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Items: 1 to 20 of 52


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.

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