SIDNEY HECHT

Summary

Affiliation: University of Virginia
Country: USA

Publications

  1. ncbi Bleomycin: new perspectives on the mechanism of action
    S M Hecht
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    J Nat Prod 63:158-68. 2000
  2. ncbi Camptothecins as probes of the microenvironments of topoisomerase I--DNA complexes
    S M Hecht
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    Ann N Y Acad Sci 922:76-91. 2000
  3. ncbi Camptothecin: roles of the D and E rings in binding to the topoisomerase I-DNA covalent binary complex
    Sidney M Hecht
    Department of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    Curr Med Chem Anticancer Agents 5:353-62. 2005
  4. ncbi DNA damaging activity of ellagic acid derivatives
    Ya ming Xu
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem 11:1593-6. 2003
  5. ncbi Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation
    Jeffrey A Smith
    Center for Cell Signaling, Department of Pathology, University of Virginia Health Science Center, 7041 Multistory Building, Charlottesville, VA 22908 0577, USA
    Cancer Res 65:1027-34. 2005
  6. ncbi Camptothecin: current perspectives
    Craig J Thomas
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem 12:1585-604. 2004
  7. ncbi Influence of rhamnose substituents on the potency of SL0101, an inhibitor of the Ser/Thr kinase, RSK
    Jeffrey A Smith
    Center for Cell Signaling, University of Virginia, Charlottesville, VA 22908, USA
    Bioorg Med Chem 14:6034-42. 2006
  8. ncbi Structural basis for the activity of the RSK-specific inhibitor, SL0101
    Jeffrey A Smith
    Center for Cell Signaling, Department of Pathology, University of Virginia, Charlottesville, VA 22908, USA
    Bioorg Med Chem 15:5018-34. 2007
  9. ncbi DNA-damaging agents from Crypteronia paniculata
    Jing Zhen Deng
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    J Nat Prod 65:1930-2. 2002
  10. ncbi DNA topoisomerase I inhibitors from Rinorea anguifera
    Ji Ma
    Department of Chemistry and Department of Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem Lett 15:813-6. 2005

Collaborators

  • Shisheng Li
  • Rong Gao
  • Zhi Fu Tao
  • Jeffrey A Smith
  • Ji Ma
  • Brian M Eisenhauer
  • Shannon H Jones
  • Nicolas J Rahier
  • Jing Zhen Deng
  • David J Maloney
  • Ali Cagir
  • Qian Ma
  • Mark A Elban
  • Craig J Thomas
  • Christopher J Leitheiser
  • Yoshitsugu Akiyama
  • Michael J Rishel
  • Kazuhide Konishi
  • Ya ming Xu
  • Rebekah Marshall
  • Shengxi Chen
  • Zhijie Gao
  • Zhidong Xu
  • Nour Eddine Fahmi
  • Larisa M Dedkova
  • Kejun Cheng
  • Shannon J Thomas
  • Shigeki Hashimoto
  • Randall K Johnson
  • Xihan Wu
  • Kenneth L Smith
  • Andrei Laikhter
  • Erin Edgar
  • Wenyue Sun
  • Shelley R Starck
  • Van Cuong Pham
  • Anil T Abraham
  • Christopher D Claeboe
  • Michael M McCormick
  • Corine Vialas
  • Raymond D Anderson
  • Jean C Chapuis
  • Fang Wei
  • Serguei Golovine
  • Mei Li
  • Benjamin R Schroeder
  • Bixun Wang
  • Larisa Dedkova
  • Deborah A Lannigan
  • Serguei Y Golovine
  • David J Newman
  • S J Thomas
  • Jih Jing Lin
  • Dianne L Newton
  • Susanna Rybak
  • Shao Nong Chen
  • Chunhong Li
  • Steven J Sucheck
  • Alexander O Chizhov
  • Jia Zhou

Detail Information

Publications53

  1. ncbi Bleomycin: new perspectives on the mechanism of action
    S M Hecht
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    J Nat Prod 63:158-68. 2000
    ....
  2. ncbi Camptothecins as probes of the microenvironments of topoisomerase I--DNA complexes
    S M Hecht
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    Ann N Y Acad Sci 922:76-91. 2000
    ....
  3. ncbi Camptothecin: roles of the D and E rings in binding to the topoisomerase I-DNA covalent binary complex
    Sidney M Hecht
    Department of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    Curr Med Chem Anticancer Agents 5:353-62. 2005
    ....
  4. ncbi DNA damaging activity of ellagic acid derivatives
    Ya ming Xu
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem 11:1593-6. 2003
    ..and Scholtzia parviflora. Although none of the isolated principles mediated frank strand scission of DNA in vitro, all of them potently inhibited the growth of yeast in the absence of expression of RAD52...
  5. ncbi Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation
    Jeffrey A Smith
    Center for Cell Signaling, Department of Pathology, University of Virginia Health Science Center, 7041 Multistory Building, Charlottesville, VA 22908 0577, USA
    Cancer Res 65:1027-34. 2005
    ..SL0101 will provide a powerful new tool to dissect the molecular functions of RSK in cancer cells...
  6. ncbi Camptothecin: current perspectives
    Craig J Thomas
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem 12:1585-604. 2004
    ..Finally, a systematic evaluation of novel and important analogues of camptothecin and their contribution to the current structure-activity profile are considered...
  7. ncbi Influence of rhamnose substituents on the potency of SL0101, an inhibitor of the Ser/Thr kinase, RSK
    Jeffrey A Smith
    Center for Cell Signaling, University of Virginia, Charlottesville, VA 22908, USA
    Bioorg Med Chem 14:6034-42. 2006
    ..Thus the discovery of 3Ac-SL0101 as a more potent RSK-specific inhibitor than SL0101 should facilitate the development of RSK inhibitors as anti-cancer chemotherapeutic agents...
  8. ncbi Structural basis for the activity of the RSK-specific inhibitor, SL0101
    Jeffrey A Smith
    Center for Cell Signaling, Department of Pathology, University of Virginia, Charlottesville, VA 22908, USA
    Bioorg Med Chem 15:5018-34. 2007
    ..These studies should facilitate the development of a RSK inhibitor, based on the SL0101 pharmacophore, as an anti-cancer chemotherapeutic agent...
  9. ncbi DNA-damaging agents from Crypteronia paniculata
    Jing Zhen Deng
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    J Nat Prod 65:1930-2. 2002
    ..The third was identified as kaempferol-3-O-alpha-l-rhamnoside (3). The three principles exhibited strong, selective cytotoxity toward the RAD52 repair-deficient yeast strain...
  10. ncbi DNA topoisomerase I inhibitors from Rinorea anguifera
    Ji Ma
    Department of Chemistry and Department of Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem Lett 15:813-6. 2005
    ..Bioassay-guided fractionation resulted in the isolation of mauritianin and (+)-syringaresinol as new topoisomerase I inhibitors, and also of the known inhibitor camptothecin...
  11. ncbi Synthesis and topoisomerase I inhibitory properties of luotonin A analogues
    Ali Cagir
    Department of Chemistry and Department of Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem 12:6287-99. 2004
    ....
  12. ncbi Synthesis of a potent and selective inhibitor of p90 Rsk
    David J Maloney
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    Org Lett 7:1097-9. 2005
    ..The synthesis verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation...
  13. doi Inhibitors of DNA polymerase beta: activity and mechanism
    Zhijie Gao
    Department of Chemistry, University of Virginia, Charlottesville, VA 22904, USA
    Bioorg Med Chem 16:4331-40. 2008
    ..The results of the unscheduled DNA synthesis assay support the thesis that the potentiation of bleomycin cytotoxicity by DNA pol beta inhibitors was a result of an inhibition of DNA repair synthesis...
  14. ncbi Water-soluble camptothecin derivatives that are intrinsic topoisomerase I poisons
    Nicolas J Rahier
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    Org Lett 6:321-4. 2004
    ..All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion...
  15. ncbi Synthesis and biological evaluation of 10,11-methylenedioxy-14-azacamptothecin
    Mark A Elban
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
    Org Lett 8:3513-6. 2006
    ..The biological testing of this compound validated a strategy for modulation of the off-rate of camptothecin analogues from the topoisomerase-DNA-CPT ternary complex via structural modification...
  16. ncbi Luotonin A. A naturally occurring human DNA topoisomerase I poison
    Ali Cagir
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    J Am Chem Soc 125:13628-9. 2003
    ..This finding identifies a putative biochemical locus for the cytotoxic action of luotonin A and has important implications for the mechanism of action of camptothecin and the design of camptothecin analogues...
  17. ncbi Conformationally constrained analogues of bleomycin A5
    Michael J Rishel
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
    J Am Chem Soc 125:10194-205. 2003
    ..The ability of the analogues to mediate the oxygenation of small molecules was also assayed, and it was shown that they were as competent in the transfer of oxygen to low molecular weight substrates as the parent compound...
  18. ncbi Analogues of vaccinia virus DNA topoisomerase I modified at the active site tyrosine
    Rong Gao
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    J Am Chem Soc 127:3321-31. 2005
    ..The pH profile for the functional analogues revealed a small shift toward lower pH when compared with wild-type topoisomerase I...
  19. doi A novel DNA hairpin substrate for bleomycin
    Yoshitsugu Akiyama
    Department of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22904, USA
    Org Lett 10:2127-30. 2008
    ..The pro-fluorescent DNA hairpin was used as a substrate for 15 bleomycin congeners, and the results were compared with those obtained following cleavage of a radiolabeled DNA duplex and PAGE analysis...
  20. ncbi Effects of modification of the active site tyrosine of human DNA topoisomerase I
    Rong Gao
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    Biochemistry 45:8402-10. 2006
    ..In addition, the poisoning of one of the modified human topoisomerase I analogues, as part of covalent binary complexes with DNA, by CPT and 20-thio CPT was evaluated...
  21. ncbi Solid-phase synthesis of bleomycin A(5) and three monosaccharide analogues: exploring the role of the carbohydrate moiety in RNA cleavage
    Craig J Thomas
    Department of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    J Am Chem Soc 124:12926-7. 2002
    ..The relatively facile solid-phase synthesis of bleomycin A5 and each of the carbohydrate analogues constitutes an important advance in the continuing mechanistic studies of bleomycin...
  22. doi Identification and cleavage site analysis of DNA sequences bound strongly by bleomycin
    Qian Ma
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
    J Am Chem Soc 131:2013-22. 2009
    ..BLM, as well as the chemistry leading to DNA degradation, are more complex than suggested by earlier studies that employed only DNA degradation product analysis as an end point...
  23. ncbi Synthesis of 14-azacamptothecin, a water-soluble topoisomerase I poison
    Nicolas J Rahier
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22904, USA
    Org Lett 7:835-7. 2005
    ..The key condensation of the AB and DE rings with concomitant formation of ring C of 14-aza CPT was carried out in two stages, the latter of which involved a radical cyclization strategy. [structure: see text]..
  24. doi Identification of strong DNA binding motifs for bleomycin
    Yoshitsugu Akiyama
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22904, USA
    J Am Chem Soc 130:9650-1. 2008
    ..Herein, we describe the development and implementation of a novel strategy to identify DNA motifs that bind BLM strongly...
  25. ncbi Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK
    Ya ming Xu
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem 14:3974-7. 2006
    ..Of these, compound 2 was found to be the best inhibitor with an IC(50) value of 89 nM...
  26. ncbi On the role of E-ring oxygen atoms in the binding of camptothecin to the topoisomerase I-DNA covalent binary complex
    Nicolas J Rahier
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    Bioorg Med Chem 13:1381-6. 2005
    ....
  27. ncbi 14-azacamptothecin: a potent water-soluble topoisomerase I poison
    Kejun Cheng
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
    J Am Chem Soc 127:838-9. 2005
    ..14-Aza CPT was found to be slightly less active than CPT in mediating cytotoxicity toward yeast expressing human topoisomerase I, possibly as a consequence of its greater off-rate from the CPT-topoisomerase I-DNA ternary complex...
  28. pmc 3'-modified oligonucleotides by reverse DNA synthesis
    Christopher D Claeboe
    Department of Chemistry and Department of Biology, University of Virginia, Charlottesville, VA 22901, USA
    Nucleic Acids Res 31:5685-91. 2003
    ....
  29. ncbi Identification of specific nonbridging phosphate oxygens important for DNA cleavage by human topoisomerase I
    Rong Gao
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    Biochemistry 43:6167-81. 2004
    ..These effects were shown to be due primarily to alteration of the binding of the modified DNA substrates by human DNA topoisomerase I...
  30. ncbi (+)-Myristinin A, a naturally occurring DNA polymerase beta inhibitor and potent DNA-damaging agent
    David J Maloney
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    J Am Chem Soc 127:4140-1. 2005
    ..Relaxation of supercoiled plasmid DNA was observed at picomolar concentrations, in addition to inhibition of polymerase beta at low micromolar concentrations...
  31. ncbi A DNA-damaging oxoaporphine alkaloid from Piper caninum
    Ji Ma
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    J Nat Prod 67:1162-4. 2004
    ..Compound 1 exhibited potent inhibitory activity in a yeast cytotoxicity assay with IC(50) values of 50.2 nM toward RS321NpRAD52 grown on glucose versus 293 nM toward the same yeast strain grown on galactose...
  32. ncbi A coumarin from Mallotus resinosus that mediates DNA cleavage
    Ji Ma
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    J Nat Prod 67:1614-6. 2004
    ..Scopoletin (1), a simple coumarin, was identified as the active principle responsible for DNA cleavage activity of the crude extract. The DNA strand scission activity of 1, as well as that of three structural analogues, is reported...
  33. ncbi Site-specific incorporation of glycosylated serine and tyrosine derivatives into proteins
    Nour Eddine Fahmi
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    J Am Chem Soc 129:3586-97. 2007
    ..For mutants containing glycosylated tyrosines, the red shift was observed only when the carbohydrate moiety was fully deacetylated...
  34. ncbi RNA cleavage and inhibition of protein synthesis by bleomycin
    Anil T Abraham
    Department of Chemistry, University of Virginia, Charlottesville, VA 22901, USA
    Chem Biol 10:45-52. 2003
    ..The correlation of protein synthesis inhibition to the previously reported site-specific RNA cleavage caused by bleomycin supports the thesis that RNA cleavage may constitute an important element of the mechanism of action of bleomycin...
  35. ncbi Synthesis and biological evaluation of cepharadiones A and B and related dioxoaporphines
    Mark A Elban
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22904, USA
    Bioorg Med Chem 15:6119-25. 2007
    ..Finally, the preparation and biological evaluation of novel dioxoaporphine analogues is described...
  36. ncbi Fluorescence resonance energy transfer between unnatural amino acids in a structurally modified dihydrofolate reductase
    Raymond D Anderson
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
    J Am Chem Soc 124:9674-5. 2002
    ....
  37. doi Total synthesis of the topopyrones: a new class of topoisomerase I poisons
    Mark A Elban
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22904, USA
    J Org Chem 73:785-93. 2008
    ..Additionally, the syntheses of two chlorinated analogues accessible from an advanced intermediate are described...
  38. ncbi Solid-phase synthesis of deglycobleomycins: a C-terminal tetraamine linker that permits direct evaluation of resin-bound bleomycins
    Zhi Fu Tao
    Department of Chemistry, University of Virginia, Charlottesville 22901, USA
    Bioconjug Chem 13:426-34. 2002
    ..Resin-bound 4 exhibited efficient DNA cleavage, indicating that its tetraamine linker moiety could be used for the elaboration and direct evaluation of bleomycin congeners attached to resins...
  39. ncbi Alteration of the selectivity of DNA cleavage by a deglycobleomycin analogue containing a trithiazole moiety
    Craig J Thomas
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    J Am Chem Soc 124:3875-84. 2002
    ..In comparison with BLM A(5), the relative efficiencies of hydrolytic cleavage at individual sites were altered...
  40. ncbi Deglycobleomycin: solid-phase synthesis and DNA cleavage by the resin-bound ligand
    Kenneth L Smith
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    Org Lett 4:1079-82. 2002
    ..The resin-bound deglycobleomycin could be completely deblocked and assayed for DNA plasmid relaxation, sequence-selective DNA cleavage, and light production from a molecular beacon...
  41. doi Synthesis of pdCpAs and transfer RNAs activated with derivatives of aspartic acid and cysteine
    Shengxi Chen
    Departments of Chemistry and Biology, University of Virginia, McCormick Road, Charlottesville, VA 22904, USA
    Bioorg Med Chem 16:9023-31. 2008
    ..Of particular interest is definition of functional group protection strategies that can be used for the preparation of the aminoacylated pdCpAs and tRNAs...
  42. ncbi Construction of modified ribosomes for incorporation of D-amino acids into proteins
    Larisa M Dedkova
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
    Biochemistry 45:15541-51. 2006
    ..Five specific amino acids in Escherichia coli dihydrofolate reductase and Photinus pyralis luciferase were replaced with D-phenylalanine and D-methionine, and the specific activities of the resulting enzymes were determined...
  43. ncbi Solid-phase synthesis of bleomycin group antibiotics. Construction of a 108-member deglycobleomycin library
    Christopher J Leitheiser
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22904, USA
    J Am Chem Soc 125:8218-27. 2003
    ..Each analogue demonstrated supercoiled plasmid DNA relaxation above background cleavage; the library included two analogues that mediated plasmid relaxation to a greater extent than the parent deglycobleomycin molecule...
  44. ncbi Phenolic acid amides: a new type of DNA strand scission agent from Piper caninum
    Ji Ma
    Department of Chemistry, University of Virginia, Charlottesville, VA, 22901, USA
    Bioorg Med Chem 12:3885-9. 2004
    ..Three active principles were isolated and identified as N-cis-feruloyl tyramine (1),N-trans-feruloyl tyramine (2), and 1-cinnamoylpyrrolidine (3). Compounds 1-3 represent a structurally new type of DNA strand scission agent...
  45. ncbi Umbelactonyl cinnamate derivatives from Crypteronia paniculata that mediate DNA strand scission
    Jing Zhen Deng
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA
    J Nat Prod 68:465-7. 2005
    ..Compound 1 exhibited strong Cu(2+)-dependent relaxation of supercoiled pSP64 DNA, while compounds 2 and 3 had only weak DNA cleavage activity...
  46. ncbi Synthesis and biochemical properties of E-ring modified luotonin A derivatives
    Ali Cagir
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem Lett 14:2051-4. 2004
    ..A study of the structural elements in luotonin A required for binary complex stabilization has revealed key differences relative to those required for camptothecin...
  47. ncbi Alkaloids from Alangium javanicum and Alangium grisolleoides that mediate Cu2+-dependent DNA strand scission
    Van Cuong Pham
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    J Nat Prod 68:1147-52. 2005
    ..Semisynthesis of javaniside from secologanin (3) established the absolute stereochemistry of javaniside...
  48. ncbi (+)-Myristinins A and D from Knema elegans, which inhibit DNA polymerase beta and cleave DNA
    Jing Zhen Deng
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22903, USA
    J Nat Prod 68:1625-8. 2005
    ..Principles 1 and 2 also induced strong Cu2+-dependent DNA strand scission in a DNA cleavage assay. Accordingly, 1 and 2 exhibit two activities, namely, DNA polymerase beta inhibition and DNA damage...
  49. ncbi Solid-phase synthesis and biochemical evaluation of conformationally constrained analogues of deglycobleomycin A5
    Ali Cagir
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
    Bioorg Med Chem 11:5179-87. 2003
    ..However, both deglycoBLM analogues exhibited diminished abilities to effect the relaxation of supercoiled plasmid DNA, and neither mediated sequence selective DNA cleavage...
  50. ncbi Stereoselective synthesis of the atropisomers of myristinin B/C
    David J Maloney
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
    Org Lett 8:1925-7. 2006
    ..The antipode, (+)-myristinin B/C, was also synthesized, providing ample material for biological evaluation of both enantiomers...
  51. ncbi A dihydroflavonol glucoside from Commiphora africana that mediates DNA strand scission
    Ji Ma
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    J Nat Prod 68:115-7. 2005
    ..The dihydroflavonol glucoside phellamurin (1) was identified as the active principle responsible for the DNA cleavage activity of the crude extract...
  52. ncbi Site-specific incorporation of (aminooxy)acetic acid into proteins
    Brian M Eisenhauer
    Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA
    Biochemistry 41:11472-8. 2002
    ..It has also been shown that the elaborated protein can be cleaved chemically at the site containing the modified amino acid...
  53. ncbi Biochemical evaluation of a 108-member deglycobleomycin library: viability of a selection strategy for identifying bleomycin analogues with altered properties
    Qian Ma
    Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22904, USA
    J Am Chem Soc 129:12439-52. 2007
    ..The present study also permits inferences to be drawn regarding the practicality of a selection strategy for the solid-phase construction and evaluation of large libraries of BLM analogues having altered properties...

Research Grants5

  1. MECHANISM AND INHIBITION OF HUMAN DNA TOPOISOMERASE I
    SIDNEY HECHT; Fiscal Year: 2003
    ..abstract_text> ..
  2. NATURAL PRODUCTS DISCOVERY - NUCLEAR AND SIGNALING TARGE
    SIDNEY HECHT; Fiscal Year: 2004
    ..preparing in quantity and evaluating promising compounds in tumor cells (for mechanism, biochemical pharmacology, interaction with known antineoplastic agents) and in animal tumor models (Programs 1-3) ..
  3. INTERACTION OF BLEOMYCIN WITH RNA AND DNA
    SIDNEY HECHT; Fiscal Year: 2006
    ..In spite of the obvious utility and importance of the bleomycins as antitumor agents, there are clear opportunities to alter the molecular behavior of bleomycin, and thereby potentially improve its antitumor efficacy. ..
  4. ELABORATION OF MODIFIED PROTEINS USING MISACYLATED TRNAS
    SIDNEY HECHT; Fiscal Year: 2007
    ..Also of interest is the exploitation of a new method for introducing a broader range of amino acid analogues into the derived proteins, and the elaboration of the modified proteins in an intact cellular system ..
  5. SYNTHESIS OF BLEOMYCIN GROUP ANTIBIOTICS AND ANALOGUES
    SIDNEY HECHT; Fiscal Year: 2007
    ..These libraries will be used to select BLMs having specific desirable properties and the identified analogues will be characterized thoroughly as potential anti-tumor agents. ..