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Development of Thyroid Hormone Receptor-Targeting Conjugates.

Development of Thyroid Hormone Receptor-Targeting Conjugates.


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Thyroid hormone receptor (TR) functions as a ligand dependent transcriptional regulator that controls the expression of a specific set of genes involved in development and homeostasis in response to triiodothyronine (T3). There are a series of mutations that happen on the AF-2 domain of TRbeta, one isoform of TR, associated with severe resistance to thyroid hormone (RTH). In this work, a TR-targeting fluorescent probe molecule, JZ01 was developed. JZ01 showed low nano-molar binding affinity to TRbeta by fluorescence polarization assay, suggesting that the scaffold that JZ01 was based on can be used as a scaffold for TR-targeting conjugates. Another TR antagonist, JZ07 was developed. JZ07 is one of most selective antagonists reported to date, in favor of TRbeta over TRalpha, another isoform of TR with a 13-fold selectivity. Based on the scaffold structure of JZ01, several TR-targeting conjugates of synthetic transcription activation domain were designed and synthesized. Their transcription activities on the above AF-2-domain RTH mutants were evaluated by cellular reporter gene assays with different DNA binding elements, different cell types and different receptor constructions. However, none of the compounds showed great activity. These results are likely due to the following reasons: (1) high binding affinity and cellular/nuclear permeability required; (2) failure of dissociation of co-repressors; (3) the improper presentation of the artificial transcription activation domain; (4) high basal transcription caused by the experiment systems. Herein, several different TR-targeting scaffold compounds were also synthesized. These compounds are aiming to develop a scaffold compound that can bind to TRbeta RTH mutant (R320C, R320H or R316H) selectively over TRbeta wild type. The further purpose of these scaffold compounds is to develop conjugates with E2-E3 ligase ligand and selectively degrade the TRbeta mutant by the proteosome pathway. Binding affinities of these scaffold compounds towards TRbeta RTH mutants and TRbeta wild type are being tested by radio-labeled ligand binding assay.


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Product Details
  • ISBN-13: 9781244029231
  • Publisher: Proquest, Umi Dissertation Publishing
  • Publisher Imprint: Proquest, Umi Dissertation Publishing
  • Height: 254 mm
  • Weight: 277 gr
  • ISBN-10: 1244029238
  • Publisher Date: 01 Sep 2011
  • Binding: Paperback
  • Spine Width: 9 mm
  • Width: 203 mm


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Development of Thyroid Hormone Receptor-Targeting Conjugates.
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