Z-Key Publications - Center for Integrative Chemical Biology and Drug Discovery

CICBDD Chemical Probe Discovery

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

Five principles of a quality chemical probe

Molecular profiling. Sufficient in vitro potency and selectivity data to confidently associate its in vitro profile to its cellular or in vivo profile.
Mechanism of action. Activity in a cell-based or cell-free assay influences a physiologic function of the target in a dose-dependent manner.
Identity of the active species. Has sufficient chemical and physical property data to interpret results as due to its intact structure or a well-characterized derivative.
Proven utility as a probe. Cellular activity data available to confidently address at least one hypothesis about the role of the molecular target in a cell’s response to its environment.
Availability. Is readily available to the academic community with no restrictions on use.

Commentary

Kimberly D Barnash, Lindsey I James & Stephen V Frye “Target class drug discovery”. Nature Chemical Biology. October 2017

Key Chemical Probe & Drug Discovery Papers

Katherine A. Minson,¹ Catherine C. Smith,² Deborah DeRyckere,^1,3 Clara Libbrecht,⁴ Alisa B. Lee-Sherick,⁴ Madeline G. Huey,¹ Elisabeth A. Lasater,² Gregory D. Kirkpatrick,⁴ Michael A. Stashko,⁵ Weihe Zhang,⁵ Craig T. Jordan,⁶ Dmitri Kireev,⁵ Xiaodong Wang,⁵ Stephen V. Frye,^5,7 H. Shelton Earp,^7,8 Neil P. Shah,² and Douglas K. Graham^1,3 “The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia”. JCI Insight. 2016;1(3):e85630. doi:10.1172/jci.insight.85630. PMID:25762638 PMCID:PMC4466645.

*Frye, S. V., Cell Voices: “Where is the Future of Drug Discovery for Cancer: Drugging the Unprecedented”. Cell 2017, 168, 564. PMID: 28187277.

Stuckey, J. I.; Dickson, B. M.; Cheng, N.; Liu, Y.; Norris, J. L.; Cholensky, S. H.; Tempel, W.; Qin, S.; Huber, K. G.; Sagum, C.; Black, K.; Li, F.; Huang, X-P; Roth, B. L.; Baughman, B. M.; Senisterra, G.; Pattenden, S. G.; Vedadi, M.; Brown, P. J.; Bedford, M. T.; Min, J.; Arrowsmith, C. H.; *James, L. I.; *Frye, S. V. “A cellular chemical probe targeting the chromodomains of Polycomb Repressive Complex 1”, , Nature Chem. Biol. January 2016, doi: 10.1038/nchembio.2007. PMID:26807715.

Zhang, W; DeRyckere, D; Hunter, D., Liu, J.; Stashko, M.A.; Minson, K.A., Cummings, C.T., Lee, M.; Glaros, T.G.; Newton, D.L.; Sather, S.; Zhang, D.; Kireev, D.; Janzen, W.P.; Earp, H.S.; Graham, D.K., Frye, S.V.; Wang, X. “UNC 2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor.” J. Med. Chem., 2014, 57, 7031-7041.

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.

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.

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.

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.

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

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., 52 (24), pp 7950–7953. DOI:10.1021/jm901543m.

Other CICBDD Publications

Stuckey JI, Simpson C, Norris-Drouin JL, Cholensky SH, Lee J, Pasca R, Cheng N, dickson BM, Pearce KH, Frye SV, James LI. “Structure-Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains.” J med Chem. 2016 Sep 19 (Epub ahead of print). PMID: 27571219. doi:10.1021/acs.jmedchem.6b00801.

Baughman BM, Pattenden SG, Norris JL, James LI, Frye SV. “The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer”. ACS Chem Biol. 2016 Mar 18;11(3):722-8. doi: 10.1021/acschembio.5b00632. Epub 2015 Sep 2. PubMed PMID: 26317848; PubMed Central PMCID: PMC4775453.

James LI, Frye SV. “Chemical probes for Methyl lysine reader domains.” Current Opinion in Chemical Biology 2016 Aug; 33:135-41. doi: 10.1016/j.cbpa.2016.06.004. Epub 2016 Jun 25. PMID: 27348158. PMCID: PMC5018434.

Barnash KD, Lamb KN, Stuckey JI, Norris JL, Cholensky SH, Kireev DB, Frye SV, James LI. “Chromodomain Ligand Optimization via Target-Class Directed Combinatorial Repurposing.” ACS Chem Biol. 2016 Sep 16;11(9):2475-83. doi: 10.1021/acschembio.6b00415. PMID:27356154. PMCID: PMC5026585 (Available on 2017-09-16).

Zhou H, Che X, Bao G, Wang N, Peng L, Barnash KD, Frye SV, James LI, Bai X. “Design, synthesis, and protein methyltransferase activity of a unique set of constrained amine containing compounds.” Bioorg Med Chem Lett, 2016 Sep 15;26(18):4436-40.doi: 10.1016/j.bmcl.2016.08.004. Epub 2016 Aug 3. PMID: 27528434. PMCID: PMC4996710.

Pattenden SG, Simon JM, Wali A, Jayakody CN, Troutman J, McFadden AW, Wooten J, Wood CC, Frye SV, Janzen WP, Davis IJ. “High-throughput small molecule screen identifies inhibitors of aberrant chromatin accessibility”. Proc Natl Acad Sci U S A. 2016 Mar 15;113(11):3018-23. doi: 10.1073/pnas.1521827113. Epub 2016 Feb 29. PubMed PMID: 26929321; PubMed Central PMCID: PMC4801272.

Simon JM, Parker JS, Liu F, Rothbart SB, Ait-Si-Ali S, Strahl BD, Jin J, Davis IJ, Mosley AL, Pattenden SG. “A Role for Widely Interspaced Zinc Finger (WIZ) in Retention of the G9a Methyltransferase on Chromatin”. J Biol Chem. 2015 Oct 23; 290(43):26088-102. doi: 10.1074/jbc.M115.654459. Epub 2015 Sep 3. PubMed PMID: 26338712.

Kasoji SK*, Pattenden SG*, Malc EP, Jayakody CN, Tsuruta JK, Mieczkowski PA, Janzen WP, Dayton PA. “Cavitation Enhancing Nanodroplets Mediate Efficient DNA Fragmentation in a Bench Top Ultrasonic Water Bath. PLoS One”. 2015 Jul 17;10(7):e0133014. doi: 10.1371/journal.pone.0133014. eCollection 2015. PubMed PMID: 26186461. *These authors contributed equally to this work.

Perfetti, MT; Baughman, BM; Dickson, BM; Mu, Y; Ciu, G; Mader, P; Dong, A; Norris, JL; Rothbart, SB; Strahl, BD; Brown, PJ; Janzen, WP; Arrowsmith, CH; Mer, G; McBride, KM; James, LI; Frye, SV. “Identification of a Fragment-like Small Molecule Ligand for the Methyl-lysine Binding Protein, 53BP1.” ACS Chem. Biol. online Jan. 15, 2015. PMID: 2559533

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.

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.

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

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.

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.

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

Wright, B.D.; Loo, L; Street, S.E.; Ma, A.; Taylor-Blake, B.; Stashko, M.A.; Jin, J., Janzen, W.P.; Frye, S.V., Zylka, M.J. “The Lipid Kinase PIP5K1C Regulates PainSignaling and Sensitization” Neuron, 2014, 82, 836-47. PMID: 24853942. PMCID: PMC4074510

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. PMID: 24195762. PMCID: PMC3980660.

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: flexibility of the dimer interface.” Med. Chem. Commun. 2013, 4, 1501-1507.

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.

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.

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. Published online before print September 26, 2012.

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 D₂Receptor 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.

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.

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

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

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

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.