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Items: 1 to 50 of 52

1.

Stabilization of the Max Homodimer with a Small Molecule Attenuates Myc-Driven Transcription.

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, Curtin BH, Tseng H, Frombach KR, Butty VL, Levine SS, Feau C, Elmiligy S, Hong JA, Lewis TA, Vetere A, Clemons PA, Malstrom SE, Ebert BL, Lin CY, Felsher DW, Koehler AN.

Cell Chem Biol. 2019 May 16;26(5):711-723.e14. doi: 10.1016/j.chembiol.2019.02.009. Epub 2019 Mar 14.

PMID:
30880155
2.

An Array-Based Ligand Discovery Platform for Proteins With Short Half-Lives.

Leifer BS, Doyle SK, Richters A, Evans HL, Koehler AN.

Methods Enzymol. 2018;610:191-218. doi: 10.1016/bs.mie.2018.09.019. Epub 2018 Oct 19.

PMID:
30390799
3.

Epigenetic Modulation Using Small Molecules - Targeting Histone Acetyltransferases in Disease.

Richters A, Koehler AN.

Curr Med Chem. 2017;24(37):4121-4150. doi: 10.2174/0929867324666170223153115.

PMID:
28240169
4.

Activity of caffeic acid phenethyl ester in Caenorhabditis elegans.

Coleman JJ, Komura T, Munro J, Wu MP, Busanelli RR, Koehler AN, Thomas M, Wagner FF, Holson EB, Mylonakis E.

Future Med Chem. 2016 Nov;8(17):2033-2046. doi: 10.4155/fmc-2016-0085. Epub 2016 Oct 14.

5.

Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β.

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.

ACS Med Chem Lett. 2016 Jul 14;7(9):852-6. doi: 10.1021/acsmedchemlett.6b00230. eCollection 2016 Sep 8.

6.

A Novel Small Molecule Activator of Nuclear Receptor SHP Inhibits HCC Cell Migration via Suppressing Ccl2.

Yang Z, Koehler AN, Wang L.

Mol Cancer Ther. 2016 Oct;15(10):2294-2301. Epub 2016 Aug 2.

7.

Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.

Boskovic ZV, Kemp MM, Freedy AM, Viswanathan VS, Pop MS, Fuller JH, Martinez NM, Figueroa Lazú SO, Hong JA, Lewis TA, Calarese D, Love JD, Vetere A, Almo SC, Schreiber SL, Koehler AN.

ACS Chem Biol. 2016 Jul 15;11(7):1844-51. doi: 10.1021/acschembio.6b00012. Epub 2016 Apr 29.

PMID:
27064299
8.

Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics.

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, Shamji AF, Koehler AN, Schenone M, Burgin AB, Schreiber SL, Greulich H, Meyerson M.

Nat Chem Biol. 2016 Feb;12(2):102-8. doi: 10.1038/nchembio.1984. Epub 2015 Dec 14.

9.

Advances in discovering small molecules to probe protein function in a systems context.

Doyle SK, Pop MS, Evans HL, Koehler AN.

Curr Opin Chem Biol. 2016 Feb;30:28-36. doi: 10.1016/j.cbpa.2015.10.032. Epub 2015 Nov 23. Review.

10.

Chemical perturbation of an intrinsically disordered region of TFIID distinguishes two modes of transcription initiation.

Zhang Z, Boskovic Z, Hussain MM, Hu W, Inouye C, Kim HJ, Abole AK, Doud MK, Lewis TA, Koehler AN, Schreiber SL, Tjian R.

Elife. 2015 Aug 28;4. doi: 10.7554/eLife.07777.

11.

Drug discovery. Tying up a transcription factor.

Chen A, Koehler AN.

Science. 2015 Feb 13;347(6223):713-4. doi: 10.1126/science.aaa6119. No abstract available.

PMID:
25678644
12.

Probing small-molecule microarrays with tagged proteins in cell lysates.

Pop MS, Wassaf D, Koehler AN.

Curr Protoc Chem Biol. 2014 Dec 1;6(4):209-20. doi: 10.1002/9780470559277.ch140101.

13.

Identification of Orai1 channel inhibitors by using minimal functional domains to screen small molecule microarrays.

Sadaghiani AM, Lee SM, Odegaard JI, Leveson-Gower DB, McPherson OM, Novick P, Kim MR, Koehler AN, Negrin R, Dolmetsch RE, Park CY.

Chem Biol. 2014 Oct 23;21(10):1278-1292. doi: 10.1016/j.chembiol.2014.08.016. Epub 2014 Oct 9.

14.

A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein.

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.

Mol Cancer Ther. 2014 Jun;13(6):1492-502. doi: 10.1158/1535-7163.MCT-13-0689. Epub 2014 Apr 15.

15.

Recent discoveries and applications involving small-molecule microarrays.

Hong JA, Neel DV, Wassaf D, Caballero F, Koehler AN.

Curr Opin Chem Biol. 2014 Feb;18:21-8. doi: 10.1016/j.cbpa.2013.09.020. Epub 2013 Nov 27. Review.

16.

Proteins from an unevolved library of de novo designed sequences bind a range of small molecules.

Cherny I, Korolev M, Koehler AN, Hecht MH.

ACS Synth Biol. 2012 Apr 20;1(4):130-8. doi: 10.1021/sb200018e. Epub 2012 Apr 2.

17.

Unbiased binding assays for discovering small-molecule probes and drugs.

Kemp MM, Weïwer M, Koehler AN.

Bioorg Med Chem. 2012 Mar 15;20(6):1979-89. doi: 10.1016/j.bmc.2011.11.071. Epub 2011 Dec 24. Review.

PMID:
22230199
18.

Ligand discovery using small-molecule microarrays.

Casalena DE, Wassaf D, Koehler AN.

Methods Mol Biol. 2012;803:249-63. doi: 10.1007/978-1-61779-364-6_17.

PMID:
22065230
19.

A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.

Kemp MM, Wang Q, Fuller JH, West N, Martinez NM, Morse EM, Weïwer M, Schreiber SL, Bradner JE, Koehler AN.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4164-9. doi: 10.1016/j.bmcl.2011.05.098. Epub 2011 Jun 2.

20.

Quantifying structure and performance diversity for sets of small molecules comprising small-molecule screening collections.

Clemons PA, Wilson JA, Dančík V, Muller S, Carrinski HA, Wagner BK, Koehler AN, Schreiber SL.

Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6817-22. doi: 10.1073/pnas.1015024108. Epub 2011 Apr 11.

21.

Roscovitine inhibits EBNA1 serine 393 phosphorylation, nuclear localization, transcription, and episome maintenance.

Kang MS, Lee EK, Soni V, Lewis TA, Koehler AN, Srinivasan V, Kieff E.

J Virol. 2011 Mar;85(6):2859-68. doi: 10.1128/JVI.01628-10. Epub 2011 Jan 5.

22.

Small molecule microarrays enable the discovery of compounds that bind the Alzheimer's Aβ peptide and reduce its cytotoxicity.

Chen J, Armstrong AH, Koehler AN, Hecht MH.

J Am Chem Soc. 2010 Dec 1;132(47):17015-22. doi: 10.1021/ja107552s. Epub 2010 Nov 9.

23.

Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles.

Clemons PA, Bodycombe NE, Carrinski HA, Wilson JA, Shamji AF, Wagner BK, Koehler AN, Schreiber SL.

Proc Natl Acad Sci U S A. 2010 Nov 2;107(44):18787-92. doi: 10.1073/pnas.1012741107. Epub 2010 Oct 18.

24.

Detecting protein-small molecule interactions using fluorous small-molecule microarrays.

Vegas AJ, Koehler AN.

Methods Mol Biol. 2010;669:43-55. doi: 10.1007/978-1-60761-845-4_4.

PMID:
20857356
25.

Towards patient-based cancer therapeutics.

Cancer Target Discovery and Development Network, 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, Sordella R, Stein L, Trotman LC, Califano A, Dalla-Favera R, Ferrando A, Iavarone A, Pasqualucci L, Silva J, Stockwell BR, Hahn WC, Chin L, DePinho RA, Boehm JS, Gopal S, Huang A, Root DE, Weir BA, Gerhard DS, Zenklusen JC, Roth MG, White MA, Minna JD, MacMillan JB, Posner BA.

Nat Biotechnol. 2010 Sep;28(9):904-6. doi: 10.1038/nbt0910-904. No abstract available.

26.

A complex task? Direct modulation of transcription factors with small molecules.

Koehler AN.

Curr Opin Chem Biol. 2010 Jun;14(3):331-40. doi: 10.1016/j.cbpa.2010.03.022. Epub 2010 Apr 13. Review.

27.

Binding affinity and kinetic analysis of targeted small molecule-modified nanoparticles.

Tassa C, Duffner JL, Lewis TA, Weissleder R, Schreiber SL, Koehler AN, Shaw SY.

Bioconjug Chem. 2010 Jan;21(1):14-9. doi: 10.1021/bc900438a.

28.

Disrupted in schizophrenia 1 regulates neuronal progenitor proliferation via modulation of GSK3beta/beta-catenin signaling.

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.

Cell. 2009 Mar 20;136(6):1017-31. doi: 10.1016/j.cell.2008.12.044.

29.

Identifying the proteins to which small-molecule probes and drugs bind in cells.

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, Schreiber SL, Carr SA.

Proc Natl Acad Sci U S A. 2009 Mar 24;106(12):4617-22. doi: 10.1073/pnas.0900191106. Epub 2009 Mar 2.

30.

A small molecule that binds Hedgehog and blocks its signaling in human cells.

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.

Nat Chem Biol. 2009 Mar;5(3):154-6. doi: 10.1038/nchembio.142. Epub 2009 Jan 18.

31.

Small-molecule microarrays as tools in ligand discovery.

Vegas AJ, Fuller JH, Koehler AN.

Chem Soc Rev. 2008 Jul;37(7):1385-94. doi: 10.1039/b703568n. Epub 2008 May 20. Review.

32.

Identification of the molecular target of small molecule inhibitors of HDL receptor SR-BI activity.

Nieland TJ, Shaw JT, Jaipuri FA, Duffner JL, Koehler AN, Banakos S, Zannis VI, Kirchhausen T, Krieger M.

Biochemistry. 2008 Jan 8;47(1):460-72. Epub 2007 Dec 8.

33.

Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors.

Vegas AJ, Bradner JE, Tang W, McPherson OM, Greenberg EF, Koehler AN, Schreiber SL.

Angew Chem Int Ed Engl. 2007;46(42):7960-4. No abstract available.

34.

Detecting binding interactions using microarrays of natural product extracts.

Schmitz K, Haggarty SJ, McPherson OM, Clardy J, Koehler AN.

J Am Chem Soc. 2007 Sep 19;129(37):11346-7. Epub 2007 Aug 24. No abstract available.

PMID:
17718493
35.

Influence of HDL-cholesterol-elevating drugs on the in vitro activity of the HDL receptor SR-BI.

Nieland TJ, Shaw JT, Jaipuri FA, Maliga Z, Duffner JL, Koehler AN, Krieger M.

J Lipid Res. 2007 Aug;48(8):1832-45. Epub 2007 May 28.

36.

A method for the covalent capture and screening of diverse small molecules in a microarray format.

Bradner JE, McPherson OM, Koehler AN.

Nat Protoc. 2006;1(5):2344-52.

PMID:
17406478
37.

Ring-opening and ring-closing reactions of a shikimic acid-derived substrate leading to diverse small molecules.

Miao H, Tallarico JA, Hayakawa H, Münger K, Duffner JL, Koehler AN, Schreiber SL, Lewis TA.

J Comb Chem. 2007 Mar-Apr;9(2):245-53.

PMID:
17348730
38.

A pipeline for ligand discovery using small-molecule microarrays.

Duffner JL, Clemons PA, Koehler AN.

Curr Opin Chem Biol. 2007 Feb;11(1):74-82. Epub 2006 Dec 13. Review.

PMID:
17169601
39.

Small molecules, big players: the National Cancer Institute's Initiative for Chemical Genetics.

Tolliday N, Clemons PA, Ferraiolo P, Koehler AN, Lewis TA, Li X, Schreiber SL, Gerhard DS, Eliasof S.

Cancer Res. 2006 Sep 15;66(18):8935-42.

40.

A robust small-molecule microarray platform for screening cell lysates.

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.

Chem Biol. 2006 May;13(5):493-504.

41.

Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis.

Koehler AN, Shamji AF, Schreiber SL.

J Am Chem Soc. 2003 Jul 16;125(28):8420-1.

PMID:
12848532
42.

Expanding the functional group compatibility of small-molecule microarrays: discovery of novel calmodulin ligands.

Barnes-Seeman D, Park SB, Koehler AN, Schreiber SL.

Angew Chem Int Ed Engl. 2003 May 30;42(21):2376-9. No abstract available.

PMID:
12783500
43.

A one-bead, one-stock solution approach to chemical genetics: part 2.

Clemons PA, Koehler AN, Wagner BK, Sprigings TG, Spring DR, King RW, Schreiber SL, Foley MA.

Chem Biol. 2001 Dec;8(12):1183-95.

44.

The ketogenic diet in refractory epilepsy: the experience of Children's Hospital of Pittsburgh.

Katyal NG, Koehler AN, McGhee B, Foley CM, Crumrine PK.

Clin Pediatr (Phila). 2000 Mar;39(3):153-9.

PMID:
10752008
45.

Coordinated interdisciplinary management of pediatric intestinal failure: a 2-year review.

Koehler AN, Yaworski JA, Gardner M, Kocoshis S, Reyes J, Barksdale EM Jr.

J Pediatr Surg. 2000 Feb;35(2):380-5.

PMID:
10693701
46.

The role of lysine 55 in determining the specificity of the purine repressor for its operators through minor groove interactions.

Glasfeld A, Koehler AN, Schumacher MA, Brennan RG.

J Mol Biol. 1999 Aug 13;291(2):347-61.

PMID:
10438625
47.

Insulinlike growth factor 1 and insulinlike growth factor 3: indices of intestinal failure in children.

Barksdale EM Jr, Koehler AN, Yaworski JA, Gardner M, Reyes J.

J Pediatr Surg. 1999 May;34(5):655-61; discussion 661-2.

PMID:
10359158
48.

Nutrition and pulmonary function predictors of delayed puberty in adolescent males with cystic fibrosis.

Boas SR, Fulton JA, Koehler AN, Orenstein DM.

Clin Pediatr (Phila). 1998 Sep;37(9):573-6. No abstract available.

PMID:
9773243
49.

Association of retinol binding protein in multiple-case families with insulin-dependent diabetes.

Krill D, O'Leary L, Koehler AN, Kramer MK, Warty V, Wagner MA, Dorman JS.

Hum Biol. 1997 Feb;69(1):89-96.

PMID:
9037897
50.

Molecular epidemiology of autoimmune thyroid disease.

Dorman J, Kramer MK, O'Lear LA, Burke JP, McCanlies E, McCarthy BJ, Trucco M, Swan JS, Steenkiste AR, Koehler AN, Foley TP.

Gac Med Mex. 1997;133 Suppl 1:97-103.

PMID:
9504111

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