Representative Publications      

Gharpure, A.*, Sulpizio, A.*, Loeffler, J.R., Fernández-Quintero, M.L., Tran, A.S., Lairson, L.L., Ward, A.B. (2025) Distinct oligomeric assemblies of STING induced by non-nucleotide agonists.  Nature Communications. 16: 3440. 

Sander, P.N., Gillen Miller, J.T., Lairson, L.L., (2024) Induced cell phenotype activity recording of DNA-tagged ligands.  RSC Chemical Biology. 6: 273. 

Beyer, B.A., Sul, A., Miller Gillen, J.T., Neumann, B., Plaisted, W.C., Kondo, T., Franklin, R.J.M., Lairson, L.L. (2023) Combination-based drug screening for induced oligodendrocyte differentiation enables mechanistic insight and identifies optimal drug pairs for remyelination. bioRxiv. Idoi:10.1101/2023.07.11.548469. 

Spangenberg, S.H., Palermo, A., Gazaniga, N., Martínez-Peña, F., Guijas, C., Chin, E.N., Rinschen, M. Sander, P.N., Webb, B., Pereira, L., Jia, Y.,  Meitz, L., Siuzdak, G., Lairson, L.L. (2023) Hydroxyproline metabolism modulates adaptive PD-L1 expression and autophagy. Cell Chemical Biology. 30: 1115. 


West T.J., Bi J., Martínez-Peña F., Curtis E.J., Gazaniga N.R., Mischel P.S., Lairson, L.L. (2023) A cell type selective YM155 prodrug targets Receptor-Interacting Protein Kinase 2 to induce brain cancer cell death. Journal of the American Chemical Society. 145: 8355-8363.

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Chin, E.N, Sulpizio, A., Lairson L.L. (2023) Targeting STING to promote anti-tumor immunity. Trends in Cell Biology. 33: 189-203.


Martínez-Peña F., Pearson A.D., Tang E.L., Kuburich N.A., Mani S.A., Schultz P.G., Bollong M.J., Lairson, L.L. (2022) Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers. European Journal of Medicinal Chemistry. 242: 114638.


Zavareh R.B., Spangenberg S.H., Woods A., Martínez-Peña F., Lairson L.L. (2021) HSP90 inhibition enhances cancer immunotherapy by modulating the surface expression of multiple immune checkpoint proteins. Cell Chemical Biology. 28:158-168.


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. 


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.
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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.



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.  

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. 


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


      
New Book Chapter

Lairson, L.L. (2023) “Small molecule drug discovery.” Advanced Chemical Biology. Edited by Hang, H. Pratt, M. and Preschner, J. J. Wiley & Sons, Inc.

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​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.