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Duckett, Derek
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Duckett, Derek

Faculty Member
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Positions

  • 2005 - Associate Scientific Director I, Translational Research Institute , Scripps Research
  • 2017 - 2018 Associate Professor of Molecular Medicine, Molecular Medicine , Scripps Research
  • 2005 - 2018 Faculty Member, Skaggs Graduate School of Chemical and Biological Sciences , Scripps Research
  • 2015 - 2017 Associate Professor of Molecular Therapeutics, Molecular Therapeutics , Scripps Research
  • 2005 - 2015 Assistant Professor, Molecular Therapeutics , Scripps Research
Work in our laboratory is aimed at evaluating small molecule kinase inhibitors of biologic and therapeutic interest. We are currently involved in refining a novel class of kinase inhibitors aimed at the therapeutic treatment of human diseases such as Parkinson’s Disease and Cancer. Protein kinases are important components of signal transduction pathways and deregulation of kinase activity can lead to human disease. Kinases have therefore become one of the most important target classes for drug development. Working closely with other disciplines such as chemistry, pharmacology, and drug metabolism, we aim to optimize lead compounds for potency and selectivity while minimizing toxicity to generate candidate molecules with appropriate drug like properties suitable for IND enabling and first time in human studies.
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Publications

recent publications

  • academic article

    • Quereda, V., Bayle, S., Vena, F., Frydman, S. M., Monastyrskyi, A., Roush, W. R., Duckett, D. R. Therapeutic targeting of CDK12/CDK13 in triple-negative breast cancer Cancer Cell  2019 36:545-558  DOI:10.1016/j.ccell.2019.09.004  PMID:31668947
    • Crawley, O., Opperman, K. J., Desbois, M., Adrados, I., Borgen, M. A., Giles, A. C., Duckett, D. R., Grill, B. Autophagy is inhibited by ubiquitin ligase activity in the nervous system Nature Communications  2019 10  DOI:10.1038/s41467-019-12804-3  PMID:31676756  PMCID:PMC6825199
    • Quereda, V., Hou, S., Madoux, F., Scampavia, L., Spicer, T. P., Duckett, D. A cytotoxic three-dimensional-spheroid, high-throughput assay using patient-derived glioma stem cells SLAS Discovery  2018 23:842-849  DOI:10.1177/2472555218775055  PMID:29750582  PMCID:PMC6102052
    • Monastyrskyi, A., Nilchan, N., Quereda, V., Noguchi, Y., Ruiz, C., Grant, W., Cameron, M., Duckett, D., Roush, W. Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer Bioorganic & Medicinal Chemistry  2018 26:590-602  DOI:10.1016/j.bmc.2017.12.020  PMID:29289448  PMCID:PMC5803353
    • Monastyrskyi, A., Bayle, S., Quereda, V., Grant, W., Cameron, M., Duckett, D., Roush, W. Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors Bioorganic & Medicinal Chemistry Letters  2018 28:400-404  DOI:10.1016/j.bmcl.2017.12.026  PMID:29277458
    • Wood, S. D., Grant, W., Adrados, I., Choi, J. Y., Alburger, J. M., Duckett, D. R., Roush, W. R. In silica HTS and structure based optimization of indazole-derived ULK1 inhibitors ACS Medicinal Chemistry Letters  2017 8:1258-1263  DOI:10.1021/acsmedchemlett.7b00344  PMID:29259744  PMCID:PMC5733266
    • Velagapudi, S. P., Cameron, M. D., Haga, C. L., Rosenberg, L. H., Lafitte, M., Duckett, D. R., Phinney, D. G., Disney, M. D. Design of a small molecule against an oncogenic noncoding RNA Proceedings of the National Academy of Sciences of the United States of America  2016 113:5898-5903  DOI:10.1073/pnas.1523975113  PMID:27170187  PMCID:PMC4889373
    • Rosenberg, L. H., Lafitte, M., Quereda, V., Grant, W., Chen, W., Bibian, M., Noguchi, Y., Fallahi, M., Yang, C., Chang, J. C., Roush, W. R., Cleveland, J. L., et al. Therapeutic targeting of casein kinase 1δ in breast cancer Science Translational Medicine  2015 7:318ra202  DOI:10.1126/scitranslmed.aac8773  PMID:26676609  PMCID:PMC4809734
    • Saunders, V. C., Lafitte, M., Adrados, I., Quereda, V., Feurstein, D., Ling, Y., Fallahi, M., Rosenberg, L. H., Duckett, D. R. Identification of an EGFRvIII-JNK2-HGF/c-Met-signaling axis required for intercellular crosstalk and glioblastoma multiforme cell invasion Molecular Pharmacology  2015 88:962-969  DOI:10.1124/mol.115.097774  PMID:26452771
    • Rosenberg, L. H., Lafitte, M., Grant, W., Chen, W., Cleveland, J. L., Duckett, D. R. Development of an HTS-compatible assay for the discovery of Ulk1 inhibitors Journal of Biomolecular Screening  2015 20:913-920  DOI:10.1177/1087057115579391  PMID:25851035  PMCID:PMC4744088
    • Corzo, C. A., Mari, Y., Chang, M. R., Khan, T., Kuruvilla, D., Nuhant, P., Kumar, N., West, G. M., Duckett, D. R., Roush, W. R., Griffin, P. R. Antiproliferation activity of a small molecule repressor of liver receptor homolog 1 Molecular Pharmacology  2015 87:296-304  DOI:10.1124/mol.114.095554  PMID:25473120  PMCID:PMC4293447
    • Sturchler, E., Chen, W., Spicer, T., Hodder, P., McDonald, P., Duckett, D. Development of an HTS-compatible assay for the discovery of ASK1 signalosome inhibitors using alphascreen technology Assay and Drug Development Technologies  2014 12:229-237  DOI:10.1089/adt.2013.558  PMID:24831789  PMCID:PMC4025566
    • He, Y., Duckett, D., Chen, W., Ling, Y. Y., Cameron, M. D., Lin, L., Ruiz, C. H., Lograsso, P. V., Kamenecka, T. M., Koenig, M. Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors Bioorganic & Medicinal Chemistry Letters  2014 24:161-164  DOI:10.1016/j.bmcl.2013.11.052  PMID:24332487  PMCID:PMC4540177
    • Bibian, M., Rahaim, R. J., Choi, J. Y., Noguchi, Y., Schurer, S., Chen, W. M., Nakanishi, S., Licht, K., Rosenberg, L. H., Li, L., Feng, Y., Cameron, M. D., et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties Bioorganic & Medicinal Chemistry Letters  2013 23:4374-4380  DOI:10.1016/j.bmcl.2013.05.075  PMID:23787102  PMCID:PMC3783656
    • Jiang, R., Frackowiak, B., Shin, Y. S., Song, X. Y., Chen, W. M., Lin, L., Cameron, M. D., Duckett, D. R., Kamenecka, T. M. Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2013 23:2683-2687  DOI:10.1016/j.bmcl.2013.02.082  PMID:23518277
    • Sturchler, E., Feurstein, D., Chen, W. M., McDonald, P., Duckett, D. Stress-induced nuclear import of apoptosis signal-regulating kinase 1 is mediated by karyopherin alpha 2/beta 1 heterodimer Biochimica et Biophysica Acta-Molecular Cell Research  2013 1833:583-592  DOI:10.1016/j.bbamcr.2012.10.023  PMID:23123190
    • Song, X., He, Y., Koenig, M., Shin, Y., Noel, R., Chen, W., Ling, Y. Y., Feurstein, D., Lin, L., Ruiz, C. H., Cameron, M. D., Duckett, D. R., et al. Synthesis and SAR of 2,4-diaminopyrimidines as potent c-jun n-terminal kinase inhibitors MedChemComm  2012 3:238-243  DOI:10.1039/c1md00219h
    • Song, X. Y., Chen, W. M., Lin, L., Ruiz, C. H., Cameron, M. D., Duckett, D. R., Kamenecka, T. M. Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2011 21:7072-7075  DOI:10.1016/j.bmcl.2011.09.090  PMID:22004719
    • Hara, M. R., Kovacs, J. J., Whalen, E. J., Rajagopal, S., Strachan, R. T., Grant, W., Towers, A. J., Williams, B., Lam, C. M., Xiao, K. H., Shenoy, S. K., Gregory, S. G., et al. A stress response pathway regulates DNA damage through beta(2)-adrenoreceptors and beta-arrestin-1 Nature  2011 477:349-353  DOI:10.1038/nature10368  PMID:21857681  PMCID:PMC3628753
    • Noel, R., Shin, Y., Song, X. Y., He, Y. J., Koenig, M., Chen, W. M., Ling, Y. Y., Lin, L., Ruiz, C. H., LoGrasso, P., Cameron, M. D., Duckett, D. R., et al. Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2011 21:2732-2735  DOI:10.1016/j.bmcl.2010.11.104  PMID:21185177  PMCID:PMC3081976
    • Chambers, J. W., Pachori, A., Howard, S., Ganno, M., Hansen, D., Song, X. Y., Kamenecka, T., Duckett, D., Chen, W. M., Ling, Y. Y., Cherry, L., Cameron, M. D. Small molecule c-jun-N-terminal Kinase (JNK) inhibitors protect dopaminergic neurons in a model of Parkinson's Disease ACS Chemical Neuroscience  2011 2:198-206  DOI:10.1021/cn100109k  PMID:21666839  PMCID:PMC3110074
    • He, Y. J., Kamenecka, T. M., Shin, Y. S., Song, X. Y., Jiang, R., Noel, R., Duckett, D., Chen, W. M., Ling, Y. Y., Cameron, M. D., Lin, L., Khan, S., et al. Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors Bioorganic & Medicinal Chemistry Letters  2011 21:1719-1723  DOI:10.1016/j.bmcl.2011.01.079  PMID:21316221  PMCID:PMC3052630
    • Kumar, N., Kojetin, D. J., Solt, L. A., Kumar, K. G., Nuhant, P., Duckett, D. R., Cameron, M. D., Butler, A. A., Roush, W. R., Griffin, P. R., Burris, T. P. Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist ACS Chemical Biology  2011 6:218-222  DOI:10.1021/cb1002762  PMID:21090593  PMCID:PMC3076127
    • Hahmann, C., Weiser, A., Duckett, D., Schroeter, T. A predictive nuclear translocation assay for spliced x-box-binding protein 1 identifies compounds with known organ toxicities Assay and Drug Development Technologies  2011 9:79-87  DOI:10.1089/adt.2010.0300  PMID:20858054
    • Duckett, D. R., Cameron, M. D. Metabolism considerations for kinase inhibitors in cancer treatment Expert Opinion on Drug Metabolism & Toxicology  2010 6:1175-1193  DOI:10.1517/17425255.2010.506873  PMID:20684746  PMCID:PMC2940961
    • Sturchler, E., Feurstein, D., McDonald, P., Duckett, D. Mechanism of oxidative stress-induced ASK1-catalyzed MKK6 phosphorylation Biochemistry  2010 49:4094-4102  DOI:10.1021/bi100010j  PMID:20364819
    • Kamenecka, T., Jiang, R., Song, X. Y., Duckett, D., Chen, W. M., Ling, Y. Y., Habel, J., Laughlin, J. D., Chambers, J., Figuera-Losada, M., Cameron, M. D., Lin, L., et al. Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors Journal of Medicinal Chemistry  2010 53:419-431  DOI:10.1021/jm901351f  PMID:19947601  PMCID:PMC2804074
    • Yin, Y., Lin, L., Ruiz, C., Cameron, M. D., Pocas, J., Grant, W., Schroter, T., Chen, W. M., Duckett, D., Schurer, S., LoGrasso, P., Feng, Y. B. Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors Bioorganic & Medicinal Chemistry Letters  2009 19:6686-6690  DOI:10.1016/j.bmcl.2009.09.115  PMID:19837589
    • Shin, Y. S., Chen, W. M., Habel, J., Duckett, D., Ling, Y. Y., Koenig, M., He, Y. J., Vojkovsky, T., LoGrasso, P., Kamenecka, T. M. Synthesis and sar of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors Bioorganic & Medicinal Chemistry Letters  2009 19:3344-3347  DOI:10.1016/j.bmcl.2009.03.086  PMID:19433357  PMCID:PMC2737472
    • Kamenecka, T., Habel, J., Duckett, D., Chen, W. M., Ling, Y. Y., Frackowiak, B., Jiang, R., Shin, Y. S., Song, X. Y., LoGrasso, P. Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-jun N-terminal kinase 3 (JNK3) over p38 Journal of Biological Chemistry  2009 284:12853-12861  DOI:10.1074/jbc.M809430200  PMID:19261605  PMCID:PMC2676016
    • Chen, Y. T., Bannister, T. D., Weiser, A., Griffin, E., Lin, L., Ruiz, C., Cameron, M. D., Schurer, S., Duckett, D., Schroter, T., LoGrasso, P., Feng, Y. B. Chroman-3-amides as potent Rho kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2008 18:6406-6409  DOI:10.1016/j.bmcl.2008.10.080  PMID:18990570
    • Heerding, D. A., Rhodes, N., Leber, J. D., Clark, T. J., Keenan, R. M., Lafrance, L. V., Li, M., Safonov, I. G., Takata, D. T., Venslavsky, J. W., Yamashita, D. S., Choudhry, A. E., et al. Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{ (3s)-3-piperidinylmethyl oxy}-1H-imidazo 4,5-c pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase Journal of Medicinal Chemistry  2008 51:5663-5679  DOI:10.1021/jm8004527  PMID:18800763
    • Rhodes, N., Heerding, D. A., Duckett, D. R., Eberwein, D. J., Knick, V. B., Lansing, T. J., McConnell, R. T., Gilmer, T. M., Zhang, S. Y., Robell, K., Kahana, J. A., Geske, R. S., et al. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity Cancer Research  2008 68:2366-2374  DOI:10.1158/0008-5472.can-07-5783  PMID:18381444
    • Jiang, R., Duckett, D., Chen, W., Habel, J., Ling, Y. Y., LoGrasso, P., Kamenecka, T. M. 3,5-disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2007 17:6378-6382  DOI:10.1016/j.bmcl.2007.08.054  PMID:17911023
    • Lansing, T. J., McConnell, R. T., Duckett, D. R., Spehar, G. M., Knick, V. B., Hassler, D. F., Noro, N., Furuta, M., Emmitte, K. A., Gilmer, T. M., Mook, R. A., Cheung, M. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1 Molecular Cancer Therapeutics  2007 6:450-459  DOI:10.1158/1535-7163.mct-06-0543  PMID:17267659
    • Rech, J. C., Yato, M., Duckett, D., Ember, B., LoGrasso, P. V., Bergman, R. G., Ellman, J. A. Synthesis of potent bicyclic bisarylimidazole c-jun N-terminal kinase inhibitors by catalytic C-H bond activation Journal of the American Chemical Society  2007 129:490-491  DOI:10.1021/ja0676004  PMID:17227002  PMCID:PMC2556147
    • Duckett, D. R., Bronstein, S. M., Taya, Y., Modrich, P. hMutS alpha- and hMutL alpha-dependent phosphorylation of p53 in response to DNA methylator damage Proceedings of the National Academy of Sciences of the United States of America  1999 96:12384-12388  DOI:10.1073/pnas.96.22.12384  PMID:10535931
    • Walter, F., Murchie, A. I. H., Duckett, D. R., Lilley, D. M. J. Global structure of four-way RNA junctions studied using fluorescence resonance energy transfer RNA-a Publication of the RNA Society  1998 4:719-728  DOI:10.1017/s135583829898030x  PMID:9622130
    • Duckett, D. R., Murchie, A. I. H., Clegg, R. M., Bassi, G. S., Giraud-Panis, M. J. E., Lilley, D. M. J. Nucleic acid structure and recognition Biophysical Chemistry  1997 68:53-62  DOI:10.1016/s0301-4622(97)00007-0  PMID:17029905
    • Mu, D., Tursun, M., Duckett, D. R., Drummond, J. T., Modrich, P., Sancar, A. Recognition and repair of compound DNA lesions (base damage and mismatch) by human mismatch repair and excision repair systems Molecular and Cellular Biology  1997 17:760-769  PMID:9001230  PMCID:PMC231802
    • Duckett, D. R., Drummond, J. T., Murchie, A. I. H., Reardon, J. T., Sancar, A., Lilley, D. M., Modrich, P. Human muts alpha recognizes damaged DNA base pairs containing O6-methylguanine, O4-methylthymine, or the cisplatin-d(GpG) adduct Proceedings of the National Academy of Sciences of the United States of America  1996 93:6443-6447  DOI:10.1073/pnas.93.13.6443  PMID:8692834
    • Duckett, D. R., Murchie, A. I. H., Lilley, D. M. J. The global folding of 4-way helical junctions in RNA, including that in U1 snRNA Cell  1995 83:1027-1036  DOI:10.1016/0092-8674(95)90218-x  PMID:8521503
    • Giraudpanis, M. J. E., Duckett, D. R., Lilley, D. M. J. The modular character of a DNA junction-resolving enzyme - a zinc-binding motif in bacteriophage-T4 endonuclease-VII Journal of Molecular Biology  1995 252:596-610  DOI:10.1006/jmbi.1995.0523  PMID:7563077
    • Duckett, D. R., Panis, Mjeg, Lilley, D. M. J. Binding of the junction-resolving enzyme bacteriophage-T7 endonuclease-I to DNA - separation of binding and catalysis by mutation Journal of Molecular Biology  1995 246:95-107  DOI:10.1006/jmbi.1994.0069  PMID:7853409
    • Duckett, D. R., Murchie, A. I. H., Giraudpanis, M. J. E., Pohler, J. R., Lilley, D. M. J. Structure of the four-way DNA junction and its interaction with proteins Philosophical Transactions of the Royal Society of London Series B-Biological Sciences  1995 347:27-36  DOI:10.1098/rstb.1995.0005  PMID:7746850
    • Pohler, J. R. G., Duckett, D. R., Lilley, D. M. J. Structure of four-way DNA junctions containing a nick in one strand Journal of Molecular Biology  1994 238:62-74  DOI:10.1006/jmbi.1994.1268  PMID:8145257
    • Welch, J. B., Duckett, D. R., Lilley, D. M. J. Structures of bulged three-way DNA junctions Nucleic Acids Research  1993 21:4548-4555  DOI:10.1093/nar/21.19.4548  PMID:8233789
    • Lilley, D. M. J., Bhattacharyya, A., McAteer, S. P., Duckett, D. R. Gel-electrophoretic analysis of the structure of nucleic-acids Biochemical Society Transactions  1993 21:111-116  PMID:7680620
    • Duckett, D. R., Murchie, A. I. H., Bhattacharyya, A., Clegg, R. M., Diekmann, S., Vonkitzing, E., Lilley, D. M. J. The structure of DNA junctions and their interaction with enzymes European Journal of Biochemistry  1992 207:285-295  DOI:10.1111/j.1432-1033.1992.tb17049.x  PMID:8425539
    • Duckett, D. R., Lilley, D. M. J. Effects of base mismatches on the structure of the four-way DNA junction Journal of Molecular Biology  1991 221:147-161  DOI:10.1016/0022-2836(91)90811-j  PMID:1920402
    • Duckett, D. R., Lilley, D. M. J. The three-way DNA junction is a Y-shaped molecule in which there is no helix-helix stacking EMBO Journal  1990 9:1659-1664  PMID:2328731  PMCID:PMC551862
    • Duckett, D. R., Murchie, A. I. H., Lilley, D. M. J. The role of metal-ions in the conformation of the four-way DNA junction EMBO Journal  1990 9:583-590  PMID:2303044  PMCID:PMC551705
    • Murchie, A. I. H., Clegg, R. M., Vonkitzing, E., Duckett, D. R., Diekmann, S., Lilley, D. M. J. Fluorescence energy-transfer shows that the four-way DNA junction is a right-handed cross of antiparallel molecules Nature  1989 341:763-766  DOI:10.1038/341763a0  PMID:2797209
    • Duckett, D. R., Murchie, A. I. H., Diekmann, S., Vonkitzing, E., Kemper, B., Lilley, D. M. J. The structure of the Holliday junction, and its resolution Cell  1988 55:79-89  DOI:10.1016/0092-8674(88)90011-6  PMID:3167979

featured in

  • Scientists Pinpoint a Cause of Stress-Related DNA Damage  Newsletter
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Research

research overview

  • Work in our laboratory is aimed at evaluating small molecule kinase inhibitors of biologic and therapeutic interest. We are currently involved in refining a novel class of kinase inhibitors aimed at the therapeutic treatment of human diseases such as Parkinson’s Disease and Cancer. Protein kinases are important components of signal transduction pathways and deregulation of kinase activity can lead to human disease. Kinases have therefore become one of the most important target classes for drug development. Working closely with other disciplines such as chemistry, pharmacology, and drug metabolism, we aim to optimize lead compounds for potency and selectivity while minimizing toxicity to generate candidate molecules with appropriate drug like properties suitable for IND enabling and first time in human studies.
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Background

education and training

  • Ph.D. in Biochemistry, The University of Dundee 1990
  • B.Sc. in Molecular Biology, University of Glasgow 1986
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Contact

full name

  • Derek R. Duckett

geographic location

  • Scripps Florida 

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