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Drug Discovery Today: Technologies最新文献

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Recent, non-classical, approaches to antibody lysine modification 最近，非经典，抗体赖氨酸修饰的方法
Drug Discovery Today: Technologies Pub Date : 2018-12-01 DOI: 10.1016/j.ddtec.2018.09.002
Guilhem Chaubet, Fabien Thoreau, Alain Wagner
{"title":"Recent, non-classical, approaches to antibody lysine modification","authors":"Guilhem Chaubet,&nbsp;Fabien Thoreau,&nbsp;Alain Wagner","doi":"10.1016/j.ddtec.2018.09.002","DOIUrl":"10.1016/j.ddtec.2018.09.002","url":null,"abstract":"<div><p>This review will discuss recent development in the bioconjugation of lysine residues on antibodies. As several chemoselective reagents have already been developed for modifying amine groups, recent strategies now tend to aim at being site-specific. Four general methods have been listed: kinetically controlled, template-directed or enzymatic strategies as well as the use of chemically programmed antibodies.</p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.09.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36774439","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: 7
Enzymatic strategies for (near) clinical development of antibody-drug conjugates 抗体-药物偶联物(接近)临床开发的酶促策略
Drug Discovery Today: Technologies Pub Date : 2018-12-01 DOI: 10.1016/j.ddtec.2018.09.005
Sander S. van Berkel , Floris L. van Delft
{"title":"Enzymatic strategies for (near) clinical development of antibody-drug conjugates","authors":"Sander S. van Berkel ,&nbsp;Floris L. van Delft","doi":"10.1016/j.ddtec.2018.09.005","DOIUrl":"10.1016/j.ddtec.2018.09.005","url":null,"abstract":"<div><p>Target-specific killing of tumor cells with antibody-drug conjugates<span> (ADCs) is an elegant concept in the continued fight against cancer. However, despite more than 20 years of clinical development, only four ADC have reached market approval, while at least 50 clinical programs were terminated early. The high attrition rate of ADCs may, at least in part, be attributed to heterogeneity and instability of conventional technologies. At present, various (chemo)enzymatic approaches for site-specific and stable conjugation of toxic payloads are making their way to the clinic, thereby potentially providing ADCs with increased therapeutic window.</span></p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.09.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36774441","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
Amanitins and their development as a payload for antibody-drug conjugates Amanitins及其作为抗体-药物偶联物有效载荷的发展
Drug Discovery Today: Technologies Pub Date : 2018-12-01 DOI: 10.1016/j.ddtec.2018.08.005
Andreas Pahl, Christian Lutz, Torsten Hechler
{"title":"Amanitins and their development as a payload for antibody-drug conjugates","authors":"Andreas Pahl,&nbsp;Christian Lutz,&nbsp;Torsten Hechler","doi":"10.1016/j.ddtec.2018.08.005","DOIUrl":"10.1016/j.ddtec.2018.08.005","url":null,"abstract":"<div><p><span><span>Amanitin-based ADCs represent a new class of ADCs using a novel mode of action. This payload introduces a novel mode of action into oncology therapy, the inhibition of RNA Polymerase II. The high potency of the toxin leads to highly efficacious ADCs. The development of the technology around this toxin will be described. These developments support the clinical development of amanitin-based ADCs by using a toxin with a new mode of action and with a favorable therapeutic index. HDP-101 is an </span>Amanitin based ADC directed against </span>BCMA and will be advancing to the clinical phase in 2019.</p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.08.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36774360","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: 60
Homogeneous antibody-drug conjugates via site-selective disulfide bridging 均相抗体-药物通过选择性二硫桥接偶联
Drug Discovery Today: Technologies Pub Date : 2018-12-01 DOI: 10.1016/j.ddtec.2018.09.004
Nafsika Forte, Vijay Chudasama, James R. Baker
{"title":"Homogeneous antibody-drug conjugates via site-selective disulfide bridging","authors":"Nafsika Forte,&nbsp;Vijay Chudasama,&nbsp;James R. Baker","doi":"10.1016/j.ddtec.2018.09.004","DOIUrl":"10.1016/j.ddtec.2018.09.004","url":null,"abstract":"<div><p><span>Antibody-drug conjugates<span><span> (ADCs) constructed using site-selective labelling methodologies are likely to dominate the next generation of these targeted therapeutics. To this end, disulfide bridging has emerged as a leading strategy as it allows the production of highly homogeneous ADCs without the need for </span>antibody engineering. It consists of targeting reduced interchain </span></span>disulfide bonds<span> with reagents which reconnect the resultant pairs of cysteine residues, whilst simultaneously attaching drugs. The 3 main reagent classes which have been exemplified for the construction of ADCs by disulfide bridging will be discussed in this review; bissulfones, next generation maleimides and pyridazinediones, along with others in development.</span></p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.09.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36786615","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: 29
Borylated reagents for multicomponent reactions 多组分反应用硼化试剂
Drug Discovery Today: Technologies Pub Date : 2018-11-01 DOI: 10.1016/j.ddtec.2018.08.002
Joanne Tan, Andrei K. Yudin
{"title":"Borylated reagents for multicomponent reactions","authors":"Joanne Tan,&nbsp;Andrei K. Yudin","doi":"10.1016/j.ddtec.2018.08.002","DOIUrl":"10.1016/j.ddtec.2018.08.002","url":null,"abstract":"<div><p>Over the past two decades, there has been an increasing interest in the therapeutic potential of organoboron reagents due to the discovery of bortezomib (Velcade). This has motivated synthetic chemists to develop novel routes for the preparation of heteroatom-rich boron-containing molecules (BCMs). In particular, the development of borylated building blocks has provided facile access to difficult-to-access heteroatom-rich BCMs. In this review, we will discuss the methods used to prepare boron-containing molecules of biological relevance from multicomponent reactions with borylated building blocks.</p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.08.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36761320","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
Recent advances of the Povarov reaction in medicinal chemistry 波瓦洛夫反应在药物化学中的最新进展
Drug Discovery Today: Technologies Pub Date : 2018-11-01 DOI: 10.1016/j.ddtec.2018.08.004
Ouldouz Ghashghaei , Carme Masdeu , Concepción Alonso , Francisco Palacios , Rodolfo Lavilla
{"title":"Recent advances of the Povarov reaction in medicinal chemistry","authors":"Ouldouz Ghashghaei ,&nbsp;Carme Masdeu ,&nbsp;Concepción Alonso ,&nbsp;Francisco Palacios ,&nbsp;Rodolfo Lavilla","doi":"10.1016/j.ddtec.2018.08.004","DOIUrl":"10.1016/j.ddtec.2018.08.004","url":null,"abstract":"<div><p>The Povarov multicomponent reaction consists on the condensation of an aniline, an aldehyde, and an activated olefin<span> to generate a tetrahydroquinoline adduct with 3 diversity points. Hereby, we report the main features of this transformation and its uses in medicinal chemistry. Relevant examples of the impact of Povarov adducts in different therapeutic areas are provided.</span></p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.08.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36713242","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: 48
Integrating biocatalysis and multicomponent reactions 整合生物催化和多组分反应
Drug Discovery Today: Technologies Pub Date : 2018-11-01 DOI: 10.1016/j.ddtec.2018.06.004
Chiara Lambruschini, Andrea Basso, Luca Banfi
{"title":"Integrating biocatalysis and multicomponent reactions","authors":"Chiara Lambruschini,&nbsp;Andrea Basso,&nbsp;Luca Banfi","doi":"10.1016/j.ddtec.2018.06.004","DOIUrl":"10.1016/j.ddtec.2018.06.004","url":null,"abstract":"<div><p><span>While often multicomponent reactions (MCR) are used for the diversity-oriented synthesis of racemic (or achiral) molecular entities, this short review describes two alternative approaches for accessing enantiopure products exploiting the power of biocatalysis. </span>Enzymes or microorganisms may be used for preparing enantiopure MCR inputs or for resolving racemic (or achiral) MCR adducts.</p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.06.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36761316","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
Multicomponent reactions in drug discovery and medicinal chemistry 药物发现和药物化学中的多组分反应
Drug Discovery Today: Technologies Pub Date : 2018-11-01 DOI: 10.1016/j.ddtec.2018.11.002
Eelco Ruijter , Romano Orru , Synthetic and BioOrganic Chemistry Group
{"title":"Multicomponent reactions in drug discovery and medicinal chemistry","authors":"Eelco Ruijter ,&nbsp;Romano Orru ,&nbsp;Synthetic and BioOrganic Chemistry Group","doi":"10.1016/j.ddtec.2018.11.002","DOIUrl":"10.1016/j.ddtec.2018.11.002","url":null,"abstract":"","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.11.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36761317","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: 22
Homologation of Ugi and Passerini reactions using ynamides 用酰胺鉴定Ugi和Passerini反应
Drug Discovery Today: Technologies Pub Date : 2018-11-01 DOI: 10.1016/j.ddtec.2018.09.001
Bo Huang, Sunliang Cui
{"title":"Homologation of Ugi and Passerini reactions using ynamides","authors":"Bo Huang,&nbsp;Sunliang Cui","doi":"10.1016/j.ddtec.2018.09.001","DOIUrl":"10.1016/j.ddtec.2018.09.001","url":null,"abstract":"<div><p>Being important biological and pharmacological units, β-amino amides and β-acyloxy amides have a privileged position in both academia and industry. Developing a methods to prepare them has gained attention. Ynamides, which possess dual nucleophilic<span> and electrophilic properties, are similar to isonitriles. In this review, usage of ynamides in the single reactant replacement approach of Ugi and Passerini reactions to develop two new multicomponent reactions to get various β-amino amides and β-acyloxy amides is reported.</span></p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.09.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36761319","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
Gold-catalyzed post-MCR transformations towards complex (poly)heterocycles 金催化的后mcr转化为复杂(多)杂环
Drug Discovery Today: Technologies Pub Date : 2018-11-01 DOI: 10.1016/j.ddtec.2018.08.003
Upendra K. Sharma , Guilong Tian , Leonid G. Voskressensky , Erik V. Van der Eycken
{"title":"Gold-catalyzed post-MCR transformations towards complex (poly)heterocycles","authors":"Upendra K. Sharma ,&nbsp;Guilong Tian ,&nbsp;Leonid G. Voskressensky ,&nbsp;Erik V. Van der Eycken","doi":"10.1016/j.ddtec.2018.08.003","DOIUrl":"10.1016/j.ddtec.2018.08.003","url":null,"abstract":"<div><p>Post multicomponent reaction (MCR) transformations are one of the most successful methods leading to high structural diversity and molecular complexity. A well-known MCR, the Ugi reaction typically affords a linear peptide backbone, enabling post-Ugi transformations as an elegant solution to rigidify the Ugi adduct into more drug-like species. Not surprisingly, the development of such transformations leading to new structural frameworks has expanded rapidly over the last few years. These reactions have reached an impressive level of performance and versatility, particularly in amalgamation with gold catalysis. This review outlines the developments achieved in the past decade, highlighting the modifications that are performed in a sequential or domino fashion with emphasis on major concepts, synthetic applications of the derived products as well as mechanistic aspects.</p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2018.08.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36761321","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
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