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dearry@email.unc.edu

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Recent publications by CICBDD Scientists

 

Click highlighted author for a link to article.

Konze, K. D.; Pattenden, S. G.; Liu, F.; Barsyte-Lovejoy, D.; Li, F.; Simon, J. M.; Davis, I. J.; Vedadi, M.; Jin, J. “A Chemical Tool for in vitro and in vivo Precipitation of the Lysine Methyltransferase G9a” ChemMedChem, 2014, DOI: 10.1002/cmdc.201300450.

Zhou, B.; Damrauer, J. S.; Hadzic, T.; Jeong, Y.; Clark, K.; Fan, C.; Murphy, L.; Lee, C. Y.; Troester, M. A.; Miller, C. R.; Jin, J.; Darr, D.; Perou, C. M.; Levine, R.; Diehn, M.; Kim, W. Y. “Erythropoietin Promotes Breast Tumorigenesis Through Tumor Initiating Cell Self-renewal”, Journal of Clinical Investigation, 2014, DOI: 10.1172/JCI69804. .

Zhang, W.; Zhang, D.; Stashko, M.A.; DeRyckere, D.; Hunter, D.; Kireev, D.; Miley, M.J.; Cummings, C.; Lee, M.; Norris-Drouin, J.; Stewart, W.M.; Sather, S.; Zhou, Y.; Kirkpatrick, G.; Machius, M.; Janzen, W.P.; Earp, H.S.; Graham, D.K..; Frye, S.V.; Wang, X. "Pseudo-Cyclization through Intramolecular Hydrogen Bond Enables Discovery of Pyridine Substituted Pyrimidines as New Mer Kinase Inhibitors." Journal of Medicinal Chemistry 2013, 56, 9683-9692.

Zhang, W.; McIver, A.L. Stashko, M.A.; DeRyckere, D.; Branchford, B.R.; Hunter, D.; Kireev, D.; Miley, M.J.; Norris-Drouin, J.; Stewart, W.M.; Lee, M.; Sather, S.; Zhou, Y.; Di Paola, J.A.; Machius, M.; Janzen, W.P.; Earp, H.S.; Graham, D.K.; Frye, S.V.; Wang, X. "Discovery of Mer Specific Tyrosine Kinase Inhibitors for the Treatment and Prevention of Thrombosis." Journal of Medicinal Chemistry 2013, 56, 9693-9700.

Camerino, M.A.; Zhong, N., Dong, A., Dickson, B.; James, L.; Baughman, B.; Norris, J.; Kireev, D.; Janzen, W.P.; Arrowsmith, C.; Frye S.V. "The structure-activity relationships of L3MBTL3 inhibitors: A second series of potent compounds which bind the L3MBTL3 dimer." Med. Chem. Commun. 2013, 4, 1501-1507.

James, L.I.; Korboukh, V.K.; Krichevsky, L.; Baughman, B.M.; Herold, J.M.; Norris, J.L.; Jin, J.; Kireev, D.K.; Janzen, W.P.; Arrowsmith, C.H.; Frye, S.V.  "Small-Molecule Ligands of Methyl-Lysine Binding Proteins: Optimization of Selectivity for L3MBTL3."  J. Med. Chem. 2013, 56, 7358-7371. 

Slusher, B.S.; Conn, P.J.; Frye, S.; Glicksman, M.; Arkin, M. "Bringing together the academic drug discovery community." Nat Rev Drug Discov 2013, 12, 811-812.

Cooper, M.J.; Cox, N.J.; Zimmerman, E.I.; Dewar, B.J.; Duncan, J.S.; Whittle, M.C.; Nguyen, T.A.; Jones, L.S.; Roy, S.G.; Smalley, D.M.; Kuan, P.F.; Richards, K.L.; Christopherson, R.I.; Jin, J.; Frye, S.V.; Johnson, G.L.; Baldwin, A.S.; Graves, LM. “Application of Multiplexed Kinase Inhibitor Beads to Study Kinome Adaptations in Drug Resistant Leukemia” PLoS ONE 2013, 8, e66755.

Rothbart, S.B.; Dickson, B.M.; Ong, M.S.; Krajewski, K.; Houliston, S.; Kireev, D.B.; Arrowsmith, C.H.;  Strahl, B.D. “Multivalent histone engagement by the linked tandem Tudor and PHD domains of UHRF1 is required for the epigenetic inheritance of DNA methylation.” Genes Dev 2013 27 (11) 1288-1298.

Konze K.D.; Ma, A.; Li, F.; Barsyte-Lovejoy, D.; Parton, T.; Macnevin, C.J.; Liu, F.; Gao, C.; Huang, X.P.; Kuznetsova, E.; Rougie, M.; Jiang, A.; Pattenden, S.G.; Norris, J.L.; James, L.I.; Roth, B.L; Brown, P.J.; Frye, S.V.; Arrowsmith, C.H.; Hahn, K.M.; Wang, G.G.; Vedadi, M.; Jin, J. “An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1.” ACS Chem. Biol. 2013, 8, 1324-1334.

Schlegel, J.; Sambade, M.J.; Sather, S.; Moschos, S.J.; Tan, A.C.; Winges, A.; DeRyckere, D.; Carson, C.C.; Trembath, D.G.; Tentler, J.J.; Eckhardt, S.G.; Kuan, P.F.; Hamilton, R.L.; Duncan, L.M.; Miller, C.R.; Nikolaishvili-Feinberg, N.; Midkiff, B.R.; Liu, J.; Zhang, W.; Yang, C.; Wang, X.; Frye, S.V.; Earp, H.S.; Shields, J.M.; Graham, D.K. “MERTK receptor tyrosine kinase is a therapeutic target in melanoma.” J. Clin. Invest. 2013, 123(5), 2257–2267.

Liu, J.; Zhang, W.; Stashko , M.; DeRyckere, D.; Cummings, C.T.; Hunter, D.; Yang, C.; Jayakody, C.N.; Cheng, N.; Simpson, C.; Norris-Drouin, J.; Sather, S.; Kireev, D; Janzen, W.P.; Earp, H.S.; Graham, D.K.; Frye, S.V.; Wang, X. “UNC 1062, a new and potent MER inhibitor.” European Journal of Medicinal Chemistry 2013, 65, 83-93.

Blancafort, P.; Jin, J.; Frye, S.V. “Writing and rewriting the epigenetic code of cancer cells: from engineered proteins to small molecules.” Mol. Pharmacol. 2013, 83, 563-576.

Liu, F., Li, F., Ma, A., Dobrovetsky, E., Dong, A., Gao, C., Korboukh, I., Liu, J., Smil, D., Brown, P.J., Frye, S.V., Arrowsmith, C.H., Schapira, M., Vedadi, M., Jin, J. "Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors." J. Med. Chem. 2013, 56, 2110-2124. PMID:23445220.

James, L.I.; Frye, S.V. “Targeting chromatin readers.” Clin. Pharmacol. Ther. 2013, 93, 312-314.

James, L.I.; Barsyte-Lovejoy, D.; Zhong, N.; Krichevsky, L.; Korboukh, V.K.; Herold, J.M.; MacNevin, C.J.; Norris, J.L.; Sagum, C.A.; Tempel, W.; Marcon, E.; Guo, H.; Gao, C.; Huang, X.-P.; Duan, S.; Emili, A.; Greenblatt, J.F.; Kireev, D.B.; Jin, J.; Janzen, W.P.; Brown, P.J.; Bedford, M.T.; Arrowsmith, C.H. and Frye, S.V. "Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain." Nature Chemical Biology 2013, 9, 184–191.

Zhang, W.; Liu, J.; Stashko, M.A.; Wang, X. "Efficient Solution-Phase Synthesis of 4,5,7-Trisubstituted Pyrrolo[3,2-d] pyrimidines." ACS Combinatorial Science 2013, 15 (1), pp 10–19. First published online Nov.26, 2012.

Herold, J.M.; James, L.I.; Korboukh, V.K.; Gao, C.; Coil, K.E.; Bua, D.J.; Norris, J.L.; Kireev, D.B.; Brown, P.J.; Jin, J.; Janzen, W.P.; Gozani, O. and Frye, S.V. "Structure–activity relationships of methyl-lysine reader antagonists." Med. Chem. Commun., 2012, 3, 45-51. First published on the web 10 Oct 2011.

Peterson, E.J.R.; Kireev, D.; Moon, A.F.; Midon, M.; Janzen, W.P.; Pingoud, A.; Pedersen, L.C.; Singleton, S.F., "Inhibitors of Streptococcus pneumoniae Surface Endonuclease EndA Discovered by High-Throughput Screening Using a PicoGreen Fluorescence Assay." J. Biomol. Screen. 2013 18, 3, 247-257. 

Hutti, J.E.; Porter, M.A.; Cheely, A.W.; Cantley, L.C.; Wang, X.; Kireev, D.; Baldwin, A.S.; Janzen, W.P., "Development of a High-Throughput Assay for Identifying Inhibitors of TBK1 and IKKepsilon." PLoS ONE 2012, 7 (7), e41494.

Peterson, E.J.R.; Janzen, W.P.; Kireev, D.; Singleton, S.F., "High-Throughput Screening for RecA Inhibitors Using a Transcreener Adenosine 5 '-O-Diphosphate Assay." Assay Drug Dev. Technol. 2012, 10 (3), 260-268.

Gao, C.; Herold, J.M.; Kireev, D., "Assessment of free energy predictors for ligand binding to a methyllysine histone code reader."  J Comput Chem 2012, 33 (6), 659-665.

Chen, X.; Sassano, M.F.; Zheng, L.; Setola, V.; Chen, M.; Bai, X.; Frye, S.V.; Wetsel, W.C.; Roth, B.L.; Jin, J. "Structure-Functional Selectivity Relationship Studies of Beta-arrestin-biased Dopamine D2 Receptor Agonists." J. Med. Chem. 2012, 55, 7141-7153.

Roberts, P.J.; Usary, J.E.; Darr, D.B.; Dillon, P.M.; Pfefferie, A.D.; Whittle, M.C.; Duncan, J.S.; Johnson, S.M.; Combest, A.J.; Jin, J.; Zamboni, W.C.; Johnson, G.L.; Perou, C.M.; Sharpless, N.E. "Combined PI3K/mTOR and MEK Inhibition Provides Broad Anti-Tumor Activity in Faithful Murine Cancer Models." Clinical Cancer Research, 2012, 18(19); 5290–303.

Korboukh, I.; Hull-Ryde, E.A.; Rittiner, J.E.; Randhawa, A.S.; Coleman, J.; Fitzpatrick, B.J.; Setola, V.; Janzen, W.P.; Frye, S.V.; Zylka, M.J.; Jin, J. "Orally Active Adenosine A1 Receptor Agonists with Antinociceptive Effects in Mice." Journal of Medicinal Chemistry 2012, 55 (14), 6467–6477.

Siarheyeva, A.; Senisterra, G.; Allali-Hassani, A.; Dong, A.; Dobrovetsky, E.; Wasney, G.A.; Chau, I.; Marcellus, R.; Hajian, T.; Liu, F.; Korboukh, I.; Smil, D.; Bolshan, Y.; Min, J.; Wu, H.; Zeng, H.; Loppnau, P.; Poda, G.; Griffin, C.; Aman, A.; Brown, P.J.; Jin, J.; Al-awar, R.; Arrowsmith, C.H.; Schapira, M.; Vedadi, M. "An Allosteric Inhibitor of Protein Arginine Methyltransferase 3." Structure 2012, 20, 8, 1425-1435.

Duncan, J.S.; Whittle, M.C.; Nakamura, K.; Abell, A.N.; Midland, A.A.; Zawistowski, J.S.; Johnson, N.L.; Granger, D.A.; Jordan, N.V.; Darr, D.B.; Usary, J.; Kuan, P.-F.; Smalley, D.M.; Major, B.; He, X.; Hoadley, K.A.; Zhou, B.; Sharpless, N.E.; Perou, C.M.; Kim, W.Y.; Gomez, S.M.; Chen, X.; Jin, J.; Frye, S.V.; Earp, H.S.; Graves, L.M.; Johnson, G.L. " Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer." Cell 2012, 149 (2), 307-321.

Liu, J.; Yang, C.; Simpson, C.; DeRyckere, D.; Van Deusen, Amy; Miley, M.J.; Kireev, D.; Norris-Drouin, J.; Sather, S.; Hunter, D.; Korboukh, V.K., Patel, H.S.; Janzen, W.P.; Machius, M.; Johnson, G.L.; Earp, H.S.; Graham, Douglas K.; Frye, Stephen V.; Wang, X. "Discovery of Small Molecule Mer Inhibitors for the Treatment of Acute Lymphoblastic Leukemia." ACS Med. Chem. Lett. 2012, 3, 129−134.

Rittiner, J.E.; Korboukh, I.; Hull-Ryde, E.A.; Jin, J.; Janzen, W.P.; Frye, Stephen V.; and Zylka, M.J. "AMP Is an Adenosine A1 Receptor Agonist." J. Biol. Chem. 2012, 287, 5301-5309.

He, Y.; Korboukh, I.; Jin, J.; Huang, J. "Targeting protein lysine methylation and demethylation in cancers."  Acta Biochim. Biophys. Sin, 2012, 44, 70-79.

Huang, H.-S.; Allen, J.A.; Mabb, A.M.; King, I.F.; Miriyala, J.; Taylor-Blake, B.: Sciaky, N.: Dutton, Jr., J.W.; Lee, H.-M.; Chen, X.; Jin, J.; Bridges, A.S.; Zylka, M.J.; Roth, B.L.; Philpot, B.D.  "Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons." Nature 2012, 481,185–189. DOI:10.1038/nature10726 published online 12/21/2011.

Allen, J.A.; Yost, J.M.; Setola, V.; Chen, X.; Sassano, M.F.; Chen, M.; Peterson, S.; Yadav, P.N., Huang, X-p; Feng, B.; Jensen, N.H.; Che, X.; Bai, X.; Frye, S.V.; Wetsel, W.C.; Caron, M.G.; Javitch, J.A.; Roth, B.L.; Jin, J. "Discovery of beta-Arrestin-Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy." PNAS Early Edition DOI:10.1073/pnas.1104807108 Oct. 24, 2011.

Janzen, W.P. and Hull-Ryde, E.A. "Kinases as Targets for Drug Discovery in an Academic Setting."  International Drug Discovery, August/September 2011, pp 8-12.

Liu, F.; Barsyte-Lovejoy, D.; Allali-Hassani, A.; He, Y.; Herold, J.M.; Chen, X.; Yates, C.M.; Frye, S.V.; Brown, P.J.; Huang, J.; Vedadi, M.; Arrowsmith, J.; and Jin J. "Optimization of Cellular Activity of G9a Inhibitors 7-Aminoalkoxy-quinazolines." Journal of Medicinal Chemistry, 2011 54 (17), pp 6139–6150.  DOI:10.1021/jm20093z

Vedadi, M.; Barsyte-Lovejoy, D.; Liu, F.; Rival-Gervier, S.; Allali-Hassani, A.; Labrie, V.; Wigle, T.J.; DiMaggio, P.A.; Wasney, G.A.; Siarheyeva, A.; Dong, A.; Tempel, W.; Wang, S-C.; Chen, X.; Chau, I.; Mangano, T.J.;  Huang, X-p.; Simpson, C.D.; Pattenden, S.G.; Norris, J.L.; Kireev, D.B.; Tripathy, A.; Edwards, A.; Roth, B.L.; Janzen, W.P.; Garcia, B.A.; Petronis, A.; Ellis, J.;  Brown, P.J.; Frye, S.V.; Arrowsmith, C.H.; & Jin, J. "A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells." Nature Chemical Biology, 2011, 7, p 648. DOI:10.1038/nchembio.599

Herold, J.M.; Wigle, T.J.; Norris, J.L.; Lam, R.; Korboukh, V.K.; Gao, C.;  Ingerman, L.A.; Kireev, D.B.; Senisterra, G; Vedadi, M.; Tripathy, A.;  Brown, P.J.; Arrowsmith, C.H.; Jin, J.; Janzen, W.P.; and Frye, S.V.  "Small-Molecule Ligands of Methyl-Lysine Binding Proteins."  J. Med. Chem., 2011, 54 (7), pp 2504–2511.  DOI: 10.1021/jm200045v

Gao, C.; Herold, J.M.; Kireev, D; Wigle, T.; Norris, J.L.; and Frye, S.  "Biophysical Probes Reveal a 'Compromise' Nature of the Methyl-lysine Binding Pocket in L3MBTL1."  J. Am. Chem. Soc., 2011, 133 (14), pp 5357–5362.  DOI: 10.1021/ja110432e.

Liu, J. and Wang, Xiaodong. "Microwave-Assisted, Divergent Solution-Phase Synthesis of 1,3,6-Trisubstituted Pyrazolo[3,4-d]pyrimidines"  ACS Comb. Sci. 2011 13 (4), pp 414–420.  DOI: 10.1021/co200039k

Kireev, D.; Wigle, T.J.; Norris-Drouin, J.; Herold, J.M.; and Frye, S.V.  "Identification of Non-Peptide Malignant Brain Tumor (MBT) Repeat Antagonists by Virtual Screening of Commercially Available Compounds."  J. Med. Chem 2010 53 (21), pp 7625–7631. DOI: 10.1021/jm1007374.

Wigle, T.J.; Provencher, L.M.; Norris, J.L.; Jin, J; Brown, P.J.; and Frye, S.V.  "Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis." Chemistry & Biology 2010, 17, 695-704.  View Cover

Jin, J.; Morales-Ramos, A.; Eidam, Patrick; Mecom, J.; Li, Yue; Brooks, C; Hilfiker, M.; Zhang, D.; Wang, N.; Shi, D.; Tseng, P-S.; Wheless, K.; Budzik, B.; Evans, K.; Jaworski, J-P.; Jugus, J.; Leon, L.; Wu, Charlene; Pullen, M.; Karamshi, B.; Rao, P.; Ward, E.; Laping, N.; Evans, C.; Leach, C.; Holt, D; Su, X.; Morrow, D.; Fries, H.; Thorneloe, K.; and Ewards, R. "Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists." ACS Med. Chem. Lett. 2010 1 (7), pp 316–320.  DOI: 10.1021/ml100077x.

Frye, Stephen V. "The art of the chemical probe." Nature Chemical Biology 2010, 6 159-161.

Wigle, T.; Herold, J.M.; Senisterra, G.A.; Vedadi, M.; Kireev, D.B.; Arrowsmith, C.A.; Frye, S.V.; and Janzen, W.P.  "Screening for Inhibitors of Low-Affinity Epigenetic Peptide-Protein Interactions: An AlphaScreenTM-Based Assay for Antagonists of Methyl-Lysine Binding Proteins."  J. Biomolecular Screening 2010, 15(1), 62-71.

Evans, K.A.; Budzik, B.W.; Ross S.A; Wisnoski, D.D.; Jin, J; Rivero, R.A.; Vimal, M.; Szewczyk, G.R.; Jayawickreme, C.; Moncol, D.L.; Rimele, T.J.; Armour, S.L.; Weaver, S.P.; Griffin, R.J.; Tadepalli, S.M.; Jeune, M.R.; Shearer, T.W.; Chen, Z.B.; Chen, L.; Hertzog, D.L.; Anderson, D.L.; Becherer, D.; De Los Frailes, M.; Colilla, F.J. "Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists." J. Med. Chem 2009, 52 (24), pp 7962–7965.  DOI: 10.1021/jm901434t.

Liu, F.; Chen, X; Allali-Hassani, A.; Quinn, A.M.; Wasney, G.A.; Dong, A.; Barsyte, D.; Kozieradzki, I.; Senisterra, G.; Chau, I.; Siarheyeva, Al; Kireev, D.B.; Jadhav, A.; Herold, J.M.; Frye, S.V.; Arrowsmith, C.H.; Brown, P.J.; Simeonov, A.; Vedadi, M.; Jin, J. "Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a." J. Med. Chem. 2009, 52 (24), pp 7950–7953.  DOI:10.1021/jm901543m.

Frye, S. and Johnson, G. "Inhibitors paradoxically prime kinases" News and Views, Nature Chemical Biology 2009, 5, 448-449. DOI10.1038/nchembio.f.11

Hilfiker, M. A.; Wang, N.; Hou, X.; Du, Z.; Pullen, M. A.; Nord, M.; Nagilla, R.; Fries, H. E.; Wu, C. W.; Sulpizio, A. C.; Jaworski, J. P.; Morrow, D.; Edwards, R. M.; Jin, J. “Discovery of Novel Aminothiadiazole Amides as Selective EP3 Receptor Antagonists” Bioorg. Med. Chem. Lett. 2009, 19, 4292-4295.

Jugus, M. J.; Jaworski, J. P.; Patra, P. B.; Jin, J.; Morrow, D. M.; Laping, N. J.; Edwards, R. M.; Thorneloe, K. S.* “Dual Modulation of Urinary Bladder Activity and Urine Flow by Prostanoid EP3 Receptors in the Conscious Rat” Br. J. Pharmacol. 2009, 158, 372-381.

Wang, Y.; Busch-Petersen, J.; Wang, F.; Kiesow T. J.; Graybill, T. L.; Jin, J.; Palovich, M.; Foley, J. J.; Hunsberger, G. E.; Schmidt, D. B.; Sarau, H. M.; Spudich, E. A.; Wu, Z.; Fisher, L. S.; McQueney, M. S.; Rivero, R. A.; Widdowson, K. L. “Camphor Sulfonamides and Derivatives as Novel, Potent and Selective CXCR3 Antagonists” Bioorg. Med. Chem. Lett. 2009, 19, 114-118.

Li, Y. H.; Zhang, L.; Tseng, P. S.; Zhang, Y.; Jin, Y.; Shen, J. K.; Jin, J. “A Facile One-Pot Synthesis of 3-Unsubstituted-2,4-Oxazolidinediones via in situ Generation of Carbamates from α-Hydroxyesters using Trichloroacetyl Isocyanate” Tetrahedron Letters 2009, 50, 790-792.

Budzik, B. W.; Wang, Y.; Shi, D.; Wang, F.; Xie, H.; Wan, Z.; Zhu, C.; Foley, J. J.; Rao, P.; Kallal, L. A.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Laine, D. I.; Jin, J. “M3 Muscarinic Acetylcholine Receptor Antagonists: SAR and Optimization of Bi-Aryl Amines” Bioorg. Med. Chem. Lett. 2009, 19, 1686-1690.

Janzen, W.P. and I.G. Popa-Burke.  "Advances in Improving the Quality and Flexibility of Compound Management.  2009 Journal of Biomolecular Screening 14:444-451.

High Throughput Screening Methods and Protocols 2nd edition (2009) W. Janzen and P. Bernasconi, editors.  Humana, Totowa, NJ.

Blackwell, L., J. Norris, C.M. Suto, and W.P. Janzen. "The use of diversity profiling to characterize chemical modulators of the histone deacetylases."  2008 Life Sci. 82:1050-8.

Janzen, W.P. and C.N. Hodge.  "A chemogenomic approach to discovering target-selective drugs." 2006 Chem Biol Drug Des 67:85-6.

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