Literature DB >> 23806555

Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions.

Yosuke Demizu1, Saori Nagoya, Manami Shirakawa, Megumi Kawamura, Nanako Yamagata, Yukiko Sato, Mitsunobu Doi, Masaaki Kurihara.   

Abstract

We synthesized stapled helical leucine-based peptides (DPI-01-07) containing 2-aminoisobutyric acid and a covalent cross-linked unit as inhibitors of vitamin D receptor (VDR)-coactivator interactions. The effects of these peptides on the human VDR were examined in an inhibition assay based on the receptor cofactor assay system, and one of them, DPI-07, exhibited potent inhibitory activity (IC₅₀: 3.2 μM).
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23806555     DOI: 10.1016/j.bmcl.2013.06.002

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Design, synthesis, and anti-HIV-1 activity of 1-aromatic methyl-substituted 3-(3,5-dimethylbenzyl)uracil and N-3,5-dimethylbenzyl-substituted urea derivatives.

Authors:  Norikazu Sakakibara; Masanori Baba; Mika Okamoto; Masaaki Toyama; Yosuke Demizu; Takashi Misawa; Masaaki Kurihara; Kohji Irie; Yoshihisa Kato; Tokumi Maruyama
Journal:  Antivir Chem Chemother       Date:  2015-02

Review 2.  Alternative binding sites at the vitamin D receptor and their ligands.

Authors:  Tania R Mutchie; Olivia B Yu; Elliot S Di Milo; Leggy A Arnold
Journal:  Mol Cell Endocrinol       Date:  2019-01-14       Impact factor: 4.102

Review 3.  High-Throughput Screening by Nuclear Magnetic Resonance (HTS by NMR) for the Identification of PPIs Antagonists.

Authors:  Bainan Wu; Elisa Barile; Surya K De; Jun Wei; Angela Purves; Maurizio Pellecchia
Journal:  Curr Top Med Chem       Date:  2015       Impact factor: 3.295

Review 4.  Inhibitors for the Vitamin D Receptor-Coregulator Interaction.

Authors:  Kelly A Teske; Olivia Yu; Leggy A Arnold
Journal:  Vitam Horm       Date:  2015-11-30       Impact factor: 3.421

  4 in total

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