Publications
2021
The in-vitro effect of famotidine on sars-cov-2 proteases and virus replication.
Loffredo, M., Lucero, H., Chen, DY., O’Connell, A.O., Bergqvist, S., Munawar, A., Bandara, A., De Graef, S., Weeks, S.D., Douam, F., Saeed, M., & Munawar, A.H.
Scientific Reports | (2021) 11:5433
2019
PD-L1 checkpoint blockade delivered by retroviral replicating vector confers anti-tumor efficacy in murine tumor models.
Mitchell, L.A., Yagiz, K., Hofacre, A., Viaud, S., Munday, A.W., Lopez, F., Espinoza, Mendoza, D., Rodriguez-Aguirre, M.E., Bergqvist, S., Haghighi, A., Miner, M.V., Accomando, W.P., Burrascano, C., Gammon, D., Gruber, H.E., Jolly, D.J. and Lin, A.H.
Oncotarget. 2019 Mar 19; 10(23): 2252–2269.
Exclusivity and Compensation in NFκB Dimer distributions and IκB inhibition.
Ramsey, K.M., Chen, W., Marion, J.D., Bergqvist, S., and Komives, E.A.
Biochemistry. 2019 May 28; 58(21): 2555–2563.
2016
Spectrum and Degree of CDK Drug Interactions Predicts Clinical Performance.
Chen, P., Lee, N.V., Hu, W., Xu, M., Ferre, P.A., Lam, H., Bergqvist, S., Solowiej, J., Diehl, W., He, Y.A., Yu, X., Nagata, A., VanArsdale, T., Murray, B.W.
Mol. Cancer Ther. 2016. Oct; 15 (10):2273-2281.
Design and Synthesis of Pyridone Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Kung, P.; Rui, E., Bergqvist, S., Bingham, P., Braganza, J., Collins, M., Cui, M., Diehl, W., Dinh, D., Fan, C., Fantin, V., Gukasyan, H., Hu, W.; Huang, B., Kephart, S., Krivacic, C., Kumpf, R., Li, G., Maegley, K., McAlpine, I., Nguyen, L., Ninkovic, S., Ornelas, M., Ryskin, M., Scales, S., Sutton, S., Tatlock, J., Verhelle, D., Wang, F., Wells, P., Wythes, M., Yamazaki, S., Yip, B., Yu, X., Zehnder, L., Zhang, W., Rollins, R., Edwards, M.
J. Med. Chem. 2016 Sep 22; 59 (18) 8306-25.
Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.
Shaw, A.T., Friboulet, L., Leshchiner, I., Gainor, J.F., Bergqvist, S., Brooun, A., Burke, B.J., Deng, Y.L., Liu, W., Dardaei, L., Frias, R.L., Schultz, K.R., Logan, J., James, L.P., Smeal, T., Timofeevski, S., Katayama, R., Iafrate, A.J., Le, L., McTigue, M., Getz, G., Johnson, T.W., Engelman, J.A.
N Engl J Med. 2016 Jan 7;374(1):54-61.
2014
Engineering of an isolated p110α subunit of PI3Kα permits crystallization and provides a platform for structure-based drug design.
Chen, P., Deng, Y.L., Bergqvist, S., Falk, M., Liu, W., Timofeevski, S., Brooun, A.
Protein Sci. 2014 23 (10), 1332-40.
Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance.
Schwartz, P.A., Kuzmic, P., Solowiej, J., Bergqvist, S., Bolonos, B., Almaden, C., Nagata, A., Ryan, K., Feng, J., Dalvie, D., Kath, J.C., Xu, M., Wani, R.; Murray, B.W.
PNAS USA. 2014 Jan 7;111(1):173-8.
2012
Identification of Cys255 in HIF-1α as a novel site for the development of covalent inhibitors of HIF-1α/ARNT PasB domain protein-protein interaction.
Cardoso, R., Love, R., Nilsson,C.L, Bergqvist, S., Nowlin, D., Yan, J., Liu, K.C., Zhu, J., Chen, P., Deng, Y., Dyson, J., Greig, M.J. and Brooun, A.
Protein Sci. 2012. 21 (12), 1885-96.
ABRF-MIRG Benchmark Study: Molecular Interactions in a Three-Component System.
Yanmiuk, S.P., Edavettal, S.C., Bergqvist, S., Yadav, S.P., Doyle, M.L., Calabrese, K., Parsons, J.F., and Eisenstein, E.
J. Biomol. Tech. 2012. 23(3) 101-114.
Snapshot of Rapidly Evolving Label-Free Technologies Used for Characterizing Molecular Interactions.
Yadav, S.P., Bergqvist, S., Doyle, M.L., Neubert, T.A., and Yamniuk, A.P. MIRG Survey 2011.
J. Biomol. Tech. 2012. 23(3) 94-100.
Anti-human Activin Receptor-like Kinase 1 (ALK1) Antibody Attenuates Bone Morphogenetic Protein 9 (BMP9)-induced ALK1 Signaling and Interferes with Endothelial Cell Sprouting.
Van Meeteren, L.A., Thorikay, M., Bergqvist, S.; Pardali, E., Stampino, G., Hu-Lowe, D., Goumans, M.J., and Ten Dijke, P.
J. Biol. Chem. 2012. May 25, 287(22):18551-61.
Osteopontin induces growth of metastatic tumours in a preclinical model of non-small lung cancer.
Shojaei, F., Scott, N., kang, X., Lappin, P.B., Fitzgerald, A.A., Karlicek, S.K., Simmons, B.H., Wu, A., Lee, J.H., Bergqvist, S., and Kraynov, E.
J. Exp. Clin. Cancer Res. 2012. Mar 23;31:26.
A Model Based Approach to Predicting the Human Pharmacokinetics of a monoclonal antibody exhibiting target mediated drug deposition.
Luu, K.T., Bergqvist, S., Chen, E, Hu-Lowe, D., and Kraynov, E.
J. Pharmacol. Exp. Ther. 2012. 341(3):702-8.
Targeting of 4-1BB by monoclonal antibody PF-05082566 enhances T-cell function and promotes anti-tumour activity.
Fisher, T.S, Kamperschroer, C., Oliphant, T., Love, V., Lira, P.D., Doyonnas, R., Bergqvist,S., Baxi,S., Rohner,A., Shen, A., Huang,C., Sokolowski, S.A., and Sharp, L.L.
Cancer Immunol Immunother. 2012. 61 (10), 1721-33.
2011
Strategies to Target Crystallographic Waters Applied to the HSP90 Molecular Chaperone.
Kung, P., Sinnema, P., Richardson, P., Hickey, M., Gajiwala, K., Wang, F., Huang, B., McClellan, G., Wang, J., Maegley, K., Bergqvist, S., Pramod, M., Kania, R. Design
Bio. Org. Med. Chem. Lett. 2011. 3557-3562.
Targeting Activin Receptor-Like Kinase 1 Inhibits Angiogenesis and Tumor Growth Through Mechanism of Action Complementary to Anti-VEGF Therapies.
Hu-Lowe, D., Chen, E., Zhang, L.,Watson, K. Mancuso, P.,Lappin, P., Wickman, G., Chen, G.,Wang, J., Jiang, X., Amundson, K., Simon, R., Erbersdobler, A., Bergqvist, S., Feng, Z., Swanson, T., Simmons, B. Lippincott, J., Casperson, G., Levin, W., Stampino, C. G., Shalinsky, D., Ferrara, K., Fiedler, W., and Bertolini, F.
Cancer Research. 2011. 15;71(4):1362-73.
The RelA nuclear localization signal of folds upon binding to IκBα.
Cervantes, C., Bergqvist, S., Kjaergaard, M., Kroon, G., Sue, S., Dyson, H.J., and Komives, E.A.
Mol. Biol. 2011. 21;405(3):754-64.
2010
Dual functional monoclonal antibody PF-04605412 targets integrin α5β1 and elicits potent antibody-dependent cellular cytotoxicity.
Li, G., Zhang, L., Chen, E., Wang, J., Jiang, X., Chen, J., Wickman, G., Amundson, K., Bergqvist, S., Zobel, J., Buckman, D., Baxi, S., Bender, S., Casperson, G., and Hu-Lowe, D.
Cancer Research. 2010. Dec 15;70(24):10243-54.
Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth.
Murray, B.W., Guo, C., Piraino, J., Westwick, J.K., Zhang, C.,Lamerdin, J., Dagostino, E., Knighton, D., Loi, C., Zager, M., Kraynov, E., Popoff, I., Christensen, J.G., Martinez, R., Kephart, S.E., Marakovits, J., Karlicek, S.K., Bergqvist, S., Smeal, T.
PNAS. 2010. 107 (20), 9441-51.
2009
Structure of HIV-1 reverse transcriptase with the inhibitor beta-Thujaplicinol bound at the RNase H active site.
Himmel, D.M., Maegley, K.A., Pauly, T.A., Bauman, J.D., Das, K., Dharia, C., Clark, A.D., Ryan, K., Hickey, M.J., Love, R.A., Hughes, S.H., Bergqvist, S., Arnold, E.
Structure. 2009. 17(12):1625-35.
Kinetic enhancement of NF-κB.DNA dissociation by IκBα.
Bergqvist, S., Alverdi, V., Mengel, B., Hoffmann, A., Ghosh, G., and Elizabeth A. Komives.
Proc. Natl. Acad. Sci. 2009. 106(46), 19328-33.
Characterization of the CHK1 Allosteric Inhibitor Binding Site.
Vanderpool, D., Johnson, T.O., Ping, C., Bergqvist, S., Alton, G., Phonephaly, S., Rui, E., Luo, C., Deng, Y.L., Grant, S., Quenzer, T., Margosiak, S., Register, J., Brown, E., and Ermolieff, J.
Biochemistry. 2009. 48, 9823-9830.
Structural and Biophysical Characterization of XIAP BIR3 G306E Mutant: Insights in Protein Dynamics and Application for Fragment-Based Drug Design.
Moore, C.D., Wu, H., Bolanos, B., Bergqvist, S., Brooun, A., Pauly, T., and Nowlin, D.
Chem. Biol. Drug. Des. 2009. 74, 212-223.
Characterizing the Effects of the Juxtamembrane Domain on the Vascular Endothelial Growth Factor Receptor-2 Enzymatic Activity, Autophosphorylation, and Inhibition by Axitinib.
Bergqvist, S., Solowiej, S., McTigue, M, Marrone, T., Quenzer, T., Cobbs, M., Ryan, K., Kania,R., Diehl, W., and Murray, B.W.
Biochemistry. 2009. 48,7019-7031.
2008
The IκBα/NF-κB complex has two hot spots, one at either end of the interface.
Bergqvist, S., Ghosh, G., and Komives, E.A.
Protein Sci. 2008. 17(12), 2051-2058.
2007
Inhibitor kappaB kinase beta binding by inhibitor kappaB kinase gamma.
Drew, D., Shimada, E., Huyn, K., Bergqvist, S., Talwar, R., Karin, M. and Ghosh, G.
Biochemistry. 2007. 46, 12482-12490.
2006
Thermodynamics reveal that helix four in the NLS of NF-κB p65 anchors IκBα, forming a very stable complex.
Bergqvist, S., Croy, C.H., Kjaergaard, M., Huxford, T., Ghosh, G., and Komives, E.A.
Mol. Biol. 2006. 360, 421-434.
2004
Biophysical Characterization of the free IκBα ankyrin repeat domain in solution.
Bergqvist, S., Croy, C.H., Huxford, T., Ghosh, G. and Komives, E. A.
Protein Science. 2004. 13, 1767-1777.
Allosteric changes in solvent accessibility observed in thrombin upon active site occupation.
Croy, C H., Koeppe, J.R., Bergqvist, S. and Komives, E.A.
Biochemistry. 2004. 43, 5246-5255.
Two different proteins that compete for folding to thrombin have opposite kinetic and thermodynamic profiles.
Baerga-Ortiz, A., Bergqvist, S., Mandell, J. G., and Komives, E. A.
Protein Sci. 2004. 13, 166-176.
Heat capacity effects of water molecules and ions at a protein-DNA interface.
Bergqvist, S., Williams, M. A., O’Brien, R. and Ladbury, J. E.
J. Mol. Biol. 2004. 336, 829-842.
2003
Halophilic adaptation of protein-DNA interactions.
Bergqvist S., Williams M. A, O’Brien R and Ladbury J. E.
Biochem. Soc. Trans. 2003. 31, 31, 677-680.
2002
Reversal of Protein Halophilicity by Limited Mutation Strategy.
Bergqvist, S., Williams, M. A., O’Brien, R. and Ladbury, J. E.
Structure. 2002. 10, 629-637.
2001
Site-Specific Cation Binding Mediates TATA Binding Protein-DNA Interaction from a Hyperthermophilic Archaeon.
Bergqvist, S., O’Brien, R. and Ladbury, J. E.
Biochemistry. 2001. 40, 2419-2425.
1999
R5-(1-propargylamino)-2’-deoxyuridine (Up): a novel thymidine analogue for generating DNA triplexes with increased stability.
Bijipur, J., Keppler, M. D., Bergqvist, S. Brown, T. and Fox, K.
Nucleic Acids Research. 1999. 27, 8, 1802-1809.
1998
The Contribution of Cytosine Protonation to the Stability of Parallel DNA Triple Helices.
Asensio J.L., Lane A.N., Dhesi J., Bergqvist, S. and Brown, T.
Mol. Biol. 1998. 275, 811-822.
