recent publications
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academic article
- Chang, J. W., Zuhl, A. M., Speers, A. E., Niessen, S., Brown, S. J., Mulvihill, M. M., Fan, Y. C., Spicer, T. P., Southern, M., Scampavia, L., Fernandez-Vega, V., Dix, M. M., et al. Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival ACS Chemical Biology 2015 10:925-932 DOI:10.1021/cb500893q PMID:25602368 PMCID:PMC4402257
- Zhao, N., Darby, C. M., Small, J., Bachovchin, D. A., Jiang, X., Burns-Huang, K. E., Botella, H., Ehrt, S., Boger, D. L., Anderson, E. D., Cravatt, B. F., Speers, A. E., et al. Target-based screen against a periplasmic serine protease that regulates intrabacterial pH homeostasis in Mycobacterium tuberculosis ACS Chemical Biology 2015 10:364-371 DOI:10.1021/cb500746z PMID:25457457 PMCID:PMC4340348
- Ward, J., Spath, S. N., Pabst, B., Carpino, P. A., Ruggeri, R. B., Xing, G., Speers, A. E., Cravatt, B. F., Ahn, K. Mechanistic characterization of a 2-thioxanthine myeloperoxidase inhibitor and selectivity assessment utilizing click chemistry-activity-based protein profiling Biochemistry 2013 52:9187-9201 DOI:10.1021/bi401354d PMID:24320749
- Hsu, K. L., Tsuboi, K., Whitby, L. R., Speers, A. E., Pugh, H., Inloes, J., Cravatt, B. F. Development and optimization of piperidyl-1,2,3-triazole ureas as selective chemical probes of endocannabinoid biosynthesis Journal of Medicinal Chemistry 2013 56:8257-8269 DOI:10.1021/jm400898x PMID:24152245 PMCID:PMC3984011
- Hsu, K. L., Tsuboi, K., Chang, J. W., Whitby, L. R., Speers, A. E., Pugh, H., Cravatt, B. F. Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6) Journal of Medicinal Chemistry 2013 56:8270-8279 DOI:10.1021/jm400899c PMID:24152295 PMCID:PMC3987869
- Nagano, J. M. G., Hsu, K. L., Whitby, L. R., Niphakis, M. J., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Hodder, P., Srinivasan, P., Gonzalez, T. D., et al. Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2) Bioorganic & Medicinal Chemistry Letters 2013 23:839-843 DOI:10.1016/j.bmcl.2012.11.061 PMID:23260346 PMCID:PMC3549684
- Liu, X. D., Dix, M., Speers, A. E., Bachovchin, D. A., Zuhl, A. M., Cravatt, B. F., Kodadek, T. J. Rapid development of a potent photo-triggered inhibitor of the serine hydrolase RBBP9 ChemBioChem 2012 13:2082-2093 DOI:10.1002/cbic.201200445 PMID:22907802 PMCID:PMC3777423
- Adibekian, A., Martin, B. R., Chang, J. W., Hsu, K. L., Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Hodder, P. S., et al. Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes Journal of the American Chemical Society 2012 134:10345-10348 DOI:10.1021/ja303400u PMID:22690931 PMCID:PMC3392194
- Saario, S. M., McKinney, M. K., Speers, A. E., Wang, C., Cravatt, B. F. Clickable, photoreactive inhibitors to probe the active site microenvironment of fatty acid amide hydrolase Chemical Science 2012 3:77-83 DOI:10.1039/c1sc00336d PMID:22737400 PMCID:PMC3378062
- Rowland, M. M., Bostic, H. E., Gong, D. H., Speers, A. E., Lucas, N., Cho, W. H., Cravatt, B. F., Best, M. D. Phosphatidylinositol 3,4,5-trisphosphate activity probes for the labeling and proteomic characterization of protein binding partners Biochemistry 2011 50:11143-11161 DOI:10.1021/bi201636s PMID:22074223 PMCID:PMC3649876
- Tsuboi, K., Bachovchin, D. A., Speers, A. E., Spicer, T. P., Fernandez-Vega, V., Hodder, P., Rosen, H., Cravatt, B. F. Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance Journal of the American Chemical Society 2011 133:16605-16616 DOI:10.1021/ja2066972 PMID:21899313 PMCID:PMC3226709
- Lone, A. M., Bachovchin, D. A., Westwood, D. B., Speers, A. E., Spicer, T. P., Fernandez-Vega, V., Chase, P., Hodder, P. S., Rosen, H., Cravatt, B. F., Saghatelian, A. A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors Journal of the American Chemical Society 2011 133:11665-11674 DOI:10.1021/ja2036095 PMID:21692504 PMCID:PMC3145007
- Bachovchin, D. A., Zuhl, A. M., Speers, A. E., Wolfe, M. R., Weerapana, E., Brown, S. J., Rosen, H., Cravatt, B. F. Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1 Journal of Medicinal Chemistry 2011 54:5229-5236 DOI:10.1021/jm200502u PMID:21639134 PMCID:PMC3144155
- Bachovchin, D. A., Mohr, J. T., Speers, A. E., Wang, C., Berlin, J. M., Spicer, T. P., Fernandez-Vega, V., Chase, P., Hodder, P. S., Schurer, S. C., Nomura, D. K., Rosen, H., et al. Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors Proceedings of the National Academy of Sciences of the United States of America 2011 108:6811-6816 DOI:10.1073/pnas.1015248108 PMID:21398589 PMCID:PMC3084096
- Speers, A. E., Cravatt, B. F. Ligands in crystal structures that aid in functional characterization Acta Crystallographica Section F-Structural Biology and Crystallization Communications 2010 66:1306-1308 DOI:10.1107/s1744309110035748 PMID:20944226 PMCID:PMC2954220
- Speers, A. E., Cravatt, B. F. Activity-based protein profiling (ABPP) and click chemistry (CC)-ABPP by MudPIT mass spectrometry Current Protocols in Chemical Biology 2009 1:29-41 DOI:10.1002/9780470559277.ch090138 PMID:21701697 PMCID:PMC3119539
- Blackler, A. R., Speers, A. E., Wu, C. C. Chromatographic benefits of elevated temperature for the proteomic analysis of membrane proteins Proteomics 2008 8:3956-3964 DOI:10.1002/pmic.200800210 PMID:18780350 PMCID:PMC2765112
- Blackler, A. R., Speers, A. E., Ladinsky, M. S., Wu, C. C. A shotgun proteomic method for the identification of membrane-embedded proteins and peptides Journal of Proteome Research 2008 7:3028-3034 DOI:10.1021/pr700795f PMID:18537282 PMCID:PMC2765231
- Speers, A. E., Wu, C. C. Proteomics of integral membrane proteins-theory and application Chemical Reviews 2007 107:3687-3714 DOI:10.1021/cr068286z PMID:17683161
- Speers, A. E., Blackler, A. R., Wu, C. C. Shotgun analysis of integral membrane proteins facilitated by elevated temperature Analytical Chemistry 2007 79:4613-4620 DOI:10.1021/ac0700225 PMID:17500534
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Weerapana, E., Speers, A. E., Cravatt, B. F. Tandem orthogonal proteolysis-activity-based protein profiling (TOP-ABPP) - a general method for mapping sites of probe modification in proteomes Nature Protocols 2007 2:1414-1425 DOI:10.1038/nprot.2007.194 PMID:17545978
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Speers, A. E., Cravatt, B. F. A tandem orthogonal proteolysis strategy for high-content chemical proteomics Journal of the American Chemical Society 2005 127:10018-10019 DOI:10.1021/ja0532842 PMID:16011363 PMCID:PMC1538546
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Speers, A. E., Cravatt, B. F. Profiling enzyme activities in vivo using click chemistry methods Chemistry & Biology 2004 11:535-546 DOI:10.1016/j.chembiol.2004.03.012 PMID:15123248
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Speers, A. E., Cravatt, B. F. Chemical strategies for activity-based proteomics ChemBioChem 2004 5:41-47 DOI:10.1002/cbic.200300721 PMID:14695510
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Speers, A. E., Adam, G. C., Cravatt, B. F. Activity-based protein profiling in vivo using a copper(i)-catalyzed azide-alkyne 3+2 cycloaddition Journal of the American Chemical Society 2003 125:4686-4687 DOI:10.1021/ja034490h PMID:12696868
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report
- Hulce, J. J., Joslyn, C., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. An in vivo active carbamate-based dual inhibitor of lysophospholipase 1 (LYPLA1) and lysophospholipase 2 (LYPLA2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:25506974
- Zuhl, A. M., Mohr, J. T., Speers, A. E., Bachovchin, D. A., Berlin, J. M., Spicer, T., Fernandez-Vega, V., Brown, S. J., Ferguson, J., Fu, G. C., Cravatt, B. F., Hodder, P., et al. Probe development efforts to identify novel inhibitors of ABHD10 Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762952
- Adibekian, A., Martin, B. R., Chang, J. W., Hsu, K. L., Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:24624468
- Adibekian, A., Martin, B. R., Chang, J. W., Hsu, K. L., Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., et al. Characterization of a selective, reversible inhibitor of lysophospholipase 1 (LYPLA1) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:24624465
- Nagano, J. M. G., Hsu, K. L., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Bahnson, B. J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a carbamate inhibitor for plasma platelet-activating factor acetylhydrolase (pPAFAH) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658952
- Dreyton, C. J., Jones, J. E., Knuckley, B. A., Subramanian, V., Anderson, E. D., Brown, S. J., Fernandez-Vega, V., Eberhart, C., Spicer, T., Zuhl, A. M., Ferguson, J., Speers, A. E., et al. Optimization and characterization of a pan protein arginine deiminase (PAD) inhibitor Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23833800
- Adibekian, A., Martin, B. R., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea dual inhibitor for lysophospholipase 1 (LYPLA1) and lysophospholipase 2 (LYPLA2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658947
- Adibekian, A., Hsu, K. L., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea inhibitor for alpha/beta hydrolase domain-containing protein 11 (ABHD11): anti-probe for LYPLA1/LYPLA2 dual inhibitor ML211 Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658953
- Hsu, K. L., Tsuboi, K., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea inhibitor for diacylglycerol lipase beta (DAGL-beta) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658950
- Adibekian, A., Hsu, K. L., Speers, A. E., Monillas, E. S., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Bahnson, B. J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of a triazole urea inhibitor for platelet-activating factor acetylhydrolase type 2 (PAFAH2) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23658960
- Tsuboi, K., Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of an inhibitor for glutathione S-tranferase omega 1 (GSTO1) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:22834034
- Hsu, K. L., Tsuboi, K., Speers, A. E., Brown, S. J., Spicer, T., Fernandez-Vega, V., Ferguson, J., Cravatt, B. F., Hodder, P., Rosen, H. Optimization and characterization of triazole urea inhibitors for abhydrolase domain containing protein 6 (ABHD6) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762934
- Bachovchin, D. A., Speers, A. E., Brown, S. J., Spicer, T. P., Fernandez, Vega, Ferguson, J., Mohr, J. T., Murphy, J., Fu, G. C., Cravatt, B. F., Hodder, P. S., Rosen, H. Probe development efforts to identify novel inhibitors of protein phosphatase methylesterase-1 (PME-1) Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:22834039
- Bachovchin, D. A., Speers, A. E., Zuhl, A. M., Brown, S. J., Cravatt, B. F., Fernandez, Vega, Spicer, T., Mercer, B. A., Ferguson, J., Hodder, P., Rosen, H. R. Probe report for PME-1 inhibitors Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21433379
- Bachovchin, D. A., Speers, A. E., Brown, S. J., Cravatt, B. F., Spicer, T., Mercer, B. A., Ferguson, J., Hodder, P., Rosen, H. R. Probe report for RBBP9 inhibitors - Probe 2 Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21433382