Koehler Group: Publications

1. Izhack Cherny, Maria Korolev, Angela N. Koehler, Michael H. Hecht. "Proteins from an unevolved library of de novo designed sequences bind a range of small molecules." ACS Synth. Biol., 1, 130-138, 2012. Link.

2. Melissa M. Kemp, Michel Weiwer, Angela N. Koehler. "Unbiased binding assays for discovering small-molecule probes and drugs." Bioorg. Med. Chem., 20, 1979-1989, 2012. Link.

3. Dominick E. Casalena, Dina Wassaf, Angela N. Koehler. "Ligand discovery using small-molecule micorarrays." Methods Mol. Biol., 803, 249-263, 2012. Link

4. Melissa M. Kemp, Qiu Wang, Jason H. Fuller, Nathan West, Nicole Martinez, Elizabeth M. Morse, Michel Weïwer, Stuart L. Schreiber, James E. Bradner, Angela N. Koehler. “A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.” Bioorg. Med. Chem. Lett., 21, 4164-4169, 2011.  PMCID: PMC3248787

5. Paul A. Clemons, J. Anthony Wilson, Vlado Dancik, Sandrine Muller, Hyman A. Carrinski, Bridget K. Wagner, Angela N. Koehler, Stuart L. Schreiber. “Quantifying structural property distributions and patterns of performance among sets of small molecules comprising small-molecule screening collections.” Proc. Natl. Acad. Sci. USA, 108, 6817-6822, 2011. PMCID: PMC3084049

6. Myung-Soo Kang, Eun Kyung Lee, Vishal Soni, Timothy A. Lewis, Angela N. Koehler, Viswanathan Srinivasana, Elliott Kieff. "Roscovitine inhibits EBNA1 Serine 393 phosphorylation, nuclear localization, transcription, and episome maintenance." J. Virol., 85, 2859-2568, 2011. PMCID: PMC3067954

7. Jermont M. Chen, Anne H. Armstrong, Angela N. Koehler, Michael H. Hecht. "Small molecule microarrays enable the discovery of compounds that bind the Alzheimer's ABeta peptide and reduce its cytotoxicity." J. Am. Chem. Soc., 132, 17015-17022, 2010. PMCID: PMC3063105

8. Paul A. Clemons, Nicole E. Bodycombe, Hyman A. Carrinski, J. Anthony Wilson, Alykhan F. Shamji, Bridget K. Wagner, Angela N. Koehler, Stuart L. Schreiber. "Small molecules of different synthetic and natural origins have distinct distributions of structural complexity that correlate with protein-binding profiles." Proc. Natl. Acad. Sci. USA, 107, 18787-18792, 2010. PMCID: PMC2973913

9. The Cancer Target Discovery and Development Network: Stuart L. Schreiber, Alykhan F. Shamji, Paul A. Clemons, Cindy Hon, Angela N. Koehler, Benito Munoz, Michelle Palmer, Andrew M. Stern, Bridget K. Wagner, Scott Powers, Scott W. Lowe, Xuecui Guo, Alex Krasnitz, Eric T. Sawey, Raffaella Sordella, Lincoln Stein, Lloyd C. Trotman, Andrea Califano, Riccardo Dalla-Favera, Adolfo Ferrando, Antonio Iavarone, Laura Pasqualucci, Jose Silva, Brent R. Stockwell, William C. Hahn, Lynda Chin, Ronald A. DePinho, Jesse S. Boehm, Shuba Gopal, Alan Huang, David E. Root, Barbara A Weir, Daniela S Gerhard, Jean Claude Zenklusen, Michael G. Roth, Michael A. White, John D. Minna, John B. MacMillan, Bruce A. Posner. "Towards a patient-based cancer therapeutics." Nat. Biotechnol., 28, 904-906, 2010. PMCID: PMC2939009

10. Angela N. Koehler. “A complex task? Direct modulation of transcription factors with small molecules.” Curr. Opin. Chem. Biol., 14, 331-340, 2010. Link

11. Arturo J. Vegas, Angela N. Koehler. “Detecting protein-small molecule interactions using fluorous small-molecule microarrays.”  Methods Mol. Biol., 669, 43-55, 2010. Link

12. Carlos Tassa, Jay L. Duffner, Timothy A. Lewis, Ralph Weissleder, Stuart L. Schreiber, Angela N. Koehler, Stanley Y. Shaw. “Binding affinity and kinetic analysis of targeted small molecule-modified nanoparticles.” Bioconjug. Chem., 21,14-19, 2010. PMCID: PMC2902264

13. Shao-En Ong, Monica Schenone, Adam A. Margolin, Xiaoyu Li, Kathy Do, Mary K. Doud, Denkanikota R. Mani, Letian Kuai, Xiang Wang, John L. Wood, Nicola J. Tolliday, Angela N. Koehler, Lisa A. Marcaurelle, Todd R. Golub, Robert J. Gould, Stuart L. Schreiber, Steve A. Carr. “Identifying the proteins to which small-molecule probes and drugs bind in cells.” Proc. Natl. Acad. Sci. USA, 106, 4617-4622, 2009. PMCID: PMC2649954

14. Yingwei Mao, Xuecai Ge, Christopher L. Frank, Jon Madison, Angela N. Koehler, Mary K. Doud, Carlos Tassa, Erin M. Berry, Tracey L. Petryshen, Takahiro Soda, Travis Biechele, Randall T. Moon, Stephen J. Haggarty, Li-Huei Tsai. “DISC1 regulates neural progenitor proliferation via modulation of GSK3β/β-catenin signaling.” Cell, 136, 1017-1031, 2009. PMCID: PMC2704382

15. Benjamin Z. Stanton, Lee F. Peng, Nicole Maloof, Kazuo Nakai, Xiang Wang, Jay L. Duffner, Kennedy M. Taveras, Joel M. Hyman, Sam W. Lee, Angela N. Koehler, James K. Chen, Julia L. Fox, Anna Mandinova, Stuart L. Schreiber. “A small molecule that binds Hedgehog and blocks signaling in human cells.” Nature Chemical Biology, 5, 154-156, 2009. PMCID: PMC2770933

16. Angela N. Koehler. “Microarrays in chemical biology.” Chapter, Wiley Encyclopedia of Chemical Biology, Tadhg Begley, Editor, ISBN: 978-0-471-75477-0, 2009. Link

17. Arturo J. Vegas, Jason H. Fuller, Angela N. Koehler. “Small-molecule microarrays as tools in ligand discovery.” Chem. Soc. Rev., 37, 1385-1394, 2008. PMCID: PMC2688956

18. Thomas J. F. Nieland, Jared T. Shaw, Firoz A. Jaipuri, Jay. L. Duffner, Angela N. Koehler, Sotirios Banakos, Vassilis I. Zannis, Tom Kirchhausen, Monty Krieger. “Identification of the molecular target for small molecule inhibitors of HDL receptor SR-BI activity.” Biochemistry, 47, 460-472, 2008. PMCID: PMC2736594

19. Katja Schmitz, Stephen J. Haggarty, Olivia M. McPherson, Jon Clardy, Angela N. Koehler. “Detecting binding interactions using microarrays of natural product extracts.” J. Am. Chem. Soc., 129, 11346-11347, 2007. Link

20. Arturo J. Vegas, James E. Bradner, Weiping Tang, Olivia M. McPherson, Edward F. Greenberg, Angela N. Koehler, Stuart L. Schreiber. “Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors.” Angew. Chem. Int. Ed. 46, 7960-7964, 2007. PMCID: PMC2790065

21. Thomas J. F. Nieland, Jared T. Shaw, Firoz A. Jaipuri, Zoltan Maliga, Jay L. Duffner, Angela N. Koehler, Monty Krieger. “Influence of clinical and experimental HDL-cholesterol elevating drugs on the activity of the HDL receptor SR-BI.” J. Lipid Res., 48, 1832-1845, 2007. Link

22. Hua Miao, John A. Tallarico, Hiroyuki Hayakawa, Karl Münger, Jay L. Duffner, Angela N. Koehler, Stuart L. Schreiber, Timothy A. Lewis. “Ring-opening and ring-closing reactions of a shikimic acid-derived substrate leading to diverse small molecules.” J. Comb. Chem. 9, 245-253, 2007. Link

23. Jay L. Duffner, Paul A. Clemons, Angela N. Koehler. “A pipeline for ligand discovery using small-molecule microarrays.” Curr. Opin. Chem. Biol. 11, 74-82, 2007. Link

24. James E. Bradner, Olivia M. McPherson, Angela N. Koehler. “A method for the covalent capture and screening of diverse small molecules in a microarray format.” Nature Protocols, 1, 2344-2352, 2006. Link

25. Nicola Tolliday, Paul A. Clemons, Paul Ferraiolo, Angela N. Koehler, Timothy A. Lewis, Xiaohua Li, Stuart L. Schreiber, Daniela S. Gerhard, Scott Eliasof. “Small molecules, big players: The National Cancer Institute’s Initiative for Chemical Genetics.” Cancer Res. 66, 1-8, 2006. Link

26. James E. Bradner, Olivia M. McPherson, Ralph Mazitschek, David Barnes-Seeman, John P. Shen, Jasmeet Dhaliwal, Jay L. Duffner, Kristen E. Stevenson, Seung Bum Park, Donna S. Neuberg, Paul Nghiem, Stuart L. Schreiber, Angela N. Koehler. “A robust small-molecule microarray platform for screening cell lysates.” Chem. Biol. 13, 493-504, 2006. Link

Graduate and Undergraduate Work

27. Angela N. Koehler, Alykhan F. Shamji, Stuart L. Schreiber. “Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis.” J. Am. Chem. Soc. 125, 8420-8421, 2003. Link

28. David Barnes-Seeman, Seung Bum Park, Angela N. Koehler, Stuart L. Schreiber. “Expanding the functional group compatibility of small-molecule microarrays: discovery of novel calmodulin ligands.” Angew. Chem. Int. Ed. 42, 2376-2379, 2003. Link

29. Paul A. Clemons, Angela N. Koehler, Bridget K. Wagner, Timothy G. Sprigings, David R. Spring, Randall W. King, Stuart L. Schreiber, Michael A. Foley. “A one bead, one stock solution approach to chemical genetics: Part 2.” Chem. Biol. 8, 1183-1195, 2001. Link

30. Gavin MacBeath, Angela N. Koehler, Stuart L. Schreiber. “Printing small molecules onto microarrays and detecting protein-ligand interactions en masse.” J. Am. Chem. Soc. 121, 7697-7698, 1999. Link

31. Arthur Glasfeld, Angela N. Koehler, Maria A. Schumacher, Richard G. Brennan. “The role of lysine 55 in determining the specificity of the purine repressor for its operators through minor groove interactions.” J. Mol. Biol. 291, 347-361, 1999. Link