Open Access Chemical Probes for Epigenetic Targets

References

• Holliday R . Epigenetics: a historical overview. Epigenetics1 (2), 76–80 (2006).
   PubMed Web of Science ®Google Scholar
• Wongtrakoongate P . Epigenetic therapy of cancer stem and progenitor cells by targeting DNA methylation machineries. World J. Stem Cells7 (1), 137–148 (2015).
   PubMed Web of Science ®Google Scholar
• Lin S , GregoryRI. MicroRNA biogenesis pathways in cancer. Nat. Rev. Cancer15 (6), 321–333 (2015).
   PubMed Web of Science ®Google Scholar
• Devaux Y , ZangrandoJ, SchroenBet al. Long noncoding RNAs in cardiac development and ageing. Nat. Rev. Cardiol. doi:10.1038/nrcardio.2015.55 (2015) ( Epub ahead of print).
   PubMed Web of Science ®Google Scholar
• Velagapudi SP , VummidiBR, DisneyMD. Small molecule chemical probes of microRNA function. Curr. Opin. Chem. Biol.24, 97–103 (2015).
   PubMed Web of Science ®Google Scholar
• Tessarz P , KouzaridesT. Histone core modifications regulating nucleosome structure and dynamics. Nat. Rev. Mol. Cell Biol.15 (11), 703–708 (2014).
   PubMed Web of Science ®Google Scholar
• Muller S , BrownPJ. Epigenetic chemical probes. Clin. Pharmacol. Ther.92 (6), 689–693 (2012).
   PubMed Web of Science ®Google Scholar
• Zwergel C , ValenteS, JacobC, MaiA. Emerging approaches for histone deacetylase inhibitor drug discovery. Expert Opin. Drug Discov.10 (6), 599–613 (2015).
   PubMed Web of Science ®Google Scholar
• Castronovo V , PeixotoP, BellahceneA, TurtoiA. Histone deacetylases and cancer-associated angiogenesis: current understanding of the biology and clinical perspectives. Crit. Rev. Oncog.20 (1–2), 119–137 (2015).
   PubMedGoogle Scholar
• Filippakopoulos P , PicaudS, MangosMet al. Histone recognition and large-scale structural analysis of the human bromodomain family. Cell149 (1), 214–231 (2012).
   PubMed Web of Science ®Google Scholar
• Filippakopoulos P , KnappS. Targeting bromodomains: epigenetic readers of lysine acetylation. Nat. Rev. Drug Discov.13 (5), 337–356 (2014).
   PubMed Web of Science ®Google Scholar
• Weiss WA , TaylorSS, ShokatKM. Recognizing and exploiting differences between RNAi and small-molecule inhibitors. Nat. Chem. Biol.3 (12), 739–744 (2007).
   PubMed Web of Science ®Google Scholar
• Frye SV . The art of the chemical probe. Nat. Chem. Biol.6 (3), 159–161 (2010).
   PubMed Web of Science ®Google Scholar
• Workman P , CollinsI. Probing the probes: fitness factors for small molecule tools. Chem. Biol.17 (6), 561–577 (2010).
   PubMedGoogle Scholar
• Bunnage ME . Getting pharmaceutical R&D back on target. Nat. Chem. Biol.7 (6), 335–339 (2011).
   PubMed Web of Science ®Google Scholar
• SGC . Epigenetics Probes Collection. www.thesgc.org/chemical-probes/epigenetics
   Google Scholar
• CEREP . ExpresSProfile. www.cerep.fr/cerep/users/pages/catalog/profiles/detailprofile.asp?profile=2117
   Google Scholar
• Weigelt J . The case for open-access chemical biology. A strategy for pre-competitive medicinal chemistry to promote drug discovery. EMBO Rep.10 (9), 941–945 (2009).
   PubMedGoogle Scholar
• Edwards AM , BountraC, KerrDJ, WillsonTM. Open access chemical and clinical probes to support drug discovery. Nat. Chem. Biol.5 (7), 436–440 (2009).
   PubMed Web of Science ®Google Scholar
• National Cancer Institute . NCI Drug Dictionary. http://www.cancer.gov/publications/dictionaries/cancer-drug.
   Google Scholar
• Berkovits BD , WolgemuthDJ. The role of the double bromodomain-containing BET genes during mammalian spermatogenesis. Curr. Top. Dev. Biol.102, 293–326 (2013).
   PubMed Web of Science ®Google Scholar
• Chung CW . Small molecule bromodomain inhibitors: extending the druggable genome. Prog. Med. Chem.51, 1–55 (2012).
   PubMedGoogle Scholar
• Filippakopoulos P , KnappS. The bromodomain interaction module. FEBS Lett.586 (17), 2692–2704 (2012).
   PubMed Web of Science ®Google Scholar
• Muller S , FilippakopoulosP, KnappS. Bromodomains as therapeutic targets. Expert Rev. Mol. Med.13, e29 (2011).
   PubMed Web of Science ®Google Scholar
• Sanchez R , MeslamaniJ, ZhouMM. The bromodomain: from epigenome reader to druggable target. Biochim. Biophys. Acta1839 (8), 676–685 (2014).
   PubMed Web of Science ®Google Scholar
• Shi J , VakocCR. The mechanisms behind the therapeutic activity of BET bromodomain inhibition. Mol. Cell54 (5), 728–736 (2014).
   PubMed Web of Science ®Google Scholar
• Huang B , YangXD, ZhouMM, OzatoK, ChenLF. Brd4 coactivates transcriptional activation of NF-kappaB via specific binding to acetylated RelA. Mol. Cell. Biol.29 (5), 1375–1387 (2009).
   PubMed Web of Science ®Google Scholar
• Stewart HJ , HorneGA, BastowS, ChevassutTJ. BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1. Cancer Med.2 (6), 826–835 (2013).
   PubMed Web of Science ®Google Scholar
• Asangani IA , DommetiVL, WangXet al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature510 (7504), 278–282 (2014).
   PubMed Web of Science ®Google Scholar
• Palermo RD , WebbHM, WestMJ. RNA polymerase II stalling promotes nucleosome occlusion and pTEFb recruitment to drive immortalization by Epstein-Barr virus. PLoS Pathog.7 (10), e1002334 (2011).
   PubMed Web of Science ®Google Scholar
• Gupta SS , MaetzigT, MaertensGNet al. Bromo- and extraterminal domain chromatin regulators serve as cofactors for murine leukemia virus integration. J. Virol.87 (23), 12721–12736 (2013).
   PubMed Web of Science ®Google Scholar
• Wang X , HelferCM, PancholiN, BradnerJE, YouJ. Recruitment of Brd4 to the human papillomavirus type 16 DNA replication complex is essential for replication of viral DNA. J. Virol.87 (7), 3871–3884 (2013).
   PubMed Web of Science ®Google Scholar
• Anders L , GuentherMG, QiJet al. Genome-wide localization of small molecules. Nat. Biotechnol.32 (1), 92–96 (2014).
   PubMed Web of Science ®Google Scholar
• Winter GE , BuckleyDL, PaulkJet al. Drug development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science348 (6241), 1376–1381 (2015).
   PubMed Web of Science ®Google Scholar
• Muller S , LingardH, KnappS. Selective Targeting of Protein Interactions Mediated by BET Bromodomains.Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, Germany (2014).
   Google Scholar
• Fu LL , TianM, LiXet al. Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery. Oncotarget6 (8), 5501–5516 (2015).
   PubMed Web of Science ®Google Scholar
• Brand M , MeasuresAM, WilsonBGet al. Small molecule inhibitors of bromodomain-acetyl-lysine interactions. ACS Chem. Biol.10 (1), 22–39 (2015).
   PubMed Web of Science ®Google Scholar
• Gallenkamp D , GelatoKA, HaendlerB, WeinmannH. Bromodomains and their pharmacological inhibitors. ChemMedChem9 (3), 438–464 (2014).
   PubMed Web of Science ®Google Scholar
• Tang Y , GholaminS, SchubertSet al. Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition. Nat. Med.20 (7), 732–740 (2014).
   PubMed Web of Science ®Google Scholar
• Kalkhoven E . CBP and p300: HATs for different occasions. Biochem. Pharmacol.68 (6), 1145–1155 (2004).
   PubMed Web of Science ®Google Scholar
• Philpott M , YangJ, TumberTet al. Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery. Mol. Biosyst.7 (10), 2899–2908 (2011).
   PubMedGoogle Scholar
• Hay DA , FedorovO, MartinSet al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J. Am. Chem. Soc.136 (26), 9308–9319 (2014).
   PubMed Web of Science ®Google Scholar
• Das C , RoyS, NamjoshiSet al. Binding of the histone chaperone ASF1 to the CBP bromodomain promotes histone acetylation. Proc. Natl Acad. Sci. USA111 (12), E1072–E1081 (2014).
   PubMed Web of Science ®Google Scholar
• Giotopoulos G , ChanWI, HortonSJet al. The epigenetic regulators CBP and p300 facilitate leukemogenesis and represent therapeutic targets in acute myeloid leukemia. Oncogene doi:10.1038/onc.2015.92 (2015) ( Epub ahead of print).
   PubMed Web of Science ®Google Scholar
• Thanasopoulou A , DumreseK, PicaudS, FedorovO, KnappS, SchwallerJ. Targeting aberrant self-renewal of leukemic cells with a novel CBP/p300 bromodomain inhibitor. Blood124 (21), 3750–3750 (2014).
   Web of Science ®Google Scholar
• Hammitzsch A , TallantC, FedorovOet al. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc. Natl Acad. Sci. USA112 (34), 10763–10773 (2015).
   Web of Science ®Google Scholar
• Roe JS , MercanF, RiveraK, PappinDJ, VakocCR. BET bromodomain inhibition suppresses the function of hematopoietic transcription factors in acute myeloid leukemia. Mol. Cell doi:10.1016/j.molcel.2015.04.011 (2015) ( Epub ahead of print).
   Web of Science ®Google Scholar
• Son EY , CrabtreeGR. The role of BAF (mSWI/SNF) complexes in mammalian neural development. Am. J. Med. Genet. C Semin. Med. Genet.166C (3), 333–349 (2014).
   PubMedGoogle Scholar
• Middeljans E , WanX, JansenPW, SharmaV, StunnenbergHG, LogieC. SS18 together with animal-specific factors defines human BAF-type SWI/SNF complexes. PLoS ONE7 (3), e33834 (2012).
   PubMed Web of Science ®Google Scholar
• Helming KC , WangX, RobertsCW. Vulnerabilities of mutant SWI/SNF complexes in cancer. Cancer Cell26 (3), 309–317 (2014).
   PubMed Web of Science ®Google Scholar
• Benusiglio PR , CouveS, Gilbert-DussardierBet al. A germline mutation in PBRM1 predisposes to renal cell carcinoma. J. Med. Genet.52 (6), 426–430 (2015).
   PubMed Web of Science ®Google Scholar
• Kim JY , LeeSH, MoonKCet al. The impact of PBRM1 expression on prognostic and predictive marker in metastatic renal cell carcinoma. J. Urol. doi:10.1016/j.juro.2015.04.114 (2015) ( Epub ahead of print).
   Google Scholar
• Hohmann AF , VakocCR. A rationale to target the SWI/SNF complex for cancer therapy. Trends Genet.30 (8), 356–363 (2014).
   PubMed Web of Science ®Google Scholar
• Scotto L , NarayanG, NandulaSVet al. Integrative genomics analysis of chromosome 5p gain in cervical cancer reveals target over-expressed genes, including Drosha. Mol. Cancer7, 58 (2008).
   PubMed Web of Science ®Google Scholar
• Chiu YH , LeeJY, CantleyLC. BRD7, a tumor suppressor, interacts with p85alpha and regulates PI3K activity. Mol. Cell54 (1), 193–202 (2014).
   PubMed Web of Science ®Google Scholar
• Clark PG , VieiraLC, TallantCet al. LP99: discovery and synthesis of the first selective BRD7/9 bromodomain inhibitor. Angew. Chem. Int. Ed. Engl.54 (21), 6217–6221 (2015).
   PubMed Web of Science ®Google Scholar
• Drost J , MantovaniF, ToccoFet al. BRD7 is a candidate tumour suppressor gene required for p53 function. Nat. Cell Biol.12 (4), 380–389 (2010).
   PubMed Web of Science ®Google Scholar
• SGC . BI-9564 – a chemical probe for BRD9 and BRD7. www.thesgc.org/chemical-probes/bi-9564.
   Google Scholar
• Theodoulou NH , BamboroughP, BannisterAJet al. Discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition. J. Med. Chem. doi:10.1021/acs.jmedchem.5b00256 (2015) ( Epub ahead of print).
   PubMed Web of Science ®Google Scholar
• Medzhitov R , HorngT. Transcriptional control of the inflammatory response. Nat. Rev. Immunol.9 (10), 692–703 (2009).
   PubMed Web of Science ®Google Scholar
• SGC . www.thesgc.org/chemical-probes/pfi-3.
   Google Scholar
• Fedorov O , CastexJ, TallantCet al. Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cells maintenance. Science Advances (2015) ( In Press).
   PubMed Web of Science ®Google Scholar
• Avvakumov N , CoteJ, The MYST family cancer of histone acetyltransferases and their intimate links to cancer. Oncogene26 (7), 5395–5407 (2007).
   PubMedGoogle Scholar
• Paggetti J , LargeotA, AucagneRet al. Crosstalk between leukemia-associated proteins MOZ and MLL regulates HOX gene expression in human cord blood CD34+ cells. Oncogene29 (36), 5019–5031 (2010).
   PubMed Web of Science ®Google Scholar
• Sheikh BN , DownerNL, PhipsonBet al. MOZ and BMI1 play opposing roles during Hox gene activation in ES cells and in body segment identity specification in vivo. Proc. Natl Acad. Sci. USA112 (17), 5437–5442 (2015).
   PubMed Web of Science ®Google Scholar
• Laue K , DaujatS, CrumpJGet al. The multidomain protein Brpf1 binds histones and is required for Hox gene expression and segmental identity. Development135 (11), 1935–1946 (2008).
   PubMed Web of Science ®Google Scholar
• You L , YanK, ZhouJet al. The lysine acetyltransferase activator Brpf1 governs dentate gyrus development through neural stem cells and progenitors. PLoS Genet.11 (3), e1005034 (2015).
   PubMed Web of Science ®Google Scholar
• Mishima Y , WangC, MiyagiSet al. Histone acetylation mediated by Brd1 is crucial for Cd8 gene activation during early thymocyte development. Nat. Commun.5, 5872 (2014).
   PubMed Web of Science ®Google Scholar
• Mishima Y , MiyagiS, SarayaAet al. The Hbo1-Brd1/Brpf2 complex is responsible for global acetylation of H3K14 and required for fetal liver erythropoiesis. Blood118 (9), 2443–2453 (2011).
   PubMed Web of Science ®Google Scholar
• SGC . OF-1 – a chemical probe for BRPF bromodomains. www.thesgc.org/chemical-probes/of-1
   Google Scholar
• SGC . NI-57 – a chemical probe for BRPF bromodomains. www.thesgc.org/chemical-probes/ni-57
   Google Scholar
• SGC . PFI-4 – a chemical probe for BRPF1B. www.thesgc.org/chemical-probes/pfi-4
   Google Scholar
• Bennett J , FedorovO, TallantCet al. Discovery of a chemical tool inhibitor targeting the bromodomains of TRIM24 and BRPF. J. Med. Chem. doi:10.1021/acs.jmedchem.5b00458 (2015) ( Epub ahead of print).
   Google Scholar
• Palmer WS , Poncet-MontangeG, LiuGet al. Structure-guided design of IACS-9571, a selective high-affinity dual TRIM24-BRPF1 bromodomain inhibitor. J. Med. Chem. doi:10.1021/acs.jmedchem.5b00405 (2015) ( Epub ahead of print).
   Google Scholar
• Kruidenier L , ChungCW, ChengZet al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature488 (7411), 404–408 (2012).
   PubMed Web of Science ®Google Scholar
• SGC . GSK-J1: an inhibitor for human H3K27me3 and H3K4me3/2/1 demethylases. www.thesgc.org/chemical-probes/gskj1.
   Google Scholar
• Swigut T , WysockaJ. H3K27 demethylases, at long last. Cell131 (1), 29–32 (2007).
   PubMed Web of Science ®Google Scholar
• Liu Z , CaoW, XuLet al. The histone H3 lysine-27 demethylase Jmjd3 plays a critical role in specific regulation of Th17 cell differentiation. J. Mol. Cell. Biol. doi:10.1093/jmcb/mjv022 (2015) ( Epub ahead of print).
   Web of Science ®Google Scholar
• Messer HG , JacobsD, DhummakuptA, BloomDC. Inhibition of H3K27me3-specific histone demethylases JMJD3 and UTX blocks reactivation of herpes simplex virus 1 in trigeminal ganglion neurons. J. Virol.89 (6), 3417–3420 (2015).
   PubMed Web of Science ®Google Scholar
• Ntziachristos P , TsirigosA, WelsteadGGet al. Contrasting roles of histone 3 lysine 27 demethylases in acute lymphoblastic leukaemia. Nature514 (7523), 513–517 (2014).
   PubMed Web of Science ®Google Scholar
• Hashizume R , AndorN, IharaYet al. Pharmacologic inhibition of histone demethylation as a therapy for pediatric brainstem glioma. Nat. Med.20 (12), 1394–1396 (2014).
   PubMed Web of Science ®Google Scholar
• Grasso CS , TangY, TruffauxNet al. Functionally defined therapeutic targets in diffuse intrinsic pontine glioma. Nat. Med.21 (6), 555–559 (2015).
   PubMed Web of Science ®Google Scholar
• Kubicek S , O’SullivanRJ, AugustEMet al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol. Cell25 (3), 473–481 (2007).
   PubMed Web of Science ®Google Scholar
• Vedadi M , Barsyte-LovejoyD, LiuFet al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat. Chem. Biol.7 (8), 566–574 (2011).
   PubMed Web of Science ®Google Scholar
• Liu F , Barsyte-LovejoyD, LiFet al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J. Med. Chem.56 (21), 8931–8942 (2013).
   PubMed Web of Science ®Google Scholar
• Ling BM , GopinadhanS, KokWKet al. G9a mediates Sharp-1-dependent inhibition of skeletal muscle differentiation. Mol. Biol. Cell23 (24), 4778–4785 (2012).
   PubMed Web of Science ®Google Scholar
• Ohno H , ShinodaK, OhyamaK, SharpLZ, KajimuraS. EHMT1 controls brown adipose cell fate and thermogenesis through the PRDM16 complex. Nature504 (7478), 163–167 (2013).
   PubMed Web of Science ®Google Scholar
• Lehnertz B , PabstC, SuLet al. The methyltransferase G9a regulates HoxA9-dependent transcription in AML. Genes Dev.28 (4), 317–327 (2014).
   PubMed Web of Science ®Google Scholar
• Sweis RF , PliushchevM, BrownPJet al. Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med. Chem. Lett.5 (2), 205–209 (2014).
   PubMed Web of Science ®Google Scholar
• Mcginty RK , KimJ, ChatterjeeC, RoederRG, MuirTW. Chemically ubiquitylated histone H2B stimulates hDot1L-mediated intranucleosomal methylation. Nature453 (7196), 812–816 (2008).
   PubMed Web of Science ®Google Scholar
• Yu W , SmilD, LiFet al. Bromo-deaza-SAH: a potent and selective DOT1L inhibitor. Bioorg. Med. Chem.21 (7), 1787–1794 (2013).
   PubMed Web of Science ®Google Scholar
• Daigle SR , OlhavaEJ, TherkelsenCAet al. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. Cancer Cell20 (1), 53–65 (2011).
   PubMed Web of Science ®Google Scholar
• Basavapathruni A , JinL, DaigleSRet al. Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L. Chem. Biol. Drug Des.80 (6), 971–980 (2012).
   PubMed Web of Science ®Google Scholar
• Yu W , ChoryEJ, WernimontAKet al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat. Commun.31288 (2012).
   PubMed Web of Science ®Google Scholar
• Wigle TJ , KnutsonSK, JinLet al. The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states. FEBS Lett.585 (19), 3011–3014 (2011).
   PubMed Web of Science ®Google Scholar
• Verma SK , TianX, LafranceLVet al. Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2. ACS Med. Chem. Lett.3 (12), 1091–1096 (2012).
   PubMed Web of Science ®Google Scholar
• Knutson SK , WigleTJ, WarholicNMet al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat. Chem. Biol.8 (11), 890–896 (2012).
   PubMed Web of Science ®Google Scholar
• Konze KD , MaA, LiFet al. An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1. ACS Chem. Biol.8 (6), 1324–1334 (2013).
   PubMed Web of Science ®Google Scholar
• Campaner S , SpreaficoF, BurgoldTet al. The methyltransferase Set7/9 (Setd7) is dispensable for the p53-mediated DNA damage response in vivo. Mol. Cell43 (4), 681–688 (2011).
   PubMed Web of Science ®Google Scholar
• Liu X , WangD, ZhaoYet al. Methyltransferase Set7/9 regulates p53 activity by interacting with Sirtuin 1 (SIRT1). Proc. Natl Acad. Sci. USA108 (5), 1925–1930 (2011).
   PubMed Web of Science ®Google Scholar
• Oudhoff MJ , FreemanSA, CouzensALet al. Control of the hippo pathway by Set7-dependent methylation of Yap. Dev. Cell26 (2), 188–194 (2013).
   PubMed Web of Science ®Google Scholar
• Barsyte-Lovejoy D , LiF, OudhoffMJet al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc. Natl Acad. Sci. USA111 (35), 12853–12858 (2014).
   PubMed Web of Science ®Google Scholar
• Cho H , HerzkaT, ZhengWet al. RapidCaP, a novel GEM model for metastatic prostate cancer analysis and therapy, reveals myc as a driver of Pten-mutant metastasis. Cancer Discov.4 (3), 318–333 (2014).
   PubMed Web of Science ®Google Scholar
• Saddic LA , WestLE, AslanianAet al. Methylation of the retinoblastoma tumor suppressor by SMYD2. J. Biol. Chem.285 (48), 37733–37740 (2010).
   PubMed Web of Science ®Google Scholar
• Huang J , Perez-BurgosL, PlacekBJet al. Repression of p53 activity by Smyd2-mediated methylation. Nature444 (7119), 629–632 (2006).
   PubMed Web of Science ®Google Scholar
• Ferguson AD , LarsenNA, HowardTet al. Structural basis of substrate methylation and inhibition of SMYD2. Structure19 (9), 1262–1273 (2011).
   PubMed Web of Science ®Google Scholar
• Nguyen H , Allali-HassaniA, AntonysamySet al. LLY-507, a cell-active, potent, and selective inhibitor of protein-lysine methyltransferase SMYD2. J. Biol. Chem.290 (22), 13641–13653 (2015).
   PubMed Web of Science ®Google Scholar
• Kaniskan HU , SzewczykMM, YuZet al. A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew. Chem. Int. Ed. Engl.54 (17), 5166–5170 (2015).
   PubMed Web of Science ®Google Scholar
• James LI , Barsyte-LovejoyD, ZhongNet al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat. Chem. Biol.9 (3), 184–191 (2013).
   PubMed Web of Science ®Google Scholar
• Senisterra G , WuH, Allali-HassaniAet al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem. J.449 (1), 151–159 (2013).
   PubMedGoogle Scholar
• Grebien F , VedadiM, GetlikMet al. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPalpha N-terminal leukemia. Nat. Chem. Biol.11 (8), 571–578 (2015).
   PubMed Web of Science ®Google Scholar