1976 …2019

Research output per year

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Research Output

2019

Erratum to: A human monoclonal antibody prevents malaria infection by targeting a new site of vulnerability on the parasite (Nature Medicine, (2018), 24, 4, (408-416), 10.1038/nm.4512)

Kisalu, N. K., Idris, A. H., Weidle, C., Flores-Garcia, Y., Flynn, B. J., Sack, B. K., Murphy, S., Schön, A., Freire, E. I., Francica, J. R., Miller, A. B., Gregory, J., March, S., Liao, H. X., Haynes, B. F., Wiehe, K., Trama, A. M., Saunders, K. O., Gladden, M. A., Monroe, A. & 18 others, Bonsignori, M., Kanekiyo, M., Wheatley, A. K., McDermott, A. B., Farney, S. K., Chuang, G. Y., Zhang, B., Kc, N., Chakravarty, S., Kwong, P. D., Sinnis, P., Bhatia, S. N., Kappe, S. H. I., Sim, B. K. L., Hoffman, S. L., Zavala, F. P., Pancera, M. & Seder, R. A., Jan 1 2019, In : Nature Medicine. 25, 1, p. 188-189 2 p.

Research output: Contribution to journalComment/debate

2018

A human monoclonal antibody prevents malaria infection by targeting a new site of vulnerability on the parasite

Kisalu, N. K., Idris, A. H., Weidle, C., Flores-Garcia, Y., Flynn, B. J., Sack, B. K., Murphy, S., Schön, A., Freire, E. I., Francica, J. R., Miller, A. B., Gregory, J., March, S., Liao, H. X., Haynes, B. F., Wiehe, K., Trama, A. M., Saunders, K. O., Gladden, M. A., Monroe, A. & 18 others, Bonsignori, M., Kanekiyo, M., Wheatley, A. K., McDermott, A. B., Farney, S. K., Chuang, G. Y., Zhang, B., Kc, N., Chakravarty, S., Kwong, P. D., Sinnis, P., Bhatia, S. N., Kappe, S. H. I., Sim, B. K. L., Hoffman, S. L., Zavala, F. P., Pancera, M. & Seder, R. A., May 1 2018, In : Nature Medicine. 24, 4, p. 408-416 9 p.

Research output: Contribution to journalArticle

Bioinspired supramolecular engineering of self-assembling immunofibers for high affinity binding of immunoglobulin G

Li, Y., Lock, L. L., Wang, Y., Ou, S. H., Stern, D., Schön, A., Freire, E. I., Xu, X., Ghose, S., Li, Z. J. & Cui, H., Jan 1 2018, (Accepted/In press) In : Biomaterials.

Research output: Contribution to journalArticle

Erratum: Publisher Correction: The β20-β21 of gp120 is a regulatory switch for HIV-1 Env conformational transitions (Nature communications (2017) 8 1 (1049))

Herschhorn, A., Gu, C., Moraca, F., Ma, X., Farrell, M., Smith, A. B., Pancera, M., Kwong, P. D., Schön, A., Freire, E. I., Abrams, C., Blanchard, S. C., Mothes, W. & Sodroski, J. G., Jan 8 2018, In : Nature Communications. 9, 1, 1 p.

Research output: Contribution to journalComment/debate

Isothermal calorimetry of a monoclonal antibody using a conventional differential scanning calorimeter

Clarkson, B. R. & Freire, E. I., Oct 1 2018, In : Analytical Biochemistry. 558, p. 50-52 3 p.

Research output: Contribution to journalArticle

Long term stability of a HIV-1 neutralizing monoclonal antibody using isothermal calorimetry

Clarkson, B. R., Chaudhuri, R., Schön, A., Cooper, J. W., Kueltzo, L. & Freire, E. I., Aug 1 2018, In : Analytical Biochemistry. 554, p. 61-69 9 p.

Research output: Contribution to journalArticle

SOSIP changes affect human immunodeficiency virus type 1 envelope glycoprotein conformation and CD4 engagement

Alsahafi, N., Anand, S. P., Castillo-Menendez, L., Verly, M. M., Medjahed, H., Prévost, J., Herschhorn, A., Richard, J., Schön, A., Melillo, B., Freire, E., Smith, A. B., Sodroski, J. & Finzia, A., Oct 1 2018, In : Journal of virology. 92, 19, e01080.

Research output: Contribution to journalArticle

2017

A novel lipoate attachment enzyme is shared by Plasmodium and Chlamydia species

Afanador, G. A., Guerra, A. J., Swift, R. P., Rodriguez, R. E., Bartee, D., Matthews, K. A., Schön, A., Freire, E. I., Meyers, C. L. & Prigge, S. T., Nov 1 2017, In : Molecular Microbiology. 106, 3, p. 439-451 13 p.

Research output: Contribution to journalArticle

Crystal structures of trimeric HIV envelope with entry inhibitors BMS-378806 and BMS-626529

Pancera, M., Lai, Y. T., Bylund, T., Druz, A., Narpala, S., O'Dell, S., Schön, A., Bailer, R. T., Chuang, G. Y., Geng, H., Louder, M. K., Rawi, R., Soumana, D. I., Finzi, A., Herschhorn, A., Madani, N., Sodroski, J., Freire, E. I., Langley, D. R., Mascola, J. R. & 2 others, McDermott, A. B. & Kwong, P. D., Oct 1 2017, In : Nature Chemical Biology. 13, 10, p. 1115-1122 8 p.

Research output: Contribution to journalArticle

Temperature stability of proteins: Analysis of irreversible denaturation using isothermal calorimetry

Schön, A., Clarkson, B. R., Jaime, M. & Freire, E. I., Nov 1 2017, In : Proteins: Structure, Function and Bioinformatics. 85, 11, p. 2009-2016 8 p.

Research output: Contribution to journalArticle

The β20-β21 of gp120 is a regulatory switch for HIV-1 Env conformational transitions

Herschhorn, A., Gu, C., Moraca, F., Ma, X., Farrell, M., Smith, A. B., Pancera, M., Kwong, P. D., Schön, A., Freire, E. I., Abrams, C., Blanchard, S. C., Mothes, W. & Sodroski, J. G., Dec 1 2017, In : Nature Communications. 8, 1, 1049.

Research output: Contribution to journalArticle

2016

Conformational stability and self-association equilibrium in biologics

Clarkson, B. R., Schön, A. & Freire, E., Jan 1 2016, In : Drug Discovery Today. 21, 2, p. 342-347 6 p.

Research output: Contribution to journalReview article

Enthalpy screen of drug candidates

Schön, A. & Freire, E., Nov 15 2016, In : Analytical biochemistry. 513, p. 1-6 6 p.

Research output: Contribution to journalArticle

Small-Molecule CD4-Mimics: Structure-Based Optimization of HIV-1 Entry Inhibition

Melillo, B., Liang, S., Park, J., Schön, A., Courter, J. R., Lalonde, J. M., Wendler, D. J., Princiotto, A. M., Seaman, M. S., Freire, E., Sodroski, J., Madani, N., Hendrickson, W. A. & Smith, A. B., Mar 10 2016, In : ACS Medicinal Chemistry Letters. 7, 3, p. 330-334 5 p.

Research output: Contribution to journalArticle

Three easy pieces

Schön, A. & Freire, E., May 1 2016, In : Biochimica et Biophysica Acta - General Subjects. 1860, 5, p. 975-980 6 p.

Research output: Contribution to journalArticle

2015

CD4 mimetics sensitize HIV-1-infected cells to ADCC

Richard, J., Veillette, M., Brassard, N., Iyer, S. S., Roger, M., Martin, L., Pazgier, M., Schön, A., Freire, E., Routy, J. P., Smith, A. B., Park, J., Jones, D. M., Courter, J. R., Melillo, B. N., Kaufmann, D. E., Hahn, B. H., Permar, S. R., Haynes, B. F., Madani, N. & 2 others, Sodroski, J. G. & Finzi, A., May 19 2015, In : Proceedings of the National Academy of Sciences of the United States of America. 112, 20, p. E2687-E2694

Research output: Contribution to journalArticle

Characterization of protein-protein interactions by isothermal titration calorimetry

Velazquez-Campoy, A., Leavitt, S. A. & Freire, E., Jan 1 2015, In : Methods in Molecular Biology. 1278, p. 183-204 22 p.

Research output: Contribution to journalArticle

Characterization of protein-protein interactions by isothermal titration calorimetry

Velazquez-Campoy, A., Leavitt, S. A. & Freire, E., Apr 9 2015, Protein-Protein Interactions: Methods and Applications: Second Edition. Springer New York, p. 183-204 22 p.

Research output: Chapter in Book/Report/Conference proceedingChapter

Crystal structure, conformational fixation and entry-related interactions of mature ligand-free HIV-1 Env

Do Kwon, Y., Pancera, M., Acharya, P., Georgiev, I. S., Crooks, E. T., Gorman, J., Joyce, M. G., Guttman, M., Ma, X., Narpala, S., Soto, C., Terry, D. S., Yang, Y., Zhou, T., Ahlsen, G., Bailer, R. T., Chambers, M., Chuang, G. Y., Doria-Rose, N. A., Druz, A. & 33 others, Hallen, M. A., Harned, A., Kirys, T., Louder, M. K., O'Dell, S., Ofek, G., Osawa, K., Prabhakaran, M., Sastry, M., Stewart-Jones, G. B. E., Stuckey, J., Thomas, P. V., Tittley, T., Williams, C., Zhang, B., Zhao, H., Zhou, Z., Donald, B. R., Lee, L. K., Zolla-Pazner, S., Baxa, U., Schön, A., Freire, E., Shapiro, L., Lee, K. K., Arthos, J., Munro, J. B., Blanchard, S. C., Mothes, W., Binley, J. M., McDermott, A. B., Mascola, J. R. & Kwong, P. D., Jul 9 2015, In : Nature Structural and Molecular Biology. 22, 7, p. 522-531 10 p.

Research output: Contribution to journalArticle

Denatured state aggregation parameters derived from concentration dependence of protein stability

Schön, A., Clarkson, B. R., Siles, R., Ross, P., Brown, R. K. & Freire, E., Nov 1 2015, In : Analytical biochemistry. 488, p. 45-50 6 p., 12149.

Research output: Contribution to journalArticle

Impact of Surface Polyethylene Glycol (PEG) Density on Biodegradable Nanoparticle Transport in Mucus ex Vivo and Distribution in Vivo

Xu, Q., Ensign, L. M., Boylan, N. J., Schön, A., Gong, X., Yang, J. C., Lamb, N. W., Cai, S., Yu, T., Freire, E. & Hanes, J., Sep 22 2015, In : ACS Nano. 9, 9, p. 9217-9227 11 p.

Research output: Contribution to journalArticle

Isothermal chemical denaturation to determine binding affinity of small molecules to G-protein coupled receptors

Ross, P., Weihofen, W., Siu, F., Xie, A., Katakia, H., Wright, S. K., Hunt, I., Brown, R. K. & Freire, E., Mar 15 2015, In : Analytical biochemistry. 473, p. 41-45 5 p.

Research output: Contribution to journalArticle

Single-chain soluble BG505.SOSIP gp140 trimers as structural and antigenic mimics of mature closed HIV-1 Env

Georgiev, I. S., Gordon Joyce, M., Yang, Y., Sastry, M., Zhang, B., Baxa, U., Chen, R. E., Druz, A., Lees, C. R., Narpala, S., Schön, A., Van Galen, J., Chuang, G. Y., Gorman, J., Harned, A., Pancera, M., Stewart-Jones, G. B. E., Cheng, C., Freire, E., McDermott, A. B. & 2 others, Mascola, J. R. & Kwong, P. D., Jan 1 2015, In : Journal of virology. 89, 10, p. 5318-5329 12 p.

Research output: Contribution to journalArticle

Synthetic, structural mimetics of the β-hairpin flap of HIV-1 protease inhibit enzyme function

Chauhan, J., Chen, S. E., Fenstermacher, K. J., Naser-Tavakolian, A., Reingewertz, T., Salmo, R., Lee, C., Williams, E., Raje, M., Sundberg, E., Destefano, J. J., Freire, E. & Fletcher, S., Nov 1 2015, In : Bioorganic and Medicinal Chemistry. 23, 21, p. 7095-7109 15 p.

Research output: Contribution to journalArticle

The Binding Thermodynamics of Drug Candidates

Freire, E. I., Jun 2 2015, Thermodynamics and Kinetics of Drug Binding. Wiley Blackwell, p. 1-13 13 p.

Research output: Chapter in Book/Report/Conference proceedingChapter

2014

CD4-mimetic small molecules sensitize human immunodeficiency virus to vaccine-elicited antibodies

Madani, N., Princiotto, A. M., Schön, A., LaLonde, J., Feng, Y., Freire, E., Park, J., Courter, J. R., Jones, D. M., Robinson, J., Liao, H. X., Moody, A. A., Permar, S., Haynes, B., Smith, A. B., Wyatt, R. & Sodroski, J., Jun 2014, In : Journal of virology. 88, 12, p. 6542-6555 14 p.

Research output: Contribution to journalArticle

HIV-1 Vif N-terminal Motif is required for recruitment of Cul5 to Suppress APOBEC3

Evans, S. L., Schön, A., Gao, Q., Han, X., Zhou, X., Freire, E. & Yu, X. F., Jan 14 2014, In : Retrovirology. 11, 1, 4.

Research output: Contribution to journalArticle

Optimization of plasmepsin inhibitor by focusing on similar structural feature with chloroquine to avoid drug-resistant mechanism of Plasmodium falciparum

Miura, T., Hidaka, K., Azai, Y., Kashimoto, K., Kawasaki, Y., Chen, S. E., De Freitas, R. F., Freire, E. & Kiso, Y., Apr 1 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 7, p. 1698-1701 4 p.

Research output: Contribution to journalArticle

Structure-based design, synthesis and validation of CD4-mimetic small molecule inhibitors of HIV-1 entry: Conversion of a viral entry agonist to an antagonist

Courter, J. R., Madani, N., Sodroski, J., Schön, A., Freire, E., Kwong, P. D., Hendrickson, W. A., Chaiken, I. M., Lalonde, J. M. & Smith, A. B., Apr 15 2014, In : Accounts of chemical research. 47, 4, p. 1228-1237 10 p.

Research output: Contribution to journalArticle

2013

Chemical denaturation as a tool in the formulation optimization of biologics

Freire, E., Schön, A., Hutchins, B. M. & Brown, R. K., Oct 1 2013, In : Drug Discovery Today. 18, 19-20, p. 1007-1013 7 p.

Research output: Contribution to journalReview article

Design, synthesis, and biological evaluation of novel dipeptide-type SARS-CoV 3CL protease inhibitors: Structure-activity relationship study

Thanigaimalai, P., Konno, S., Yamamoto, T., Koiwai, Y., Taguchi, A., Takayama, K., Yakushiji, F., Akaji, K., Kiso, Y., Kawasaki, Y., Chen, S. E., Naser-Tavakolian, A., Schön, A., Freire, E. & Hayashi, Y., Jan 1 2013, In : European Journal of Medicinal Chemistry. 65, p. 436-447 12 p.

Research output: Contribution to journalArticle

Design and synthesis of new tripeptide-type SARS-CoV 3CL protease inhibitors containing an electrophilic arylketone moiety

Konno, S., Thanigaimalai, P., Yamamoto, T., Nakada, K., Kakiuchi, R., Takayama, K., Yamazaki, Y., Yakushiji, F., Akaji, K., Kiso, Y., Kawasaki, Y., Chen, S. E., Freire, E. & Hayashi, Y., Jan 15 2013, In : Bioorganic and Medicinal Chemistry. 21, 2, p. 412-424 13 p.

Research output: Contribution to journalArticle

Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: Design, synthesis, biological evaluation, and docking studies

Thanigaimalai, P., Konno, S., Yamamoto, T., Koiwai, Y., Taguchi, A., Takayama, K., Yakushiji, F., Akaji, K., Chen, S. E., Naser-Tavakolian, A., Schön, A., Freire, E. & Hayashi, Y., Jan 1 2013, In : European Journal of Medicinal Chemistry. 68, p. 372-384 13 p.

Research output: Contribution to journalArticle

Discrimination of potent inhibitors of toxoplasma gondii Enoyl-Acyl carrier protein reductase by a thermal shift assay

Afanador, G. A., Muench, S. P., McPhillie, M., Fomovska, A., Schön, A., Zhou, Y., Cheng, G., Stec, J., Freundlich, J. S., Shieh, H. M., Anderson, J. W., Jacobus, D. P., Fidock, D. A., Kozikowski, A. P., Fishwick, C. W., Rice, D. W., Freire, E., McLeod, R. & Prigge, S. T., Dec 23 2013, In : Biochemistry. 52, 51, p. 9155-9166 12 p.

Research output: Contribution to journalArticle

Ligand binding analysis and screening by chemical denaturation shift

Schön, A., Brown, R. K., Hutchins, B. M. & Freire, E., Jan 1 2013, In : Analytical biochemistry. 443, 1, p. 52-57 6 p.

Research output: Contribution to journalArticle

Nudel/NudE and Lis1 promote dynein and dynactin interaction in the context of spindle morphogenesis

Wang, S., Ketcham, S. A., Schön, A., Goodman, B., Wang, Y., Yates, J., Freire, E., Schroer, T. A. & Zheng, Y., Nov 15 2013, In : Molecular biology of the cell. 24, 22, p. 3522-3533 12 p.

Research output: Contribution to journalArticle

Optimization of CD4/gp120 Inhibitors by Thermodynamic-Guided Alanine-Scanning Mutagenesis

Liu, Y., Schön, A. & Freire, E., Jan 1 2013, In : Chemical Biology and Drug Design. 81, 1, p. 72-78 7 p.

Research output: Contribution to journalArticle

Optimizing biologics stability testing

Brown, R., Freire, E. & Hutchins, B., Sep 15 2013, In : Genetic Engineering and Biotechnology News. 33, 16, p. 26-27 2 p.

Research output: Contribution to journalArticle

Structure-based design and synthesis of an HIV-1 entry inhibitor exploiting X-ray and thermodynamic characterization

LaLonde, J. M., Le-Khac, M., Jones, D. M., Courter, J. R., Park, J., Schön, A., Princiotto, A. M., Wu, X., Mascola, J. R., Freire, E., Sodroski, J., Madani, N., Hendrickson, W. A. & Smith, A. B., Mar 14 2013, In : ACS Medicinal Chemistry Letters. 4, 3, p. 338-343 6 p.

Research output: Contribution to journalArticle

2012

Inhibiting early-stage events in HIV-1 replication by small-molecule targeting of the HIV-1 capsid

Kortagere, S., Madani, N., Mankowski, M. K., Schön, A., Zentner, I., Swaminathan, G., Princiotto, A., Anthony, K., Oza, A., Sierra, L. J., Passic, S. R., Wang, X., Jones, D. M., Stavale, E., Krebs, F. C., Martín-García, J., Freire, E., Ptak, R. G., Sodroski, J., Cocklin, S. & 1 others, Smith, A. B., Aug 1 2012, In : Journal of virology. 86, 16, p. 8472-8481 10 p.

Research output: Contribution to journalArticle

Photochemical control of RNA structure by disrupting π-stacking

Resendiz, M. J. E., Schön, A., Freire, E. & Greenberg, M. M., Aug 1 2012, In : Journal of the American Chemical Society. 134, 30, p. 12478-12481 4 p.

Research output: Contribution to journalArticle

Structure-based design, synthesis, and characterization of dual hotspot small-molecule HIV-1 Entry Inhibitors

Lalonde, J. M., Kwon, Y. D., Jones, D. M., Sun, A. W., Courter, J. R., Soeta, T., Kobayashi, T., Princiotto, A. M., Wu, X., Schön, A., Freire, E., Kwong, P. D., Mascola, J. R., Sodroski, J., Madani, N. & Smith, A. B., May 10 2012, In : Journal of medicinal chemistry. 55, 9, p. 4382-4396 15 p.

Research output: Contribution to journalArticle

2011

Characterisation of ligand binding by calorimetry

Freire, E., Kawasaki, Y., Velazquez-Campoy, A. & Schön, A., Dec 1 2011, Biophysical Approaches Determining Ligand Binding to Biomolecular Targets: Detection, Measurement and Modelling. Podjarny, A., Dejaegere, A. & Kieffer, B. (eds.). p. 275-299 25 p. (RSC Biomolecular Sciences).

Research output: Chapter in Book/Report/Conference proceedingChapter

Conformational and structural features of HIV-1 gp120 underlying the dual receptor antagonism by cross-reactive neutralizing antibody m18

Gift, S. K., Zentner, I. J., Schön, A., McFadden, K., Umashankara, M., Rajagopal, S., Contarino, M., Duffy, C., Courter, J. R., Zhang, M. Y., Gershoni, J. M., Cocklin, S., Dimitrov, D. S., Smith, A. B., Freire, E. & Chaiken, I. M., Apr 12 2011, In : Biochemistry. 50, 14, p. 2756-2768 13 p.

Research output: Contribution to journalArticle

Design, synthesis and biological evaluation of small molecule inhibitors of CD4-gp120 binding based on virtual screening

Lalonde, J. M., Elban, M. A., Courter, J. R., Sugawara, A., Soeta, T., Madani, N., Princiotto, A. M., Kwon, Y. D., Kwong, P. D., Schön, A., Freire, E., Sodroski, J. & Smith, A. B., Jan 1 2011, In : Bioorganic and Medicinal Chemistry. 19, 1, p. 91-101 11 p.

Research output: Contribution to journalArticle

Finding a better path to drug selectivity

Kawasaki, Y. & Freire, E., Nov 1 2011, In : Drug Discovery Today. 16, 21-22, p. 985-990 6 p.

Research output: Contribution to journalReview article

ITC: More Than Just Binding Affinities

Freire, E., Feb 24 2011, Label-Free Technologies for Drug Discovery. John Wiley and Sons, p. 303-312 10 p.

Research output: Chapter in Book/Report/Conference proceedingChapter

Some Binding-Related Drug Properties are Dependent on Thermodynamic Signature

Schön, A., Madani, N., Smith, A. B., Lalonde, J. M. & Freire, E., Mar 1 2011, In : Chemical Biology and Drug Design. 77, 3, p. 161-165 5 p.

Research output: Contribution to journalArticle

Synthesis and biochemical evaluation of triazole/tetrazole-containing sulfonamides against thrombin and related serine proteases

Siles, R., Kawasaki, Y., Ross, P. & Freire, E., Sep 15 2011, In : Bioorganic and Medicinal Chemistry Letters. 21, 18, p. 5305-5309 5 p.

Research output: Contribution to journalArticle

The plasmepsin family as antimalarial drug targets

Ruben, A. J., Kiso, Y. & Freire, E., Apr 4 2011, Aspartic Acid Proteases as Therapeutic Targets. Wiley-VCH Verlag, Vol. 45. p. 511-547 37 p.

Research output: Chapter in Book/Report/Conference proceedingChapter