Expert Opinion on Drug Discovery最新文献_第7页

Recent advances in computational and experimental protein-ligand affinity determination techniques. 计算和实验蛋白质配体亲和力测定技术的最新进展。

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-06-01 Epub Date: 2024-05-07 DOI: 10.1080/17460441.2024.2349169

Visvaldas Kairys, Lina Baranauskiene, Migle Kazlauskiene, Asta Zubrienė, Vytautas Petrauskas, Daumantas Matulis, Egidijus Kazlauskas

{"title":"Recent advances in computational and experimental protein-ligand affinity determination techniques.","authors":"Visvaldas Kairys, Lina Baranauskiene, Migle Kazlauskiene, Asta Zubrienė, Vytautas Petrauskas, Daumantas Matulis, Egidijus Kazlauskas","doi":"10.1080/17460441.2024.2349169","DOIUrl":"10.1080/17460441.2024.2349169","url":null,"abstract":"Introduction: Modern drug discovery revolves around designing ligands that target the chosen biomolecule, typically proteins. For this, the evaluation of affinities of putative ligands is crucial. This has given rise to a multitude of dedicated computational and experimental methods that are constantly being developed and improved.Areas covered: In this review, the authors reassess both the industry mainstays and the newest trends among the methods for protein - small-molecule affinity determination. They discuss both computational affinity predictions and experimental techniques, describing their basic principles, main limitations, and advantages. Together, this serves as initial guide to the currently most popular and cutting-edge ligand-binding assays employed in rational drug design.Expert opinion: The affinity determination methods continue to develop toward miniaturization, high-throughput, and in-cell application. Moreover, the availability of data analysis tools has been constantly increasing. Nevertheless, cross-verification of data using at least two different techniques and careful result interpretation remain of utmost importance.","PeriodicalId":12267,"journal":{"name":"Expert Opinion on Drug Discovery","volume":" ","pages":"649-670"},"PeriodicalIF":6.3,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140876172","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Hits and misses with animal models of narcolepsy and the implications for drug discovery. 嗜睡症动物模型的成功与失败以及对药物研发的影响。

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-06-01 Epub Date: 2024-05-15 DOI: 10.1080/17460441.2024.2354293

Ramakrishna Nirogi, Pradeep Jayarajan, Vijay Benade, Renny Abraham, Vinod Kumar Goyal

{"title":"Hits and misses with animal models of narcolepsy and the implications for drug discovery.","authors":"Ramakrishna Nirogi, Pradeep Jayarajan, Vijay Benade, Renny Abraham, Vinod Kumar Goyal","doi":"10.1080/17460441.2024.2354293","DOIUrl":"10.1080/17460441.2024.2354293","url":null,"abstract":"Introduction: Narcolepsy is a chronic and rare neurological disorder characterized by disordered sleep. Based on animal models and further research in humans, the dysfunctional orexin system was identified as a contributing factor to the pathophysiology of narcolepsy. Animal models played a larger role in the discovery of some of the pharmacological agents with established benefit/risk profiles.Areas covered: In this review, the authors examine the phenotypes observed in animal models of narcolepsy and the characteristics of clinically used pharmacological agents in these animal models. Additionally, the authors compare the effects of clinically used pharmacological agents on the phenotypes in animal models with those observed in narcolepsy patients.Expert opinion: Research in canine and mouse models have linked narcolepsy to the O×R2mutation and orexin deficiency, leading to new diagnostic criteria and a drug development focus. Advancements in pharmacological therapies have significantly improved narcolepsy management, with insights from both clinical experience and from animal models having led to new treatments such as low sodium oxybate and solriamfetol. However, challenges persist in addressing symptoms beyond excessive daytime sleepiness and cataplexy, highlighting the need for further research, including the development of diurnal animal models to enhance understanding and treatment options for narcolepsy.","PeriodicalId":12267,"journal":{"name":"Expert Opinion on Drug Discovery","volume":" ","pages":"755-768"},"PeriodicalIF":6.3,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140920935","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

What is the plausibility that all drugs will be designed by computers by the end of the decade? 到本十年末，所有药物都由计算机设计的可能性有多大？

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-05-01 Epub Date: 2024-03-19 DOI: 10.1080/17460441.2024.2331734

José L Medina-Franco, Edgar López-López

引用次数: 0

Identification of the abnormalities in astrocytic functions as potential drug targets for neurodegenerative disease. 将星形胶质细胞功能异常确定为治疗神经退行性疾病的潜在药物靶点。

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-05-01 Epub Date: 2024-02-26 DOI: 10.1080/17460441.2024.2322988

Valtteri Syvänen, Jari Koistinaho, Šárka Lehtonen

{"title":"Identification of the abnormalities in astrocytic functions as potential drug targets for neurodegenerative disease.","authors":"Valtteri Syvänen, Jari Koistinaho, Šárka Lehtonen","doi":"10.1080/17460441.2024.2322988","DOIUrl":"10.1080/17460441.2024.2322988","url":null,"abstract":"Introduction: Historically, astrocytes were seen primarily as a supportive cell population within the brain; with neurodegenerative disease research focusing exclusively on malfunctioning neurons. However, astrocytes perform numerous tasks that are essential for maintenance of the central nervous system`s complex processes. Disruption of these functions can have negative consequences; hence, it is unsurprising to observe a growing amount of evidence for the essential role of astrocytes in the development and progression of neurodegenerative diseases. Targeting astrocytic functions may serve as a potential disease-modifying drug therapy in the future.Areas covered: The present review emphasizes the key astrocytic functions associated with neurodegenerative diseases and explores the possibility of pharmaceutical interventions to modify these processes. In addition, the authors provide an overview of current advancement in this field by including studies of possible drug candidates.Expert opinion: Glial research has experienced a significant renaissance in the last quarter-century. Understanding how disease pathologies modify or are caused by astrocyte functions is crucial when developing treatments for brain diseases. Future research will focus on building advanced models that can more precisely correlate to the state in the human brain, with the goal of routinely testing therapies in these models.","PeriodicalId":12267,"journal":{"name":"Expert Opinion on Drug Discovery","volume":" ","pages":"603-616"},"PeriodicalIF":6.3,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139971487","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Using automated patch clamp electrophysiology platforms in ion channel drug discovery: an industry perspective. 在离子通道药物发现中使用自动膜片钳电生理学平台：行业视角。

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-05-01 Epub Date: 2024-03-13 DOI: 10.1080/17460441.2024.2329104

Marc Rogers, Alison Obergrussberger, Artem Kondratskyi, Niels Fertig

{"title":"Using automated patch clamp electrophysiology platforms in ion channel drug discovery: an industry perspective.","authors":"Marc Rogers, Alison Obergrussberger, Artem Kondratskyi, Niels Fertig","doi":"10.1080/17460441.2024.2329104","DOIUrl":"10.1080/17460441.2024.2329104","url":null,"abstract":"Introduction: Automated patch clamp (APC) is now well established as a mature technology for ion channel drug discovery in academia, biotech and pharma companies, and in contract research organizations (CRO), for a variety of applications including channelopathy research, compound screening, target validation and cardiac safety testing.Areas covered: Ion channels are an important class of drugged and approved drug targets. The authors present a review of the current state of ion channel drug discovery along with new and exciting developments in ion channel research involving APC. This includes topics such as native and iPSC-derived cells in ion channel drug discovery, channelopathy research, organellar and biologics in ion channel drug discovery.Expert opinion: It is our belief that APC will continue to play a critical role in ion channel drug discovery, not only in 'classical' hit screening, target validation and cardiac safety testing, but extending these applications to include high throughput organellar recordings and optogenetics. In this way, with advancements in APC capabilities and applications, together with high resolution cryo-EM structures, ion channel drug discovery will be re-invigorated, leading to a growing list of ion channel ligands in clinical development.","PeriodicalId":12267,"journal":{"name":"Expert Opinion on Drug Discovery","volume":" ","pages":"523-535"},"PeriodicalIF":6.3,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140119220","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

C. elegans: a prominent platform for modeling and drug screening in neurological disorders. elegans: 神经系统疾病建模和药物筛选的重要平台。

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-05-01 Epub Date: 2024-03-20 DOI: 10.1080/17460441.2024.2329103

Stefano Romussi, Sebastián Giunti, Natalia Andersen, María José De Rosa

{"title":"C. elegans: a prominent platform for modeling and drug screening in neurological disorders.","authors":"Stefano Romussi, Sebastián Giunti, Natalia Andersen, María José De Rosa","doi":"10.1080/17460441.2024.2329103","DOIUrl":"10.1080/17460441.2024.2329103","url":null,"abstract":"Introduction: Human neurodevelopmental and neurodegenerative diseases (NDevDs and NDegDs, respectively) encompass a broad spectrum of disorders affecting the nervous system with an increasing incidence. In this context, the nematode C. elegans, has emerged as a benchmark model for biological research, especially in the field of neuroscience.Areas covered: The authors highlight the numerous advantages of this tiny worm as a model for exploring nervous system pathologies and as a platform for drug discovery. There is a particular focus given to describing the existing models of C. elegans for the study of NDevDs and NDegDs. Specifically, the authors underscore their strong applicability in preclinical drug development. Furthermore, they place particular emphasis on detailing the common techniques employed to explore the nervous system in both healthy and diseased states.Expert opinion: Drug discovery constitutes a long and expensive process. The incorporation of invertebrate models, such as C. elegans, stands as an exemplary strategy for mitigating costs and expediting timelines. The utilization of C. elegans as a platform to replicate nervous system pathologies and conduct high-throughput automated assays in the initial phases of drug discovery is pivotal for rendering therapeutic options more attainable and cost-effective.","PeriodicalId":12267,"journal":{"name":"Expert Opinion on Drug Discovery","volume":" ","pages":"565-585"},"PeriodicalIF":6.3,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140174135","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Lessons learned from the failure of solanezumab as a prospective treatment strategy for Alzheimer’s disease 从索拉尼珠单抗作为阿尔茨海默病前瞻性治疗策略的失败中汲取教训

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-04-29 DOI: 10.1080/17460441.2024.2348142

Madia Lozupone, Vittorio Dibello, Rodolfo Sardone, Fabio Castellana, Roberta Zupo, Luisa Lampignano, Ilaria Bortone, Roberta Stallone, Mario Altamura, Antonello Bellomo, Antonio Daniele, Vincenzo Solfrizzi, Francesco Panza

引用次数: 0

Treatment of highly virulent mammarenavirus infections—status quo and future directions 高致病性猛玛病毒感染的治疗--现状与未来方向

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-04-12 DOI: 10.1080/17460441.2024.2340494

Ivette A. Nuñez, Anya Crane, Ian Crozier, Gabriella Worwa, Jens H. Kuhn

引用次数: 0

Omega-3 polyunsaturated fatty acid derived lipid mediators: a comprehensive update on their application in anti-cancer drug discovery 欧米伽-3 多不饱和脂肪酸衍生脂质介质：抗癌药物研发应用的全面更新

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-04-09 DOI: 10.1080/17460441.2024.2340493

Michael Murray

引用次数: 0

Potential Alzheimer’s disease drug targets identified through microglial biology research 通过小胶质细胞生物学研究确定阿尔茨海默病潜在药物靶点

IF 6.3 2区医学

Expert Opinion on Drug Discovery Pub Date : 2024-04-08 DOI: 10.1080/17460441.2024.2335210

Izabela Lepiarz-Raba, Taufik Hidayat, Anthony J. Hannan, Ali Jawaid

引用次数: 0