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

Negar Khazan, Kyu Kwang Kim, Jeanne N. Hansen, Niloy A. Singh, Taylor Moore, Cameron Snyder, Ravina Pandita, Myla Strawderman, Michiko Fujihara, Yuta Takamura, Jian Ye, 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 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

2022Journal of Medicinal Chemistry11 citationsDOIOpen Access PDF

Abstract

induces major changes in the binding motifs, which potentially result in VDR antagonistic effects. These data highlight the therapeutic benefits of targeting VDR for the treatment of malignancies and demonstrate the creation of selective VDR antagonists that are easy to synthesize.

Topics & Concepts

Calcitriol receptorIn vivoChemistryAntagonistCancer researchPharmacologyNeuroblastomaReceptorRetinoid X receptorCell cultureTranscription factorNuclear receptorBiochemistryBiologyGeneGeneticsNeuroblastoma Research and TreatmentsCancer, Hypoxia, and MetabolismNeuroendocrine Tumor Research Advances
Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors <i>In Vivo</i> | Litcius