发布求助
文献互助 智能选刊 最新文献

Progress in medicinal chemistry最新文献

筛选
英文 中文
Discovery and development of ASK1 inhibitors. ASK1抑制剂的发现和开发。
Progress in medicinal chemistry Pub Date : 2020-01-01 Epub Date: 2020-04-22 DOI: 10.1016/bs.pmch.2020.02.001
Reginald Brys, Karl Gibson, Tanja Poljak, Steven Van Der Plas, David Amantini
{"title":"Discovery and development of ASK1 inhibitors.","authors":"Reginald Brys,&nbsp;Karl Gibson,&nbsp;Tanja Poljak,&nbsp;Steven Van Der Plas,&nbsp;David Amantini","doi":"10.1016/bs.pmch.2020.02.001","DOIUrl":"https://doi.org/10.1016/bs.pmch.2020.02.001","url":null,"abstract":"<p><p>Aberrant activation of mitogen-activated protein kinases (MAPKs) like c-Jun N-terminal kinase (JNK) and p38 is an event involved in the pathophysiology of numerous human diseases. The apoptosis signal-regulating kinase 1 (ASK1) is an upstream target that gets activated only under pathological conditions and as such is a promising target for therapeutic intervention. In the first part of this review the molecular mechanisms leading to ASK1 activation and regulation will be described as well as the evidences supporting a pathogenic role for ASK1 in human disease. In the second part, an update on drug discovery efforts towards the discovery and development of ASK1-targeting therapies will be provided.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2020.02.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37895679","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: 12
Copyright 版权
Progress in medicinal chemistry Pub Date : 2020-01-01 DOI: 10.1016/s0079-6468(20)30007-2
{"title":"Copyright","authors":"","doi":"10.1016/s0079-6468(20)30007-2","DOIUrl":"https://doi.org/10.1016/s0079-6468(20)30007-2","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/s0079-6468(20)30007-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"55877952","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
Covalent binders in drug discovery. 药物发现中的共价结合物。
Progress in medicinal chemistry Pub Date : 2019-01-01 Epub Date: 2019-03-11 DOI: 10.1016/bs.pmch.2018.12.002
Anil Vasudevan, Maria A Argiriadi, Aleksandra Baranczak, Michael M Friedman, Julia Gavrilyuk, Adrian D Hobson, Jonathan J Hulce, Sami Osman, Noel S Wilson
{"title":"Covalent binders in drug discovery.","authors":"Anil Vasudevan,&nbsp;Maria A Argiriadi,&nbsp;Aleksandra Baranczak,&nbsp;Michael M Friedman,&nbsp;Julia Gavrilyuk,&nbsp;Adrian D Hobson,&nbsp;Jonathan J Hulce,&nbsp;Sami Osman,&nbsp;Noel S Wilson","doi":"10.1016/bs.pmch.2018.12.002","DOIUrl":"https://doi.org/10.1016/bs.pmch.2018.12.002","url":null,"abstract":"<p><p>Covalent modulation of protein function can have multiple utilities including therapeutics, and probes to interrogate biology. While this field is still viewed with scepticism due to the potential for (idiosyncratic) toxicities, significant strides have been made in terms of understanding how to tune electrophilicity to selectively target specific residues. Progress has also been made in harnessing the potential of covalent binders to uncover novel biology and to provide an enhanced utility as payloads for Antibody Drug Conjugates. This perspective covers the tenets and applications of covalent binders.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2018.12.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37238417","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: 24
Rewriting the (tran)script: Application to spinal muscular atrophy. 改写(tran)脚本:在脊髓性肌萎缩症中的应用。
Progress in medicinal chemistry Pub Date : 2019-01-01 Epub Date: 2019-02-01 DOI: 10.1016/bs.pmch.2018.12.003
Hasane Ratni, Lutz Mueller, Martin Ebeling
{"title":"Rewriting the (tran)script: Application to spinal muscular atrophy.","authors":"Hasane Ratni,&nbsp;Lutz Mueller,&nbsp;Martin Ebeling","doi":"10.1016/bs.pmch.2018.12.003","DOIUrl":"https://doi.org/10.1016/bs.pmch.2018.12.003","url":null,"abstract":"<p><p>Targeting RNA drastically expands our target space to therapeutically modulate numerous cellular processes implicated in human diseases. Of particular interest, drugging pre-mRNA splicing appears a very viable strategy; to control levels of splicing product by promoting the inclusion or exclusion of exons. After describing the concept of \"splicing modulation\", this chapter will cover the outstanding progress achieved in this field, by highlighting the breakthrough accomplished recently for the treatment of spinal muscular atrophy using two therapeutic modalities: splice switching oligonucleotides and small molecules. This review discusses the vital but feasible requirement for such drugs to deliver selectivity, and critical safety aspects are highlighted. Transformational medicines such as those developed to treat SMA are likely just the beginning of this story.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2018.12.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37063941","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: 5
Contributors 贡献者
Progress in medicinal chemistry Pub Date : 2019-01-01 DOI: 10.1016/s0079-6468(19)30008-6
{"title":"Contributors","authors":"","doi":"10.1016/s0079-6468(19)30008-6","DOIUrl":"https://doi.org/10.1016/s0079-6468(19)30008-6","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/s0079-6468(19)30008-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"55877941","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
Natural product drug delivery: A special challenge? 天然产物给药:一个特殊的挑战?
Progress in medicinal chemistry Pub Date : 2019-01-01 Epub Date: 2019-03-01 DOI: 10.1016/bs.pmch.2019.01.001
Neil J Press, Emilie Joly, Peter Ertl
{"title":"Natural product drug delivery: A special challenge?","authors":"Neil J Press,&nbsp;Emilie Joly,&nbsp;Peter Ertl","doi":"10.1016/bs.pmch.2019.01.001","DOIUrl":"https://doi.org/10.1016/bs.pmch.2019.01.001","url":null,"abstract":"<p><p>Natural products have a long-standing and critical role in drug development and medical use. The structural and physicochemical properties of natural products, while derived evolutionarily to be effective in living systems, may create challenges in translation to a pharmaceutical product. Molecular complexity, low solubility, functional group reactivity and general instability are among the challenges that typically need to be overcome. This review looks at some of the ways that natural products have been formulated and delivered to enable the successful application of these vitally important medicines to patients.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2019.01.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37063942","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: 9
Copyright 版权
Progress in medicinal chemistry Pub Date : 2019-01-01 DOI: 10.1016/s0079-6468(19)30006-2
{"title":"Copyright","authors":"","doi":"10.1016/s0079-6468(19)30006-2","DOIUrl":"https://doi.org/10.1016/s0079-6468(19)30006-2","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/s0079-6468(19)30006-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"55877930","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
Amyotrophic lateral sclerosis. 肌萎缩侧索硬化症。
Progress in medicinal chemistry Pub Date : 2019-01-01 Epub Date: 2019-03-08 DOI: 10.1016/bs.pmch.2018.12.001
Klara Valko, Lukasz Ciesla
{"title":"Amyotrophic lateral sclerosis.","authors":"Klara Valko,&nbsp;Lukasz Ciesla","doi":"10.1016/bs.pmch.2018.12.001","DOIUrl":"https://doi.org/10.1016/bs.pmch.2018.12.001","url":null,"abstract":"<p><p>Amyotrophic lateral sclerosis (ALS) is caused by selective and progressive loss of spinal, bulbar and cortical motoneurons and leads to irreversible paralysis, loss of speech, inability to swallow and respiratory malfunctions with the eventual death of the affected individual in a rapid disease course. Several suggested molecular pathways are reviewed including SOD1 gene mutation, protein nitrosylation, phosphorylation and oxidative stress, excitotoxicity, glutamate transporter deprivation, mitochondrial involvement, protein aggregation and motor neuron trophic factors. The role of insulin and its receptor in the brain is described. It is very possible that in 90% of the sporadic ALS cases, the cause of the motor neuron degeneration is different or that multiple mechanisms are involved that would need drugs with multiple mechanisms or action. Several marketed drugs have been selected for clinical trials. Only two drugs have been approved by the FDA as showing positive effect in ALS: Riluzole and Edaravone. Two other drugs that have a significant benefit in ALS are Talampanel and Tamoxifen. The results for modulation of the neurotrophic factor Insulin Growth Factor-1 (IGF1) as a potential treatment are inconclusive. Several compounds are discussed that show a positive effect in the mouse model but which have failed in clinical trials. New approaches using different modalities such as peptides, proteins and stem cells are promising. Our ability to design better drugs would be enhanced by investigating the endogenous factors in neuron death, protein aggregation and oxidative stress that would improve our understanding of the potential pathways that result in neurodegeneration.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2018.12.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37063943","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
Performance of the high-efficiency thermal neutron BAND-GEM detector 高效热中子BAND-GEM探测器的性能
Progress in medicinal chemistry Pub Date : 2018-02-01 DOI: 10.1093/PTEP/PTY005
A. Muraro, G. Croci, E. Cippo, G. Grosso, C. Höglund, G. Albani, R. Hall-Wilton, K. Kanaki, F. Murtas, D. Raspino, L. Robinson, Nigel Rodhes, M. Rebai, S. Schmidt, E. Schooneveld, M. Tardocchi, G. Gorini
{"title":"Performance of the high-efficiency thermal neutron BAND-GEM detector","authors":"A. Muraro, G. Croci, E. Cippo, G. Grosso, C. Höglund, G. Albani, R. Hall-Wilton, K. Kanaki, F. Murtas, D. Raspino, L. Robinson, Nigel Rodhes, M. Rebai, S. Schmidt, E. Schooneveld, M. Tardocchi, G. Gorini","doi":"10.1093/PTEP/PTY005","DOIUrl":"https://doi.org/10.1093/PTEP/PTY005","url":null,"abstract":"Newhigh-count-rate detectors are required for future spallation neutron sources where large-area and high-efficiency (amp;gt;50%) detectors are envisaged. In this framework, Gas Electron Multiplier ...","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1093/PTEP/PTY005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49262863","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: 15
Current Trends in Macrocyclic Drug Discovery and beyond-Ro5. 大环药物发现的最新趋势及超越ro5。
Progress in medicinal chemistry Pub Date : 2018-01-01 Epub Date: 2018-03-22 DOI: 10.1016/bs.pmch.2018.01.002
Sulejman Alihodžić, Mirjana Bukvić, Ivaylo J Elenkov, Antun Hutinec, Sanja Koštrun, Dijana Pešić, Gordon Saxty, Linda Tomašković, Dinko Žiher
{"title":"Current Trends in Macrocyclic Drug Discovery and beyond-Ro5.","authors":"Sulejman Alihodžić,&nbsp;Mirjana Bukvić,&nbsp;Ivaylo J Elenkov,&nbsp;Antun Hutinec,&nbsp;Sanja Koštrun,&nbsp;Dijana Pešić,&nbsp;Gordon Saxty,&nbsp;Linda Tomašković,&nbsp;Dinko Žiher","doi":"10.1016/bs.pmch.2018.01.002","DOIUrl":"https://doi.org/10.1016/bs.pmch.2018.01.002","url":null,"abstract":"<p><p>This chapter will discuss the recent literature of macrocycles and drug-like property space moving beyond the rule of five (bRo5). Trends in chemical classes that fall within this definition are discussed and the impact of the latest technologies in the field assessed. The physicochemical properties, which have provided both successes and challenges, especially in scale-up, are discussed. A recent patent literature is reviewed and the chapter concludes with a perspective on the future of macrocyclic drug discovery.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2018.01.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36029510","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: 13
首页 上一页 下一页 尾页
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整，为了账户安全，请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们：info@booksci.cn Book学术提供免费学术资源搜索服务，方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号：481959085
Book学术官方微信