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Angela N. Koehler, Ph.D. - Publications

Affiliations: 
2014- Biological Engineering Massachusetts Institute of Technology, Cambridge, MA, United States 
Area:
Chemical biology, Deregulated transcription in disease
Website:
https://koehler-lab.mit.edu
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54 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2020 Annand JR, Henderson AR, Cole KS, Maurais AJ, Becerra J, Liu Y, Weerapana E, Koehler AN, Mapp AK, Schindler CS. Gibberellin JRA-003: A Selective Inhibitor of Nuclear Translocation of IKKα. Acs Medicinal Chemistry Letters. 11: 1913-1918. PMID 33062173 DOI: 10.1021/Acsmedchemlett.9B00613  0.374
2020 Quinnell SP, Leifer BS, Nestor ST, Tan K, Sheehy DF, Ceo L, Doyle SK, Koehler AN, Vegas AJ. A Small-Molecule Inhibitor to the Cytokine Interleukin-4. Acs Chemical Biology. PMID 32902255 DOI: 10.1021/Acschembio.0C00615  0.736
2020 Chen A, Koehler AN. Transcription Factor Inhibition: Lessons Learned and Emerging Targets. Trends in Molecular Medicine. 26: 508-518. PMID 32359481 DOI: 10.1016/J.Molmed.2020.01.004  0.471
2019 Struntz NB, Chen A, Deutzmann A, Wilson RM, Stefan E, Evans HL, Ramirez MA, Liang T, Caballero F, Wildschut MHE, Neel DV, Freeman DB, Pop MS, McConkey M, Muller S, ... ... Koehler AN, et al. Stabilization of the Max Homodimer with a Small Molecule Attenuates Myc-Driven Transcription. Cell Chemical Biology. PMID 30880155 DOI: 10.1016/J.Chembiol.2019.02.009  0.72
2018 Leifer BS, Doyle SK, Richters A, Evans HL, Koehler AN. An Array-Based Ligand Discovery Platform for Proteins With Short Half-Lives. Methods in Enzymology. 610: 191-218. PMID 30390799 DOI: 10.1016/Bs.Mie.2018.09.019  0.816
2017 Richters A, Koehler AN. Epigenetic Modulation using Small Molecules - Targeting Histone Acetyltransferases in Disease. Current Medicinal Chemistry. PMID 28240169 DOI: 10.2174/0929867324666170223153115  0.748
2017 Evans HL, Doyle SK, Pop MS, Leifer B, Ziadkhanpour K, Koehler AN. Abstract 5221: Target engagement approaches to validate small-molecule binders of the pioneering transcription factor FOXA1 Cancer Research. 77: 5221-5221. DOI: 10.1158/1538-7445.Am2017-5221  0.426
2016 Wang Y, Wach JY, Sheehan P, Zhong C, Zhan C, Harris R, Almo SC, Bishop J, Haggarty SJ, Ramek A, Berry KN, O'Herin C, Koehler AN, Hung AW, Young DW. Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β. Acs Medicinal Chemistry Letters. 7: 852-6. PMID 27660690 DOI: 10.1021/Acsmedchemlett.6B00230  0.792
2016 Yang Z, Koehler AN, Wang L. A novel small molecule activator of nuclear receptor SHP inhibits HCC cell migration via suppressing Ccl2. Molecular Cancer Therapeutics. PMID 27486225 DOI: 10.1158/1535-7163.Mct-16-0153  0.456
2016 Boskovic ZV, Kemp MM, Freedy AM, Viswanathan VS, Pop MS, Fuller JH, Martinez NM, Figuero Lazu SO, Hong JA, Lewis TA, Calarese D, Love JD, Vetere A, Almo SC, Schreiber SL, ... Koehler AN, et al. Inhibition of zinc-dependent histone deacetylases with a chemically triggered electrophile. Acs Chemical Biology. PMID 27064299 DOI: 10.1021/Acschembio.6B00012  0.783
2016 Zhang Z, Boskovic Z, Hussain M, Hu W, Inouye C, Koehler A, Schreiber S, Tjian R. Chemical Perturbation of an Intrinsically Disordered Region of TFIID Distinguishes de novo Transcription Initiation from Reinitiation Biophysical Journal. 110: 557a. DOI: 10.1016/J.Bpj.2015.11.2980  0.776
2015 de Waal L, Lewis TA, Rees MG, Tsherniak A, Wu X, Choi PS, Gechijian L, Hartigan C, Faloon PW, Hickey MJ, Tolliday N, Carr SA, Clemons PA, Munoz B, Wagner BK, ... ... Koehler AN, et al. Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nature Chemical Biology. PMID 26656089 DOI: 10.1038/Nchembio.1984  0.81
2015 Doyle SK, Pop MS, Evans HL, Koehler AN. Advances in discovering small molecules to probe protein function in a systems context. Current Opinion in Chemical Biology. 30: 28-36. PMID 26615565 DOI: 10.1016/J.Cbpa.2015.10.032  0.781
2015 Zhang Z, Boskovic Z, Hussain MM, Hu W, Inouye C, Kim HJ, Abole AK, Doud MK, Lewis TA, Koehler AN, Schreiber SL, Tjian R. Chemical perturbation of an intrinsically disordered region of TFIID distinguishes two modes of transcription initiation. Elife. 4. PMID 26314865 DOI: 10.7554/Elife.07777  0.755
2015 Chen A, Koehler AN. Drug discovery. Tying up a transcription factor. Science (New York, N.Y.). 347: 713-4. PMID 25678644 DOI: 10.1126/Science.Aaa6119  0.478
2015 Zhang Z, Boskovic Z, Hussain MM, Hu W, Inouye C, Kim H, Abole AK, Doud MK, Lewis TA, Koehler AN, Schreiber SL, Tjian R. Author response: Chemical perturbation of an intrinsically disordered region of TFIID distinguishes two modes of transcription initiation Elife. DOI: 10.7554/Elife.07777.021  0.756
2015 Waal Ld, Lewis TA, Rees MG, Tsherniak A, Wu X, Choi PS, Gechijian L, Hartigan C, Faloon PW, Hickey MJ, Tolliday N, Carr SA, Clemons PA, Munoz B, Wagner BK, ... ... Koehler AN, et al. Abstract C136: Identification of selective cancer cytotoxic modulators of phosphodiesterase 3a by predictive chemogenomics Molecular Cancer Therapeutics. 14. DOI: 10.1158/1535-7163.Targ-15-C136  0.8
2014 Pop MS, Wassaf D, Koehler AN. Probing small-molecule microarrays with tagged proteins in cell lysates. Current Protocols in Chemical Biology. 6: 209-20. PMID 25445177 DOI: 10.1002/9780470559277.Ch140101  0.786
2014 Sadaghiani AM, Lee SM, Odegaard JI, Leveson-Gower DB, McPherson OM, Novick P, Kim MR, Koehler AN, Negrin R, Dolmetsch RE, Park CY. Identification of Orai1 channel inhibitors by using minimal functional domains to screen small molecule microarrays. Chemistry & Biology. 21: 1278-92. PMID 25308275 DOI: 10.1016/J.Chembiol.2014.08.016  0.384
2014 Pop MS, Stransky N, Garvie CW, Theurillat JP, Hartman EC, Lewis TA, Zhong C, Culyba EK, Lin F, Daniels DS, Pagliarini R, Ronco L, Koehler AN, Garraway LA. A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein. Molecular Cancer Therapeutics. 13: 1492-502. PMID 24737027 DOI: 10.1158/1535-7163.Mct-13-0689  0.814
2014 Hong JA, Neel DV, Wassaf D, Caballero F, Koehler AN. Recent discoveries and applications involving small-molecule microarrays. Current Opinion in Chemical Biology. 18: 21-8. PMID 24534749 DOI: 10.1016/J.Cbpa.2013.09.020  0.788
2014 Waal LMd, Lewis TA, Gechijian L, Tsherniak A, Youngsaye W, Rees M, Mikse O, Hickey M, Faloon P, Tolliday N, Koehler A, Schenone M, Wong K, Shamji A, Munoz B, et al. Abstract 4596: An integrated genomic characterization of the target of a small molecule identifies a novel cancer dependency Cancer Research. 74: 4596-4596. DOI: 10.1158/1538-7445.Am2014-4596  0.761
2014 Pop M, Stransky N, Garvie C, Theurillat J, Lewis T, Zhong C, Culyba E, Lin F, Daniels D, Pagliarini R, Ronco L, Koehler A, Garraway L. Abstract 2519: A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein Cancer Research. 74: 2519-2519. DOI: 10.1158/1538-7445.Am2014-2519  0.79
2012 Cherny I, Korolev M, Koehler AN, Hecht MH. Proteins from an unevolved library of de novo designed sequences bind a range of small molecules. Acs Synthetic Biology. 1: 130-8. PMID 23651114 DOI: 10.1021/Sb200018E  0.477
2012 Kemp MM, Weïwer M, Koehler AN. Unbiased binding assays for discovering small-molecule probes and drugs. Bioorganic & Medicinal Chemistry. 20: 1979-89. PMID 22230199 DOI: 10.1016/J.Bmc.2011.11.071  0.736
2012 Casalena DE, Wassaf D, Koehler AN. Ligand discovery using small-molecule microarrays. Methods in Molecular Biology (Clifton, N.J.). 803: 249-63. PMID 22065230 DOI: 10.1007/978-1-61779-364-6_17  0.519
2011 Kemp MM, Wang Q, Fuller JH, West N, Martinez NM, Morse EM, Weïwer M, Schreiber SL, Bradner JE, Koehler AN. A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. Bioorganic & Medicinal Chemistry Letters. 21: 4164-9. PMID 21696956 DOI: 10.1016/J.Bmcl.2011.05.098  0.819
2011 Clemons PA, Wilson JA, Dan?ík V, Muller S, Carrinski HA, Wagner BK, Koehler AN, Schreiber SL. Quantifying structure and performance diversity for sets of small molecules comprising small-molecule screening collections. Proceedings of the National Academy of Sciences of the United States of America. 108: 6817-22. PMID 21482810 DOI: 10.1073/Pnas.1015024108  0.785
2011 Kang MS, Lee EK, Soni V, Lewis TA, Koehler AN, Srinivasan V, Kieff E. Roscovitine inhibits EBNA1 serine 393 phosphorylation, nuclear localization, transcription, and episome maintenance. Journal of Virology. 85: 2859-68. PMID 21209116 DOI: 10.1128/Jvi.01628-10  0.357
2010 Chen J, Armstrong AH, Koehler AN, Hecht MH. Small molecule microarrays enable the discovery of compounds that bind the Alzheimer's Aβ peptide and reduce its cytotoxicity. Journal of the American Chemical Society. 132: 17015-22. PMID 21062056 DOI: 10.1021/Ja107552S  0.477
2010 Clemons PA, Bodycombe NE, Carrinski HA, Wilson JA, Shamji AF, Wagner BK, Koehler AN, Schreiber SL. Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles. Proceedings of the National Academy of Sciences of the United States of America. 107: 18787-92. PMID 20956335 DOI: 10.1073/Pnas.1012741107  0.826
2010 Vegas AJ, Koehler AN. Detecting protein-small molecule interactions using fluorous small-molecule microarrays. Methods in Molecular Biology (Clifton, N.J.). 669: 43-55. PMID 20857356 DOI: 10.1007/978-1-60761-845-4_4  0.772
2010 Schreiber SL, Shamji AF, Clemons PA, Hon C, Koehler AN, Munoz B, Palmer M, Stern AM, Wagner BK, Powers S, Lowe SW, Guo X, Krasnitz A, Sawey ET, et al. Towards patient-based cancer therapeutics. Nature Biotechnology. 28: 904-6. PMID 20829823 DOI: 10.1038/Nbt0910-904  0.785
2010 Koehler AN. A complex task? Direct modulation of transcription factors with small molecules. Current Opinion in Chemical Biology. 14: 331-40. PMID 20395165 DOI: 10.1016/J.Cbpa.2010.03.022  0.495
2010 Tassa C, Duffner JL, Lewis TA, Weissleder R, Schreiber SL, Koehler AN, Shaw SY. Binding affinity and kinetic analysis of targeted small molecule-modified nanoparticles. Bioconjugate Chemistry. 21: 14-9. PMID 20028085 DOI: 10.1021/Bc900438A  0.496
2010 Pop M, Doug K, Bradner J, Koehler A, Garraway L. Abstract 3693: Small molecule microarray screens for inhibitors of oncogenic ETS factors Cancer Research. 70: 3693-3693. DOI: 10.1158/1538-7445.Am10-3693  0.82
2009 Mao Y, Ge X, Frank CL, Madison JM, Koehler AN, Doud MK, Tassa C, Berry EM, Soda T, Singh KK, Biechele T, Petryshen TL, Moon RT, Haggarty SJ, Tsai LH. Disrupted in schizophrenia 1 regulates neuronal progenitor proliferation via modulation of GSK3beta/beta-catenin signaling. Cell. 136: 1017-31. PMID 19303846 DOI: 10.1016/J.Cell.2008.12.044  0.751
2009 Ong SE, Schenone M, Margolin AA, Li X, Do K, Doud MK, Mani DR, Kuai L, Wang X, Wood JL, Tolliday NJ, Koehler AN, Marcaurelle LA, Golub TR, Gould RJ, et al. Identifying the proteins to which small-molecule probes and drugs bind in cells. Proceedings of the National Academy of Sciences of the United States of America. 106: 4617-22. PMID 19255428 DOI: 10.1073/Pnas.0900191106  0.825
2009 Stanton BZ, Peng LF, Maloof N, Nakai K, Wang X, Duffner JL, Taveras KM, Hyman JM, Lee SW, Koehler AN, Chen JK, Fox JL, Mandinova A, Schreiber SL. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nature Chemical Biology. 5: 154-6. PMID 19151731 DOI: 10.1038/Nchembio.142  0.689
2008 Vegas AJ, Fuller JH, Koehler AN. Small-molecule microarrays as tools in ligand discovery. Chemical Society Reviews. 37: 1385-94. PMID 18568164 DOI: 10.1039/B703568N  0.779
2007 Vegas AJ, Bradner JE, Tang W, McPherson OM, Greenberg EF, Koehler AN, Schreiber SL. Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors. Angewandte Chemie (International Ed. in English). 46: 7960-4. PMID 17868168 DOI: 10.1002/Anie.200703198  0.817
2007 Schmitz K, Haggarty SJ, McPherson OM, Clardy J, Koehler AN. Detecting binding interactions using microarrays of natural product extracts. Journal of the American Chemical Society. 129: 11346-7. PMID 17718493 DOI: 10.1021/Ja073965S  0.653
2007 Miao H, Tallarico JA, Hayakawa H, Münger K, Duffner JL, Koehler AN, Schreiber SL, Lewis TA. Ring-opening and ring-closing reactions of a shikimic acid-derived substrate leading to diverse small molecules. Journal of Combinatorial Chemistry. 9: 245-53. PMID 17348730 DOI: 10.1021/Cc060135M  0.547
2007 Duffner JL, Clemons PA, Koehler AN. A pipeline for ligand discovery using small-molecule microarrays. Current Opinion in Chemical Biology. 11: 74-82. PMID 17169601 DOI: 10.1016/J.Cbpa.2006.11.031  0.688
2006 Bradner JE, McPherson OM, Koehler AN. A method for the covalent capture and screening of diverse small molecules in a microarray format. Nature Protocols. 1: 2344-52. PMID 17406478 DOI: 10.1038/Nprot.2006.282  0.624
2006 Tolliday N, Clemons PA, Ferraiolo P, Koehler AN, Lewis TA, Li X, Schreiber SL, Gerhard DS, Eliasof S. Small molecules, big players: the National Cancer Institute's Initiative for Chemical Genetics. Cancer Research. 66: 8935-42. PMID 16982730 DOI: 10.1158/0008-5472.Can-06-2552  0.693
2006 Bradner JE, McPherson OM, Mazitschek R, Barnes-Seeman D, Shen JP, Dhaliwal J, Stevenson KE, Duffner JL, Park SB, Neuberg DS, Nghiem P, Schreiber SL, Koehler AN. A robust small-molecule microarray platform for screening cell lysates. Chemistry & Biology. 13: 493-504. PMID 16720270 DOI: 10.1016/J.Chembiol.2006.03.004  0.779
2004 Bradner J, Kim Y, Koehler A, Kawasumi M, Li X, Schreiber SL, Nghiem P. Identification and Characterization of Novel Small-Molecule Inhibitors of the Replication Checkpoint. Blood. 104: 763-763. DOI: 10.1182/Blood.V104.11.763.763  0.73
2003 Koehler AN, Shamji AF, Schreiber SL. Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis. Journal of the American Chemical Society. 125: 8420-1. PMID 12848532 DOI: 10.1021/Ja0352698  0.768
2003 Barnes-Seeman D, Park SB, Koehler AN, Schreiber SL. Expanding the functional group compatibility of small-molecule microarrays: discovery of novel calmodulin ligands. Angewandte Chemie (International Ed. in English). 42: 2376-9. PMID 12783500 DOI: 10.1002/Anie.200351043  0.534
2003 Barnes-Seeman D, Park SB, Koehler AN, Schreiber SL. Cover Picture: Expanding the Functional Group Compatibility of Small-Molecule Microarrays: Discovery of Novel Calmodulin Ligands (Angew. Chem. Int. Ed. 21/2003) Angewandte Chemie International Edition. 42: 2319-2319. DOI: 10.1002/Anie.200390464  0.536
2003 Barnes-Seeman D, Park SB, Koehler AN, Schreiber SL. Titelbild: Expanding the Functional Group Compatibility of Small-Molecule Microarrays: Discovery of Novel Calmodulin Ligands (Angew. Chem. 21/2003) Angewandte Chemie. 115: 2421-2421. DOI: 10.1002/Ange.200390491  0.535
2001 Clemons PA, Koehler AN, Wagner BK, Sprigings TG, Spring DR, King RW, Schreiber SL, Foley MA. A one-bead, one-stock solution approach to chemical genetics: part 2. Chemistry & Biology. 8: 1183-95. PMID 11755397 DOI: 10.1016/S1074-5521(01)00086-2  0.8
1999 Glasfeld A, Koehler AN, Schumacher MA, Brennan RG. The role of lysine 55 in determining the specificity of the purine repressor for its operators through minor groove interactions. Journal of Molecular Biology. 291: 347-61. PMID 10438625 DOI: 10.1006/Jmbi.1999.2946  0.698
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