Representative Publications
Zavareh R.B., Spangenberg S.H., Woods A., Martínez-Peña F., Lairson L.L. (2020) HSP90 Inhibition Enhances Cancer Immunotherapy by Modulating the Surface Expression of Multiple Immune Checkpoint Proteins. Cell Chemical Biology. S2451-9456(20)30384-6. Online ahead of print.
Chin E.N., Yu C., Vartabedian V.F., Jia Y., Kumar M., Gamo A.M., Vernier W., Ali S.H., Kissai M., Lazar D.C., Nguyen N., Pereira L.E., Benish B., Woods A.K., Joseph S.B., Chu A., Johnson K.A., Sander P.N., Martínez-Peña F., Hampton E.N., Young T.S., Wolan D.W., Chatterjee A.K., Schultz P.G., Petrassi H.M., Teijaro J.R., Lairson, L.L. (2020) Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic.
Science. 369: 993-999.
SR-717 selected as a Drug Hunter Molecule of the Month
Nature Reviews Drug Discovery Research Highlight
Nature Reviews Immunology Research Highlight
Lucki N.C., Villa G.R., Vergani N., Bollong M.J., Beyer B.A., Lee J.W., Anglin J.L., Spangenberg S.H., Chin E.N., Sharma A., Johnson K., Sander P.N., Gordon P., Skirboll S.L., Wurdak H., Schultz P.G., Mischel P.S., Lairson L.L. (2019) A cell type-selective apoptosis-inducing small molecule for the treatment of brain cancer. Proceedings of the National Academy of Science USA. 116: 6435-6440.
Bollong M.J., Lee G., Coukos J.S., Yun H., Zambaldo C., Chang J.W., Chin E.N., Ahmad I., Chatterjee A.K., Lairson L.L.*, Schultz P.G.*, Moellering R.E.* (2018) A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signalling. Nature. 562: 600-604. * co-corresponding author
Anglin J., Zavareh R.B., Sander P.N., Haldar D., Mullarky E., Cantley L.C., Kimmelman A.C., Lyssiotis C.A., Lairson L.L. (2018) Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorganic & Medicinal Chemistry Letters. 28: 2675-2678. (special issue dedicated to Prof. Dale Boger)
Beyer B.A., Fang M., Sadrian B., Montenegro-Burke J.R., Plaisted W.C. Kok. B.P.C., Saez E., Kondo T., Siuzdak G., Lairson L.L. (2018) Metabolomics-based discovery of a metabolite that enhances oligodendrocyte maturation. Nature Chemical Biology. 14: 22-28.
Bollong M.J., Pietila M., Pearson A.D. Sarkar, T. R. Ahmad I., Soundararajan R., Lyssiotis C.A., Mani S.A., Schultz P.G., Lairson L.L. (2017) A vimentin binding small molecule leads to mitotic disruption in mesenchymal cancers. Proceedings of the National Academy of Science USA. 14: E9903-E9912.
Lum K.M., Sato Y., Beyer B.A., Plaisted W.C., Anglin J.L., Lairson L.L.*, Cravatt B.F.* (2017) Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chemical Biology. 12: 2671-81. * co-corresponding author
Bollong M.J., Yang B., Vergani N., Beyer B.A., Chin E.N., Zambaldo C., Wang D., Chatterjee A.K., Lairson L.L.*, Schultz P.G.* (2017) Small molecule-mediated inhibition of myofibroblast transdifferentiation for the treatment of fibrosis. Proceedings of the National Academy of Science USA. 114: 4679-84. * co-corresponding author
Faculty of 1000 Article Recommendation
Mullarky E., Lucki N., Beheshti Zavareh R., Anglin J., Gomes A.P., Nicolay N.G., Wong J.C.Y, Christen S., Takahashi H., Singh P.K., Blenisa J., Warren D., Fend S.M., Asarai J.M., DeNicola G.M., Lyssiotis C.A., Lairson L.L.* and Cantley L.C.* (2016) Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. Proceedings of the National Academy of Science USA. 113: 1778-83 * co-corresponding author
Deshmukh V.A., Tardif V., Lyssiotis C.A., Green C.C., Kerman B., Kim H.J., Padmanabhan K., Swoboda J.G.,
Ahmad I., Kondo T., Gage F.H., Theofilopoulos A.N., Lawson B.R., Schultz P.G., Lairson L.L. (2013)
A regenerative approach to the treatment of multiple sclerosis. Nature. 502: 327-332.
Faculty of 1000 Article Recommendation
Postdoctoral and Graduate
Lyssiotis C.A., Lairson L.L., Boitano A.E., Wurdak H., Zhu S., Schultz P.G. (2011) Chemical control of stem cell fate and developmental potential. Angewandte Chemie International Edition. 50: 200-242.
Chan, P.H., Lairson, L.L., Lee, H.J., Wakarchuk, W.W., Strynadka, N.C., Withers, S.G., and McIntosh, L.P. (2009) NMR Spectroscopic Characterization of the sialyltransferase CstII from Campylobacter jejuni: histidine 188 is the general base. Biochemistry. 48: 11220-11230.
Lairson, L.L., Henrissat, B., Davies, G.J., and Withers, S.G. (2008) Glycosyltransferases: Structures, Functions, and Mechanisms. Annual Review of Biochemistry. 77: 521-555.
Lairson, L.L., Wakarchuk, W.W., and Withers, S.G. (2007) Alternative donor substrates for inverting and retaining glycosyltransferases. Chemical Communications (Camb.). (4): 365-367.
Faculty of 1000 Article Recommendation
Lairson, L.L., Watts, A.G., Wakarchuk, W.W., and Withers, S.G. (2006) Using Substrate Engineering to Harness Enzyme Promiscuity and Expand Biological Catalysis. Nature Chemical Biology 2: 724-728.
Research Highlight in Nature
(Same key, different lock. Nature. 444: 657).
Lairson, L.L., Withers, S.G. (2004) Mechanistic analogies amongst carbohydrate modifying enzymes. Chemical Communications (Camb.). (20): 2243- 2248.
Lairson, L.L., Chiu, C.P.C., Ly, H.D., He, S., Wakarchuk, W.W., Strynadka, N.C.J., Withers, S.G. (2004) Intermediate trapping on a mutant retaining alpha-galactosyltransferase identifies an unexpected aspartate residue. Journal of Biological Chemistry. 279: 28339-28344.
Chiu, C.P.C., Watts, A.G., Lairson, L.L., Gilbert, M., Lim, D., Wakarchuk, W.W., Withers, S.G., Strynadka, N.C.J. (2004) Structural analysis of the sialyltransferase CstII from Campylobacter jejuni in complex with a substrate analog. Nature Structural and Molecular Biology. 11: 163-170.