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Garbaccio, Robert
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Garbaccio, Robert

Graduate Student
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Positions

  • 2001 - Senior Principal Scientist, Merck & Co., Inc.
  • 1999 - 2001 Postdoctoral Research Fellow, Memorial Sloan Kettering Cancer Center

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Publications

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    • Campos, K. R., Coleman, P. J., Alvarez, J. C., Dreher, S. D., Garbaccio, R. M., Terrett, N. K., Tillyer, R. D., Truppo, M. D., Parmee, E. R. The importance of synthetic chemistry in the pharmaceutical industry Science  2019 363  DOI:10.1126/science.aat0805  PMID:30655413
    • Brandish, P. E., Palmieri, A., Antonenko, S., Beaumont, M., Benso, L., Cancilla, M., Cheng, M., Fayadat-Dilman, L., Feng, G., Figueroa, I., Firdos, J., Garbaccio, R., et al. Development of anti-CD74 antibody-drug conjugates to target glucocorticoids to immune cells Bioconjugate Chemistry  2018 29:2357-2369  DOI:10.1021/acs.bioconjchem.8b00312  PMID:29923706
    • Layton, M. E., Reif, A. J., Hartingh, T. J., Rodzinak, K., Dudkin, V., Wang, C., Arrington, K., Kelly, M. J., Garbaccio, R. M., O'Brien, J. A., Magliaro, B. C., Uslaner, J. M., et al. Discovery of 5-aryl-1,3-dihydro-2H-imidazo 4,5-b pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis Bioorganic & Medicinal Chemistry Letters  2016 26:1260-1264  DOI:10.1016/j.bmcl.2016.01.021  PMID:26810316
    • Kern, J. C., Cancilla, M., Dooney, D., Kwasnjuk, K., Zhang, R., Beaumont, M., Figueroa, I., Hsieh, S., Liang, L. D., Tomazela, D., Zhang, J., Brandish, P. E., et al. Discovery of pyrophosphate diesters as tunable, soluble, and bioorthogonal linkers for site-specific antibody-drug conjugates Journal of the American Chemical Society  2016 138:1430-1445  DOI:10.1021/jacs.5b12547
    • Kern, J. C., Dooney, D., Zhang, R., Liang, L., Brandish, P. E., Cheng, M., Feng, G., Beck, A., Bresson, D., Firdos, J., Gately, D., Knudsen, N., et al. Novel phosphate modified cathepsin B linkers: improving aqueous solubility and enhancing payload scope of ADCs Bioconjugate Chemistry  2016 27:2081-2088  DOI:10.1021/acs.bioconjchem.6b00337  PMID:27469406
    • Pero, J. E., Rossi, M. A., Kelly, M. J., Lehman, Hdgf, Layton, M. E., Garbaccio, R. M., O'Brien, J. A., Magliaro, B. C., Uslaner, J. M., Huszar, S. L., Fillgrove, K. L., Tang, C., et al. Optimization of novel Aza-benzimidazolone mGluR2 PAMs with respect to LLE and PK properties and mitigation of CYP TDI ACS Medicinal Chemistry Letters  2016 7:312-317  DOI:10.1021/acsmedchemlett.5b00459  PMID:26985321  PMCID:PMC4789683
    • Pei, T., Liao, J., Williams, J. M., Xiang, R., Garbaccio, R. M., Barrett, S. E., Guidry, E. N. Size controlled synthesis of ornithine‐based polypeptides by ring‐opening polymerization of α‐(amino acid)‐N‐carboxyanhydrides Journal of Polymer Science Part a-Polymer Chemistry  2016 54:311-315  DOI:10.1002/pola.27920
    • Garbaccio, R. M., Parmee, E. R. The impact of chemical probes in drug discovery: a pharmaceutical industry perspective Cell Chemical Biology  2016 23:10-17  DOI:10.1016/j.chembiol.2015.11.011
    • Garbaccio, R. M., Johnson, D. S., Hong, J., Disney, M. D. Recent advances in medicinal chemistry and chemical biology. Preface. Bioorganic & Medicinal Chemistry Letters  2015 25:4714-4714  DOI:10.1016/j.bmcl.2015.08.083
    • Converso, A., Hartingh, T., Fraley, M. E., Garbaccio, R. M., Hartman, G. D., Huang, S. Y., Majercak, J. M., McCampbell, A., Na, S. J., Ray, W. J., Savage, M. J., Wolffe, C., et al. Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase Bioorganic & Medicinal Chemistry Letters  2014 24:2737-2740  DOI:10.1016/j.bmcl.2014.04.034  PMID:24813734
    • Barrett, S. E., Abrams, M. T., Burke, R., Carr, B. A., Crocker, L. S., Garbaccio, R. M., Howell, B. J., Kemp, E. A., Kowtoniuk, R. A., Latham, A. H., Leander, K. R., Leone, A. M., et al. An in vivo evaluation of amphiphilic, biodegradable peptide copolymers as siRNA delivery agents International Journal of Pharmaceutics  2014 466:58-67  DOI:10.1016/j.ijpharm.2014.03.011  PMID:24607208
    • Barrett, S. E., Burke, R. S., Abrams, M. T., Bason, C., Busuek, M., Carlini, E., Carr, B. A., Crocker, L. S., Fan, H., Garbaccio, R. M., Guidry, E. N., Heo, J. H., et al. Development of a liver-targeted siRNA delivery platform with a broad therapeutic window utilizing biodegradable polypeptide-based polymer conjugates Journal of Controlled Release  2014 183:124-137  DOI:10.1016/j.jconrel.2014.03.028  PMID:24657948
    • Guidry, E. N., Farand, J., Soheili, A., Parish, C. A., Kevin, N. J., Pipik, B., Calati, K. B., Ikemoto, N., Waldman, J. H., Latham, A. H., Howell, B. J., Leone, A., et al. Improving the in vivo therapeutic index of siRNA polymer conjugates through increasing pH responsiveness Bioconjugate Chemistry  2014 25:296-307  DOI:10.1021/bc400442p  PMID:24409989
    • Parmar, R. G., Poslusney, M., Busuek, M., Williams, J. M., Garbaccio, R., Leander, K., Walsh, E., Howell, B., Sepp-Lorenzino, L., Riley, S., Patel, M., Kemp, E., et al. Novel endosomolytic poly(amido amine) polymer conjugates for systemic delivery of siRNA to hepatocytes in rodents and nonhuman primates Bioconjugate Chemistry  2014 25:896-906  DOI:10.1021/bc400527e  PMID:24742200
    • Kowtoniuk, R. A., Pei, T., DeAngelo, C. M., Waldman, J. H., Guidry, E. N., Williams, J. M., Garbaccio, R. M., Barrett, S. E. Optimization of an α‐(Amino acid)‐N‐carboxyanhydride polymerization using the high vacuum technique: Examining the effects of monomer concentration, polymerization kinetics, polymer molecular weight, and monomer purity Journal of Polymer Science Part a-Polymer Chemistry  2014 52:1385-1391  DOI:10.1002/pola.27132
    • Parmar, R. G., Busuek, M., Walsh, E. S., Leander, K. R., Howell, B. J., Sepp-Lorenzino, L., Kemp, E., Crocker, L. S., Leone, A., Kochansky, C. J., Carr, B. A., Garbaccio, R. M., et al. Endosomolytic bioreducible poly(amido amine disulfide) polymer conjugates for the in vivo systemic delivery of siRNA therapeutics Bioconjugate Chemistry  2013 24:640-647  DOI:10.1021/bc300600a  PMID:23496378
    • Brnardic, E. J., Fraley, M. E., Garbaccio, R. M., Layton, M. E., Sanders, J. M., Culberson, C., Jacobson, M. A., Magliaro, B. C., Hutson, P. H., O'Brien, J. A., Huszar, S. L., Uslaner, J. M., et al. 3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts Bioorganic & Medicinal Chemistry Letters  2010 20:3129-3133  DOI:10.1016/j.bmcl.2010.03.089  PMID:20409708
    • Cox, C. D., Garbaccio, R. M. Discovery of allosteric inhibitors of kinesin spindle protein (KSP) for the treatment of taxane-refractory cancer: MK-0731 and analogs Anti-Cancer Agents in Medicinal Chemistry  2010 10:697-712  DOI:10.2174/187152010794479807  PMID:21235439
    • Garbaccio, R. M., Brnardic, E. J., Fraley, M. E., Hartman, G. D., Hutson, P. H., O'Brien, J. A., Magliaro, B. C., Uslaner, J. M., Huszar, S. L., Fillgrove, K. L., Small, J. H., Tang, C., et al. Discovery of oxazolobenzimidazoles as positive allosteric modulators for the mGluR2 receptor ACS Medicinal Chemistry Letters  2010 1:406-410  DOI:10.1021/ml100115a  PMID:24900224  PMCID:PMC4007895
    • Li, C., Lu, B., Garbaccio, R. M., Tasber, E. S., Fraley, M. E., Hartman, G. D., Ye, J., Harrelson, J. C., Prueksaritanont, T. Stereospecific reduction of a potent kinesin spindle protein (KSP) inhibitor in human tissues Biochemical Pharmacology  2010 79:1526-1533  DOI:10.1016/j.bcp.2010.01.024  PMID:20109439
    • Converso, A., Hartingh, T., Garbaccio, R. M., Tasber, E., Rickert, K., Fraley, M. E., Yan, Y., Kreatsoulas, C., Stirdivant, S., Drakas, B., Walsh, E. S., Hamilton, K., et al. Development of thioquinazolinones, allosteric Chk1 kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2009 19:1240-1244  DOI:10.1016/j.bmcl.2008.12.076  PMID:19155174
    • Rickert, K. W., Schaber, M., Torrent, M., Neilson, L. A., Tasber, E. S., Garbaccio, R., Coleman, P. J., Harvey, D., Zhang, Y., Yang, Y., Marshall, G., Lee, L., et al. Discovery and biochemical characterization of selective ATP competitive inhibitors of the human mitotic kinesin KSP Archives of Biochemistry and Biophysics  2008 469:220-231  DOI:10.1016/j.abb.2007.10.016  PMID:17999913
    • Cox, C. D., Coleman, P. J., Breslin, M. J., Whitman, D. B., Garbaccio, R. M., Fraley, M. E., Buser, C. A., Walsh, E. S., Hamilton, K., Schaber, M. D., Lobell, R. B., Tao, W., et al. Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]- 2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer Journal of Medicinal Chemistry  2008 51:4239-4252  DOI:10.1021/jm800386y  PMID:18578472
    • Coleman, P. J., Schreler, J. D., Cox, C. D., Fraley, M. E., Garbaccio, R. M., Buser, C. A., Walsh, E. S., Hamilton, K., Lobell, R. B., Rickert, K., Tao, W. K., Diehl, R. E., et al. Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP Bioorganic & Medicinal Chemistry Letters  2007 17:5390-5395  DOI:10.1016/j.bmcl.2007.07.046  PMID:17761419
    • Garbaccio, R. M., Tasbera, E. S., Neilson, L. A., Coleman, P. J., Fraley, M. E., Olson, C., Bergman, J., Torrent, M., Buser, C. A., Rickert, K., Walsh, E. S., Hamilton, K., et al. Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP Bioorganic & Medicinal Chemistry Letters  2007 17:5671-5676  DOI:10.1016/j.bmcl.2007.07.067  PMID:17804233
    • Cox, C. D., Breslin, M. J., Whitman, D. B., Coleman, P. J., Garbaccio, R. M., Fraley, M. E., Zrada, M. M., Buser, C. A., Walsh, E. S., Hamilton, K., Lobell, R. B., Tao, W., et al. Kinesin spindle protein (KSP) inhibitors. Part V: Discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein Bioorganic & Medicinal Chemistry Letters  2007 17:2697-2702  DOI:10.1016/j.bmcl.2007.03.006  PMID:17395460
    • Brnardic, E. J., Garbaccio, R. M., Fraley, M. E., Tasber, E. S., Steen, J. T., Arrington, K. L., Dudkin, V. Y., Hartman, G. D., Stirdivant, S. M., Drakas, B. A., Rickert, K., Walsh, E. S., et al. Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2007 17:5989-5994  DOI:10.1016/j.bmcl.2007.07.051  PMID:17804227
    • Garbaccio, R. M., Huang, S., Tasber, E. S., Fraley, M. E., Yan, Y., Munshi, S., Ikuta, M., Kuo, L., Kreatsoulas, C., Stirdivant, S., Drakas, B., Rickert, K., et al. Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase Bioorganic & Medicinal Chemistry Letters  2007 17:6280-6285  DOI:10.1016/j.bmc1.2007.09.007  PMID:17900896
    • Huang, S. E., Garbaccio, R. M., Fraley, M. E., Steen, J., Kreatsoulas, C., Hartman, G., Stirdivant, S., Drakas, B., Rickert, K., Walsh, E., Hamilton, K., Buser, C. A., et al. Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2006 16:5907-5912  DOI:10.1016/j.bmcl.2006.08.053  PMID:16990002
    • Fraley, M. E., Garbaccio, R. M., Arrington, K. L., Hoffman, W. F., Tasber, E. S., Coleman, P. J., Buser, C. A., Walsh, E. S., Hamilton, K., Fernandes, C., Schaber, M. D., Lobell, R. B., et al. Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP Bioorganic & Medicinal Chemistry Letters  2006 16:1775-1779  DOI:10.1016/j.bmcl.2006.01.030  PMID:16439123
    • Garbaccio, R. M., Fraley, M. E., Tasber, E. S., Olson, C. M., Hoffman, W. F., Arrington, K. L., Torrent, M., Buser, C. A., Walsh, E. S., Hamilton, K., Schaber, M. D., Fernandes, C., et al. Kinesin spindle protein (KSP) inhibitors. Part 3: Synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility Bioorganic & Medicinal Chemistry Letters  2006 16:1780-1783  DOI:10.1016/j.bmcl.2005.12.094  PMID:16439122
    • Tasber, E. S., Garbaccio, R. M. Thermodynamic equilibration of dihydropyridone enolates: application to the total synthesis of (+/-)-epiuleine Tetrahedron Letters  2003 44:9185-9188  DOI:10.1016/j.tetlet.2003.10.030
    • Yamamoto, K., Garbaccio, R. M., Stachel, S. J., Solit, D. B., Chiosis, G., Rosen, N., Danishefsky, S. J. Total synthesis as a resource in the discovery of potentially valuable antitumor agents: cycloproparadicicol Angewandte Chemie - International Edition  2003 42:1280-1284  DOI:10.1002/anie.200390329  PMID:12645064
    • Garbaccio, R. M., Stachel, S. J., Baeschlin, D. K., Danishefsky, S. J. Concise asymmetric syntheses of radicicol and monocillin I Journal of the American Chemical Society  2001 123:10903-10908  DOI:10.1021/ja011364+  PMID:11686693
    • degree-related publication Boger, D. L., Brunette, S. R., Garbaccio, R. M. Synthesis and evaluation of a series of C3-substituted CBI analogues of CC-1065 and the duocarmycins Journal of Organic Chemistry  2001 66:5163-5173  DOI:10.1021/jo010309g  PMID:11463270
    • Garbaccio, R. M., Danishefsky, S. J. Efficient asymmetric synthesis of radicicol dimethyl ether: A novel application of ring-forming olefin metathesis Organic Letters  2000 2:3127-3129  DOI:10.1021/ol0063252  PMID:11009362
    • degree-related publication Boger, D. L.*, Garbaccio, R. M.* A novel class of CC-1065 and duocarmycin analogues subject to mitomycin-related reductive activation Journal of Organic Chemistry  1999 64:8350-8362  DOI:10.1021/jo991301y  PMID:11674758 (* = equal contribution)
    • degree-related publication Boger, D. L.*, Garbaccio, R. M.* Are the duocarmycin and CC-1065 DNA alkylation reactions acid-catalyzed? Solvolysis pH-rate profiles suggest they are not Journal of Organic Chemistry  1999 64:5666-5669  DOI:10.1021/jo990762g  PMID:11674637 (* = equal contribution)
    • degree-related publication Boger, D. L.*, Boyce, C. W.*, Garbaccio, R. M., Searcey, M., Jin, Q. CBI prodrug analogs of CC-1065 and the duocarmycins Synthesis-Stuttgart  1999 1505-1509 (* = equal contribution)
    • degree-related publication Boger, D. L.*, Garbaccio, R. M.* Shape-dependent catalysis: Insights into the source of catalysis for the CC-1065 and duocarmycin DNA alkylation reaction Accounts of Chemical Research  1999 32:1043-1052  DOI:10.1021/ar9800946 (* = equal contribution)
    • degree-related publication Boger, D. L., Schaum, R. P., Garbaccio, R. M. Regioselective inverse electron demand Diels-Alder reactions of N-acyl 6-amino-3-(methylthio)-1,2,4,5-tetrazines Journal of Organic Chemistry  1998 63:6329-6337  DOI:10.1021/jo980795g  PMID:11672266
    • degree-related publication Boger, D. L.*, Boyce, C. W.*, Garbaccio, R. M., Searcey, M. Synthesis of CC-1065 and duocarmycin analogs via intramolecular aryl radical cyclization of a tethered vinyl chloride Tetrahedron Letters  1998 39:2227-2230  DOI:10.1016/s0040-4039(98)00232-9 (* = equal contribution)
    • degree-related publication Boger, D. L.*, Boyce, C. W.*, Garbaccio, R. M., Goldberg, J. A. CC-1065 and the duocarmycins: Synthetic studies Chemical Reviews  1997 97:787-828  DOI:10.1021/cr960095g  PMID:11848889 (* = equal contribution)
    • degree-related publication Boger, D. L.*, Garbaccio, R. M.* Catalysis of the CC-1065 and duocarmycin DNA alkylation reaction: DNA binding induced conformational change in the agent results in activation Bioorganic & Medicinal Chemistry  1997 5:263-276  DOI:10.1016/s0968-0896(96)00238-6  PMID:9061191 (* = equal contribution)
    • degree-related publication Boger, D. L., Bollinger, B., Hertzog, D. L., Johnson, D. S., Cai, H., Mesini, P., Garbaccio, R. M., Jin, Q., Kitos, P. A. Reversed and sandwiched analogs of duocarmycin SA: Establishment of the origin of the sequence-selective alkylation of DNA and new insights into the source of catalysis Journal of the American Chemical Society  1997 119:4987-4998  DOI:10.1021/ja9637210
    • degree-related publication Boger, D. L.*, Garbaccio, R. M.*, Jin, Q. Synthesis and evaluation of CC-1065 and duocarmycin analogues incorporating the iso-CI and iso-CBI alkylation subunits: impact of relocation of the C-4 carbonyl Journal of Organic Chemistry  1997 62:8875-8891  DOI:10.1021/jo971686p (* = equal contribution)
    • Panek, J. S.*, Garbaccio, R. M.*, Jain, N. F. Diastereoselectivity in cyclopropanation and epoxidation reactions of chiral (E)-crotylsilanes: asymmetric synthesis of substituted tetrahydrofurans Tetrahedron Letters  1994 35:6453-6456  DOI:10.1016/s0040-4039(00)78244-x (* = equal contribution)
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Background

education and training

  • Ph.D. in Chemistry, Scripps Research 1994 - 1999
  • B.A. in Chemistry, Boston University 1990 - 1994

advisee of

  • faculty mentoring relationship

    • Boger, Dale, Ph.D.  candidacy, 1995 - 1999
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Contact

full name

  • Robert Michael Garbaccio

geographic location

  • Scripps California 

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