Medicine in Drug Discovery最新文献_第5页

Understanding drug resistance in breast cancer: Mechanisms and emerging therapeutic strategies 了解乳腺癌的耐药性：机制和新兴的治疗策略

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2025-05-21 DOI: 10.1016/j.medidd.2025.100210

Shreastha Gautam , Rashmi Maurya , Akash Vikal , Preeti Patel , Shubham Thakur , Amandeep Singh , Ghanshyam Das Gupta , Balak Das Kurmi

Breast cancer is one of the primary reasons for cancer-related death all around the world, and drug resistance poses a big challenge in its effective treatment. This review gives a detailed explanation regarding the complex mechanisms causing drug resistance in breast cancer, that are of two types one being intrinsic, and the other being acquired resistance. An elaborate discussion regarding hormone receptor-mediated resistance, including progesterone receptor and estrogen receptor pathways, is provided, emphasizing alterations in signaling cascades and epigenetic modifications. Similarly, the role of human epidermal growth factor receptor 2-positive breast cancer in developing resistance through mutations, receptor crosstalk, and downstream signaling disruptions is thoroughly examined. To combat multidrug resistance in breast cancer, several therapeutic strategies have been explored. This review discusses how nanotherapeutics show promise in managing drug efflux alongside enhancing drug targeting capabilities. The article discusses combination therapy strategies because they aim to combat resistance through multiple simultaneous target pathways. The application of phytochemicals represents a new approach for managing drug resistance through their natural bioactive compounds, which demonstrate anti-cancer capabilities. Understanding these molecular mechanisms and novel therapeutic interventions is essential for enhancing breast cancer outcomes and developing more effective strategies to combat resistance.

乳腺癌是世界范围内癌症相关死亡的主要原因之一，而耐药性对其有效治疗提出了巨大挑战。本文对乳腺癌耐药的复杂机制进行了详细的阐述，主要分为内在耐药和获得性耐药两种类型。详细讨论了激素受体介导的耐药性，包括孕激素受体和雌激素受体途径，强调信号级联和表观遗传修饰的改变。类似地，人类表皮生长因子受体2阳性乳腺癌在通过突变、受体串扰和下游信号中断产生耐药性中的作用也得到了彻底的研究。为了对抗乳腺癌的多药耐药，已经探索了几种治疗策略。这篇综述讨论了纳米疗法如何在管理药物外排和增强药物靶向能力方面显示出希望。本文讨论了联合治疗策略，因为它们旨在通过多个同时的靶点途径来对抗耐药性。植物化学物质的应用代表了通过其天然生物活性化合物来控制耐药性的新途径，这些化合物具有抗癌能力。了解这些分子机制和新的治疗干预措施对于提高乳腺癌预后和制定更有效的对抗耐药性策略至关重要。

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引用次数: 0

Timing of benzodiazepine treatment and mortality in adult patients with generalized convulsive status epilepticus 全身性惊厥癫痫持续状态成人患者的苯二氮卓类药物治疗时机和死亡率

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2025-05-16 DOI: 10.1016/j.medidd.2025.100209

Au Auvichayapat , Verajit Chotmongkol , Kittisak Sawanyawisuth , Somsak Tiamkao

Status epilepticus is an emergency condition with a high mortality rate. However, there is currently limited data on the timing of antiepileptic drugs (AED) and mortality, particularly generalized convulsive status epilepticus. This study aims to evaluate if early AED treatment is associated with mortality in patients with generalized convulsive status epilepticus. This was a retrospective cohort study, which enrolled patients 18 years or over who had been diagnosed with generalized convulsive status epilepticus and had discharge status. Eligible patients were selected from the database of University Hospital. Predictors for mortality were analyzed by logistic regression analysis. A total of 77 patients met the study criteria; of those 27 patients (35.06 %) died. There were seven factors included in the stepwise multivariable logistic regression analysis. Among those, only five factors were retained in the predictive model for mortality: These included the time from seizure onset to benzodiazepine treatment, the time from the seizure onset to the first AED, number of AEDs, AED withdrawal, and Status Epilepticus Severity Score (STESS). Of those, only the time from seizure onset to benzodiazepine treatment and the STESS were independently associated with mortality with adjusted odds ratios of 1.03 (95 % confidence interval of 1.01, 1.06) and 1.54 (95 % confidence interval of 1.08, 2.22), respectively. Sensitivity of time from seizure onset to benzodiazepine treatment of five minutes or more had a sensitivity of 100 %. Early treatment with benzodiazepine, that is within five minutes after the occurrence of status epilepticus may lower mortality rate in adult patients with generalized convulsive status epilepticus.

癫痫持续状态是一种死亡率很高的紧急情况。然而，目前关于抗癫痫药物（AED）的使用时间和死亡率的数据有限，特别是广泛性癫痫持续状态。本研究旨在评估早期AED治疗是否与全身性惊厥癫痫持续状态患者的死亡率相关。这是一项回顾性队列研究，纳入了18岁或以上被诊断为全身性惊厥癫痫持续状态并有出院状态的患者。从大学医院数据库中选取符合条件的患者。死亡率预测因子采用logistic回归分析。共有77例患者符合研究标准；死亡27例（35.06%）。逐步多变量logistic回归分析包括7个因素。其中，只有5个因素保留在死亡率的预测模型中：从癫痫发作到苯二氮卓类药物治疗的时间，从癫痫发作到第一次使用AED的时间，AED的数量，AED的停药和癫痫持续状态严重程度评分（ess）。其中，只有癫痫发作到苯二氮卓类药物治疗的时间和应激压力与死亡率独立相关，校正比值比分别为1.03（95%可信区间为1.01,1.06）和1.54（95%可信区间为1.08,2.22）。从癫痫发作到苯二氮卓类药物治疗5分钟或更长时间的敏感性为100%。早期应用苯二氮卓类药物治疗，即在癫痫持续状态发生后5分钟内，可降低全面性惊厥癫痫持续状态的成人患者的死亡率。

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引用次数: 0

Impact of bariatric surgery on vitamin D metabolism and micronutrient deficiencies in severe obesity 减肥手术对严重肥胖患者维生素D代谢和微量营养素缺乏的影响

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2025-04-04 DOI: 10.1016/j.medidd.2025.100207

Letícia de Oliveira Souza Bratti , Bruno Fonseca Nunes , Daphany Marah Gorges , Emerita Quintina de Andrade Moura , Ana Carolina Rabello de Moraes , Fabíola Branco Filippin-Monteiro

Objective

This study aimed to investigate the impact of bariatric surgery on vitamin D metabolism and associated micronutrient deficiencies in individuals with obesity, emphasizing the prevalence of vitamin D deficiency in patients with severe obesity—a persistent concern after significant weight loss.

Methods

A comprehensive analysis of serum levels of 25(OH)D, parathyroid hormone (PTH), and calcium was conducted in patients with obesity before and after bariatric surgery, with a six-month follow-up. Medication usage was examined, and outcomes between different surgical techniques were compared.

Results

Notable metabolic improvements, linked to reduced BMI and diminished medication reliance post-surgery, were observed. Sleeve gastrectomy (SG) demonstrated potential advantages in preventing micronutrient deficiencies. Many patients had preoperative vitamin D deficiency and elevated PTH levels. Correlation analysis revealed that among those with preoperative PTH levels exceeding 70 pg/mL, higher PTH levels were associated with lower weight loss after six months. No significant correlation was found for vitamin D.

Conclusion

This study underscores the importance of critically assessing bone health in bariatric surgery candidates, emphasizing the need for meticulous preoperative evaluation and postoperative monitoring, particularly in cases of secondary hyperparathyroidism. These considerations are pivotal for optimizing the long-term well-being of bariatric surgery patients.

目的：本研究旨在探讨减肥手术对肥胖患者维生素D代谢和相关微量营养素缺乏的影响，强调严重肥胖患者维生素D缺乏的患病率，这是体重显著减轻后持续关注的问题。方法对肥胖患者减肥手术前后血清25(OH)D、甲状旁腺激素（PTH）、钙水平进行综合分析，随访6个月。检查药物使用情况，并比较不同手术方式的结果。结果观察到显著的代谢改善，与术后BMI降低和药物依赖性降低有关。袖式胃切除术（SG）在预防微量营养素缺乏方面显示出潜在的优势。许多患者术前维生素D缺乏，甲状旁腺激素水平升高。相关分析显示，术前PTH水平超过70 pg/mL的患者，PTH水平越高，6个月后体重减轻越少。结论本研究强调了对减肥手术患者进行骨骼健康评估的重要性，强调了术前和术后监测的必要性，特别是在继发性甲状旁腺功能亢进的情况下。这些考虑对于优化减肥手术患者的长期健康至关重要。

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引用次数: 0

From Fins to Furs: Unlocking the Therapeutic Potential of Animal-derived Bioactives for Wound Care 从鳍到毛皮：释放动物源性生物活性物质的治疗潜力，用于伤口护理

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2025-03-22 DOI: 10.1016/j.medidd.2025.100206

Hui Sin Lim , Christopher J. Serpell , Satoshi Ogawa , Yong Yu Hu , Eng Hwa Wong

Animal-derived products, such as organs, secretions, and mucus, have been part and parcel of traditional medicine and are often overlooked in the modern healthcare system. Nevertheless, researchers have begun to explore the untapped potential of bioactive compounds from marine organisms, reptiles, amphibians, and insects, thus offering innovative solutions for wound care. This review delved into the medicinal properties of animal-based bioactive compounds in wound healing based on in vitro and in vivo studies. A comparative analysis of the empirical evidence was performed to determine the benefits and limitations of animal-derived bioactive compounds. In summary, the literature suggests that animal-derived products could regulate biological pathways involved in inflammation and tissue regeneration. Clinical trials are underway to affirm the feasibility and safety of these compounds for human health applications.

动物来源的产品，如器官、分泌物和粘液，一直是传统医学的重要组成部分，但在现代卫生保健系统中往往被忽视。尽管如此，研究人员已经开始从海洋生物、爬行动物、两栖动物和昆虫中探索尚未开发的生物活性化合物的潜力，从而为伤口护理提供创新的解决方案。本文在体外和体内研究的基础上，深入探讨了动物源性生物活性化合物在伤口愈合中的药用特性。对经验证据进行了比较分析，以确定动物源性生物活性化合物的优点和局限性。综上所述，文献表明动物源性产品可以调节炎症和组织再生的生物学途径。临床试验正在进行，以确认这些化合物对人类健康应用的可行性和安全性。

引用次数: 0

Bacterial-based drug delivery systems: A new way to combat infectious disease 基于细菌的药物输送系统：对抗传染病的新方法

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2025-03-18 DOI: 10.1016/j.medidd.2025.100205

Parastoo TabibzadehTehrani , Mina Nazari , Pedram Rastgoo , Niloofar Seyed Bolouri , Reyhaneh HeydariKarsaf , Abtin Hadiani , Zeinab Mohsenipour

Recent advances in targeted drug delivery system (DDS) have generated high expectations for the treatment of various diseases. The main advantages of DDS are precise and efficient drug delivery, increased concentration and effectiveness of drugs at the site of action, minimal systemic distribution of harmful drugs, and reduced side effects. The choice of DDS often depends on the specific disease being treated, with common options including liposomes, nanoparticles, microspheres, and various biomaterials such as cell lines and microbial components.

DDS is most prominent in cancer therapy, where challenges such as limited access to tumor tissues and drug-inactivating environments complicate treatment. However, in recent decades, the emergence of antibiotic resistance and the therapeutic difficulties associated with chronic and intracellular bacterial infections have made infectious diseases a key focus for DDS development. Initial DDS approaches for bacterial infections were based on nano-derivatives. During more advanced stages of research, even the bacteria themselves became vehicles for DDS focused on microbial infections. All aspects of the bacteria- cell lysates, envelopes, derived vesicles, spores, and so forth-have been evaluated as DDS. This form of DDS does not only promote the immediate treatment of an infection but also expedites recovery times through immunological manipulation. Despite these advancements, there remains a lack of cohesive data regarding bacterial DDS in the treatment of infectious diseases. Therefore, this review aims to provide an overview of the various types of bacterial DDS, their applications, advancements, and the challenges they face.

靶向给药系统（targeted drug delivery system， DDS）近年来的进展使人们对多种疾病的治疗产生了很高的期望。DDS的主要优点是给药精确和高效，增加作用部位药物的浓度和有效性，减少有害药物的全身分布，减少副作用。DDS的选择通常取决于所治疗的特定疾病，常见的选择包括脂质体、纳米颗粒、微球和各种生物材料，如细胞系和微生物成分。DDS在癌症治疗中最为突出，在癌症治疗中，诸如限制进入肿瘤组织和药物失活环境等挑战使治疗复杂化。然而，近几十年来，抗生素耐药性的出现以及与慢性和细胞内细菌感染相关的治疗困难使传染病成为DDS发展的关键焦点。最初用于细菌感染的DDS方法是基于纳米衍生物的。在更高级的研究阶段，甚至细菌本身也成为专注于微生物感染的DDS的载体。细菌的所有方面——细胞裂解物、包膜、衍生囊泡、孢子等等——都被评估为DDS。这种形式的DDS不仅促进感染的立即治疗，而且通过免疫操作加快恢复时间。尽管取得了这些进展，但仍然缺乏关于细菌DDS治疗传染病的一致数据。因此，本文就不同类型的细菌DDS及其应用、进展和面临的挑战进行综述。

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引用次数: 0

Recent approaches in nanotoxicity assessment for drug delivery applications: Challenges and prospects 纳米毒性评估在给药应用中的最新进展：挑战与前景

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2025-02-01 DOI: 10.1016/j.medidd.2025.100204

Jithin Thomas , Vinay Kumar , Neha Sharma , Nayomi John , Mridul Umesh , Lohith Kumar Dasarahally Huligowda , Komalpreet Kaur , Divya Utreja

Nanoparticles have emerged as a promising tool in the field of drug delivery, offering targeted and controlled release of therapeutic agents. However, the increasing use of nanoparticles has raised concerns about their potential toxicity and adverse effects on human health and the environment. This review article provides a comprehensive overview of the recent approaches in nanotoxicity assessment for drug delivery applications, highlighting the challenges and future prospects in this rapidly evolving field. The article explores into the cellular and molecular mechanisms underlying nanoparticle toxicity, including oxidative stress, inflammation, genotoxicity, and neurotoxicity. The importance of nanoparticle characterization and the role of physicochemical properties, such as size, shape, surface chemistry, and composition, in determining their toxicological profile are emphasized. The article also discusses the current trends in nanotoxicity assessment, focusing on advanced in vitro and in vivo models, high-throughput screening techniques, and the use of alternative animal models, such as zebrafish and C. elegans. The regulatory landscape surrounding nanotoxicology is explored, emphasizing the need for standardized testing protocols and risk assessment frameworks. Furthermore, the article highlights the importance of a multidisciplinary approach, integrating expertise from fields such as material science, toxicology, and pharmacology, to address the complexities of nanotoxicity assessment. By providing a critical analysis of the current state of nanotoxicity research and identifying key knowledge gaps, this review article aims to guide future research efforts and contribute to the development of safer and more effective nanoparticle-based drug delivery systems.

纳米颗粒作为一种很有前途的药物递送工具，提供靶向和控制释放治疗药物。然而，纳米粒子的日益使用引起了人们对其潜在毒性和对人类健康和环境的不利影响的关注。本文综述了纳米毒性评估在药物传递应用中的最新研究方法，强调了这一快速发展领域的挑战和未来前景。本文探讨了纳米颗粒毒性的细胞和分子机制，包括氧化应激、炎症、遗传毒性和神经毒性。强调了纳米颗粒表征的重要性以及物理化学性质（如大小、形状、表面化学和组成）在确定其毒理学特征方面的作用。本文还讨论了纳米毒性评估的当前趋势，重点是先进的体外和体内模型，高通量筛选技术，以及替代动物模型的使用，如斑马鱼和秀丽隐杆线虫。围绕纳米毒理学的监管景观进行了探索，强调需要标准化的测试协议和风险评估框架。此外，本文强调了多学科方法的重要性，整合了材料科学、毒理学和药理学等领域的专业知识，以解决纳米毒性评估的复杂性。通过对纳米毒性研究现状的批判性分析和识别关键的知识空白，本文旨在指导未来的研究工作，并为开发更安全、更有效的纳米颗粒给药系统做出贡献。

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引用次数: 0

The distribution of Hypocretin/Orexin receptor mRNA in the mouse and human brain 视网膜下素/视黄醛受体 mRNA 在小鼠和人脑中的分布

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2024-10-10 DOI: 10.1016/j.medidd.2024.100202

Sanjida Mir , Ryan J. Keenan , Romke Bron , Cameron J. Nowell , Catriona McLean , Leah C. Beauchamp , Laura J. Vella , Brian Dean , Daniel Hoyer , Laura H. Jacobson

Hypocretin (Hcrtr, HCRTR) / orexin (OX) receptors modulate a range of neurobiological functions and are drug targets for several disorders. Mapping the distribution of receptors in the brain can inform their function and guide targeting of specific disorders. Although studied in rodents, orexin receptor distribution has remained relatively unexplored in humans, and thus there is also a paucity of comparative anatomy. The aim of this study was therefore to map the distribution of hypocretin/orexin receptor mRNA in selected regions of the mouse and human brain by non-radioactive in situ hybridization (ISH) using digoxigenin (DIG)-labelled cRNA anti-sense probes. Data revealed both distinct and overlapping patterns of distributions of Hcrtr1/HCRTR1 and Hcrtr2/HCRTR2 mRNA suggesting that the functions of the orexin system are mediated differently by each receptor. In the mouse brain, the highest expression of Hcrtr1 mRNA was in the locus coeruleus (LC) whereas Hcrtr2 mRNA was most abundant in the lateral hypothalamus (LH). The human caudate nuclei showed significant expression of both HCRTR1 and HCRTR2 mRNA, whereas the mouse predominantly expressed Hcrtr2 mRNA. The noradrenergic neurons of the human LC showed high signals for both HCRTR1 (71.7%) and HCRTR2 (81.5%) mRNA. Expression of HCRTR2 mRNA in non-noradrenergic human LC cells was also notable. The distribution pattern in mouse and human brains is consistent with the involvement of the orexin system in arousal and the sleep/wake cycle in both species, however, variations in receptor subtype expression profiles suggests that species differences in responses to orexin receptor ligands may be expected.

视网膜下素（Hcrtr，HCRTR）/奥曲肽受体（OX）可调节一系列神经生物学功能，是治疗多种疾病的药物靶点。绘制受体在大脑中的分布图可以了解受体的功能，并指导针对特定疾病的治疗。虽然在啮齿类动物中对奥曲肽受体的分布进行了研究，但在人类中的研究相对较少，因此也缺乏比较解剖学研究。因此，本研究的目的是利用地高辛（DIG）标记的 cRNA 反义探针，通过非放射性原位杂交（ISH）绘制小鼠和人类大脑选定区域的视网膜下素/奥曲肽受体 mRNA 分布图。数据显示，Hcrtr1/HCRTR1和Hcrtr2/HCRTR2 mRNA的分布既有区别又有重叠，这表明奥曲肽系统的功能是由每种受体以不同方式介导的。在小鼠大脑中，Hcrtr1 mRNA 的最高表达量在脑室（LC），而 Hcrtr2 mRNA 在下丘脑外侧（LH）的表达量最高。人类尾状核显示 HCRTR1 和 HCRTR2 mRNA 均有显著表达，而小鼠则主要表达 Hcrtr2 mRNA。人LC的去甲肾上腺素能神经元的HCRTR1（71.7%）和HCRTR2（81.5%）mRNA均显示高信号。在非去甲肾上腺素能的人 LC 细胞中，HCRTR2 mRNA 的表达也很显著。小鼠和人脑中的分布模式与奥曲肽系统参与两种动物的唤醒和睡眠/觉醒周期是一致的，但是，受体亚型表达谱的差异表明，物种对奥曲肽受体配体的反应可能存在差异。

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引用次数: 0

Structural features of arrestin-mediated GPCR signaling 捕获素介导的 GPCR 信号的结构特征

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2024-10-10 DOI: 10.1016/j.medidd.2024.100201

Wenqin Xie , Jinglin Lai , Hongmin Cai , H. Eric Xu , Wanchao Yin

G protein-coupled receptors (GPCRs) constitute a diverse and extensive array of cell surface receptors, rendering them essential targets for drugs aimed at various human diseases. Responding to a range of extracellular or intracellular cues, GPCRs regulate cellular signaling through downstream transducers such as heterotrimer G proteins, GPCR kinases (GRKs), and arrestins. The wealth of 3D structures available for GPCRs and their signaling complexes significantly enhances our understanding of GPCR biology and expedites the development of structure-based drug discovery methods aimed at GPCR signaling. While the structural exploration of GPCR-G protein complexes has advanced, recent years have seen substantial breakthroughs in unraveling the mechanism behind arrestin-mediated GPCR signaling. This review aims to explore emerging insights into arrestin activation and its interaction with GPCRs, shedding light on the various ways GPCRs engage with arrestins both conservatively and diversely. Additionally, we summarize recent endeavors focused on designing functionally selective (’biased’) ligands targeting GPCRs, with desired effects on/off arrestin signaling. Our goal with this review is to spotlight studies investigating the structural aspects of GPCR activation and arrestin-binding modes, with a specific emphasis on arrestin-mediated GPCR signaling.

G 蛋白偶联受体（GPCR）构成了多种多样的细胞表面受体，使它们成为治疗各种人类疾病药物的重要靶点。GPCR 可对一系列细胞外或细胞内线索做出反应，并通过异三聚 G 蛋白、GPCR 激酶 (GRK) 和抑制素等下游传导因子调节细胞信号传导。大量 GPCR 及其信号复合物的三维结构大大增强了我们对 GPCR 生物学的了解，并加快了针对 GPCR 信号转导的基于结构的药物发现方法的开发。在对 GPCR-G 蛋白复合物进行结构探索的同时，近年来在揭示 arrestin 介导的 GPCR 信号转导机制方面也取得了重大突破。这篇综述旨在探讨关于捕获素激活及其与 GPCR 相互作用的新见解，揭示 GPCR 与捕获素保守和多样化接触的各种方式。此外，我们还总结了最近在设计针对 GPCR 的功能选择性（"偏向性"）配体方面所做的努力，这些配体对/对 arrestin 信号转导具有理想的效果。我们撰写这篇综述的目的是重点介绍有关 GPCR 激活和 arrestin 结合模式的结构方面的研究，并特别强调 arrestin 介导的 GPCR 信号转导。

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引用次数: 0

Targeting BCL-2 family proteins using BH3 mimetic drugs for cancer therapy: A systematic review of randomized clinical trials 使用 BH3 拟态药物靶向 BCL-2 家族蛋白治疗癌症：随机临床试验系统回顾

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2024-09-29 DOI: 10.1016/j.medidd.2024.100199

Fatimah Alharbi, Eyad Almanifi, Md. Ashrafuzzaman

Apoptosis plays a significant role in both carcinogenesis and cancer treatment. Apoptotic dysfunction may allow cancer cells to survive. Overexpression of anti-apoptotic B cell lymphoma-2 (BCL-2) family protein members is predicted to majorly contribute to apoptotic dysfunction. Therefore, targeting proteins in cancer has been of interest to scientists and drug developers. The most successful method to regulate apoptosis in cancer cells so far has been found in the development of BH3-mimetic drugs that may work towards downregulating anti-apoptotic BCL-2 protein functions. Clinical trials have dealt with a few molecules that mimic the function of BH3-only proteins and therefore inhibit their anti-apoptotic functions. Currently, this approach is one of the most promising and effective strategies for cancer treatment. Since the family has more than fifteen protein members, this review will focus on three members that have garnered interest as therapeutic targets: Bcl-2, Bcl-X_L, and myeloid cell leukaemia 1 (Mcl-1), all are anti-apoptosis proteins. In addition, it covers the major functions of Bcl-2, Bcl-X_L, and MCL-1, their implication in malignancy, as well as their pharmacologic inhibitors. The Food and Drug Administration has approved the first BH-3 mimetic, venetoclax, an oral Bcl-2 inhibitor shown to treat chronic lymphocytic leukemia. This systematic review of clinical trials investigates the efficacy and clinical relevance of BCL-2 family protein inhibitors in managing malignancies.

细胞凋亡在致癌和癌症治疗中都发挥着重要作用。凋亡功能障碍可能使癌细胞得以存活。据预测，抗凋亡 B 细胞淋巴瘤-2（BCL-2）家族蛋白成员的过度表达是导致细胞凋亡功能障碍的主要原因。因此，针对癌症蛋白的研究一直备受科学家和药物开发人员的关注。迄今为止，调控癌细胞凋亡最成功的方法是开发 BH3 拟态药物，这些药物可以下调抗凋亡 BCL-2 蛋白的功能。临床试验已经涉及了一些分子，这些分子可模仿纯 BH3 蛋白的功能，从而抑制其抗凋亡功能。目前，这种方法是最有前途和最有效的癌症治疗策略之一。由于该家族有超过 15 个蛋白成员，本综述将重点介绍其中作为治疗靶点而备受关注的三个成员：Bcl-2、Bcl-XL 和骨髓细胞白血病 1（Mcl-1）都是抗凋亡蛋白。此外，该书还介绍了 Bcl-2、Bcl-XL 和 MCL-1 的主要功能、它们在恶性肿瘤中的作用以及它们的药物抑制剂。美国食品和药物管理局已经批准了第一种 BH-3 拟效药 venetoclax，这是一种口服 Bcl-2 抑制剂，可用于治疗慢性淋巴细胞白血病。这篇临床试验系统综述探讨了BCL-2家族蛋白抑制剂在治疗恶性肿瘤方面的疗效和临床意义。

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引用次数: 0

Pharmacological effects of dragon’s blood from Dranaena cochinchinensis (Lour.) S.C. Chen and its application in cardiovascular diseases 陈氏龙血的药理作用及其在心血管疾病中的应用

Q2 Medicine

Medicine in Drug Discovery

Pub Date : 2024-09-27 DOI: 10.1016/j.medidd.2024.100200

Hui-juan Zhang , Kai-xuan Lin , Li-dan Fu , Francis Chanda , Abdallah Iddy Chaurembo , Jian-yuan Huang , Yun-jing Xu , Chi Shu , Ke Yang , Na Xing , Wei-bo Dai , Han-bin Lin

Dragon’s blood (Resina Draconis) is the red resin of Dracaena spp, which has a variety of biological activities and pharmacological effects, including anti-thrombotic, anti-inflammatory, anti-bacterial, analgesic, anti-oxidant, anti-tumor, and immunosuppressive. In China, the main source of dragon’s blood is Dranaena Cochinchinensis (Lour.) S.C.Chen. A wide array of studies have speculated that the dragon’s blood derived from Dranaena Cochinchinensis (Lour.) S.C.Chen possesses cardiovascular protective effects. It has been reported that Chinese dragon’s blood can potentially alleviate and treat conditions such as coronary heart disease, myocardial infarction, and myocardial ischemia–reperfusion through its anti-inflammatory and antioxidant properties, which have not been systematically stated in previous reviews. Moreover, the precise underlying pharmacological mechanisms through which the Chinese dragon’s blood exhibits cardioprotective effects are not fully understood. Therefore, this article discusses the pharmacological action and biomolecular mechanism of dragon’s blood from Dranaena Cochinchinensis (Lour.) S.C.Chen and how it prevents and protects against cardiovascular diseases. The review article concludes with prospects for further application of dragon’s blood in respect to cardiovascular diseases.

龙血树（Resina Draconis）是龙血树属植物的红色树脂，具有抗血栓、抗炎、抗菌、镇痛、抗氧化、抗肿瘤、免疫抑制等多种生物活性和药理作用。在中国，龙血树的主要产地是陈氏龙血树（Dranaena Cochinchinensis (Lour.) S.C.Chen）。大量研究推测，从陈皮中提取的龙血具有保护心血管的作用。据报道，中国龙血可通过其抗炎和抗氧化特性，缓解和治疗冠心病、心肌梗塞和心肌缺血再灌注等疾病，但在以往的综述中尚未系统地阐述这些特性。此外，中国龙血具有心脏保护作用的确切药理机制尚未完全清楚。因此，本文探讨了陈氏龙血的药理作用和生物分子机制，以及它如何预防和保护心血管疾病。综述文章最后对龙血在心血管疾病方面的进一步应用进行了展望。

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