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Progress in medicinal chemistry最新文献

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Recent progress in the discovery and development of N-type calcium channel modulators for the treatment of pain. 治疗疼痛的n型钙通道调节剂的发现与开发进展。
Progress in medicinal chemistry Pub Date : 2014-01-01 DOI: 10.1016/B978-0-444-63380-4.00004-4
Margaret S Lee
{"title":"Recent progress in the discovery and development of N-type calcium channel modulators for the treatment of pain.","authors":"Margaret S Lee","doi":"10.1016/B978-0-444-63380-4.00004-4","DOIUrl":"https://doi.org/10.1016/B978-0-444-63380-4.00004-4","url":null,"abstract":"<p><p>The importance of voltage-gated calcium channels (VGCCs) in basic physiological processes such as cardiac and neurological function has generated intense interest in these proteins as targets of pharmacological intervention. N-type calcium channels are a subset of VGCCs distinguished by their physiology, pharmacology and significance to the pathology of chronic pain. Despite decades of investigation, only a single drug targeting N-type channel function has entered the marketplace. This review will summarize our current understanding of the biology, physiology and pharmacology of N-type calcium channels and the implication of these features for therapeutic intervention. From this basis of understanding, recent efforts to discover and develop peptide based and small molecule modulators of N-type calcium channel function will be discussed. </p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-63380-4.00004-4","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32023743","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: 25
Preface. 前言。
Progress in medicinal chemistry Pub Date : 2014-01-01 DOI: 10.1016/B978-0-444-63380-4.09989-3
Geoff Lawton, David Witty
{"title":"Preface.","authors":"Geoff Lawton,&nbsp;David Witty","doi":"10.1016/B978-0-444-63380-4.09989-3","DOIUrl":"https://doi.org/10.1016/B978-0-444-63380-4.09989-3","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-63380-4.09989-3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32023744","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
γ-Secretase modulators: current status and future directions. γ-分泌酶调节剂:现状及未来发展方向
Progress in medicinal chemistry Pub Date : 2014-01-01 DOI: 10.1016/B978-0-444-63380-4.00003-2
Adrian Hall, Toshal R Patel
{"title":"γ-Secretase modulators: current status and future directions.","authors":"Adrian Hall,&nbsp;Toshal R Patel","doi":"10.1016/B978-0-444-63380-4.00003-2","DOIUrl":"https://doi.org/10.1016/B978-0-444-63380-4.00003-2","url":null,"abstract":"<p><p>This chapter reviews the current status of γ-secretase modulators, highlighting key compounds by each company involved in the area. The review focuses on the three main chemotypes: acids, imidazoles and related derivatives and natural products. A section on chemical biology and ligand-binding site elucidation studies is also included. The primary source of information is drawn from peer reviewed literature as this permits analysis of PK-PD relationships and subsequent comment. Discussion of the patent literature is included for completeness. From this analysis, the key issues and challenges in the area are highlighted. The review concludes with a summary of the clinical development status and comment on future prospects of the field. </p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-63380-4.00003-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32023742","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: 45
Advances in the discovery of selective JAK inhibitors. 选择性JAK抑制剂的发现进展。
Progress in medicinal chemistry Pub Date : 2013-01-01 DOI: 10.1016/B978-0-444-62652-3.00004-1
Christel J Menet, Luc Van Rompaey, Raphaël Geney
{"title":"Advances in the discovery of selective JAK inhibitors.","authors":"Christel J Menet,&nbsp;Luc Van Rompaey,&nbsp;Raphaël Geney","doi":"10.1016/B978-0-444-62652-3.00004-1","DOIUrl":"https://doi.org/10.1016/B978-0-444-62652-3.00004-1","url":null,"abstract":"<p><p>In this review, we describe the current knowledge of the biology of the JAKs. The JAK family comprises the four nonreceptor tyrosine kinases JAK1, JAK2, JAK3, and Tyk2, all key players in the signal transduction from cytokine receptors to transcription factor activation. We also review the progresses made towards the optimization of JAK inhibitors and the importance of their selectivity profile. Indeed, the full array of many medicinal chemistry enabling tools (HTS, X-ray crystallography, scaffold morphing, etc.) has been deployed to successfully design molecules that discriminate among JAK family and other kinases. While the first JAK inhibitor was launched in 2011, this review also summarizes the status of several other small-molecule JAK inhibitors currently in development to treat arthritis, psoriasis, organ rejection, and multiple cancer types.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-62652-3.00004-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31217738","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: 70
Glucokinase. Preface. 葡糖激酶。前言。
Progress in medicinal chemistry Pub Date : 2013-01-01 DOI: 10.1016/B978-0-444-62652-3.10000-6
Geoff Lawton, David R Witty
{"title":"Glucokinase. Preface.","authors":"Geoff Lawton,&nbsp;David R Witty","doi":"10.1016/B978-0-444-62652-3.10000-6","DOIUrl":"https://doi.org/10.1016/B978-0-444-62652-3.10000-6","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-62652-3.10000-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31217739","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
Antimalarial drug discovery: recent progress and future directions. 抗疟药物的发现:最新进展和未来方向。
Progress in medicinal chemistry Pub Date : 2013-01-01 DOI: 10.1016/B978-0-444-62652-3.00003-X
Félix Calderón, David M Wilson, Francisco-Javier Gamo
{"title":"Antimalarial drug discovery: recent progress and future directions.","authors":"Félix Calderón,&nbsp;David M Wilson,&nbsp;Francisco-Javier Gamo","doi":"10.1016/B978-0-444-62652-3.00003-X","DOIUrl":"https://doi.org/10.1016/B978-0-444-62652-3.00003-X","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-62652-3.00003-X","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31217737","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: 31
Medicinal chemistry of glucagon-like peptide receptor agonists. 胰高血糖素样肽受体激动剂的药物化学。
Progress in medicinal chemistry Pub Date : 2013-01-01 DOI: 10.1016/B978-0-444-62652-3.00002-8
Lyn H Jones, David A Price
{"title":"Medicinal chemistry of glucagon-like peptide receptor agonists.","authors":"Lyn H Jones,&nbsp;David A Price","doi":"10.1016/B978-0-444-62652-3.00002-8","DOIUrl":"https://doi.org/10.1016/B978-0-444-62652-3.00002-8","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-62652-3.00002-8","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31217736","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
Property-based design in the optimisation of benzamide glucokinase activators: from hit to clinic. 苯甲酰胺葡萄糖激酶活化剂优化中的基于性能的设计:从hit到临床。
Progress in medicinal chemistry Pub Date : 2013-01-01 DOI: 10.1016/B978-0-444-62652-3.00001-6
Darren McKerrecher, Michael J Waring
{"title":"Property-based design in the optimisation of benzamide glucokinase activators: from hit to clinic.","authors":"Darren McKerrecher,&nbsp;Michael J Waring","doi":"10.1016/B978-0-444-62652-3.00001-6","DOIUrl":"https://doi.org/10.1016/B978-0-444-62652-3.00001-6","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-444-62652-3.00001-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31217735","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
Hematopoietic prostaglandin D synthase inhibitors. 造血前列腺素D合成酶抑制剂。
Progress in medicinal chemistry Pub Date : 2012-01-01 DOI: 10.1016/B978-0-12-396493-9.00004-2
Sukanthini Thurairatnam
{"title":"Hematopoietic prostaglandin D synthase inhibitors.","authors":"Sukanthini Thurairatnam","doi":"10.1016/B978-0-12-396493-9.00004-2","DOIUrl":"https://doi.org/10.1016/B978-0-12-396493-9.00004-2","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-12-396493-9.00004-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40171225","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: 20
TRPV1 antagonists: clinical setbacks and prospects for future development. TRPV1拮抗剂:临床挫折及未来发展前景
Progress in medicinal chemistry Pub Date : 2012-01-01 DOI: 10.1016/B978-0-12-396493-9.00002-9
Michael E Kort, Philip R Kym
{"title":"TRPV1 antagonists: clinical setbacks and prospects for future development.","authors":"Michael E Kort,&nbsp;Philip R Kym","doi":"10.1016/B978-0-12-396493-9.00002-9","DOIUrl":"https://doi.org/10.1016/B978-0-12-396493-9.00002-9","url":null,"abstract":"","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/B978-0-12-396493-9.00002-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40171223","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: 57
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