{"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":null,"pages":null},"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}
{"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":null,"pages":null},"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}
{"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":null,"pages":null},"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}
{"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":null,"pages":null},"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}
{"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":null,"pages":null},"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}
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.
{"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":null,"pages":null},"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}
{"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":null,"pages":null},"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}
{"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":null,"pages":null},"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}
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.
{"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":null,"pages":null},"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}
Xingcai Zhang, Gaurav Parekh, Baolin Guo, Xing Huang, Yuqing Dong, W. Han, Xing Chen, G. Xiao
[Formula: see text]
[公式:见正文]
{"title":"Polyphenol and self-assembly: metal polyphenol nanonetwork for drug delivery and pharmaceutical applications","authors":"Xingcai Zhang, Gaurav Parekh, Baolin Guo, Xing Huang, Yuqing Dong, W. Han, Xing Chen, G. Xiao","doi":"10.4155/FDD-2019-0001","DOIUrl":"https://doi.org/10.4155/FDD-2019-0001","url":null,"abstract":"[Formula: see text]","PeriodicalId":73122,"journal":{"name":"Future drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-04-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.4155/FDD-2019-0001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43824831","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}
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