Recent publications by CICBDD Scientists
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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 Tratment 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 lyine 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, 2011, 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-Arrentin-Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy." PNAS Early Edition DOI:10.1073/pnas.1104807108 Oct. 24, 2011.
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 relationship of methyl-lysine reader antagonists." Med. Chem. Commun. DOI:10.1039/C1MD00195G Oct. 20, 2011.
Janzen, W.P. and Hull-Ryde, E.A. "Kinases as Targets for Drug Discovery in an Academic Setting." International Drug Discovery, August/Sepetmber 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. "Identifiation 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.
