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Future drug discovery最新文献

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Prospects for drug discovery in osteoarthritis 骨关节炎药物发现前景
Future drug discovery Pub Date : 2019-08-28 DOI: 10.4155/fdd-2019-0015
C. Malemud
{"title":"Prospects for drug discovery in osteoarthritis","authors":"C. Malemud","doi":"10.4155/fdd-2019-0015","DOIUrl":"https://doi.org/10.4155/fdd-2019-0015","url":null,"abstract":"","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/fdd-2019-0015","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43002939","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The advent of directed protein degraders in drug discovery 定向蛋白质降解剂在药物发现中的出现
Future drug discovery Pub Date : 2019-08-20 DOI: 10.4155/FDD-2019-0019
M. Benchekroun
{"title":"The advent of directed protein degraders in drug discovery","authors":"M. Benchekroun","doi":"10.4155/FDD-2019-0019","DOIUrl":"https://doi.org/10.4155/FDD-2019-0019","url":null,"abstract":"","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0019","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49498934","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
RxNet Glossary of Drug Discovery RxNet药物发现术语表
Future drug discovery Pub Date : 2019-08-01 DOI: 10.4155/fdd-2019-0101s
{"title":"RxNet Glossary of Drug Discovery","authors":"","doi":"10.4155/fdd-2019-0101s","DOIUrl":"https://doi.org/10.4155/fdd-2019-0101s","url":null,"abstract":"","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/fdd-2019-0101s","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45896854","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Welcome to the first issue of Future Drug Discovery 欢迎来到《未来药物发现》的第一期
Future drug discovery Pub Date : 2019-07-02 DOI: 10.4155/FDD-2019-0020
F. Lake
{"title":"Welcome to the first issue of Future Drug Discovery","authors":"F. Lake","doi":"10.4155/FDD-2019-0020","DOIUrl":"https://doi.org/10.4155/FDD-2019-0020","url":null,"abstract":"","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0020","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46112569","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Perlecan-targeted nanoparticles for drug delivery to triple-negative breast cancer 用于三阴性乳腺癌药物递送的perlecan靶向纳米颗粒
Future drug discovery Pub Date : 2019-07-01 DOI: 10.4155/fdd-2019-0005
Vidhi Khanna, Stephen Kalscheuer, Ameya R. Kirtane, Wenqiu Zhang, J. Panyam
{"title":"Perlecan-targeted nanoparticles for drug delivery to triple-negative breast cancer","authors":"Vidhi Khanna, Stephen Kalscheuer, Ameya R. Kirtane, Wenqiu Zhang, J. Panyam","doi":"10.4155/fdd-2019-0005","DOIUrl":"https://doi.org/10.4155/fdd-2019-0005","url":null,"abstract":"Aim: We previously developed two antibodies that bind to a cell surface protein, perlecan, overexpressed in triple-negative breast cancer (TNBC). The goal of this study was to investigate these antibodies as targeting ligands for nanoparticle-mediated drug delivery. Methods: Paclitaxel-loaded poly(D,L-lactide-co-glycolide) nanoparticles were functionalized with antibodies using thiol–maleimide chemistry. Effect of antibody functionalization on therapeutic efficacy of drug-loaded nanoparticles was investigated using in vitro and in vivo models of TNBC. Results: The antibodies were covalently conjugated to nanoparticles without affecting antibody binding affinity or nanoparticle properties. Perlecan-targeted nanoparticles showed improved cell uptake, retention, cytotoxicity in vitro and enhanced tumor growth inhibition in vivo. Conclusion: The data presented here indicates that perlecan-targeted nanoparticles can improve tumor drug delivery to TNBC.","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/fdd-2019-0005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46516197","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 21
Pharma expats: a Q&A with two who made the move to a contract research organization 制药公司的外派人员:与两位转到合同研究机构的人的问答
Future drug discovery Pub Date : 2019-06-18 DOI: 10.4155/FDD-2019-0014
I. Waddell, Chris Hill
{"title":"Pharma expats: a Q&A with two who made the move to a contract research organization","authors":"I. Waddell, Chris Hill","doi":"10.4155/FDD-2019-0014","DOIUrl":"https://doi.org/10.4155/FDD-2019-0014","url":null,"abstract":"","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0014","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41372049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
In silico and in vitro evaluation of brain penetration properties of selected nootropic agents 所选促神经药物脑渗透特性的计算机和体外评估
Future drug discovery Pub Date : 2019-06-10 DOI: 10.4155/FDD-2019-0009
Ahmed Alsarrani, P. Kaplita
{"title":"In silico and in vitro evaluation of brain penetration properties of selected nootropic agents","authors":"Ahmed Alsarrani, P. Kaplita","doi":"10.4155/FDD-2019-0009","DOIUrl":"https://doi.org/10.4155/FDD-2019-0009","url":null,"abstract":"Aim: Predictive ( in silico) data suggested that nootropic supplements may penetrate the blood–brain barrier (BBB). We evaluated, in vitro, the ability of nootropics to enter the brain based on the high throughput screening (HTS) measurement of interactions with the P-gp efflux transporter and physicochemical properties and correlated these data with the in silico predictions. Methods & results: The software predicted that piracetam, docosahexaenoic acid (DHA), amantadine and thioflavin-T can best penetrate the BBB. The lipophilicity of these compounds may be predicted by measuring the critical micelle concentration (CMC). DHA and verapamil demonstrated high lipophilicity. DHA, verapamil and phosphatidylserine (PS) may be good substrates of the P-gp transporter. Conclusion: Permeability of nootropics may be successfully predicted by high throughput screening-lead optimization assay technologies.","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0009","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47887219","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
Benefits of life in a science incubator 在科学孵化器中生活的好处
Future drug discovery Pub Date : 2019-06-10 DOI: 10.4155/FDD-2019-0010
Michael S. Holzwarth
{"title":"Benefits of life in a science incubator","authors":"Michael S. Holzwarth","doi":"10.4155/FDD-2019-0010","DOIUrl":"https://doi.org/10.4155/FDD-2019-0010","url":null,"abstract":"","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70334078","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Independent consultancy in drug discovery and development: a personal perspective 药物发现和开发的独立咨询：个人视角
Future drug discovery Pub Date : 2019-05-28 DOI: 10.4155/FDD-2019-0007
P. Lukey
{"title":"Independent consultancy in drug discovery and development: a personal perspective","authors":"P. Lukey","doi":"10.4155/FDD-2019-0007","DOIUrl":"https://doi.org/10.4155/FDD-2019-0007","url":null,"abstract":"","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0007","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45156338","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Application of biomimetic HPLC to estimate in vivo behavior of early drug discovery compounds 应用仿生高效液相色谱法估计早期药物发现化合物的体内行为
Future drug discovery Pub Date : 2019-04-26 DOI: 10.4155/FDD-2019-0004
K. Valko
{"title":"Application of biomimetic HPLC to estimate in vivo behavior of early drug discovery compounds","authors":"K. Valko","doi":"10.4155/FDD-2019-0004","DOIUrl":"https://doi.org/10.4155/FDD-2019-0004","url":null,"abstract":"Characterizing the properties of large numbers of compounds and estimating their potential absorption, distribution, metabolism and elimination properties are important early stages in the process of drug discovery and help to reduce later stage attrition. The chromatographic separation principles using stationary phases that contain proteins and phospholipids are more suitable for compound characterization and estimation of the pharmacokinetic properties than the traditional octanol/water partition coefficient. This technology, when standardized, enables the prediction of in vivo behavior and the selection of compounds with the best potential, thus reducing the number of animal experiments. Chromatography may be involved more widely in the future to measure kinetic aspects of compounds’ binding to proteins and receptors which would enable designing compounds that require a lower frequency of doses and have more predictable pharmacokinetic profiles.","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48565468","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 17
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