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Select item 99983511.

Murine Toxicology and Pharmacokinetics of Lead Next Generation Galeterone Analog, VNPP433–3β

Elizabeth Thomas, Retheesh S. Thankan, Puranik Purushottamachar, Jianxia Guo, Robert A. Parise, Jan H. Beumer, Vincent C. O. Njar

Steroids. Author manuscript; available in PMC 2024 Apr 1.

Published in final edited form as: Steroids. 2023 Apr; 192: 109184. Published online 2023 Jan 24. doi: 10.1016/j.steroids.2023.109184

PMCID:: PMC9998351

Abstract Article PDF–1023K

Select item 93222742.

Transcriptome profiling reveals that VNPP433‐3β, the lead next‐generation galeterone analog inhibits prostate cancer stem cells by downregulating epithelial–mesenchymal transition and stem cell markers

Elizabeth Thomas, Retheesh S. Thankan, Puranik Purushottamachar, Weiliang Huang, Maureen A. Kane, Yuji Zhang, Nicholas Ambulos, David J. Weber, Vincent C. O. Njar

Mol Carcinog. 2022 Jul; 61(7): 643–654. Published online 2022 May 5. doi: 10.1002/mc.23406

PMCID:: PMC9322274

Abstract Article PDF–4.7M

Select item 68531883.

Efficacy of Therapies After Galeterone in Patients With Castration-resistant Prostate Cancer

Rana R. McKay, Lillian Werner, Matthew Fiorillo, Jennifer Roberts, Elisabeth I. Heath, Glenn J. Bubley, Robert Bruce Montgomery, Mary-Ellen Taplin

Clin Genitourin Cancer. Author manuscript; available in PMC 2019 Nov 13.

Published in final edited form as: Clin Genitourin Cancer. 2017 Aug; 15(4): 463–471. Published online 2016 Oct 27. doi: 10.1016/j.clgc.2016.10.006

PMCID:: PMC6853188

Abstract Article PDF–415K

Select item 55330904.

Steroidogenic metabolism of galeterone reveals a diversity of biochemical activities

Mohammad Alyamani, Zhenfei Li, Michael Berk, Jianneng Li, Jingjie Tang, Sunil Upadhyay, Richard J. Auchus, Nima Sharifi

Cell Chem Biol. Author manuscript; available in PMC 2018 Jul 20.

Published in final edited form as: Cell Chem Biol. 2017 Jul 20; 24(7): 825–832.e6. Published online 2017 Jun 22. doi: 10.1016/j.chembiol.2017.05.020

PMCID:: PMC5533090

Abstract Article PDF–954K

Select item 54381095.

Structural and Functional Evaluation of Clinically Relevant Inhibitors of Steroidogenic Cytochrome P450 17A1

Elyse M. Petrunak, Steven A. Rogers, Jeffrey Aubé, Emily E. Scott

Drug Metab Dispos. 2017 Jun; 45(6): 635–645. Published online 2017 Jun. doi: 10.1124/dmd.117.075317

PMCID:: PMC5438109

Abstract Article PDF–1.7M

Select item 51181396.

Galeterone and VNPT55 disrupt Mnk-eIF4E to inhibit prostate cancer cell migration and invasion

Andrew K. Kwegyir-Afful, Robert D. Bruno, Puranik Purushottamachar, Francis N. Murigi, Vincent C. O. Njar

FEBS J. Author manuscript; available in PMC 2017 Nov 1.

Published in final edited form as: FEBS J. 2016 Nov; 283(21): 3898–3918. Published online 2016 Oct 1. doi: 10.1111/febs.13895

PMCID:: PMC5118139

Abstract Article PDF–2.3M

Select item 50462257.

The hunt for a selective 17,20 lyase inhibitor; learning lessons from nature

Ian M Bird, David H Abbott

J Steroid Biochem Mol Biol. Author manuscript; available in PMC 2017 Oct 1.

Published in final edited form as: J Steroid Biochem Mol Biol. 2016 Oct; 163: 136–146. Published online 2016 May 3. doi: 10.1016/j.jsbmb.2016.04.021

PMCID:: PMC5046225

Abstract Article PDF–951K

Select item 49560598.

Galeterone for the treatment of advanced prostate cancer: the evidence to date

Diogo A Bastos, Emmanuel S Antonarakis

Drug Des Devel Ther. 2016; 10: 2289–2297. Published online 2016 Jul 15. doi: 10.2147/DDDT.S93941

PMCID:: PMC4956059

Abstract Article PDF–601K

Select item 46950019.

Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts in vivo

Andrew K. Kwegyir-Afful, Senthilmurugan Ramalingam, Puranik Purushottamachar, Vidya P. Ramamurthy, Vincent C.O. Njar

Oncotarget. 2015 Sep 29; 6(29): 27440–27460. Published online 2015 Jul 14. doi: 10.18632/oncotarget.4578

PMCID:: PMC4695001

Abstract Article PDF–2.4M

Select item 456380410.

Treatment with Galeterone in An Elderly Man with Castration-Resistant Prostate Cancer: A Case Report

Rana R. McKay, Khalid Mamlouk, Bruce Montgomery, Mary-Ellen Taplin

Clin Genitourin Cancer. Author manuscript; available in PMC 2015 Sep 9.

Published in final edited form as: Clin Genitourin Cancer. 2015 Aug; 13(4): e325–e328. Published online 2014 Dec 31. doi: 10.1016/j.clgc.2014.12.015

PMCID:: PMC4563804

Article PDF–276K

Select item 416715611.

Changing paradigms in management of metastatic Castration Resistant Prostate Cancer (mCRPC)

Eva Gupta, Troy Guthrie, Winston Tan

BMC Urol. 2014; 14: 55. Published online 2014 Jul 25. doi: 10.1186/1471-2490-14-55

PMCID:: PMC4167156

Abstract Article PDF–388K

Select item 411949612.

Galeterone Prevents Androgen Receptor Binding to Chromatin and Enhances Degradation of Mutant Androgen Receptor

Ziyang Yu, Changmeng Cai, Shuai Gao, Nicholas I. Simon, Howard C. Shen, Steven P. Balk

Clin Cancer Res. Author manuscript; available in PMC 2015 Aug 1.

Published in final edited form as: Clin Cancer Res. 2014 Aug 1; 20(15): 4075–4085. Published online 2014 May 29. doi: 10.1158/1078-0432.CCR-14-0292

PMCID:: PMC4119496

Abstract Article PDF–1.5M

Select item 404097913.

17α-Hydroxylase/17,20 lyase inhibitor VN/124-1 inhibits growth of androgen-independent prostate cancer cells via induction of the endoplasmic reticulum stress response

Robert D. Bruno, Tony D. Gover, Angelika M. Burger, Angela M. Brodie, Vincent C. O. Njar

Mol Cancer Ther. Author manuscript; available in PMC 2014 Jun 2.

Published in final edited form as: Mol Cancer Ther. 2008 Sep; 7(9): 2828–2836. doi: 10.1158/1535-7163.MCT-08-0336

PMCID:: PMC4040979

Abstract Article PDF–868K

Select item 402336414.

Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer

Mark N Stein, Neal Patel, Alexander Bershadskiy, Alisa Sokoloff, Eric A Singer

Asian J Androl. 2014 May-Jun; 16(3): 387–400. Published online 2014 Apr 18. doi: 10.4103/1008-682X.129133

PMCID:: PMC4023364

Abstract Article PDF–1.1M

Select item 395974415.

Systematic Structure Modifications of Multi-target Prostate Cancer Drug Candidate Galeterone to Produce Novel Androgen Receptor Down-regulating Agents as an Approach to Treatment of Advanced Prostate Cancer

Puranik Purushottamachar, Abhijit M. Godbole, Lalji K. Gediya, Marlena S. Martin, Tadas S. Vasaitis, Andrew K. Kwegyir-Afful, Senthilmurugan Ramalingam, Zeynep Ates-Alagoz, Vincent C. O. Njar

J Med Chem. Author manuscript; available in PMC 2014 Jun 27.

Published in final edited form as: J Med Chem. 2013 Jun 27; 56(12): 4880–4898. Published online 2013 Jun 7. doi: 10.1021/jm400048v

PMCID:: PMC3959744

Abstract Article PDF–2.6M

Select item 328167716.

Direct Regulation of Androgen Receptor Activity by Potent CYP17 Inhibitors in Prostate Cancer Cells

Harris S. Soifer, Naira Souleimanian, Sijian Wu, Anatoliy M. Voskresenskiy, Filiz Kisaayak Collak, Bekir Cinar, Cy A. Stein

J Biol Chem. 2012 Feb 3; 287(6): 3777–3787. Published online 2011 Dec 15. doi: 10.1074/jbc.M111.261933

PMCID:: PMC3281677

Abstract Article PDF–2.1M

Select item 327113917.

CYTOCHROME P450 17A1 STRUCTURES WITH PROSTATE CANCER DRUGS ABIRATERONE AND TOK-001

Natasha M. DeVore, Emily E. Scott

Nature. Author manuscript; available in PMC 2012 Aug 2.

Published in final edited form as: Nature. 2012 Feb 2; 482(7383): 116–119. Published online 2012 Jan 22. doi: 10.1038/nature10743

PMCID:: PMC3271139

Abstract Article PDF–2.3M

Select item 317156718.

Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001) analogs: Head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model

Robert D. Bruno, Tadas S. Vasaitis, Lalji K. Gediya, Puranik Purushottamachar, Abhijit M. Godbole, Zeynep Ates-Alagoz, Angela M. H. Brodie, Vincent C. O. Njar

Steroids. Author manuscript; available in PMC 2012 Nov 1.

Published in final edited form as: Steroids. 2011 Nov; 76(12): 1268–1279. Published online 2011 Jun 24. doi: 10.1016/j.steroids.2011.06.002

PMCID:: PMC3171567

Abstract Article PDF–2.3M

Select item 304760319.

CYP17 inhibitors for prostate cancer therapy

Tadas S. Vasaitis, Robert D. Bruno, Vincent C. O. Njar

J Steroid Biochem Mol Biol. Author manuscript; available in PMC 2012 May 1.

Published in final edited form as: J Steroid Biochem Mol Biol. 2011 May; 125(1-2): 23–31. Published online 2010 Nov 17. doi: 10.1016/j.jsbmb.2010.11.005

PMCID:: PMC3047603

Abstract Article PDF–1.8M

Select item 296587920.

Prolonging hormone sensitivity in prostate cancer xenografts through dual inhibition of AR and mTOR

A Schayowitz, G Sabnis, O Goloubeva, V C O Njar, A M H Brodie

Br J Cancer. 2010 Sep 28; 103(7): 1001–1007. Published online 2010 Sep 14. doi: 10.1038/sj.bjc.6605882

PMCID:: PMC2965879

Abstract Article PDF–432K

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