Literature DB >> 17154490

Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor.

Konrad Koehler1, Sandra Gordon, Peter Brandt, Bo Carlsson, Anna Bäcksbro-Saeidi, Theresa Apelqvist, Peter Agback, Gary J Grover, William Nelson, Marlena Grynfarb, Mathias Färnegårdh, Stefan Rehnmark, Johan Malm.   

Abstract

A new high-affinity thyroid hormone antagonist 6 with druglike properties was designed and synthesized. The compound behaved as an antagonist in a cell transactivation assay, and in a first in vivo experiment in rats.

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Year:  2006        PMID： 17154490     DOI： 10.1021/jm060521i

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  8 in total

1.  Silanol: a traceless directing group for Pd-catalyzed o-alkenylation of phenols.

Authors:  Chunhui Huang; Buddhadeb Chattopadhyay; Vladimir Gevorgyan
Journal:  J Am Chem Soc       Date:  2011-07-21       Impact factor: 15.419

2.  Copper-catalyzed ortho-acylation of phenols with aryl aldehydes and its application in one-step preparation of xanthones.

Authors:  Jun Hu; Enoch A Adogla; Yong Ju; Daping Fan; Qian Wang
Journal:  Chem Commun (Camb)       Date:  2012-10-15       Impact factor: 6.222

3.  Prediction of binding affinity and efficacy of thyroid hormone receptor ligands using QSAR and structure-based modeling methods.

Authors:  Regina Politi; Ivan Rusyn; Alexander Tropsha
Journal:  Toxicol Appl Pharmacol       Date:  2014-07-21       Impact factor: 4.219

4.  Atom-based 3D-QSAR, molecular docking and molecular dynamics simulation assessment of inhibitors for thyroid hormone receptor α and β.

Authors:  Manish Kumar Gupta; Krishna Misra
Journal:  J Mol Model       Date:  2014-06-05       Impact factor: 1.810

5.  A dual-acceptor time-resolved Föster resonance energy transfer assay for simultaneous determination of thyroid hormone regulation of corepressor and coactivator binding to the thyroid hormone receptor: Mimicking the cellular context of thyroid hormone action.

Authors:  M Jeyakumar; John A Katzenellenbogen
Journal:  Anal Biochem       Date:  2008-12-07       Impact factor: 3.365

6.  (-) Arctigenin and (+) pinoresinol are antagonists of the human thyroid hormone receptor β.

Authors:  Ifedayo Victor Ogungbe; Rebecca A Crouch; Teresa Demeritte
Journal:  J Chem Inf Model       Date:  2014-11-13       Impact factor: 4.956

7.  Halogen Bonding in Haspin-Halogenated Tubercidin Complexes: Molecular Dynamics and Quantum Chemical Calculations.

Authors:  Yujing Zhou; Ming Wah Wong
Journal:  Molecules       Date:  2022-01-21       Impact factor: 4.411

8.  Revealing a Mutant-Induced Receptor Allosteric Mechanism for the Thyroid Hormone Resistance.

Authors:  Benqiang Yao; Yijuan Wei; Shuchi Zhang; Siyu Tian; Shuangshuang Xu; Rui Wang; Weili Zheng; Yong Li
Journal:  iScience       Date:  2019-10-02
  8 in total

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