Dale Boger

Summary

Affiliation: The Scripps Research Institute
Country: USA

Publications

  1. pmc Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase
    F Anthony Romero
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 50:1058-68. 2007
  2. pmc Bryostatin analog: improving on Nature's design
    Dale Boger
    The Scripps Cancer Research Institute, CA, USA
    Oncotarget 3:116-7. 2012
  3. pmc Structural requirements for 5-HT2A and 5-HT1A serotonin receptor potentiation by the biologically active lipid oleamide
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Proc Natl Acad Sci U S A 95:4102-7. 1998
  4. ncbi request reprint Cytokine receptor dimerization and activation: prospects for small molecule agonists
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem 9:557-62. 2001
  5. ncbi request reprint alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 11:1517-20. 2001
  6. ncbi request reprint Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 11:2021-4. 2001
  7. ncbi request reprint Synthesis and evaluation of a series of C3-substituted CBI analogues of CC-1065 and the duocarmycins
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 66:5163-73. 2001
  8. ncbi request reprint Thiazole orange as the fluorescent intercalator in a high resolution fid assay for determining DNA binding affinity and sequence selectivity of small molecules
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 9:2511-8. 2001
  9. ncbi request reprint Parallel synthesis and evaluation of 132 (+)-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) analogues of CC-1065 and the duocarmycins defining the contribution of the DNA-binding domain
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 66:6654-61. 2001
  10. ncbi request reprint Vancomycin, teicoplanin, and ramoplanin: synthetic and mechanistic studies
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, USA
    Med Res Rev 21:356-81. 2001

Research Grants

  1. ANTITUMOR ANTIBIOTICS: CC-1065 AND BLEOMYCINS
    Dale Boger; Fiscal Year: 1991
  2. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2003
  3. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2005
  4. THE ANTITUMOR ANTIBIOTICS CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2003
  5. THE ANTITUMOR ANTIBIOTICS CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2007
  6. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2000
  7. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2007
  8. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale L Boger; Fiscal Year: 2010
  9. THE ANTITUMOR ANTIBIOTICS CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2009
  10. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2001

Collaborators

Detail Information

Publications94

  1. pmc Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase
    F Anthony Romero
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 50:1058-68. 2007
    ..Proteomic-wide screening of the inhibitors revealed that most are exquisitely selective for FAAH over all other mammalian proteases, reversing the 100-fold preference of 20a (C5 substituent = H) for the enzyme TGH...
  2. pmc Bryostatin analog: improving on Nature's design
    Dale Boger
    The Scripps Cancer Research Institute, CA, USA
    Oncotarget 3:116-7. 2012
    ....
  3. pmc Structural requirements for 5-HT2A and 5-HT1A serotonin receptor potentiation by the biologically active lipid oleamide
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Proc Natl Acad Sci U S A 95:4102-7. 1998
    ....
  4. ncbi request reprint Cytokine receptor dimerization and activation: prospects for small molecule agonists
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem 9:557-62. 2001
    ..The prospects of discovering small-molecule mimetics of such receptor agonists are discussed, including strategies which have led to the identification of a small number of peptide and non-peptide cytokine mimetics...
  5. ncbi request reprint alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 11:1517-20. 2001
    ..Both the electrophilic carbonyl and the degree of alpha-substitution markedly affect inhibitor potency...
  6. ncbi request reprint Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 11:2021-4. 2001
    ....
  7. ncbi request reprint Synthesis and evaluation of a series of C3-substituted CBI analogues of CC-1065 and the duocarmycins
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 66:5163-73. 2001
    ..The implications of these observations on the source of catalysis for the DNA alkylation reaction of the natural products are discussed...
  8. ncbi request reprint Thiazole orange as the fluorescent intercalator in a high resolution fid assay for determining DNA binding affinity and sequence selectivity of small molecules
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 9:2511-8. 2001
    ..Utilizing a library of hairpin deoxyoligonucleotides containing all possible four base-pair sequences, the method provides a high resolution profile of the DNA binding properties of small molecules in a high throughput format...
  9. ncbi request reprint Parallel synthesis and evaluation of 132 (+)-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) analogues of CC-1065 and the duocarmycins defining the contribution of the DNA-binding domain
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 66:6654-61. 2001
    ....
  10. ncbi request reprint Vancomycin, teicoplanin, and ramoplanin: synthetic and mechanistic studies
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, USA
    Med Res Rev 21:356-81. 2001
    ..This work lays the foundation for ongoing structure-function studies on the antibiotics that may clarify or define their site and mechanism of action leading to the development of improved or reengineered antibiotics...
  11. pmc Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics
    Dale L Boger
    Department of Chemistry, Cell Biology, and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 48:1849-56. 2005
    ....
  12. ncbi request reprint Solution-phase combinatorial libraries: modulating cellular signaling by targeting protein-protein or protein-DNA interactions
    Dale L Boger
    Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Angew Chem Int Ed Engl 42:4138-76. 2003
    ....
  13. ncbi request reprint Synthesis, chemical properties, and biological evaluation of CC-1065 and duocarmycin analogues incorporating the 5-methoxycarbonyl-1,2,9,9a-tetrahydrocyclopropa
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 66:2207-16. 2001
    ....
  14. ncbi request reprint Total synthesis of Amaryllidaceae alkaloids utilizing sequential intramolecular heterocyclic azadiene Diels-Alder reactions of an unsymmetrical 1,2,4,5-tetrazine
    D L Boger
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 65:9120-4. 2000
    ..Convergent total syntheses of anhydrolycorinone, hippadine, and anhydrolycorinium chloride are detailed, enlisting sequential inverse electron demand Diels-Alder reactions of an unsymmetrical N-acyl-6-amino-1,2,4,5-tetrazine...
  15. ncbi request reprint Fatty acid amide hydrolase substrate specificity
    D L Boger
    Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 10:2613-6. 2000
    ..FAAH hydrolyzes a range of fatty acid amides, and the present study examines the relative rates of hydrolysis of a variety of natural and unnatural fatty acid primary amide substrates using pure recombinant rat FAAH...
  16. pmc Chemical requirements for inhibition of gap junction communication by the biologically active lipid oleamide
    D L Boger
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Proc Natl Acad Sci U S A 95:4810-5. 1998
    ..A select set of agents has been identified that serves both as oleamide agonists and as inhibitors of fatty acid amide hydrolase, which is responsible for the rapid inactivation of oleamide...
  17. ncbi request reprint Oleamide: an endogenous sleep-inducing lipid and prototypical member of a new class of biological signaling molecules
    D L Boger
    Department of Chemistry, Scripps Research Institute, La Jolla, California 92037, USA
    Curr Pharm Des 4:303-14. 1998
    ..Oleamide has been shown to modulate serotonergic neurotransmission and inhibit intercellular gap junction communication and detailed studies of its well defined and selective structural features required for activity have been disclosed...
  18. ncbi request reprint Bifunctional alkylating agents derived from duocarmycin SA: potent antitumor activity with altered sequence selectivity
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 10:495-8. 2000
    ..The series of four dimers derived from head to tail coupling of the two enantiomers of the duocarmycin SA alkylation subunit are described...
  19. pmc Exceptionally potent inhibitors of fatty acid amide hydrolase: the enzyme responsible for degradation of endogenous oleamide and anandamide
    D L Boger
    Department of Chemistry, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Proc Natl Acad Sci U S A 97:5044-9. 2000
    ....
  20. ncbi request reprint A new class of highly cytotoxic diketopiperazines
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 10:1019-20. 2000
    ..The discovery of a novel class of diketopiperazines possessing potent cytotoxic activity is described...
  21. ncbi request reprint Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem 8:1075-86. 2000
    ....
  22. ncbi request reprint Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 10:1471-5. 2000
    ..These agents incorporate an electrophilic fluoronitrophenyl group that can potentially react with an active site nucleophile or the substrate GAR/AICAR amine via nucleophilic aromatic substitution...
  23. ncbi request reprint Synthesis and evaluation of aza HUN-7293
    D L Boger
    Department of Chemistry, The Scripps Research Institute, La Jolla, California 92037, USA
    Bioorg Med Chem Lett 10:1741-4. 2000
    ..Biological evaluations of these two compounds as inhibitors of cell adhesion molecules expression are detailed...
  24. ncbi request reprint Development of a solution-phase synthesis of minor groove binding bis-intercalators based on triostin A suitable for combinatorial synthesis
    D L Boger
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 65:5996-6000. 2000
    ....
  25. ncbi request reprint Assessment of solution-phase positional scanning libraries based on distamycin A for the discovery of new DNA binding agents
    D L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem 8:2049-57. 2000
    ..Thus, the disadvantages associated with the loss of some information contained within the library must be balanced against the advantages of the ease of library synthesis and judged in light of the library screening objectives...
  26. ncbi request reprint Solution-phase synthesis of combinatorial libraries designed to modulate protein-protein or protein-DNA interactions
    Dale L Boger
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 11:1607-13. 2003
    ....
  27. pmc Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase
    Joie Garfunkle
    Department of Chemistry, The Skaggs Institute for Chemical Biology, La Jolla, California 92037, USA
    J Med Chem 51:4392-403. 2008
    ..These trends, exemplified herein, emerge from both enhancements in the FAAH activity and simultaneous disruption of binding affinity for competitive off-target enzymes...
  28. pmc Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase
    Ian M Slaymaker
    Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 18:5847-50. 2008
    ....
  29. pmc Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts
    Thorsten Berg
    Department of Molecular and Experimental Medicine, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Proc Natl Acad Sci U S A 99:3830-5. 2002
    ..Our work provides proof of principle for the identification of small molecule inhibitors of protein-protein interactions by using high-throughput screens of combinatorial chemical libraries...
  30. ncbi request reprint High-resolution assessment of protein DNA binding affinity and selectivity utilizing a fluorescent intercalator displacement (FID) assay
    Young Wan Ham
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 13:3805-7. 2003
    ....
  31. ncbi request reprint Erythropoietin mimetics derived from solution phase combinatorial libraries
    Joel Goldberg
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 124:544-55. 2002
    ..An additional compound library, based on a symmetrical isoindoline-5,6-dicarboxylic acid template and including the optimized binding subunits, was synthesized and screened leading to the identification of additional EPO mimetics...
  32. pmc Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase
    F Scott Kimball
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 51:937-47. 2008
    ..Combination of these independent features, which display generalized trends across a range of inhibitor series, simultaneously improves FAAH potency and selectivity and can provide exquisitely selective and potent FAAH inhibitors...
  33. pmc Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase
    Jessica K DeMartino
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 N Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 18:5842-6. 2008
    ..90) with a slope of 3.37 (rho=3.37), that is of a magnitude that indicates that of the electron-withdrawing character of the substituent dominates its effects (a one unit change in sigma(m) provides a >1000-fold change in K(i))...
  34. pmc X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase
    Mauro Mileni
    Department of Chemistry, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 53:230-40. 2010
    ..The detailed analysis of their key active site interactions and their implications on the interpretation of the available structure-activity relationships are discussed providing important insights for future design...
  35. ncbi request reprint Discovering potent and selective reversible inhibitors of enzymes in complex proteomes
    Donmienne Leung
    The Skaggs Institute for Chemical Biology and the Department of Chemistry, The Scripps Research Institute, 10550 N Torrey Pines Road, La Jolla, California 92037, USA
    Nat Biotechnol 21:687-91. 2003
    ..In this way, promiscuous inhibitors were readily rejected in favor of equally potent compounds with 500-fold or greater selectivity for their targets...
  36. ncbi request reprint Sequence-selective DNA recognition: natural products and nature's lessons
    Winston C Tse
    Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA
    Chem Biol 11:1607-17. 2004
    ..These attributes arise in compact structures of complex integrated function...
  37. ncbi request reprint Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity
    Donmienne Leung
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 15:1423-8. 2005
    ....
  38. ncbi request reprint Inhibitors of cell migration that inhibit intracellular paxillin/alpha4 binding: a well-documented use of positional scanning libraries
    Yves Ambroise
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Chem Biol 9:1219-26. 2002
    ..Their parallel testing provided the rare opportunity to critically compare two approaches...
  39. pmc Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase
    Christophe Hardouin
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 50:3359-68. 2007
    ..Proteome-wide screening of selected inhibitors from the systematic series of >100 candidates prepared revealed that they are selective for FAAH over all other mammalian serine proteases...
  40. pmc Rational design, synthesis, and evaluation of key analogues of CC-1065 and the duocarmycins
    Mark S Tichenor
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 129:14092-9. 2007
    ..Both exhibited efficiencies of DNA alkylation that correlate with this enhanced potency without impacting the intrinsic selectivity characteristic of this class of antitumor agents...
  41. ncbi request reprint Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase
    Thomas H Marsilje
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 11:4487-501. 2003
    ....
  42. pmc Design, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions
    Alex Shaginian
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 131:5564-72. 2009
    ..g., an alpha-helix mediated protein-protein interaction) and define the key residues and their characteristics responsible for recognition...
  43. pmc Binding and inactivation mechanism of a humanized fatty acid amide hydrolase by alpha-ketoheterocycle inhibitors revealed from cocrystal structures
    Mauro Mileni
    Departments of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 131:10497-506. 2009
    ....
  44. pmc Synthesis and evaluation of vancomycin aglycon analogues that bear modifications in the N-terminal D-leucyl amino acid
    Christine M Crane
    Department of Chemistry, The Scripps Research Institute, La Jolla, California 92037, USA
    J Med Chem 52:1471-6. 2009
    ....
  45. ncbi request reprint Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
    Yan Zhang
    Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Biochemistry 42:6043-56. 2003
    ....
  46. ncbi request reprint Design, synthesis, and biological evaluation of 10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF, and 10-methylthio-DDACTHF as potent inhibitors of GAR Tfase and the de novo purine biosynthetic pathway
    Heng Cheng
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 13:3577-85. 2005
    ..0 microM and 2, IC50 = 2.0 microM)...
  47. ncbi request reprint Elucidation of fatty acid amide hydrolase inhibition by potent alpha-ketoheterocycle derivatives from Monte Carlo simulations
    Cristiano Ruch Werneck GuimarĂ£es
    Department of Chemistry, Yale University, 225 Prospect Street, New Haven, Connecticut 06520 8107, USA
    J Am Chem Soc 127:17377-84. 2005
    ..The results also attribute the activity boost upon substitution of oxazole by oxadiazole to reduced steric interactions in the active site and a lower torsional energy penalty upon binding...
  48. pmc Total synthesis and evaluation of iso-duocarmycin SA and iso-yatakemycin
    Karen S MacMillan
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 131:1187-94. 2009
    ..The implications of these observations on the source of the DNA alkylation selectivity and catalysis for this class of natural products are discussed...
  49. pmc Synthesis and evaluation of a series of C5'-substituted duocarmycin SA analogs
    William M Robertson
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 20:2722-5. 2010
    ..The synthesis and evaluation of a key series of analogs of duocarmycin SA, bearing a single substituent at the C5' position of the DNA binding subunit, are described...
  50. pmc Systematic exploration of the structural features of yatakemycin impacting DNA alkylation and biological activity
    Mark S Tichenor
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 129:10858-69. 2007
    ....
  51. ncbi request reprint A powerful selection assay for mixture libraries of DNA alkylating agents
    Young Wan Ham
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 126:9194-5. 2004
    ....
  52. ncbi request reprint Comprehensive high-resolution analysis of hairpin polyamides utilizing a fluorescent intercalator displacement (FID) assay
    Winston C Tse
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550N Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 11:4479-86. 2003
    ..Thus, we report the discovery of a novel five base pair high affinity binding site of the form 5'-WWCWW (vs 5'-WGWWW) for the polyamide ImPyPy-gamma-PyPyPy-beta-Dp and its structural basis...
  53. ncbi request reprint Determination of binding affinities of triplex forming oligonucleotides using a fluorescent intercalator displacement (FID) assay
    Bryan K S Yeung
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 13:3801-4. 2003
    ..The binding affinities of several triplex forming oligonucleotides were determined using a fluorescent intercalator displacement (FID) assay...
  54. ncbi request reprint Synthesis of isochrysohermidin-distamycin hybrids
    Bryan K S Yeung
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 68:5249-53. 2003
    ..The DNA binding properties of these agents were compared to that of distamycin A, using a fluorescence intercalator displacement (FID) assay...
  55. ncbi request reprint Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway
    Joel Desharnais
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 11:4511-21. 2003
    ..120 microM) and very selective (> or =100-fold) for rh versus E. coli GAR Tfase. Additional key analogues of 1 were examined (7 and 8) and found to be much less active (1000-fold) highlighting the exceptional characteristics of 1...
  56. ncbi request reprint 10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase
    Thomas H Marsilje
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 11:4503-9. 2003
    ..Ketone 1 and the corresponding alcohol 13 were evaluated for inhibition of GAR Tfase and AICAR Tfase and the former was found to be a potent inhibitor of recombinant human (rh) GAR Tfase (Ki=600 nM)...
  57. pmc Asymmetric total synthesis of (+)- and ent-(-)-yatakemycin and duocarmycin SA: evaluation of yatakemycin key partial structures and its unnatural enantiomer
    Mark S Tichenor
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, USA
    J Am Chem Soc 128:15683-96. 2006
    ..Nonetheless, even ent-(-)-yatakemycin alkylates DNA at a faster rate and with a greater thermodynamic stability than (+)-duocarmycin SA, illustrating the unique characteristics of such "sandwiched" agents...
  58. ncbi request reprint Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase
    Lan Xu
    Department of Molecular Biology, The Scripps Research Institute, La Jolla, California 92037, USA
    J Biol Chem 282:13033-46. 2007
    ..Provocatively, the nucleotide inhibitor 3 also binds to the AICAR Tfase domain of ATIC, which now provides a lead compound for the design of inhibitors that simultaneously target both active sites of this bifunctional enzyme...
  59. ncbi request reprint Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition
    Suzanne B Buck
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 125:15694-5. 2003
    ..This 200-fold increase in PP2A inhibition attributable to the unsaturated lactone potentially may be due to reversible C269 alkylation within the PP beta12-beta13 active site loop accounting for PP2A/4 potency and selectivity...
  60. ncbi request reprint Establishment of substituent effects in the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065
    Jay P Parrish
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 11:3815-38. 2003
    ....
  61. pmc Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase
    Jessica K DeMartino
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 51:5441-8. 2008
    ....
  62. ncbi request reprint The DNA phosphate backbone is not involved in catalysis of the duocarmycin and CC-1065 DNA alkylation reaction
    Yves Ambroise
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 12:303-6. 2002
    ..All were found to react at comparable rates establishing that these backbone phosphates do not participate in catalysis of the DNA alkylation reaction...
  63. pmc Discovery of inhibitors of aberrant gene transcription from Libraries of DNA binding molecules: inhibition of LEF-1-mediated gene transcription and oncogenic transformation
    James S Stover
    Department of Chemistry, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 131:3342-8. 2009
    ....
  64. ncbi request reprint 10-Formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway
    Thomas H Marsilje
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 10:2739-49. 2002
    ..coli enzyme (K(i) for 3, 14nM against rhGAR Tfase versus 6 microM against E. coli GAR Tfase) which also accounts for their exceptional cytotoxic potency...
  65. ncbi request reprint A new and improved method for deglycosidation of glycopeptide antibiotics exemplified with vancomycin, ristocetin, and ramoplanin
    Jutta Wanner
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 13:1169-73. 2003
    ..Treatment of vancomycin, ristocetin, and ramoplanin with anhydrous HF results in efficient cleavage of the sugars to provide the corresponding aglycons in high yield...
  66. pmc Synthesis and evaluation of selected key methyl ether derivatives of vancomycin aglycon
    Christine M Crane
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 53:7229-35. 2010
    ....
  67. ncbi request reprint Establishing the parabolic relationship between reactivity and activity for derivatives and analogues of the duocarmycin and CC-1065 alkylation subunits
    Jay P Parrish
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 126:80-1. 2004
    ..When combined with the results of an extensive series of N-acyl CBI analogues and derivatives assembled over the past 15 years, the studies define a fundamental parabolic relationship between reactivity and cytotoxic potency...
  68. ncbi request reprint Synthesis and DNA binding properties of iminodiacetic acid-linked polyamides: characterization of cooperative extended 2:1 side-by-side parallel binding
    Craig R Woods
    Department of Chemistry, Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    J Am Chem Soc 124:10676-82. 2002
    ....
  69. pmc Total synthesis of piericidin A1 and B1 and key analogues
    Martin J Schnermann
    Departments of Chemistry and Molecular and Experimental Medicine, and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, USA
    J Am Chem Soc 128:11799-807. 2006
    ....
  70. ncbi request reprint Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase
    Wu Du
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 15:103-6. 2005
    ....
  71. pmc Total synthesis of piericidin A1 and B1
    Martin J Schnermann
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 127:15704-5. 2005
    ....
  72. ncbi request reprint Synthesis and evaluation of methyl ether derivatives of the vancomycin, teicoplanin, and ristocetin aglycon methyl esters
    Casey C McComas
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 13:2933-6. 2003
    ..These derivatives exhibit increased activity against VanB resistant strains of bacteria equipotent with that observed with sensitive bacteria...
  73. ncbi request reprint Reversible inhibitors of fatty acid amide hydrolase that promote analgesia: evidence for an unprecedented combination of potency and selectivity
    Aron H Lichtman
    Department of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, P O Box 980613, Richmond, VA 23298 0613, USA
    J Pharmacol Exp Ther 311:441-8. 2004
    ....
  74. ncbi request reprint Chemistry and biology of ramoplanin: a lipoglycodepsipeptide with potent antibiotic activity
    Suzanne Walker
    The Department of Microbiology and Molecular Genetics, Harvard Medical School, Boston, Massachusetts 02115, USA
    Chem Rev 105:449-76. 2005
  75. ncbi request reprint A fluorescent intercalator displacement assay for establishing DNA binding selectivity and affinity
    Winston C Tse
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Acc Chem Res 37:61-9. 2004
    ....
  76. ncbi request reprint Multidrug resistance reversal activity of permethyl ningalin B amide derivatives
    Houchao Tao
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 14:5979-81. 2004
    ..A series of amide derivatives of permethyl ningalin B were prepared and examined as multidrug resistance (MDR) reversal agents illustrating that the C5 carboxylate is widely tolerant of such derivatization...
  77. ncbi request reprint Effective asymmetric synthesis of 1,2,9,9a-tetrahydrocyclopropa[c]benzo[e]indol-4-one (CBI)
    David B Kastrinsky
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 69:2284-9. 2004
    ..lipase resolved the racemic intermediate 19, affording advanced intermediates of CBI in good conversions and optical purity (99% ee), and provided an alternative approach to the preparation of optically active CBI derivatives...
  78. ncbi request reprint Dissecting ramoplanin: mechanistic analysis of synthetic ramoplanin analogues as a guide to the design of improved antibiotics
    Lan Chen
    Department of Chemistry, Princeton University, Princeton, New Jersey 08544, USA
    J Am Chem Soc 126:7462-3. 2004
    ..The results should serve as a foundation for the design of synthetically accessible analogues with improved biological properties...
  79. ncbi request reprint Synthesis and inverse electron demand Diels-Alder reactions of 3,6-bis(3,4-dimethoxybenzoyl)-1,2,4,5-tetrazine
    Danielle R Soenen
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Org Chem 68:3593-8. 2003
    ....
  80. ncbi request reprint A human single-chain antibody specific for integrin alpha3beta1 capable of cell internalization and delivery of antitumor agents
    Antonietta M Lillo
    Department of Chemistry, The Scripps Research Institute and The Skaggs Institute for Chemical Biology, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Chem Biol 11:897-906. 2004
    ..Our Pan10-drug conjugates may be promising candidates for targeted chemotherapy of malignant diseases associated with overexpression of integrin alpha3beta1...
  81. ncbi request reprint Alkylation of duplex DNA in nucleosome core particles by duocarmycin SA and yatakemycin
    John D Trzupek
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Nat Chem Biol 2:79-82. 2006
    ..These findings highlight the dynamic nature of NCP-bound DNA and illustrate that cell- and protein-free DNA-alkylation studies of members of this class of antitumor drugs provide valuable insights into their properties...
  82. ncbi request reprint DNA alkylation properties of yatakemycin
    Jay P Parrish
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 125:10971-6. 2003
    ..Thus, the event, sequence selectivity, relative rate and efficiency, and reversibility of the DNA alkylation reaction of yatakemycin are described...
  83. doi request reprint A fluorescent intercalator displacement assay for establishing DNA binding selectivity and affinity
    Winston C Tse
    Gilead Sciences, Foster City, California, USA
    Curr Protoc Nucleic Acid Chem . 2005
    ..A protocol for a fluorescent intercalator displacement (FID) assay useful for establishing DNA binding selectivity, affinity, stoichiometry, and binding site size, and for distinguishing modes of DNA binding is presented...
  84. pmc Total synthesis and evaluation of cytostatin, its C10-C11 diastereomers, and additional key analogues: impact on PP2A inhibition
    Brian G Lawhorn
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    J Am Chem Soc 128:16720-32. 2006
    ....
  85. ncbi request reprint Potent reversal of multidrug resistance by ningalins and its use in drug combinations against human colon carcinoma xenograft in nude mice
    Ting Chao Chou
    Molecular Pharmacology and Chemistry Program, Sloan Kettering Institute for Cancer Research, 1275 York Avenue, New York, NY 10021, USA
    Cancer Chemother Pharmacol 56:379-90. 2005
    ....
  86. ncbi request reprint Synthesis and biological evaluation of N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid as a potential inhibitor of GAR Tfase and the de novo purine biosynthetic pathway
    Heng Cheng
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem 13:3593-9. 2005
    ..coli GAR Tfase as well as recombinant human AICAR Tfase. Compound 2 exhibited modest, purine-sensitive growth inhibitory activity against the CCRF-CEM cell line (IC50 = 6.0 microM)...
  87. ncbi request reprint Synthesis and DNA binding properties of saturated distamycin analogues
    Craig R Woods
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550North Torrey Pines Road, CA 92037, La Jolla, USA
    Bioorg Med Chem Lett 12:2647-50. 2002
    ..It is observed that saturated heterocycles greatly reduce the DNA binding relative to distamycin...
  88. pmc Alanine scan of [L-Dap(2)]ramoplanin A2 aglycon: assessment of the importance of each residue
    Joonwoo Nam
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 129:8747-55. 2007
    ..The antimicrobial activity of the resulting library of analogues provides insight into the importance and potential role of each residue of this complex glycopeptide antibiotic...
  89. ncbi request reprint NMR structure of the (+)-CPI-indole/d(GACTAATTGAC)-d(GTCAATTAGTC) covalent complex
    Carla Bassarello
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Salerno, 84084 Fisciano, Salerno, Italy
    Chembiochem 4:1188-93. 2003
    ....
  90. ncbi request reprint Hairpin versus extended DNA binding of a substituted beta-alanine linked polyamide
    Craig R Woods
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Am Chem Soc 124:2148-52. 2002
    ....
  91. pmc Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase
    Jessica K DeMartino
    Department of Chemistry, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 49:2998-3002. 2006
    ....
  92. ncbi request reprint Disruption of the MYC transcriptional function by a small-molecule antagonist of MYC/MAX dimerization
    Xiaohong Lu
    Northern Institute for Cancer Research, Newcastle University, Newcastle upon Tyne, NE2 4HH, UK
    Oncol Rep 19:825-30. 2008
    ....
  93. doi request reprint Yatakemycin: total synthesis, DNA alkylation, and biological properties
    Mark S Tichenor
    Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Nat Prod Rep 25:220-6. 2008
    ..Studies on the DNA alkylation properties of (+)-and ent-(-)-yatakemycin and related analogues have demonstrated the enhanced DNA alkylation properties of this class of agents and provided insight into their interaction with DNA...
  94. ncbi request reprint Multidrug resistance reversal activity of key ningalin analogues
    Danielle R Soenen
    The Scripps Research Institute and The Skaggs Institute for Chemical Biology, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 13:1777-81. 2003
    ....

Research Grants66

  1. ANTITUMOR ANTIBIOTICS: CC-1065 AND BLEOMYCINS
    Dale Boger; Fiscal Year: 1991
    ..The initiation of efforts on the total sythesis of bleomycins (glycopeptide antitumor-antibiotics), and the initiation of structure activity studies employing synthetic bleomyins, are detailed...
  2. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2003
    ..abstract_text> ..
  3. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2005
    ..abstract_text> ..
  4. THE ANTITUMOR ANTIBIOTICS CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2003
    ..The introduction and continued development of new techniques for establishing DNA binding selectivity and affinity promises to facilitate these and related studies. ..
  5. THE ANTITUMOR ANTIBIOTICS CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2007
    ..Public Health Relevance: New drugs for the treatment of cancer will be explored and new general concepts of drug design may emerge from the investigations. ..
  6. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2000
    ....
  7. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2007
    ..abstract_text> ..
  8. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale L Boger; Fiscal Year: 2010
    ..The development of selective and potent inhibitors for each unannotated serine hydrolase will facilitate the delineation of their endogenous role and their evaluation as new therapeutic targets. ..
  9. THE ANTITUMOR ANTIBIOTICS CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2009
    ..Public Health Relevance: New drugs for the treatment of cancer will be explored and new general concepts of drug design may emerge from the investigations. ..
  10. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2001
    ....
  11. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2002
    ....
  12. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2004
    ..abstract_text> ..
  13. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale Boger; Fiscal Year: 2005
    ..These studies have provided a set of a-ketoheterocycle FAAH inhibitors with Ki's that drop below 200 pM and that are l00-1000 times more potent than the corresponding trifluoromethyl ketones. ..
  14. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2004
    ..abstract_text> ..
  15. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2005
    ..abstract_text> ..
  16. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale Boger; Fiscal Year: 2006
    ..These studies have provided a set of a-ketoheterocycle FAAH inhibitors with Ki's that drop below 200 pM and that are l00-1000 times more potent than the corresponding trifluoromethyl ketones. ..
  17. Vindoline and Vinblastine
    Dale L Boger; Fiscal Year: 2010
    ..abstract_text> ..
  18. ANTITUMOR ANTIBIOTICS
    Dale L Boger; Fiscal Year: 2010
    ..PUBLIC HEALTH RELEVANCE: New insights into new classes of drugs for the treatment of cancer and methods for their preparation will emerge from the proposed studies. ..
  19. THE ANTITUMOR ANTIBIOTICS CC-1065 AND THE DUOCARMYCINS
    Dale L Boger; Fiscal Year: 2010
    ..Public Health Relevance: New drugs for the treatment of cancer will be explored and new general concepts of drug design may emerge from the investigations. ..
  20. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2009
    ..abstract_text> ..
  21. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2009
    ..PUBLIC HEALTH RELEVANCE: New insights into new classes of drugs for the treatment of cancer and methods for their preparation will emerge from the proposed studies. ..
  22. Vindoline and Vinblastine
    Dale Boger; Fiscal Year: 2009
    ..abstract_text> ..
  23. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2007
    ..abstract_text> ..
  24. Vindoline and Vinblastine
    Dale Boger; Fiscal Year: 2007
    ....
  25. Vindoline and Vinblastine
    Dale Boger; Fiscal Year: 2006
    ....
  26. ANTITUMOR ANTIBIOTICS--CC-1065 AND BLEOMYCINS
    Dale Boger; Fiscal Year: 1992
    ..These studies will be fully developed in the current grant period...
  27. ANTITUMOR AGENTS: BOUVARDIN AND LUZOPEPTINS
    Dale Boger; Fiscal Year: 1993
    ..Studies will be pursued to delineate the structural features of the agents contributing to their DNA binding affinityand specificity...
  28. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 1999
    ....
  29. LUZOPEPTINS, VANCOMYCIN AND RELATED AGENTS
    Dale Boger; Fiscal Year: 1999
    ..Exciting new studies on the design, synthesis, and evaluation of DNA alkylation, cross-linking and cleaving agents based on the sandramycin template structure are detailed. ..
  30. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2000
    ....
  31. ANTITUMOR ANTIBIOTIC: CC-1065
    Dale Boger; Fiscal Year: 1993
    ..These studies will be fully developed in the current grant period...
  32. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2002
    ..abstract_text> ..
  33. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale Boger; Fiscal Year: 2002
    ..These studies have provided a set of a-ketoheterocycle FAAH inhibitors with Ki's that drop below 200 pM and that are l00-1000 times more potent than the corresponding trifluoromethyl ketones. ..
  34. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2001
    ....
  35. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 1999
    ....
  36. Fostriecin and Related Protein Phosphatase Inhibitors
    Dale Boger; Fiscal Year: 2003
    ....
  37. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale Boger; Fiscal Year: 2003
    ..These studies have provided a set of a-ketoheterocycle FAAH inhibitors with Ki's that drop below 200 pM and that are l00-1000 times more potent than the corresponding trifluoromethyl ketones. ..
  38. Fostriecin and Related Protein Phosphatase Inhibitors
    Dale Boger; Fiscal Year: 2004
    ....
  39. Fostriecin and Related Protein Phosphatase Inhibitors
    Dale Boger; Fiscal Year: 2002
    ....
  40. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 2001
    ....
  41. Fostriecin and Related Protein Phosphatase Inhibitors
    Dale Boger; Fiscal Year: 2005
    ....
  42. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2001
    ..abstract_text> ..
  43. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2000
    ....
  44. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 2006
    ..abstract_text> ..
  45. ANTITUMOR ANTIBIOTICS--CC-1065 AND THE DUOCARMYCINS
    Dale Boger; Fiscal Year: 1999
    ....
  46. BIOLOGICALLY ACTIVE CYCLIC PEPTIDES
    Dale Boger; Fiscal Year: 2000
    ..abstract_text> ..
  47. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale Boger; Fiscal Year: 2004
    ..These studies have provided a set of a-ketoheterocycle FAAH inhibitors with Ki's that drop below 200 pM and that are l00-1000 times more potent than the corresponding trifluoromethyl ketones. ..
  48. ANTITUMOR AGENTS--BOUVARDINS AND LUZOPEPTINS
    Dale Boger; Fiscal Year: 1992
    ..Studies will be pursued to delineate the structural features of the agents contributing to their DNA binding affinityand specificity...
  49. ANTITUMOR ANTIBIOTICS
    Dale Boger; Fiscal Year: 1993
    ..Evaluation of the antitumor properties of partial structures and synthetic agents related to fredericamycin A...