摘要
了解去势耐药前列腺癌的耐药机制。 背景:左旋脲(MDV 3100,XTANDI)是第二代雄激素受体抑制剂,专为治疗去势耐药前列腺癌(Crpc)而设计,具有较长的生存期。是时候了。MDV 3100耐药的机制尚不清楚,大多数接受治疗的患者,无论是先天的还是后天的,都会出现耐药性。 目的:本综述旨在总结MDV3100抗性机制中可用的主要数据。 了解所引起的阻力对und具有临床意义在日常实践和改进策略中,对预后和预测生物标志物的有效性进行了评价。 结果:MDV 3100的耐药主要可分为两种不同的途径,一是依赖于雄激素受体的活性,二是与雄激素受体的活性无关。雄激素受体(AR)轴位于第一位。前列腺癌细胞的重要通路,目前仍被认为是一种重要的耐药机制。 结论:靶向这些新识别的信号,尤其是AR轴,可能通过新的治疗剂潜在地克服,协同地改善CRPC中的ADT。
关键词: 去势抵抗性前列腺癌,enzalutamide,耐药性,雄激素受体,生物标志物,抑制剂。
Current Drug Targets
Title:Drug Resistance of Enzalutamide in CRPC
Volume: 19 Issue: 6
关键词: 去势抵抗性前列腺癌,enzalutamide,耐药性,雄激素受体,生物标志物,抑制剂。
摘要: Understanding and targeting the mechanisms of resistance to enzalutamide in castration resistant prostate cancer.
Background: Enzalutamide (MDV3100, XTANDI) is a second generation androgen receptor inhibitor that is designed for the treatment of castration-resistant prostate cancer (CRPC) and has prolonged survival time. The mechanisms of mdv3100 resistance have not yet been clearly clarified and the majority of treated patients, innate or acquiring resistance invariably arises.
Objective: The purpose of this review is to summarize the main data available on the mechanisms of resistance to mdv3100. Understanding how the resistance aroused may have clinical implications in underlying the usefulness of prognostic and predictive biomarkers in daily practice and improving the strategies.
Results: Resistance to MDV3100 could be basically divided into two distinct pathways, either dependent or independent of the androgen receptor activity. Androgen receptor (AR) axis is sitll the most important pathway for prostate cancer cells and it is still currently regarded as a critical resistant mechanism.
Conclusion: Targeting these newly identified signals, especially AR axis, could be potentially overcome through novel therapeutic agents, synergically improve the ADT in CRPC.
Export Options
About this article
Cite this article as:
Drug Resistance of Enzalutamide in CRPC, Current Drug Targets 2018; 19 (6) . https://dx.doi.org/10.2174/1389450118666170417144250
DOI https://dx.doi.org/10.2174/1389450118666170417144250 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
Drug-Targeted Approach with Polymer Nanocomposites for Improved Therapeutics
Polymer nanocomposites have been recognized as an advanced and cutting-edge technique in drug targeting administration. These materials combine the unique features of nanoparticles with the adaptability of polymers to produce highly personalized drug administration devices. Integrating nanoparticles containing pharmaceuticals into a polymer matrix enables researchers to regulate the rates at ...read more
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...read more
Therapeutic Chemical and RNA Design with Artificial Intelligence
Computer-Aided Drug Design (CADD) has emerged as a fundamental component of modern drug discovery. Molecular docking facilitates virtual screening on a large scale through structural simulations. However, traditional CADD approaches face significant limitations, as they can only screen known compounds from existing libraries. PubChem, as the most widely used chemical ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
A Complete Overview of the Polycystic Ovarian Syndrome with Recent Advancement in Clinical Trial
Current Women`s Health Reviews Noscapine and its Analogs as Chemotherapeutic Agent: Current updates
Current Topics in Medicinal Chemistry Applications of Aptamers in Targeted Imaging: State of the Art
Current Topics in Medicinal Chemistry 30 Years Lost in Anesthesia Theory
Cardiovascular & Hematological Agents in Medicinal Chemistry The Metastatic Process: Methodological Advances and Pharmacological Challenges
Current Medicinal Chemistry HCN Channels Modulators: The Need for Selectivity
Current Topics in Medicinal Chemistry Marizomib, a Proteasome Inhibitor for All Seasons: Preclinical Profile and a Framework for Clinical Trials
Current Cancer Drug Targets Cancer-Type Organic Anion Transporting Polypeptide 1B3: Current Knowledge of the Gene Structure, Expression Profile, Functional Implications and Future Perspectives
Current Drug Metabolism Poxvirus-Based Vaccines for Cancer Immunotherapy: New Insights from Combined Cytokines/Co-Stimulatory Molecules Delivery and “Uncommon” Strains
Anti-Cancer Agents in Medicinal Chemistry NF-κB Signaling and Carcinogenesis
Current Pharmaceutical Design Targeting Cancer Cells by an Oxidant-Based Therapy
Current Molecular Pharmacology The Human Glioma-Associated Oncogene Homolog 1 (GLI1) Family of Transcription Factors in Gene Regulation and Diseases
Current Genomics Inhibitors of HDACs - Effective Drugs Against Cancer?
Current Cancer Drug Targets Potential Anti-cancer Drugs Commonly Used for Other Indications
Current Cancer Drug Targets Analysis of Differential Gene Expression Based on Bayesian Estimation of Variance
Current Bioinformatics Anticancer Agents: Towards the Future
Current Medicinal Chemistry - Anti-Cancer Agents Synthesis of bis(indolyl)methanes Using Naturally Occurring, Biodegradable Itaconic Acid as a Green and Reusable Catalyst
Current Organic Synthesis Targeting DNA Minor Groove by Hybrid Molecules as Anticancer Agents
Current Medicinal Chemistry Chemical and Radiochemical Considerations in Radiolabeling with α-Emitting Radionuclides
Current Radiopharmaceuticals Therapeutic Option of Plasmid-DNA Based Gene Transfer
Current Topics in Medicinal Chemistry