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Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo

Authors :
Negar Khazan
Kyu Kwang Kim
Jeanne N. Hansen
Niloy A. Singh
Taylor Moore
Cameron W. A. Snyder
Ravina Pandita
Myla Strawderman
Michiko Fujihara
Yuta Takamura
Ye Jian
Nicholas Battaglia
Naohiro Yano
Yuki Teramoto
Leggy A. Arnold
Russell Hopson
Keshav Kishor
Sneha Nayak
Debasmita Ojha
Ashoke Sharon
John M. Ashton
Jian Wang
Michael T. Milano
Hiroshi Miyamoto
David C. Linehan
Scott A. Gerber
Nada Kawar
Ajay P. Singh
Erdem D. Tabdanov
Nikolay V. Dokholyan
Hiroki Kakuta
Peter W. Jurutka
Nina F. Schor
Rachael B. Rowswell-Turner
Rakesh K. Singh
Richard G. Moore
Source :
Journal of Medicinal Chemistry. 65:6039-6055
Publication Year :
2022
Publisher :
American Chemical Society (ACS), 2022.

Abstract

Vitamin-D receptor (VDR) mRNA is overexpressed in neuroblastoma and carcinomas of lung, pancreas, and ovaries and predicts poor prognoses. VDR antagonists may be able to inhibit tumors that overexpress VDR. However, the current antagonists are arduous to synthesize and are only partial antagonists, limiting their use. Here, we show that the VDR antagonist MeTC7 (

Details

ISSN :
15204804 and 00222623
Volume :
65
Database :
OpenAIRE
Journal :
Journal of Medicinal Chemistry
Accession number :
edsair.doi.dedup.....a731dde934c1ad5d7982410ca3a6bd23
Full Text :
https://doi.org/10.1021/acs.jmedchem.1c01878