Sumer Jasmine, Adel Mandl, Timothy E. G. Krueger, Susan L. Dalrymple, Lizamma Antony, Jennifer Dias, Cassandra A. Celatka, Amy E. Tapper, Maria Kleppe, Mayuko Kanayama, Yuezhou Jing, Valentina Speranzini, Yuzhuo Z. Wang, Jun Luo, Bruce J. Trock, Samuel R. Denmeade, Michael A. Carducci, Andrea Mattevi, Hugh Y. Rienhoff, John T. Isaacs, W. Nathaniel Brennen
{"title":"Characterization of structural, biochemical, pharmacokinetic, and pharmacodynamic properties of the LSD1 inhibitor bomedemstat in preclinical models","authors":"Sumer Jasmine, Adel Mandl, Timothy E. G. Krueger, Susan L. Dalrymple, Lizamma Antony, Jennifer Dias, Cassandra A. Celatka, Amy E. Tapper, Maria Kleppe, Mayuko Kanayama, Yuezhou Jing, Valentina Speranzini, Yuzhuo Z. Wang, Jun Luo, Bruce J. Trock, Samuel R. Denmeade, Michael A. Carducci, Andrea Mattevi, Hugh Y. Rienhoff, John T. Isaacs, W. Nathaniel Brennen","doi":"10.1002/pros.24707","DOIUrl":null,"url":null,"abstract":"Lysine-specific demethylase 1 (LSD1) is emerging as a critical mediator of tumor progression in metastatic castration-resistant prostate cancer (mCRPC). Neuroendocrine prostate cancer (NEPC) is increasingly recognized as an adaptive mechanism of resistance in mCRPC patients failing androgen receptor axis-targeted therapies. Safe and effective LSD1 inhibitors are necessary to determine antitumor response in prostate cancer models. For this reason, we characterize the LSD1 inhibitor bomedemstat to assess its clinical potential in NEPC as well as other mCRPC pathological subtypes.","PeriodicalId":501684,"journal":{"name":"The Prostate","volume":"32 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"The Prostate","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1002/pros.24707","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
Lysine-specific demethylase 1 (LSD1) is emerging as a critical mediator of tumor progression in metastatic castration-resistant prostate cancer (mCRPC). Neuroendocrine prostate cancer (NEPC) is increasingly recognized as an adaptive mechanism of resistance in mCRPC patients failing androgen receptor axis-targeted therapies. Safe and effective LSD1 inhibitors are necessary to determine antitumor response in prostate cancer models. For this reason, we characterize the LSD1 inhibitor bomedemstat to assess its clinical potential in NEPC as well as other mCRPC pathological subtypes.
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