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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

Molecular carcinogenesis, 2022-07, Vol.61 (7), p.643-654

2022

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Targeted Degradation of Androgen Receptor by VNPP433-3β in Castration-Resistant Prostate Cancer Cells Implicates Interaction with E3 Ligase MDM2 Resulting in Ubiquitin-Proteasomal Degradation

Cancers, 2023-02, Vol.15 (4), p.1198

2023

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Systematic Structure Modifications of Multitarget Prostate Cancer Drug Candidate Galeterone To Produce Novel Androgen Receptor Down-Regulating Agents as an Approach to Treatment of Advanced Prostate Cancer

Journal of medicinal chemistry, 2013-06, Vol.56 (12), p.4880-4898

2013

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VNLG-152R and its deuterated analogs potently inhibit/repress triple/quadruple negative breast cancer of diverse racial origins in vitro and in vivo by upregulating E3 Ligase Synoviolin 1 (SYVN1) and inducing proteasomal degradation of MNK1/2

Frontiers in oncology, 2023-09, Vol.13, p.1240996-1240996

2023

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The Novel Mnk1/2 Degrader and Apoptosis Inducer VNLG-152 Potently Inhibits TNBC Tumor Growth and Metastasis

Cancers, 2019-03, Vol.11 (3), p.299

2019

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Novel AR/AR-V7 and Mnk1/2 Degrader, VNPP433-3β: Molecular Mechanisms of Action and Efficacy in AR-Overexpressing Castration Resistant Prostate Cancer In Vitro and In Vivo Models

Cells (Basel, Switzerland), 2022-08, Vol.11 (17), p.2699

2022

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Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases

Bioorganic & medicinal chemistry, 2006-07, Vol.14 (13), p.4323-4340

2006

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Competitive Antagonism between the Nicotinic Allosteric Potentiating Ligand Galantamine and Kynurenic Acid at α7 Nicotinic Receptors

The Journal of pharmacology and experimental therapeutics, 2007-07, Vol.322 (1), p.48-58

2007

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Autophagy inhibition synergistically enhances anticancer efficacy of RAMBA, VN/12-1 in SKBR-3 cells, and tumor xenografts

Molecular cancer therapeutics, 2012-04, Vol.11 (4), p.898-908

2012

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Abstract LBA027: Mechanistic insights on the effects of the lead next generation galeterone analog, VNPP433-3β in castration resistant prostate cancer

Molecular cancer therapeutics, 2021-12, Vol.20 (12_Supplement), p.LBA027-LBA027

2021

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Novel deuterated Mnk1/2 protein degrader VNLG-152R analogs: Synthesis, In vitro Anti-TNBC activities and pharmacokinetics in mice

European journal of medicinal chemistry, 2022-08, Vol.238, p.114441-114441, Article 114441

2022

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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

Oncotarget, 2015-09, Vol.6 (29), p.27440-27460

2015

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Abstract LB235: Mechanistic studies on VNLG-152R-mediated tumor inhibition of triple negative breast cancer

Cancer research (Chicago, Ill.), 2023-04, Vol.83 (8_Supplement), p.LB235-LB235

2023

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Large-scale synthesis of galeterone and lead next generation galeterone analog VNPP433-3β

Steroids, 2022-09, Vol.185, p.109062-109062, Article 109062

2022

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Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model

Bioorganic chemistry, 2023-10, Vol.139, p.106700-106700, Article 106700

2023

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Design, Synthesis and Biological Activity of Certain 3,4-Disubstituted-5-mercapto-1,2,4-triazoles and Their Hydrazino Derivatives

Bulletin of the Korean Chemical Society, 2007, 28(12), , pp.2235-2240

2007

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Murine toxicology and pharmacokinetics of lead next generation galeterone analog, VNPP433-3β

Steroids, 2023-04, Vol.192, p.109184-109184, Article 109184

2023

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Sulforaphane covalently interacts with the transglutaminase 2 cancer maintenance protein to alter its structure and suppress its activity

Molecular carcinogenesis, 2022-01, Vol.61 (1), p.19-32

2022

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

The FEBS journal, 2016-11, Vol.283 (21), p.3898-3918

2016

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Galeterone and VNPT 55 disrupt Mnk‐ eIF 4E to inhibit prostate cancer cell migration and invasion

The FEBS journal, 2016-11, Vol.283 (21), p.3898-3918

2016

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Novel Approach: Androgen Receptor Down-Regulating Agents for the Treatment of All Stages of Prostate Cancer Disease

Biochemistry & pharmacology, 2012, Vol.1 (3)

Purushottamachar, Puranik

2012

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Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia

Molecular cancer therapeutics, 2015-08, Vol.14 (8), p.1777-1793

2015

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Improved Procedures for Gram-Scale Synthesis of Galeterone 3β-Imidazole and Galeterone 3β-Pyridine Methoxylate, Potent Androgen Receptor/Mnk Degrading Agents

Organic process research & development, 2016-09, Vol.20 (9), p.1654-1661

2016

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Abstract 1764: Galeterone and its novel analogs induce profound anti-cancer activities in human pancreatic cancer cell lines: Implications for pancreatic cancer therapy

Cancer research (Chicago, Ill.), 2015-08, Vol.75 (15_Supplement), p.1764-1764

2015

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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

Targeted Degradation of Androgen Receptor by VNPP433-3β in Castration-Resistant Prostate Cancer Cells Implicates Interaction with E3 Ligase MDM2 Resulting in Ubiquitin-Proteasomal Degradation

Systematic Structure Modifications of Multitarget Prostate Cancer Drug Candidate Galeterone To Produce Novel Androgen Receptor Down-Regulating Agents as an Approach to Treatment of Advanced Prostate Cancer

VNLG-152R and its deuterated analogs potently inhibit/repress triple/quadruple negative breast cancer of diverse racial origins in vitro and in vivo by upregulating E3 Ligase Synoviolin 1 (SYVN1) and inducing proteasomal degradation of MNK1/2

Galeterone and The Next Generation Galeterone Analogs, VNPP414 and VNPP433-3β Exert Potent Therapeutic Effects in Castration-/Drug-Resistant Prostate Cancer Preclinical Models In Vitro and In Vivo

The Novel Mnk1/2 Degrader and Apoptosis Inducer VNLG-152 Potently Inhibits TNBC Tumor Growth and Metastasis

Novel AR/AR-V7 and Mnk1/2 Degrader, VNPP433-3β: Molecular Mechanisms of Action and Efficacy in AR-Overexpressing Castration Resistant Prostate Cancer In Vitro and In Vivo Models

Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases

Competitive Antagonism between the Nicotinic Allosteric Potentiating Ligand Galantamine and Kynurenic Acid at α7 Nicotinic Receptors

Autophagy inhibition synergistically enhances anticancer efficacy of RAMBA, VN/12-1 in SKBR-3 cells, and tumor xenografts

Abstract LBA027: Mechanistic insights on the effects of the lead next generation galeterone analog, VNPP433-3β in castration resistant prostate cancer

Novel deuterated Mnk1/2 protein degrader VNLG-152R analogs: Synthesis, In vitro Anti-TNBC activities and pharmacokinetics in mice

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

Abstract LB235: Mechanistic studies on VNLG-152R-mediated tumor inhibition of triple negative breast cancer

Large-scale synthesis of galeterone and lead next generation galeterone analog VNPP433-3β

Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model

Design, Synthesis and Biological Activity of Certain 3,4-Disubstituted-5-mercapto-1,2,4-triazoles and Their Hydrazino Derivatives

Murine toxicology and pharmacokinetics of lead next generation galeterone analog, VNPP433-3β

Sulforaphane covalently interacts with the transglutaminase 2 cancer maintenance protein to alter its structure and suppress its activity

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

Galeterone and VNPT 55 disrupt Mnk‐ eIF 4E to inhibit prostate cancer cell migration and invasion

Novel Approach: Androgen Receptor Down-Regulating Agents for the Treatment of All Stages of Prostate Cancer Disease

Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia

Improved Procedures for Gram-Scale Synthesis of Galeterone 3β-Imidazole and Galeterone 3β-Pyridine Methoxylate, Potent Androgen Receptor/Mnk Degrading Agents

Abstract 1764: Galeterone and its novel analogs induce profound anti-cancer activities in human pancreatic cancer cell lines: Implications for pancreatic cancer therapy

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