Selected DARTS Publications


--DARTS method development--

Lomenick B, Hao R, Jonai N, Chin RM, Aghajan M, Warburton S, Wang J, Wu RP, Gomez F, Loo JA, Wohlschlegel J, Vondriska M, Pelletier J, Herschman HR, Clardy J, Clarke CF, and Huang J (2009) Target identification using drug affinity responsive target stability (DARTS). Proc Natl Acad Sci USA 106, 21984-21989. PDF

Lomenick B, Olsen RW, and Huang J (2011) Identification of direct protein targets of small molecules. ACS Chemical Biology 6, 34-46. PDF

Lomenick B, Jung G, Wohlschlegel JA, Huang J (2011) Target identification using drug affinity responsive target stability (DARTS). Current Protocols in Chemical Biology 3, 163-180. PDF

Huang J (2013) Tracking Drugs. New England Journal of Medicine 369, 1168-1169. PDF

Pai MY, Lomenick B, Hwang H, Schiestl R, McBride W, Loo JA, Huang J (2015) Drug affinity responsive target stability (DARTS) for small-molecule target identification. Methods in Molecular Biology 1263, 287-98. PDF

--Applications of DARTS--

Chin RM, Fu X, Pai MY, Vergnes L, Hwang H, Deng G, Diep S, Lomenick B, Meli VS, Monsalve GC, Hu E, Whelan SA, Wang JX, Jung G, Solis GM, Fazlollahi F, Kaweeteerawat C, Quach A, Nili M, Krall AS, Godwin HA, Chang HR, Faull KF, Guo F, Jiang M, Trauger SA, Saghatelian A, Braas D, Christofk HR, Clarke CF, Teitell MA, Petrascheck M, Reue K, Jung ME, Frand AR, Huang J (2014) The metabolite alpha-ketoglutarate extends lifespan by inhibiting ATP synthase and TOR. Nature 510, 397-401. PDF

Fu X, Chin RM, Vergnes L, Hwang H, Deng G, Xing Y, Pai MY, Li S, Ta L, Fazlollahi F, Chen C, Prins RM, Teitell MA, Nathanson DA, Lai A, Faull KF, Jiang M, Clarke SG, Cloughesy TF, Graeber TG, Braas D, Christofk HR, Jung ME, Reue K, Huang J (2015) 2-Hydroxyglutarate inhibits ATP synthase and mTOR signaling. Cell Metabolism 22, 508-515. PDF

Benjamin D, Colombi M, Hindupur SK, Betz C, Lane HA, El-Shemerly MYM, Lu M, Quagliata L, Terracciano L, Moes S, Sharpe T, Wodnar-Filipowicz A, Moroni C, Hall MN (2016) Syrosingopine sensitizes cancer cells to killing by metformin. Science Advances 2, e1601756. PDF

Qu Y, Gharbi N, Yuan X, Olsen JR, Blicher P, Dalhus B, Brokstad KA, Lin B, Øyan AM, Zhang W, Kalland KH, Ke X (2016) Axitinib blocks Wnt/beta-catenin signaling and directs asymmetric cell division in cancer. Proc Natl Acad Sci USA 113, 9339-9344. PDF

Jiang B, Zhang J, Xia J, Zhao W, Wu Y, Shi M, Luo L, Zhou H, Chen A, Ma H, Zhao Q, Suleman M, Lin F, Zhou L, Wang J, Zhang Y, He Y, Li X, Hung LM, Mak TW, Li Q (2017) IDH1 Mutation Promotes Tumorigenesis by Inhibiting JNK Activation and Apoptosis Induced by Serum Starvation. Cell Reports 19, 389-400. PDF

Aghajan M, Jonai N, Flick K, Fu F, Luo M, Cai X, Ouni I, Pierce N, Tang X, Lomenick B, Damoiseaux R, Hao R, del Moral PM, Verma R, Li Y, Li C, Houk KN, Jung ME, Zheng N, Huang L, Deshaies RJ, Kaiser P, Huang J (2010) Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase. Nature Biotechnology 28, 682-684. PDF

Robinson T, Pai M, Liu JC, Vizeacoumar F, Sun T, Egan SE, Datti A, Huang J, Zacksenhaus E (2013) High-throughput screen identifies disulfiram as a potential therapeutic for triple-negative breast cancer cells: Interaction with IQ motif-containing factors. Cell Cycle 12, 3013-3024. PDF

Gao S, Wang Q, Wang G, Lomenick B, Liu J, Fan CW, Deng LW, Huang J, Lum L, and Chen C (2012) The Chemistry and Biology of Nakiterpiosin - C-nor-D-Homosteroids. Synlett 16, 2298-2310. PDF

Park YD, Sun W, Salas A, Antia A, Carvajal C, Wang A, Xu X, Meng Z, Zhou M, Tawa GJ, Dehdashti J, Zheng W, Henderson CM, Zelazny AM, Williamson PR (2016) Identification of multiple cryptococcal fungicidal drug targets by combined gene dosing and drug affinity responsive target stability screening. Mbio 7, e01073-16. PDF

Gao W, Kim JY, Anderson JR, Akopian T, Hong S, Jin YY, Kandror O, Kim JW, Lee IA, Lee SY, McAlpine JB, Mulugeta S, Sunoqrot S, Wang Y, Yang SH, Yoon TM, Goldberg AL, Pauli GF, Suh JW, Franzblau SG, Cho S (2015) The cyclic peptide ecumicin targeting ClpC1 is active against Mycobacterium tuberculosis in vivo. Antimicrobial Agents and Chemotherapy 59, 880-889. PDF

Xiao M, Wang J, Lin Z, Lu Y, Li Z, White SW, Miller DD, Li W (2015) Design, synthesis and structure-activity relationship studies of novel survivin inhibitors with potent anti-proliferative properties. PLOS One 10, e0129807. PDF

Kost GC, Yang MY, Li L, Zhang Y, Liu C, Kim DJ, Ahn C, Lee YB, Liu Z (2015) A Novel Anti-Cancer Agent, 1-(3,5-Dimethoxyphenyl)-4-[(6-Fluoro-2-Methoxyquinoxalin-3-yl)Aminocarbonyl] Piperazine (RX-5902), interferes with beta-catenin function through Y593 phospho-p68 RNA helicase. Journal of Cellular Biochemistry 116, 1595-1601. PDF

Wang N, Wang Z, Peng C, You J, Shen J, Han S, Chen J (2014) Dietary compound isoliquiritigenin targets GRP78 to chemosensitize breast cancer stem cells via beta-catenin/ABCG2 signaling. Carcinogenesis 35, 2544-2554. PDF

Tohda C, Urano T, Umezaki M, Nemere I & Kuboyama T (2012) Diosgenin is an exogenous activator of 1,25D(3)-MARRS/Pdia3/ERp57 and improves Alzheimer's disease pathologies in 5XFAD mice. Scientific Reports 2, doi:10.1038/srep00535. PDF

Chen T, Ozel D, Qiao Y, Harbinski F, Chen L, Denoyelle S, He X, Zvereva N, Supko JG, Chorev M, Halperin JA, Aktas BH (2011) Chemical genetics identify eIF2α kinase heme-regulated inhibitor as an anticancer target. Nature Chemical Biology 7, 610-616. PDF