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Preface. 前言。
Progress in medicinal chemistry Pub Date : 2020-01-01 DOI: 10.1016/S0079-6468(20)30010-2
David R Witty, Brian Cox
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引用次数: 0
Contributors 贡献者
Progress in medicinal chemistry Pub Date : 2020-01-01 DOI: 10.1016/s0079-6468(20)30009-6
{"title":"Contributors","authors":"","doi":"10.1016/s0079-6468(20)30009-6","DOIUrl":"https://doi.org/10.1016/s0079-6468(20)30009-6","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":"1 1","pages":""},"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)30009-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"55877970","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
Small molecules-Giant leaps for immuno-oncology. 小分子——免疫肿瘤学的巨大飞跃。
Progress in medicinal chemistry Pub Date : 2020-01-01 Epub Date: 2020-01-20 DOI: 10.1016/bs.pmch.2019.11.001
Lisa Kötzner, Bayard Huck, Sakshi Garg, Klaus Urbahns
{"title":"Small molecules-Giant leaps for immuno-oncology.","authors":"Lisa Kötzner,&nbsp;Bayard Huck,&nbsp;Sakshi Garg,&nbsp;Klaus Urbahns","doi":"10.1016/bs.pmch.2019.11.001","DOIUrl":"https://doi.org/10.1016/bs.pmch.2019.11.001","url":null,"abstract":"<p><p>Immuno-oncology therapies are revolutionizing the oncology landscape with checkpoint blockade becoming the treatment backbone for many indications. While inspiring, much work remains to increase the number of cancer patients that can benefit from these treatments. Thus, a new era of immuno-oncology research has begun which is focused on identifying novel combination regimes that lead to improved response rates. This review highlights the significance of small molecules in this approach and illustrates the huge progress that has been made to date.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":"59 ","pages":"1-62"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2019.11.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37895677","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
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":"59 ","pages":"101-179"},"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":"1 1","pages":""},"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":"58 ","pages":"1-62"},"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":"58 ","pages":"119-156"},"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":"7 1","pages":""},"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":"58 ","pages":"157-187"},"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":"1 1","pages":""},"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
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