Development of 17β-hydroxysteroid dehydrogenase type 3 as a target in hormone-dependent prostate cancer therapy

Ning, Xiaohui; Yang, Yan; Deng, Hong; Zhang, Qi-Hao; Huang, Yadong; Su, Zhijian; Fu, Yongmei; Xiang, Qi; Zhang, Shu

doi:10.1016/j.steroids.2017.02.003

Cited by 14 publications

(14 citation statements)

References 42 publications

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“…4–12 Steroidal derivatives comprise one of the broadest spectra of the therapeutic class of compounds and are being used extensively in modern medicine to treat different anomalies, including cancer. 10,13 Both natural and synthetic steroidal derivatives are known for their therapeutic properties such as agonists of cell-surface G-protein coupled bile acid receptor 1 (GP-BAR1), 8 neuroactive, 9 anticancer, 14 anti-Alzheimer, 15 and several other medicinal properties. 16 Thiazole derivatives are another class of pharmacologically important compounds with several approved drugs in this category including dasatinib and ritonavir.…”

mentioning

confidence: 99%

Benign Synthesis of Thiazolo-androstenone Derivatives as Potent Anticancer Agents

et al. 2018

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An unprecedented reaction of thiourea derivatives with 6β-bromoandrostenedione has been discovered for the formation of aminothiazolo-androstenones via a simple, safer, cascade protocol that enables the syntheses of novel molecules by using readily available reagents. The reaction mechanism of product formation has been rationalized by density functional theory calculations. This benign methodology accentuates a domino protocol deploying a renewable solvent, ethanol, while generating novel compounds that display potent growth inhibitory effects in in vitro studies for several cancer cell lines at submicromolar concentrations.

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confidence: 99%

Benign Synthesis of Thiazolo-androstenone Derivatives as Potent Anticancer Agents

et al. 2018

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“…Recently, a review describing HSD17B3 as a target in hormone-dependent PCa therapy has been published [77] , which described the main structure, function and reporting only a few examples of steroidal and non-steroidal inhibitors of HSD17B3. Here we provide a discussion of the most active nonsteroidal inhibitors developed to-date.…”

Section: Hsd17b3mentioning

confidence: 99%

Androgen-AR axis in primary and metastatic prostate cancer: chasing steroidogenic enzymes for therapeutic intervention

Pippione¹,

Boschi²,

Pors³

et al. 2017

JCMT

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Androgens play an important role in prostate cancer (PCa) development and progression. Although androgen deprivation therapy remains the front-line treatment for advanced prostate cancer, patients eventually relapse with the lethal form of the disease. The prostate tumor microenvironment is characterised by elevated tissue androgens that are capable of activating the androgen receptor (AR). Inhibiting the steroidogenic enzymes that play vital roles in the biosynthesis of testosterone (T) and dihydrotestosterone (DHT) seems to be an attractive strategy for PCa therapies. Emerging data suggest a role for the enzymes mediating pre-receptor control of T and DHT biosynthesis by alternative pathways in controlling intratumoral androgen levels, and thereby influencing PCa progression. This supports the idea for the development of multi-targeting strategies, involving both dual and multiple inhibitors of androgen-metabolising enzymes that are able to affect androgen synthesis and signalling at different points in the biosynthesis. In this review, we will focus on CYP17A1, AKR1C3, HSD17B3 and SRD5A, as these enzymes play essential roles in all the three androgenic pathways. We will review also the AR as an additional target for the design of bifunctional drugs. Targeting intracrine androgens and AKR1C3 have potential to overcome enzalutamide and abiraterone resistance and improve survival of advanced prostate cancer patients.

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“…Inhibitors of 17β-HSD3 enzyme may be superior to the existing endocrine therapies regarding the off-target effects since they could act selectively in an intracrine manner. 7) Because of its unique expression profile and substrate specificity, 17β-HSD3 could overall be a good target. Several groups have developed many of steroids so far, and non-steroidal 17β-HSD3 inhibitors had been also synthesized successively, such as RM-532-105, STX1383 and STX217.…”

Section: Introductionmentioning

confidence: 99%

Preclinical Pharmacokinetics, Tissue Distribution and Primary Safety Evaluation of a Novel Curcumin Analogue H10 Suspension, a Potential 17β Hydroxysteroid Dehydrogenase Type 3 Inhibitor

Xiao¹,

Yu²,

Li³

et al. 2021

CHEMICAL & PHARMACEUTICAL BULLETIN

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Development of 17β-hydroxysteroid dehydrogenase type 3 as a target in hormone-dependent prostate cancer therapy

Cited by 14 publications

References 42 publications

Benign Synthesis of Thiazolo-androstenone Derivatives as Potent Anticancer Agents

Benign Synthesis of Thiazolo-androstenone Derivatives as Potent Anticancer Agents

Androgen-AR axis in primary and metastatic prostate cancer: chasing steroidogenic enzymes for therapeutic intervention

Preclinical Pharmacokinetics, Tissue Distribution and Primary Safety Evaluation of a Novel Curcumin Analogue H10 Suspension, a Potential 17β Hydroxysteroid Dehydrogenase Type 3 Inhibitor

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