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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.新型雄激素受体/雄激素受体剪接变异体 7 及丝裂原活化蛋白激酶 1/2 降解剂 VNPP433-3β:在雄激素受体过表达的去势抵抗性前列腺癌体外和体内模型中的作用机制及疗效。
Cells. 2022 Aug 30;11(17):2699. doi: 10.3390/cells11172699.

本文引用的文献

1
Androgen receptor antagonism drives cytochrome P450 17A1 inhibitor efficacy in prostate cancer.雄激素受体拮抗作用驱动细胞色素P450 17A1抑制剂在前列腺癌中的疗效。
J Clin Invest. 2017 Jun 1;127(6):2326-2338. doi: 10.1172/JCI87328. Epub 2017 May 2.
2
Targeting of CYP17A1 Lyase by VT-464 Inhibits Adrenal and Intratumoral Androgen Biosynthesis and Tumor Growth of Castration Resistant Prostate Cancer.VT-464 通过靶向 CYP17A1 裂解酶抑制去势抵抗性前列腺癌的肾上腺和肿瘤内雄激素生物合成及肿瘤生长。
Sci Rep. 2016 Oct 17;6:35354. doi: 10.1038/srep35354.
3
Galeterone and VNPT55 disrupt Mnk-eIF4E to inhibit prostate cancer cell migration and invasion.加列酮和VNPT55破坏Mnk-eIF4E以抑制前列腺癌细胞的迁移和侵袭。
FEBS J. 2016 Nov;283(21):3898-3918. doi: 10.1111/febs.13895. Epub 2016 Oct 1.
4
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.加列酮和VNPT55可诱导AR/AR-V7的蛋白酶体降解,通过细胞色素c释放诱导显著的细胞凋亡,并在体内抑制去势抵抗性前列腺癌异种移植物的生长。
Oncotarget. 2015 Sep 29;6(29):27440-60. doi: 10.18632/oncotarget.4578.
5
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.用于治疗各阶段前列腺癌的加列酮(TOK-001或VN/124-1)的发现与研发。
J Med Chem. 2015 Mar 12;58(5):2077-87. doi: 10.1021/jm501239f. Epub 2015 Jan 28.
6
Galeterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptor.加列酮可防止雄激素受体与染色质结合,并增强突变型雄激素受体的降解。
Clin Cancer Res. 2014 Aug 1;20(15):4075-85. doi: 10.1158/1078-0432.CCR-14-0292. Epub 2014 May 29.
7
Androgen receptor antagonists for prostate cancer therapy.用于前列腺癌治疗的雄激素受体拮抗剂。
Endocr Relat Cancer. 2014 Aug;21(4):T105-18. doi: 10.1530/ERC-13-0545. Epub 2014 Mar 17.
8
CYP17 inhibitors--abiraterone, C17,20-lyase inhibitors and multi-targeting agents.CYP17 抑制剂——阿比特龙、C17,20 裂解酶抑制剂和多靶点药物。
Nat Rev Urol. 2014 Jan;11(1):32-42. doi: 10.1038/nrurol.2013.274. Epub 2013 Nov 26.
9
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.系统地对多靶点前列腺癌候选药物 galeterone 进行结构修饰,以产生新型的雄激素受体下调剂,作为治疗晚期前列腺癌的一种方法。
J Med Chem. 2013 Jun 27;56(12):4880-98. doi: 10.1021/jm400048v. Epub 2013 Jun 7.
10
Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100.阿比特龙、依普利酮和泼尼松龙与野生型和突变型雄激素受体的相互作用:增加阿比特龙暴露量或与 MDV3100 联合用药的原理。
Cancer Res. 2012 May 1;72(9):2176-82. doi: 10.1158/0008-5472.CAN-11-3980. Epub 2012 Mar 12.

Androgen receptor antagonism and impact on inhibitors of androgen synthesis in prostate cancer therapy.

作者信息

Njar Vincent C O

机构信息

Department of Pharmacology, University of Maryland School of Medicine, Baltimore, MD, USA.

Center for Biomolecular Therapeutics, University of Maryland School of Medicine, Baltimore, MD, USA.

出版信息

Transl Cancer Res. 2017 Oct;6(Suppl 7):S1128-S1131. doi: 10.21037/tcr.2017.08.29.

DOI:10.21037/tcr.2017.08.29
PMID:30613487
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6319962/
Abstract
摘要