Selected Publications (Graphical Abstracts)

Read up on the latest publications in diversity-oriented synthesis, rational drug design, chemical biology, and drug discovery research from the Tan Lab!

Selected Publications: Text Only | Graphical Abstracts
Complete Publications: Text Only | Graphical Abstracts

Full-text versions of articles are available from the publisher with online journal subscription. PubMed Central (PMC) versions of articles are available free of charge.


  1. Mechanism of MenE inhibition by acyl-adenylate analogues and discovery of novel antibacterial agents.
    Matarlo, J. S.; Evans, C. E.; Sharma, I.; Lavaud, L. J.; Ngo, S. C.; Shek, R.; Rajashankar, K. R.; French, J. B.; Tan, D. S.*; Tonge, P. J.* Biochemistry 2015, 54, 6514–6524.
    Abstract | PubMed | PMC ]

  2. Cheminformatic comparison of approved drugs from natural product versus synthetic origins.
    Stratton, C. F.; Newman, D. J.; Tan, D. S.* Bioorg. Med. Chem. Lett. 2015, 25, 4802–4807.
    Abstract | PubMed | PMC ]

  3. Principal component analysis as a tool for library design: A case study investigating natural products, brand-name drugs, natural product-like libraries, and drug-like libraries.
    Wenderski, T. A.; Stratton, C. F.; Bauer, R. A.; Kopp, F.; Tan, D. S.* Methods Mol. Biol. 2015, 1263, 225–242.
    Abstract | PubMed | PMC ]

  4. General platform for systematic quantitative evaluation of small-molecule permeability in bacteria.
    Davis, T. D.; Gerry, C. J.; Tan, D. S.* ACS Chem. Biol. 2014, 9, 2535–2544.
    Abstract | PubMed | PMC ]

    (Highlighted in ACS Chem. Biol.)

  5. Solvent-dependent divergent functions of Sc(OTf)3 in stereoselective epoxide-opening spiroketalizations.
    Sharma, I.; Wurst, J. M.; Tan, D. S.* Org. Lett. 2014, 16, 2474–2477.
    Abstract | PubMed | PMC ]

  6. Pharmacokinetic and in vivo efficacy studies of the mycobactin biosynthesis inhibitor salicyl-AMS in mice.
    Lun, S.; Guo, H.; Adamson, J.; Cisar, J. S.; Davis, T. D.; Sundaramn Chavadi, S.; Warren, J. D.; Quadri, L. E. N.*; Tan, D. S.*; Bishai, W. R.* Antimicrob. Agents Chemother. 2013, 57, 5138–5140.
    Abstract | PubMed | PMC ]

  7. Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion.
    Bauer, R. A.; Wenderski, T. A.; Tan, D. S.* Nat. Chem. Biol. 2013, 9, 21–29.
    Abstract | PubMed | PMC ]

  8. Stereoselective synthesis of acortatarins A and B.
    Wurst, J. M.; Verano, A. L.; Tan, D. S.* Org. Lett. 2012, 14, 4442–4445.
    Abstract | PubMed | PMC ]

  9. A diversity-oriented synthesis approach to macrocycles via oxidative ring expansion.
    Kopp, F.; Stratton, C. F.; Akella, L. B.; Tan, D. S.* Nat. Chem. Biol. 2012, 8, 358–365.
    Abstract | PubMed | PMC ]

    (Highlighted in SciBX )

  10. Hydrogen-bonding catalysis and inhibition by simple solvents in the stereoselective kinetic epoxide-opening spirocyclization of glycal epoxides to form spiroketals.
    Wurst, J. M.; Liu, G.; Tan, D. S.* J. Am. Chem. Soc. 2011, 133, 7916–7925.
    Abstract | PubMed | PMC ]

  11. Solid-phase synthesis and chemical space analysis of a 190-membered alkaloid/terpenoid-like library.
    Moura-Letts, G.; DiBlasi, C. M.; Bauer, R. A.; Tan, D. S.* Proc. Natl. Acad. Sci. USA 2011, 108, 6745–6750.
    Abstract | PubMed | PMC ]

  12. The tert-butylsulfinamide lynchpin in transition-metal-mediated multiscaffold library synthesis.
    Bauer, R. A.; DiBlasi, C. M.; Tan, D. S.* Org. Lett. 2010, 12, 2084–2087.
    Abstract | PubMed | PMC ]

  13. Expanding the range of ’druggable’ targets with natural product-based libraries: An academic perspective.
    Bauer, R. A.; Wurst, J. M.; Tan, D. S.* Curr. Opin. Chem. Biol. 2010, 14, 308–314.
    Abstract | PubMed | PMC ]

  14. Active site remodelling accompanies thioester bond formation in the SUMO E1.
    Olsen, S. K.; Capili. A. D.; Lu, X.; Tan, D. S.*; Lima, C. D.* Nature 2010, 463, 906–912.
    Abstract | PubMed | PMC ]

    (Highlighted in Nature, Chem. Eng. News, Nat. Rev. Mol. Cell Biol., Nat. Chem. Biol., Structure, ACS Chem. Biol., and Faculty of 1000 Biology )

  15. Designed semisynthetic protein inhibitors of Ub/Ubl E1 activating enzymes.
    Lu, X.; Olsen, S. K.; Capili, A. D.; Cisar, J. S.; Lima, C. D.*; Tan, D. S.* J. Am. Chem. Soc. 2010, 132, 1748–1749.
    Abstract | PubMed | PMC ]

    (Highlighted in Chem. Eng. News, Nat. Rev. Mol. Cell Biol., ACS Chem. Biol., and Faculty of 1000 Biology )

  16. Stereoselective synthesis of benzannulated spiroketals: Influence of the aromatic ring on reactivity and conformation.
    Liu, G.; Wurst, J. M.; Tan, D. S.* Org. Lett. 2009, 11, 3670–3673.
    Abstract | PubMed | PMC ]

  17. Small molecule inhibition of microbial natural product biosynthesis – An emerging antibiotic strategy.
    Cisar, J. S.; Tan, D. S.* Chem. Soc. Rev. 2008, 37, 1320–1329.
    Abstract | PubMed | PMC ]

  18. Exploiting ligand conformation in selective inhibition of non-ribosomal peptide synthetase amino acid adenylation with designed macrocyclic small molecules.
    Cisar, J. S.; Ferreras, J. A.; Soni, R. K.; Quadri, L. E. N.*; Tan, D. S.* J. Am. Chem. Soc. 2007, 129, 7752–7753.
    Abstract | PubMed | PMC ]

    (Highlighted in Faculty of 1000 Biology )

  19. A unified synthetic approach to polyketides having both skeletal and stereochemical diversity.
    Shang, S.; Iwadare, H.; Macks, D. E.; Ambrosini, L. M.; Tan, D. S.* Org. Lett. 2007, 9, 1895–1898.
    Abstract | PubMed | PMC ]

  20. Stereocontrolled synthesis of spiroketals via Ti(Oi-Pr)4-mediated kinetic spirocyclization of glycal epoxides with retention of configuration.
    Moilanen, S. B.; Potuzak, J. S.; Tan, D. S.* J. Am. Chem. Soc. 2006, 128, 1792–1793.
    Abstract | PubMed | PMC ]

    (Highlighted in Nature )

  21. Stereocontrolled synthesis of spiroketals via a remarkable methanol-induced kinetic spirocyclization reaction.
    Potuzak, J. S.; Moilanen, S. B.; Tan, D. S.* J. Am. Chem. Soc. 2005, 127, 13796–13797.
    Abstract | PubMed  ]

  22. Diversity-oriented synthesis: Exploring the intersections between chemistry and biology.
    Tan, D. S.* Nat. Chem. Biol. 2005, 1, 74–84.
    Abstract | PubMed ]

  23. Small-molecule inhibition of siderophore biosynthesis in Mycobacterium tuberculosis and Yersinia pestis.
    Ferreras, J. A.; Ryu, J.-S.; Di Lello, F.; Tan, D. S.*, Quadri, L. E. N.* Nat. Chem. Biol. 2005, 1, 29–32.
    Abstract | PubMed ]

    (Highlighted in Nature, Nat. Chem. Biol., Chem. Eng. News., and Mercosur Económico )

  24. An acid-stable tert-butyldiarylsilyl (TBDAS) linker for solid-phase organic synthesis.
    DiBlasi, C. M.; Macks, D. E.; Tan, D. S.* Org. Lett. 2005, 7, 1777–1780.
    Abstract | PubMed ]

    (Highlighted in Lett. Org. Chem. [PDF] )

  25. Synthesis of the functionalized tricyclic skeleton of guanacastepene A: A tandem epoxide-opening β-elimination/Knoevenagel cyclization.
    Tan, D. S.; Dudley, G. B; Danishefsky, S. J.* Angew. Chem., Int. Ed. 2002, 41, 2185–2188.
    Abstract | PubMed ]

  26. A stereoselective route to guanacastepene A through a surprising epoxidation.
    Lin, S.; Dudley, G. B.; Tan, D. S.; Danishefsky, S. J.* Angew. Chem., Int. Ed. 2002, 41, 2188–2191.
    Abstract | PubMed ]

  27. Synthesis and preliminary evaluation of a library of polycyclic small molecules for use in chemical genetic assays.
    Tan, D. S.; Foley, M. A.; Stockwell, B. R.; Shair, M. D.; Schreiber, S. L.* J. Am. Chem. Soc. 1999, 121, 9073–9087.
    Abstract ]

  28. Stereoselective synthesis of over two million compounds having structural features both reminiscent of natural products and compatible with miniaturized cell-based assays.
    Tan, D. S.; Foley, M. A.; Shair, M. D.; Schreiber, S. L.* J. Am. Chem. Soc. 1998, 120, 8565–8566.
    Abstract ]

    (Highlighted in Science, Chem. Eng. News. )

  29. Enzymatic resolution coupled with substrate racemization using a thioester substrate.
    Tan, D. S.; Günter, M. M.; Drueckhammer, D. G.* J. Am. Chem. Soc. 1995, 117, 9093–9094.
    Abstract ]