John Koh

Summary

Affiliation: University of Delaware
Country: USA

Publications

  1. ncbi request reprint Engineering selectivity and discrimination into ligand-receptor interfaces
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Chem Biol 9:17-23. 2002
  2. ncbi request reprint The new biomimetic chemistry: artificial transcription factors
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    ACS Chem Biol 2:599-601. 2007
  3. ncbi request reprint Ligand-receptor engineering and its application towards the complementation of genetic disease and target identification
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Curr Top Med Chem 5:413-20. 2005
  4. pmc Making virtual screening a reality
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Proc Natl Acad Sci U S A 100:6902-3. 2003
  5. pmc A functionally orthogonal ligand-receptor pair created by targeting the allosteric mechanism of the thyroid hormone receptor
    A Quamrul Hassan
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    J Am Chem Soc 128:8868-74. 2006
  6. ncbi request reprint Chemical biology of steroid and nuclear hormone receptors
    John B Biggins
    Department of Chemistry and Biochemistry, University of Delaware, Newark DE 19716, USA
    Curr Opin Chem Biol 11:99-110. 2007
  7. doi request reprint Development of a thyroid hormone receptor targeting conjugate
    Jianfei Zheng
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    Bioconjug Chem 19:1227-34. 2008
  8. ncbi request reprint Functionally orthogonal ligand-receptor pairs for the selective regulation of gene expression generated by manipulation of charged residues at the ligand-receptor interface of ER alpha and ER beta
    Youheng Shi
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    J Am Chem Soc 124:6921-8. 2002
  9. ncbi request reprint Rational design of vitamin D3 analogues which selectively restore activity to a vitamin D receptor mutant associated with rickets
    Steve L Swann
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    Org Lett 4:3863-6. 2002
  10. ncbi request reprint Light-activated transcription and repression by using photocaged SERMs
    Youheng Shi
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Chembiochem 5:788-96. 2004

Research Grants

Collaborators

  • Cindy Farach-Carson
  • Gary Posner
  • Paul M O'Neill
  • Sara Peleg
  • Youheng Shi
  • Kristian H Link
  • A Quamrul Hassan
  • John B Biggins
  • Atsushi Hashimoto
  • Steve L Swann
  • Daniel J Sauers
  • Jianfei Zheng
  • Paula L McGinley
  • Sarah Dowdell
  • Murali K Temburni
  • Deni S Galileo
  • Luke M Ceo
  • Katherine Miller
  • Marc Putnam
  • Haifen Ye
  • Marc C Putnam
  • Isaac Hubner
  • Katherine Drake
  • Federico G Cruz
  • Kathryn E O'Reilly
  • Hai Fen Ye
  • Joel J Bergh
  • Cory A Ocasio
  • Mary C Farach-Carson
  • Joel Bergh
  • M Cindy Farach-Carson

Detail Information

Publications19

  1. ncbi request reprint Engineering selectivity and discrimination into ligand-receptor interfaces
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Chem Biol 9:17-23. 2002
    ..New design strategies and potential applications of ligand-receptor engineering are also discussed...
  2. ncbi request reprint The new biomimetic chemistry: artificial transcription factors
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    ACS Chem Biol 2:599-601. 2007
    ..The goal of synthesizing small-molecule ATFs holds promise as a means to independently control the expression of genes such as those that are misregulated in cancer and disease...
  3. ncbi request reprint Ligand-receptor engineering and its application towards the complementation of genetic disease and target identification
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Curr Top Med Chem 5:413-20. 2005
    ....
  4. pmc Making virtual screening a reality
    John T Koh
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Proc Natl Acad Sci U S A 100:6902-3. 2003
  5. pmc A functionally orthogonal ligand-receptor pair created by targeting the allosteric mechanism of the thyroid hormone receptor
    A Quamrul Hassan
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    J Am Chem Soc 128:8868-74. 2006
    ..QH2 does not show antagonist behavior with the wild-type TRs. QH2's functionally orthogonal behavior with TRbeta(H435A) is preserved on the three consensus thyroid hormone response elements...
  6. ncbi request reprint Chemical biology of steroid and nuclear hormone receptors
    John B Biggins
    Department of Chemistry and Biochemistry, University of Delaware, Newark DE 19716, USA
    Curr Opin Chem Biol 11:99-110. 2007
    ..These advancements come on the heels of exciting new modes of hormone action that challenge and expand upon the classic paradigms of hormone receptor function...
  7. doi request reprint Development of a thyroid hormone receptor targeting conjugate
    Jianfei Zheng
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    Bioconjug Chem 19:1227-34. 2008
    ..A related analogue JZ07 was a potent TR antagonist that is 13-fold selective for TRbeta over TRalpha. JZ01 localizes in the nuclei of TRbeta expressing cells and may serve as a prototype for other TR-targeting conjugates...
  8. ncbi request reprint Functionally orthogonal ligand-receptor pairs for the selective regulation of gene expression generated by manipulation of charged residues at the ligand-receptor interface of ER alpha and ER beta
    Youheng Shi
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    J Am Chem Soc 124:6921-8. 2002
    ..Attempts to modify the cationic residues by complementing Arg394-->Ala or Arg394-->Glu were not successful...
  9. ncbi request reprint Rational design of vitamin D3 analogues which selectively restore activity to a vitamin D receptor mutant associated with rickets
    Steve L Swann
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    Org Lett 4:3863-6. 2002
    ..The three analogues were 17 to 286 times more potent than 1,25(OH)2D3 with the mutant in cell-based assays and did not substantially activate cellular calcium influx...
  10. ncbi request reprint Light-activated transcription and repression by using photocaged SERMs
    Youheng Shi
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Chembiochem 5:788-96. 2004
    ..NB-Gtam and NB-Tam provide a light-activated transcription response at AP1-driven reporters, thus illustrating the unique ability of photocaged SERMs to simultaneously mediate light-activated transcription and repression...
  11. ncbi request reprint Mutant-selective thyromimetics for the chemical rescue of thyroid hormone receptor mutants associated with resistance to thyroid hormone
    Youheng Shi
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    Biochemistry 44:4612-26. 2005
    ....
  12. ncbi request reprint Structure-based design of selective agonists for a rickets-associated mutant of the vitamin d receptor
    Steve L Swann
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    J Am Chem Soc 124:13795-805. 2002
    ..3-121 nM). Significantly, the analogues are selective for the nuclear VDR and did not stimulate cellular calcium influx, which is associated with activation of the membrane-associated vitamin D receptor...
  13. pmc Circumventing anti-androgen resistance by molecular design
    Paula L McGinley
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    J Am Chem Soc 129:3822-3. 2007
  14. ncbi request reprint Design and synthesis of complementing ligands for mutant thyroid hormone receptor TRbeta(R320H): a tailor-made approach toward the treatment of resistance to thyroid hormone
    Atsushi Hashimoto
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Bioorg Med Chem 13:3627-39. 2005
    ....
  15. ncbi request reprint Photo-caged agonists of the nuclear receptors RARgamma and TRbeta provide unique time-dependent gene expression profiles for light-activated gene patterning
    Kristian H Link
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19176, USA
    Bioorg Med Chem 12:5949-59. 2004
    ....
  16. pmc Light activated recombination
    Kristian H Link
    Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
    J Am Chem Soc 127:13088-9. 2005
    ..Nv-HTaz and Cre-ER represent perhaps the first compound that can be used to photopattern gene expression through recombination...
  17. doi request reprint Selective chemical rescue of a thyroid-hormone-receptor mutant, TRbeta(H435Y), identified in pituitary carcinoma and resistance to thyroid hormone
    A Quamrul Hassan
    Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
    Angew Chem Int Ed Engl 47:7280-3. 2008
  18. doi request reprint Light-activated gene expression directs segregation of co-cultured cells in vitro
    Daniel J Sauers
    Departments of Chemistry and Biochemistry and Biological Sciences, University of Delaware, Newark, 19716, USA
    ACS Chem Biol 5:313-20. 2010
    ..The ability to direct the arrangement of cells on living cell monolayers through the action of light may serve as a model system for engineering artificial tissues...
  19. pmc Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation
    Gary H Posner
    Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA
    J Steroid Biochem Mol Biol 103:213-21. 2007
    ..The transcriptional activity of the 25-CHF(2) analog 3 is higher than that of the 1-CHF(2) analog 4...

Research Grants20

  1. Novel Ligand-Dependent Transcription Systems
    John Koh; Fiscal Year: 2004
    ..Applications of these compounds as biologically inert activators of conditional recombinases will also be explored. ..
  2. Molecular Complementation of Nuclear Receptors
    John Koh; Fiscal Year: 2007
    ..We will further develop these "functionally orthogonal" estrogen/ER pairs as novel chemical biology tools for dissecting the seven or more estrogen dependent signaling pathways. ..
  3. Photo-Inducible Transcriptional Regulators
    John Koh; Fiscal Year: 2007
    ..abstract_text> ..
  4. Molecular Complementation of Nuclear Receptors
    John Koh; Fiscal Year: 2009
    ..We will further develop these "functionally orthogonal" estrogen/ER pairs as novel chemical biology tools for dissecting the seven or more estrogen dependent signaling pathways. ..
  5. NOVEL LIGAND DEPENDENT TRANSCRIPTION SYSTEMS
    John Koh; Fiscal Year: 2000
    ..If successful this would represent a new and powerful strategy of treating a genetic disease by rational molecular design. ..
  6. Molecular Complementation of Nuclear Receptors
    John T Koh; Fiscal Year: 2010
    ..We will further develop these "functionally orthogonal" estrogen/ER pairs as novel chemical biology tools for dissecting the seven or more estrogen dependent signaling pathways. ..