Research Topics
| John KohSummaryAffiliation: University of Delaware Country: USA Publications
Research Grants
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Detail Information
Publications
Engineering selectivity and discrimination into ligand-receptor interfacesJohn 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...
The new biomimetic chemistry: artificial transcription factorsJohn 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...
Ligand-receptor engineering and its application towards the complementation of genetic disease and target identificationJohn T Koh
Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
Curr Top Med Chem 5:413-20. 2005....
Making virtual screening a realityJohn 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
A functionally orthogonal ligand-receptor pair created by targeting the allosteric mechanism of the thyroid hormone receptorA 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...
Chemical biology of steroid and nuclear hormone receptorsJohn 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...
Development of a thyroid hormone receptor targeting conjugateJianfei 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...
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 betaYouheng 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...
Rational design of vitamin D3 analogues which selectively restore activity to a vitamin D receptor mutant associated with ricketsSteve 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...
Light-activated transcription and repression by using photocaged SERMsYouheng 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...
Mutant-selective thyromimetics for the chemical rescue of thyroid hormone receptor mutants associated with resistance to thyroid hormoneYouheng Shi
Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19716, USA
Biochemistry 44:4612-26. 2005....
Structure-based design of selective agonists for a rickets-associated mutant of the vitamin d receptorSteve 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...
Circumventing anti-androgen resistance by molecular designPaula L McGinley
Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
J Am Chem Soc 129:3822-3. 2007
Design and synthesis of complementing ligands for mutant thyroid hormone receptor TRbeta(R320H): a tailor-made approach toward the treatment of resistance to thyroid hormoneAtsushi Hashimoto
Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
Bioorg Med Chem 13:3627-39. 2005....
Photo-caged agonists of the nuclear receptors RARgamma and TRbeta provide unique time-dependent gene expression profiles for light-activated gene patterningKristian H Link
Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19176, USA
Bioorg Med Chem 12:5949-59. 2004....
Light activated recombinationKristian 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...
Selective chemical rescue of a thyroid-hormone-receptor mutant, TRbeta(H435Y), identified in pituitary carcinoma and resistance to thyroid hormoneA Quamrul Hassan
Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, USA
Angew Chem Int Ed Engl 47:7280-3. 2008
Light-activated gene expression directs segregation of co-cultured cells in vitroDaniel 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...
Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluationGary 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 Grants
- Novel Ligand-Dependent Transcription SystemsJohn Koh; Fiscal Year: 2004..Applications of these compounds as biologically inert activators of conditional recombinases will also be explored. ..
- Molecular Complementation of Nuclear ReceptorsJohn 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. ..
- Photo-Inducible Transcriptional RegulatorsJohn Koh; Fiscal Year: 2007..abstract_text> ..
- Molecular Complementation of Nuclear ReceptorsJohn 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. ..
- NOVEL LIGAND DEPENDENT TRANSCRIPTION SYSTEMSJohn Koh; Fiscal Year: 2000..If successful this would represent a new and powerful strategy of treating a genetic disease by rational molecular design. ..
- Molecular Complementation of Nuclear ReceptorsJohn 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. ..
