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17 October 2022
This journal European Journal of Medicinal Chemistry Reports is currently running a special issue entitled 'The Application of Click Chemistry and Bioorthogonal Chemistry to Enable Drug Discovery'.
Guest editors:
Dr. Peng Zhan
School of Pharmaceutical Science, Shandong University, Shandong, China
zhanpeng1982@sdu.edu.cn
Professor Bin Yu
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, China
yubin@zzu.edu.cn
Dr. Liang Ouyang
State Key Laboratory of Biotherapy and Cancer Center, Sichuan University, Chengdu, China
ouyangliang@scu.edu.cn
Professor Zhenming Liu
School of Pharmaceutical Science, Peking University, Beijing, China
zmliu@bjmu.edu.cn
Special issue information:
The Royal Swedish Academy of Sciences has decided to award Carolyn R. Bertozzi, Morten Meldal, and K. Barry Sharpless the Nobel Prize in Chemistry 2022, for the development of click chemistry and bioorthogonal chemistry.
As well known, one of the most formidable challenges in medicinal chemistry is rationalizing and accelerating lead discovery and optimization. A versatile chemical toolbox is essential for this purpose. Reactions united by the “click” family have a strong energy driving force that ensures starting compounds to react promptly, efficiently, and with no undesired byproducts even under physiological conditions, which make these transformations perfect models of biorthogonality. Click chemistry and bioorthogonal chemistry reactions are an important part of the medicinal chemistry toolbox and offer substantial advantages to medicinal chemists in terms of overcoming the limitations of useful chemical synthesis, increasing throughput, and improving the quality of compound libraries.
Notably, Copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry is the prime example of current bioorthogonal reactions. It leads to the selective formation of 1,4-disubstituted 1,2,3-triazole units connecting readily accessible building blocks via a stable and biocompatible linkage. Tethering in situ CuAAC click chemistry can generate novel lead compounds even from fragments with weak target-binding affinity.
Meanwhile, the potential of other bioorthogonal reactions for drug discovery has only just started to be explored, including strain-promoted azide-alkyne cycloaddition (SPAAC) reaction, strain-promoted alkyne-nitrone cycloaddition (SPANC) reaction, alkene and tetrazine inverse-demand diels-alder reaction, alkene and tetrazole photoclick reaction, sulfur (VI) fluorine exchange (SuFEx) reaction, thio acid/sulfonyl azide amidation (‘sulfo-click’ reaction), metal mediated amine-to-nitrile addition, thiol-ene click chemistry, and oxime-forming reaction, etc.
We envisioned that the combination of click chemistry and bioorthogonal chemistry with combinatorial synthesis, high-throughput synthesis/screening, miniaturized and parallelized methodologies, late stage functionalization, or molecular self-assembly systems (dynamic combinatorial chemistry) will provide more rapid, efficient and reliable approaches for the discovery of bioactive molecules.
To explore new chemical spaces for drug-like molecules containing a high degree of structural diversity, it may be useful to merge the diversity-oriented synthesis and ‘privileged’ substructure-based strategy with bioorthogonal reactions using sophisticated automation and flow systems to improve productivity.
SI Keywords:
Click chemistry
Bioorthogonal chemistry
Drug discovery
Lead diversification
In situ click chemistry
Dynamic combinatorial chemistry
Late stage functionalization
High-throughput synthesis
Combinatorial synthesis
Manuscript submission information:
You are invited to submit your manuscript at any time before the submission deadline. For any inquiries about the appropriateness of contribution topics, please contact Dr. Peng Zhan via Email zhanpeng1982@sdu.edu.cn.
In case of accepting our invitation please note that the journal has moved to a new web-based manuscript submission and tracking system, and we respectfully request that you please log in and submit your paper via the following website: https://www.editorialmanager.com/ejmcrp/default2.aspx. You will be asked to choose an article type, please choose “VSI: Click Chemistry” to ensure that your manuscript will be submitted correctly.
To ensure the timely processing of your manuscript the system will allow you instant access to the current status of your paper as it moves through review. Full instructions for using the system are available on the website: https://www.sciencedirect.com/journal/european-journal-of-medicinal-chemistry-reports. And if you have any questions during the submission process, please do not hesitate to contact us.
The deadline for submission is 30-Jun-2023
Why publish in this Special Issue?
Special Issue articles are published together on ScienceDirect, making it incredibly easy for other researchers to discover your work.
Special content articles are downloaded on ScienceDirect twice as often within the first 24 months than articles published in regular issues.
Special content articles attract 20% more citations in the first 24 months than articles published in regular issues.
All articles in this special issue will be reviewed by no fewer than two independent experts to ensure the quality, originality and novelty of the work published.
Learn more about the benefits of publishing in a special issue: https://www.elsevier.com/authors/submit-your-paper/special-issues
Interested in becoming a guest editor? Discover the benefits of guest editing a special issue and the valuable contribution that you can make to your field: https://www.elsevier.com/editors/role-of-an-editor/guest-editors
Call for papers - European Journal of Medicinal Chemistry Reports | ScienceDirect.com by Elsevier
