Zhou Y, Bushweller JH, Prestegard JH, Xu Y, Optimal mutation sites for PRE data collection and membrane protein structure prediction., 2011; Structure (London, England : 1993). 19(4) 484-95 PMID: 21481772 | PMCID: PMC3099474

Corpora T, Roudaia L, Oo ZM, Chen W, Manuylova E, Cai X, Chen MJ, Cierpicki T, Speck NA, Bushweller JH, Structure of the AML1-ETO NHR3-PKA(RII?) complex and its contribution to AML1-ETO activity., 2010; Journal of molecular biology. 402(3) 560-77 PMID: 20708017 | PMCID: PMC2945414

Park S, Osmers U, Raman G, Schwantes RH, Diaz MO, Bushweller JH, The PHD3 domain of MLL acts as a CYP33-regulated switch between MLL-mediated activation and repression ., 2010; Biochemistry. 49(31) 6576-86 PMID: 20677832 | PMCID: PMC2916634

Kamikubo Y, Zhao L, Wunderlich M, Corpora T, Hyde RK, Paul TA, Kundu M, Garrett L, Compton S, Huang G, Wolff L, Ito Y, Bushweller J, Mulloy JC, Liu PP, Accelerated leukemogenesis by truncated CBF beta-SMMHC defective in high-affinity binding with RUNX1., 2010; Cancer cell. 17(5) 455-68 PMID: 20478528 | PMCID: PMC2874204

Fr?h V, Zhou Y, Chen D, Loch C, Ab E, Grinkova YN, Verheij H, Sligar SG, Bushweller JH, Siegal G, Application of fragment-based drug discovery to membrane proteins: identification of ligands of the integral membrane enzyme DsbB., 2010; Chemistry & biology. 17(8) 881-91 PMID: 20797617 | PMCID: PMC4104428

Cierpicki T, Risner LE, Grembecka J, Lukasik SM, Popovic R, Omonkowska M, Shultis DD, Zeleznik-Le NJ, Bushweller JH, Structure of the MLL CXXC domain-DNA complex and its functional role in MLL-AF9 leukemia., 2009; Nature structural & molecular biology. 17(1) 62-8 PMID: 20010842 | PMCID: PMC2908503

Cierpicki T, Bielnicki J, Zheng M, Gruszczyk J, Kasterka M, Petoukhov M, Zhang A, Fernandez EJ, Svergun DI, Derewenda U, Bushweller JH, Derewenda ZS, The solution structure and dynamics of the DH-PH module of PDZRhoGEF in isolation and in complex with nucleotide-free RhoA., 2009; Protein science : a publication of the Protein Society. 18(10) 2067-79 PMID: 19670212 | PMCID: PMC2786971

Park S, Speck NA, Bushweller JH, The role of CBFbeta in AML1-ETO's activity., 2009; Blood. 114(13) 2849-50 PMID: 19779050 |

Zheng M, Cierpicki T, Momotani K, Artamonov MV, Derewenda U, Bushweller JH, Somlyo AV, Derewenda ZS, On the mechanism of autoinhibition of the RhoA-specific nucleotide exchange factor PDZRhoGEF., 2009; BMC structural biology. 9() 36 PMID: 19460155 | PMCID: PMC2695464

Park S, Chen W, Cierpicki T, Tonelli M, Cai X, Speck NA, Bushweller JH, Structure of the AML1-ETO eTAFH domain-HEB peptide complex and its contribution to AML1-ETO activity., 2009; Blood. 113(15) 3558-67 PMID: 19204326 | PMCID: PMC2668852

Roudaia L, Cheney MD, Manuylova E, Chen W, Morrow M, Park S, Lee CT, Kaur P, Williams O, Bushweller JH, Speck NA, CBFbeta is critical for AML1-ETO and TEL-AML1 activity., 2009; Blood. 113(13) 3070-9 PMID: 19179469 | PMCID: PMC2662647

Zhou Y, Cierpicki T, Jimenez RH, Lukasik SM, Ellena JF, Cafiso DS, Kadokura H, Beckwith J, Bushweller JH, NMR solution structure of the integral membrane enzyme DsbB: functional insights into DsbB-catalyzed disulfide bond formation., 2008; Molecular cell. 31(6) 896-908 PMID: 18922471 | PMCID: PMC2622435

Erfurth FE, Popovic R, Grembecka J, Cierpicki T, Theisler C, Xia ZB, Stuart T, Diaz MO, Bushweller JH, Zeleznik-Le NJ, MLL protects CpG clusters from methylation within the Hoxa9 gene, maintaining transcript expression., 2008; Proceedings of the National Academy of Sciences of the United States of America. 105(21) 7517-22 PMID: 18483194 | PMCID: PMC2396713

Liu Y, Chen W, Gaudet J, Cheney MD, Roudaia L, Cierpicki T, Klet RC, Hartman K, Laue TM, Speck NA, Bushweller JH, Structural basis for recognition of SMRT/N-CoR by the MYND domain and its contribution to AML1/ETO's activity., 2007; Cancer cell. 11(6) 483-97 PMID: 17560331 | PMCID: PMC1978186

Matheny CJ, Speck ME, Cushing PR, Zhou Y, Corpora T, Regan M, Newman M, Roudaia L, Speck CL, Gu TL, Griffey SM, Bushweller JH, Speck NA, Disease mutations in RUNX1 and RUNX2 create nonfunctional, dominant-negative, or hypomorphic alleles., 2007; The EMBO journal. 26(4) 1163-75 PMID: 17290219 | PMCID: PMC1852839

Gorczynski MJ, Grembecka J, Zhou Y, Kong Y, Roudaia L, Douvas MG, Newman M, Bielnicka I, Baber G, Corpora T, Shi J, Sridharan M, Lilien R, Donald BR, Speck NA, Brown ML, Bushweller JH, Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta., 2007; Chemistry & biology. 14(10) 1186-97 PMID: 17961830 |

Li Z, Lukasik SM, Liu Y, Grembecka J, Bielnicka I, Bushweller JH, Speck NA, A mutation in the S-switch region of the Runt domain alters the dynamics of an allosteric network responsible for CBFbeta regulation., 2006; Journal of molecular biology. 364(5) 1073-83 PMID: 17059830 | PMCID: PMC1783549

Cierpicki T, Kim MH, Cooper DR, Derewenda U, Bushweller JH, Derewenda ZS, The DC-module of doublecortin: dynamics, domain boundaries, and functional implications., 2006; Proteins. 64(4) 874-82 PMID: 16835924 |

Cierpicki T, Liang B, Tamm LK, Bushweller JH, Increasing the accuracy of solution NMR structures of membrane proteins by application of residual dipolar couplings. High-resolution structure of outer membrane protein A., 2006; Journal of the American Chemical Society. 128(21) 6947-51 PMID: 16719475 | PMCID: PMC2527590

Liu Y, Cheney MD, Gaudet JJ, Chruszcz M, Lukasik SM, Sugiyama D, Lary J, Cole J, Dauter Z, Minor W, Speck NA, Bushweller JH, The tetramer structure of the Nervy homology two domain, NHR2, is critical for AML1/ETO's activity., 2006; Cancer cell. 9(4) 249-60 PMID: 16616331 |

Grembecka J, Cierpicki T, Devedjiev Y, Derewenda U, Kang BS, Bushweller JH, Derewenda ZS, The binding of the PDZ tandem of syntenin to target proteins., 2006; Biochemistry. 45(11) 3674-83 PMID: 16533050 |

Liang B, Bushweller JH, Tamm LK, Site-directed parallel spin-labeling and paramagnetic relaxation enhancement in structure determination of membrane proteins by solution NMR spectroscopy., 2006; Journal of the American Chemical Society. 128(13) 4389-97 PMID: 16569016 | PMCID: PMC3199951

Lukasik SM, Cierpicki T, Borloz M, Grembecka J, Everett A, Bushweller JH, High resolution structure of the HDGF PWWP domain: a potential DNA binding domain., 2005; Protein science : a publication of the Protein Society. 15(2) 314-23 PMID: 16384999 | PMCID: PMC2242466

Cierpicki T, Bushweller JH, Derewenda ZS, Probing the supramodular architecture of a multidomain protein: the structure of syntenin in solution., 2005; Structure (London, England : 1993). 13(2) 319-27 PMID: 15698575 |

Li Y, Han X, Lai AL, Bushweller JH, Cafiso DS, Tamm LK, Membrane structures of the hemifusion-inducing fusion peptide mutant G1S and the fusion-blocking mutant G1V of influenza virus hemagglutinin suggest a mechanism for pore opening in membrane fusion., 2005; Journal of virology. 79(18) 12065-76 PMID: 16140782 | PMCID: PMC1212637

Brautigan DL, Brown M, Grindrod S, Chinigo G, Kruszewski A, Lukasik SM, Bushweller JH, Horal M, Keller S, Tamura S, Heimark DB, Price J, Larner AN, Larner J, Allosteric activation of protein phosphatase 2C by D-chiro-inositol-galactosamine, a putative mediator mimetic of insulin action., 2005; Biochemistry. 44(33) 11067-73 PMID: 16101290 |

Cierpicki T, Bushweller JH, Charged gels as orienting media for measurement of residual dipolar couplings in soluble and integral membrane proteins., 2004; Journal of the American Chemical Society. 126(49) 16259-66 PMID: 15584763 |

Yan J, Liu Y, Lukasik SM, Speck NA, Bushweller JH, CBFbeta allosterically regulates the Runx1 Runt domain via a dynamic conformational equilibrium., 2004; Nature structural & molecular biology. 11(9) 901-6 PMID: 15322525 |

Gorczynski MJ, Leal RM, Mooberry SL, Bushweller JH, Brown ML, Synthesis and evaluation of substituted 4-aryloxy- and 4-arylsulfanyl-phenyl-2-aminothiazoles as inhibitors of human breast cancer cell proliferation., 2004; Bioorganic & medicinal chemistry. 12(5) 1029-36 PMID: 14980616 |

Everett AD, Bushweller J, Hepatoma derived growth factor is a nuclear targeted mitogen., 2003; Current drug targets. 4(5) 367-71 PMID: 12816346 |

Zhang L, Li Z, Yan J, Pradhan P, Corpora T, Cheney MD, Bravo J, Warren AJ, Bushweller JH, Speck NA, Mutagenesis of the Runt domain defines two energetic hot spots for heterodimerization with the core binding factor beta subunit., 2003; The Journal of biological chemistry. 278(35) 33097-104 PMID: 12807883 |

Li Z, Yan J, Matheny CJ, Corpora T, Bravo J, Warren AJ, Bushweller JH, Speck NA, Energetic contribution of residues in the Runx1 Runt domain to DNA binding., 2003; The Journal of biological chemistry. 278(35) 33088-96 PMID: 12807882 |

Zhang L, Lukasik SM, Speck NA, Bushweller JH, Structural and functional characterization of Runx1, CBF beta, and CBF beta-SMMHC., 2003; Blood cells, molecules & diseases. 30(2) 147-56 PMID: 12732176 |

Kim MH, Cierpicki T, Derewenda U, Krowarsch D, Feng Y, Devedjiev Y, Dauter Z, Walsh CA, Otlewski J, Bushweller JH, Derewenda ZS, The DCX-domain tandems of doublecortin and doublecortin-like kinase., 2003; Nature structural biology. 10(5) 324-33 PMID: 12692530 |

Cierpicki T, Kim MH, Otlewski J, Derewenda ZS, Bushweller JH, Assignment of 1H, 13C and 15N resonances of the N-terminal microtubule-binding domain of human doublecortin., 2003; Journal of biomolecular NMR. 25(1) 81-2 PMID: 12567003 |

Tamm LK, Abildgaard F, Arora A, Blad H, Bushweller JH, Structure, dynamics and function of the outer membrane protein A (OmpA) and influenza hemagglutinin fusion domain in detergent micelles by solution NMR., 2003; FEBS letters. 555(1) 139-43 PMID: 14630334 |

Lukasik SM, Zhang L, Corpora T, Tomanicek S, Li Y, Kundu M, Hartman K, Liu PP, Laue TM, Biltonen RL, Speck NA, Bushweller JH, Altered affinity of CBF beta-SMMHC for Runx1 explains its role in leukemogenesis., 2002; Nature structural biology. 9(9) 674-9 PMID: 12172539 |

Yan J, Corpora T, Pradhan P, Bushweller JH, MQ-hCN-based pulse sequences for the measurement of 13C1'-1H1', 13C1'-15N, 1H1'-15N, 13C1'-13C2', 1H1'-13C2',13C6/8-1H6/8, 13C6/8-15N, 1H6/8-15N, 13C6-13C5, 1H6-13C5 dipolar couplings in 13C, 15N-labeled DNA (and RNA)., 2002; Journal of biomolecular NMR. 22(1) 9-20 PMID: 11885985 |

Han X, Bushweller JH, Cafiso DS, Tamm LK, Membrane structure and fusion-triggering conformational change of the fusion domain from influenza hemagglutinin., 2001; Nature structural biology. 8(8) 715-20 PMID: 11473264 |

Yan J, Bushweller JH, An optimized PCR-based procedure for production of 13C/15N-labeled DNA., 2001; Biochemical and biophysical research communications. 284(2) 295-300 PMID: 11394876 |

Arora A, Abildgaard F, Bushweller JH, Tamm LK, Structure of outer membrane protein A transmembrane domain by NMR spectroscopy., 2001; Nature structural biology. 8(4) 334-8 PMID: 11276254 |

Bailey-Kellogg C, Widge A, Kelley JJ, Berardi MJ, Bushweller JH, Donald BR, The NOESY jigsaw: automated protein secondary structure and main-chain assignment from sparse, unassigned NMR data., 2000; Journal of computational biology : a journal of computational molecular cell biology. 7(3) 537-58 PMID: 11108478 |

Bushweller JH, CBF--a biophysical perspective., 2000; Seminars in cell & developmental biology. 11(5) 377-82 PMID: 11105902 |

Tang YY, Shi J, Zhang L, Davis A, Bravo J, Warren AJ, Speck NA, Bushweller JH, Energetic and functional contribution of residues in the core binding factor beta (CBFbeta ) subunit to heterodimerization with CBFalpha., 2000; The Journal of biological chemistry. 275(50) 39579-88 PMID: 10984496 |

Tang YY, Crute BE, Kelley JJ, Huang X, Yan J, Shi J, Hartman KL, Laue TM, Speck NA, Bushweller JH, Biophysical characterization of interactions between the core binding factor alpha and beta subunits and DNA., 2000; FEBS letters. 470(2) 167-72 PMID: 10734228 |

Huang X, Peng JW, Speck NA, Bushweller JH, Solution structure of core binding factor beta and map of the CBF alpha binding site., 1999; Nature structural biology. 6(7) 624-7 PMID: 10404216 |

Berardi MJ, Sun C, Zehr M, Abildgaard F, Peng J, Speck NA, Bushweller JH, The Ig fold of the core binding factor alpha Runt domain is a member of a family of structurally and functionally related Ig-fold DNA-binding domains., 1999; Structure (London, England : 1993). 7(10) 1247-56 PMID: 10545320 |

Song WJ, Sullivan MG, Legare RD, Hutchings S, Tan X, Kufrin D, Ratajczak J, Resende IC, Haworth C, Hock R, Loh M, Felix C, Roy DC, Busque L, Kurnit D, Willman C, Gewirtz AM, Speck NA, Bushweller JH, Li FP, Gardiner K, Poncz M, Maris JM, Gilliland DG, Haploinsufficiency of CBFA2 causes familial thrombocytopenia with propensity to develop acute myelogenous leukaemia., 1999; Nature genetics. 23(2) 166-75 PMID: 10508512 |

Berardi MJ, Bushweller JH, Binding specificity and mechanistic insight into glutaredoxin-catalyzed protein disulfide reduction., 1999; Journal of molecular biology. 292(1) 151-61 PMID: 10493864 |

Huang X, Speck NA, Bushweller JH, Complete heteronuclear NMR resonance assignments and secondary structure of core binding factor beta (1-141)., 1998; Journal of biomolecular NMR. 12(3) 459-60 PMID: 9835054 |

Chen X, Mariappan SV, Kelley JJ, Bushweller JH, Bradbury EM, Gupta G, A PCR-based method for uniform 13C/15N labeling of long DNA oligomers., 1998; FEBS letters. 436(3) 372-6 PMID: 9801151 |

Kelley JJ, Bushweller JH, 1H, 13C and 15N NMR resonance assignments of vaccinia glutaredoxin-1 in the fully reduced form., 1998; Journal of biomolecular NMR. 12(2) 353-5 PMID: 9752005 |

Sun C, Berardi MJ, Bushweller JH, The NMR solution structure of human glutaredoxin in the fully reduced form., 1998; Journal of molecular biology. 280(4) 687-701 PMID: 9677297 |

Berardi MJ, Pendred CL, Bushweller JH, Preparation, characterization, and complete heteronuclear NMR resonance assignments of the glutaredoxin (C14S)-ribonucleotide reductase B1 737-761 (C754S) mixed disulfide., 1998; Biochemistry. 37(17) 5849-57 PMID: 9558318 |

Huang X, Crute BE, Sun C, Tang YY, Kelley JJ, Lewis AF, Hartman KL, Laue TM, Speck NA, Bushweller JH, Overexpression, purification, and biophysical characterization of the heterodimerization domain of the core-binding factor beta subunit., 1998; The Journal of biological chemistry. 273(4) 2480-7 PMID: 9442100 |

Kelley JJ, Caputo TM, Eaton SF, Laue TM, Bushweller JH, Comparison of backbone dynamics of reduced and oxidized Escherichia coli glutaredoxin-1 using 15N NMR relaxation measurements., 1997; Biochemistry. 36(16) 5029-44 PMID: 9125525 |

Sun C, Holmgren A, Bushweller JH, Complete 1H, 13C, and 15N NMR resonance assignments and secondary structure of human glutaredoxin in the fully reduced form., 1997; Protein science : a publication of the Protein Society. 6(2) 383-90 PMID: 9041640 | PMCID: PMC2143634

Wang Q, Stacy T, Miller JD, Lewis AF, Gu TL, Huang X, Bushweller JH, Bories JC, Alt FW, Ryan G, Liu PP, Wynshaw-Boris A, Binder M, Mar?n-Padilla M, Sharpe AH, Speck NA, The CBFbeta subunit is essential for CBFalpha2 (AML1) function in vivo., 1996; Cell. 87(4) 697-708 PMID: 8929538 |

Crute BE, Lewis AF, Wu Z, Bushweller JH, Speck NA, Biochemical and biophysical properties of the core-binding factor alpha2 (AML1) DNA-binding domain., 1996; The Journal of biological chemistry. 271(42) 26251-60 PMID: 8824275 |

Gribble GW, Switzer FL, Bushweller JH, Jewett JG, Brown JH, Dion JL, Bushweller CH, Byrn MP, Strouse CE, Stereodynamics of 9,11-Diphenyl-10-azatetracyclo[6.3.0.0.(4,11)0.(5,9)]undecanes. Highly Restricted Nitrogen Inversion and Isolated Phenyl Rotation. X-ray Crystallographic, Dynamic NMR, and Molecular Mechanics Studies., 1996; The Journal of organic chemistry. 61(13) 4319-4327 PMID: 11667332 |

Bushweller JH, Billeter M, Holmgren A, W?thrich K, The nuclear magnetic resonance solution structure of the mixed disulfide between Escherichia coli glutaredoxin(C14S) and glutathione., 1994; Journal of molecular biology. 235(5) 1585-97 PMID: 8107093 |

Bushweller JH, Holmgren A, W?thrich K, Biosynthetic 15N and 13C isotope labelling of glutathione in the mixed disulfide with Escherichia coli glutaredoxin documented by sequence-specific NMR assignments., 1993; European journal of biochemistry. 218(2) 327-34 PMID: 8269921 |

Szyperski T, Wider G, Bushweller JH, W?thrich K, 3D 13C-15N-heteronuclear two-spin coherence spectroscopy for polypeptide backbone assignments in 13C-15N-double-labeled proteins., 1993; Journal of biomolecular NMR. 3(1) 127-32 PMID: 8448432 |

Xia TH, Bushweller JH, Sodano P, Billeter M, Bj?rnberg O, Holmgren A, W?thrich K, NMR structure of oxidized Escherichia coli glutaredoxin: comparison with reduced E. coli glutaredoxin and functionally related proteins., 1992; Protein science : a publication of the Protein Society. 1(3) 310-21 PMID: 1304339 | PMCID: PMC2142208

Bushweller JH, Aslund F, W?thrich K, Holmgren A, Structural and functional characterization of the mutant Escherichia coli glutaredoxin (C14----S) and its mixed disulfide with glutathione., 1992; Biochemistry. 31(38) 9288-93 PMID: 1390715 |

Sodano P, Xia TH, Bushweller JH, Bj?rnberg O, Holmgren A, Billeter M, W?thrich K, Sequence-specific 1H n.m.r. assignments and determination of the three-dimensional structure of reduced Escherichia coli glutaredoxin., 1991; Journal of molecular biology. 221(4) 1311-24 PMID: 1942053 |

Bushweller JH, Bartlett PA, Investigation of an octapeptide inhibitor of Escherichia coli ribonucleotide reductase by transferred nuclear Overhauser effect spectroscopy., 1991; Biochemistry. 30(33) 8144-51 PMID: 1868090 |