Rêve et douleur

Zadra, Antonio; Manzini, Christiane

doi:10.1007/bf03007108

Cited by 2 publications

(1 citation statement)

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“…As a result, the ubiquitination and ubiquitin-proteasome-dependent degradation of AR and AR-V7 were increased (Xu, Sun et al, 2020). Other agents, including fatty acid synthase inhibitor (FASN) IPI-9119, luteolin, triterpenoid antioxidant drug bardoxolone-methyl (CDDO-Me), and GnRH antagonist degarelix (Firmagon), have also been identified as inhibitors of the AR-V7 protein in Enz-resistant CRPC (Zadra, Ribeiro et al, 2019, Naiki-Ito, Naiki et al, 2019, Cucchiara, Yang et al, 2019.…”

Section: Androgen Receptor Splice Variantsmentioning

confidence: 99%

Mechanisms of Enzalutamide Resistance in Castration-Resistant Prostate Cancer and Therapeutic Strategies to Overcome It

Wang

Chen

et al. 2020

Preprint

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Prostate cancer (PCa) is the second most common malignancy in men, and androgen deprivation therapy (ADT) is the first-line therapy. However, most cases will eventually develop into castration-resistant prostate cancer (CRPC) after ADT treatment. Enzalutamide (Enz) is a second-generation androgen receptor inhibitor approved by the Food and Drug Administration to treat patients with CRPC. Unfortunately, patients receiving Enz treatment will ultimately develop resistance via various complicated mechanisms. In this review, we introduce the emerging information on resistance mechanisms, including androgen receptorrelated signalling pathways, glucocorticoid receptor-related pathways, and metabolic mechanisms. Notably, lineage plasticity and phenotype switching, gene polymorphisms, and the relationship between microRNAs and drug resistance are addressed. Furthermore, potential therapeutic strategies for Enz-resistant CRPC treatment are suggested, which can help in the discovery of more effective and specific regimens to overcome Enz resistance.

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Section: Androgen Receptor Splice Variantsmentioning

confidence: 99%