Archive for the ‘Editors Choice’ Category

Editor’s Choice Collection: Sankar Guchhait

RSC Medicinal Chemistry is delighted to introduce our Editor’s choice collection

This collection showcases some of the best articles published in the journal, handpicked by our Associate Editors and Editorial Board members.

Below we have a selection of recent RSC Medicinal Chemistry articles chosen by Associate Editor Sankar Guchhait (National Institute of Pharmaceutical Education and Research (NIPER), India). Take a look at which articles he chose and why.

Sankar Guchhait’s favourite articles

 

Graphical abstract for article: d4md00850b. Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting (Open Access)

Debora Iaculli, Jade Montgomery, Arthur Lamouroux, Anne Caufriez, Rafael Gozalbes, Mathieu Vinken, Filippo Molica, Brenda R. Kwak and Steven Ballet*

RSC Med. Chem., 2025, 16, 1289-1303

 

Sankar’s comments:

“The article made a highly significant contribution to the field of cardiovascular disease treatment, with selective inhibitor ligands of Connexins Cx43 HC activity. The work is hypothesis-led research and includes a novel approach, C- and N-terminal modification and cyclization of Cx43 region of protein, new peptides with proteolytic stability and bioavailability, high inhibitory capacity, and a cardiac endothelium targeting strategy. It is a scientifically sound work.”


Antimicrobial triazinedione inhibitors of the translocase MraY–protein E interaction site: synergistic effects with bacitracin imply a new mechanism of action (Open Access)

Julia A. Fairbairn, Rachel V. Kerr, Nika-Kare A. Pierre-White, Anthony Jacovides, Becca W. A. Baileeves, Phillip J. Stansfeld, Gerhard Bringmann, Andrew T. Merritt and Timothy D. H. Bugg*

RSC Med. Chem., 2025, 16, 1641-1653

Graphical abstract for article: d4md00937a.

 

Sankar’s comments:

“The work is scientifically highly impressive, considering its exploration of a new mechanism of action, translocase MraY–protein E interaction inhibition, by antimicrobial triazinedione inhibitors. The article presented a novel antibacterial mechanism and discovery of potent peptidomimetics. The work is useful in the field.”


Graphical abstract for article: d4md00122b. Novel PROTAC probes targeting KDM3 degradation to eliminate colorectal cancer stem cells through inhibition of Wnt/β-catenin signaling (Open Access)

Shadid U. Zaman, Piyusha P. Pagare, Hongguang Ma, Rosalie G. Hoyle, Yan Zhang* and Jiong Li*

RSC Med. Chem., 2024, 15, 3746-3758

 

Sankar’s comments:

“The article presented a high-quality work in the PROTAC field. The work demonstrated the development of PROTACs from the IOX1 skeleton with structure–activity relationship and structure-based design strategy, a favourable profile of isoform-selective degradation of KDM3 to eliminate colorectal CSCs via suppressing oncogenic Wnt signaling, in vivo efficacy, tumor growth inhibition with around 10- to 35-fold increased potency over IOX1, and metabolic profile and no hERG-associated cardiotoxicity. The studies are focused and impressive.”


Meet the Editor

 Photo of RSC Medicinal Chemistry Associate Editor, Sankar Guchhait. Sankar Guchhait, RSC Medicinal Chemistry Associate Editor

National Institute of Pharmaceutical Education and Research, India

Sankar K. Guchhait is a Professor in the Department of Medicinal Chemistry at NIPER, India. He did his PhD research at the Indian Association for the Cultivation of Science (IACS), Kolkata. Following his postdoctoral research for four years at the University of Tennessee, Knoxville, the University of Illinois at Chicago, and the University of California, Riverside, he started his research and teaching career at NIPER in 2007.

His research focuses majorly on medicinal chemistry, anticancer drug discovery, and synthesis of natural product-based and pharmaceutically important heterocyclic compounds.


We hope you enjoyed reading these articles. Be sure to check out the rest of our Editor’s choice collection, with new articles added regularly.

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Editor’s Choice Collection: Maria Duca

RSC Medicinal Chemistry is delighted to introduce our Editor’s choice collection

This collection showcases some of the best articles published in the journal, handpicked by our Associate Editors and Editorial Board members.

Below we have a selection of recent RSC Medicinal Chemistry articles chosen by Associate Editor Maria Duca (Université Côte d’Azur – CNRS, France). Take a look at which articles she chose and why.

Maria Duca’s favourite articles

 

Graphical abstract for article: d4md00123k. Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction (Open Access)

Sydney L. Rosenblum, Dalia M. Soueid, George Giambasu, Steve Vander Roest, Alexander Pasternak, Erin F. DiMauro, Vladimir Simov* and Amanda L. Garner*

RSC Med. Chem., 2024, 15, 1539-1546

 

Maria’s comments:

“This study, belonging to the journal’s Targeting RNA collection, exemplifies an important advance in RNA-targeted drug discovery by harnessing live-cell high-throughput screening to identify small-molecule disruptors of the oncogenic pre-let-7–Lin28 interaction. This highlights the potential of RiPCA approach in modulating RNA-protein interfaces in disease.”


Identification of lysosomotropism using explainable machine learning and morphological profiling cell painting data (Open Access)

Aishvarya Tandon, Anna Santura, Herbert Waldmann*, Axel Pahl* and Paul Czodrowski*

RSC Med. Chem., 2024, 15, 2677-2691

Graphical abstract for article: d4md00107a.

 

Maria’s comments:

“This study uses morphological profiling by means of the Cell Painting Assay (CPA) as a reliable surrogate to identify lysosomotropism. It combines Explainable Machine Learning with high-content morphological profiling to describe the physicochemical drivers of lysosomotropism, offering a predictive framework with practical implications for drug discovery and safety assessment.”


Graphical abstract for article: d3md00746d. 1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists (Open Access)

Robin van der Straat, Rosalie Draijer, Ewa Surmiak, Roberto Butera, Lennart Land, Katarzyna Magiera-Mularz, Bogdan Musielak, Jacek Plewka, Tad A. Holak and Alexander Dömling*

RSC Med. Chem., 2024, 15, 1210-1215

 

Maria’s comments:

“This impactful study reports a novel class of 1,5-disubstituted tetrazoles as potent small-molecule PD-L1 antagonists, leveraging multicomponent reaction chemistry for rapid scaffold assembly. It opens new avenues in immune checkpoint modulation beyond monoclonal antibodies.”


Meet the Editor

Photo of Associate Editor, Maria Duca. Maria Duca, RSC Medicinal Chemistry Associate Editor

Université Côte d’Azur – CNRS, France

Dr Maria Duca is head of the Targeting of Nucleic Acids research group in the Institute of Chemistry of Nice. She obtained her PhD in Molecular Biochemistry under the supervision of Dr Paola B. Arimondo (National Natural History Museum, Paris) working on topoisomerase II inhibitors. Her post-doctoral training in Sydney Hecht’s lab (University of Virginia, USA) allowed her to pursue the study of nucleic acids working on targeted protein mutagenesis upon chemical modification of tRNAs.

Her research activities at CNRS focus on the targeting of non-coding RNAs using synthetic small molecules toward innovative therapeutic approaches for anticancer, antiviral and antimicrobial applications.


We hope you enjoyed reading these articles. Keep an eye out on our collection webpage for more of our Editors’ favourite articles.

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Editors’ Choice: Structure-guided design of a selective BCL-XL inhibitor

This article describes the structure-guided optimisation of a screening hit against the pro-survival protein BCL-XL, which is often overexpressed in solid tumors and results in malignant tumor cells showing resistance to anticancer treatments.

Structure-guided design of a selective BCL-XL inhibitor
Guillaume Lessene, Peter E Czabotar, Brad E Sleebs, Kerry Zobel, Kym N Lowes, Jerry M Adams, Jonathan B Baell, Peter M Colman, Kurt Deshayes, Wayne J Fairbrother, John A Flygare, Paul Gibbons, Wilhelmus J A Kersten, Sanji Kulasegaram, Rebecca M Moss, John P Parisot, Brian J Smith, Ian P Street, Hong Yang, David C S Huang and Keith G Watson
Nature Chemical Biology, 9, 390–397, (2013)

Editors’ Choice articles are articles identified as being of high potential interest to medicinal chemists, selected from the wider literature by members of the Editorial Board.

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Editors’ Choice: Target validation using chemical probes

In this commentary article, Mark Bunnage and colleagues propose that by developing a ‘chemical probe tool kit’, chemical biology can play a more important part in seeking out potentially relevant targets.

Target validation using chemical probes
Mark E Bunnage, Eugene L Piatnitski Chekler & Lyn H Jones
Nature Chemical Biology, 9, 195–199 (2013)

Editors’ Choice articles are articles identified as being of high potential interest to medicinal chemists, selected from the wider literature by members of the Editorial Board.

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