Publications

MIT

44. André Richters, Angela N. Koehler. "Epigenetic modulation using small molecules - targeting histone acetyltransferases in disease." Curr. Med. Chem. in press, 2017.

43. Yikai Wang, Jean-Yves Wach, Patrick Sheehan, Cheng Zhong, Chenyang Zhan, Richard Harris, Steven C. Almo, Joshua Bishop, Stephen H. Haggarty, Alexander Ramek, Kayla Berry, Conor O'Herin, Angela N. Koehler, Alvin Hung, Damian W. Young. "Application of diversity-oriented synthesis as a strategy for fragment evolution against GSK3beta." ACS Med. Chem. Lett., 7, 852-856, 2016.

42. Jeffrey J. Coleman, Tomomi Kimura, Julia Munro, Michael P. Wu, Rakhee R. Busanelli, Angela N. Koehler, Meryl Thomas, Florence F. Wagner, Edward B. Holson, Eleftherios Mylanokis. "The immunomodulatory activity of caffeic acid phenethyl ester in Caenorhabditis elegans is mediated by the CED-10 (Rac-1)/PAK-1 pathway." Future Medicinal Chemistry, published online. October 14, 2016.

41. Zhihong Yang, Angela N. Koehler, Li Wang. "A novel small molecule activator of nuclear receptor SHP inhibits HCC cell migration via suppressing Ccl2." Mol. Cancer Ther., 15, 2294-2301, 2016.

40. Zarko V. Boskovic, Melissa M. Kemp, Allyson M. Freedy, Vasanthi S. Viswanathan, Marius S. Pop, Jason H. Fuller, Nicole M. Martinez, Samuel O. Figueroa Lazu, Jiyoung A. Hong, Timothy A. Lewis, Daniel Calarese, James D. Love, Amedeo Vetere, Steven C. Almo, Stuart L. Schreiber, Angela N. Koehler. "Inhibition of zinc-dependent histone deacetylases with a chemically triggered electrophile." ACS Chem. Biol. 11, 1844-1851, 2016.

39. Shelby K. Doyle, Marius S. Pop, Helen L. Evans, Angela N. Koehler. "Advances in discovering small molecules to probe protein function in a systems context." Curr. Opin. Chem. Biol. 30, 28-36, 2016.

38. Luc de Waal, Timothy A. Lewis, Matthew G. Rees, Aviad Tsherniak, Xiaoyun Wu, Peter S. Choi, Lara Gechjjian, Christina Hartigan, Patrick W. Faloon, Marc J. Hickey, Nicola Tolliday, Steve A. Carr, Paul A. Clemons, Benito Munoz, Bridget K. Wagner, Alykhan F. Shamji, Angela N. Koehler. Monica Schenone, Alex B. Burgin, Stuart. L. Schreiber, Heidi Greulich, Matthew Meyerson. "Identification of cancer-cytotoxic modulators of PDE3a by predictive chemogenomics." Nat. Chem. Biol. 12(2), 102-108, 2016.

37. Zhengjian Zhang, Zarko Boskovic, Mahmud M. Hussain, Wenxin Hu, Carla Inouye, Han-Je Kim, Anna K. Abole, Mary K. Doud, Timothy A. Lewis, Angela N. Koehler, Stuart L. Schreiber, Robert Tjian. "Chemical perturbation of an intrinsically disordered region of TFIID distinguishes two modes of transcription initiation." eLife. 10.7554/eLife.07777, 2015.

36. Andrew Chen, Angela N. Koehler. "Tying up a transcription factor - An engineered bivalent small molecule inhibits the activity of a rogue transcription factor in leukemia." Science. 347, 713-714, 2015.

35. Marius S. Pop, Dina Wassaf, Angela N. Koehler. "Probing small-molecule microarrays with tagged proteins in cell lysates." Curr. Prot. Chem. Biol. 6, 209-220, 2014.

34. Masoud Sadaghiani, Sang Min Lee, Justin I. Odegaard, Dennis B. Leveson-Gower, Olivia M. McPherson, Paul Novick, Mi Ri Kim, Angela N. Koehler, Robert Negrin, Ricardo E. Dolmetsch, Chan Young Park. "Identification of Orai1 channel inhibitors by using minimal functional domains to screen small molecule microarrays." Chem. Biol., 21, 1278-1292, 2014.

33. Marius S. Pop, Nicolas Stransky, Colin W. Garvie, Jean-Philippe Theurillat, Timothy A. Lewis, Cheng Zhong, Elizabeth K. Culyba, Fallon Lin, Doug S. Daniels, Raymond Pagliarini, Lucienne Ronco, Angela N. Koehler, Levi. A. Garraway. “A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein.” Mol. Cancer Ther., 6, 1492-1502, 2014.

32. Jiyoung A. Hong, Dylan V. Neel, Dina Wassaf, Francisco Caballero, Angela N. Koehler. “Recent discoveries and applications involving small-molecule microarrays.” Curr. Opin. Chem. Biol. 18, 21-28, 2014.

 

Broad Institute Fellow

31. 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.

30. 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.

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

28. 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.

27. 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.

26. 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.

25. 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.

24. 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.

23. 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.

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

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

20. 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.

19. 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.

18. 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.

17. 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.

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

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

14. 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.

13. 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.

12. 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.

11. 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.

10. 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.

9. 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.

8. 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.

7. 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.

6. 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.

 

Graduate and Undergraduate Work

5. 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.

4. 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.

3. 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.

2. 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.

1. 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.