Archive for the ‘Article collections’ Category

Celebrating the 65th birthdays of Jay Siegel and Kim Baldridge

We are delighted to share with you a joint themed collection in Organic & Biomolecular Chemistry and Organic Chemistry Frontiers celebrating the 65th birthdays of Jay Siegel and Kim Baldridge!

This themed collection, guest edited by Henning Jessen (University of Freiburg), Mihaiela Stuparu (Nanyang Technological University) and Eli Zysman-Colman (University of St. Andrews) highlights research reflecting the interests of Kim and Jay, known for their pioneering contributions to molecular design, quantum chemical methodologies, dynamic stereochemistry, non-planar polyarenes, materials science and supramolecular chemistry. Please read the articles in the collection below and check back for future additions.

 

Editorial

Celebrating Jay Siegel’s and Kim Baldridge’s 65th birthdays

Henning J. Jessen*, Mihaiela C. Stuparu* & Eli Zysman-Colman*

Org. Biomol. Chem., 2026, 24, 6708-6709

Research Articles

Design and synthesis of thiophene-based C2-symmetric chiral phosphoric acids on a decahydroquinoxaline scaffold for stereoselective transformations (Open Access)

Margherita Gazzotti, Vincenzo Mirco Abbinante, Fabrizio Medici, Sara Ghirardi, Sergio Rossi*, Tiziana Benincori, Roberto Cirilli & Maurizio Benaglia*

Org. Biomol. Chem., 2026, 24, 3490-3495

 

Pentaphosphorylated magic spot nucleotides: chemoenzymatic synthesis and disassembly-based sensing (Open Access)

Patrick Moser, Subhra Kanti Roy, Marvin Herzog, Felix Bauer, Felix Wollensack, Bernhard Breit & Henning J. Jessen*

Org. Biomol. Chem., 2026, 24, 3918-3925

 

Linker dependence of 1O2 generation by G4-binding tetra-imidazolium porphyrins (Open Access)

Çetin Çelik, Naoko Kakusho, Tianyu Xu, Sung Sik Lee, Naoko Yoshizawa-Sugata*, Hisao Masai* & Yoko Yamakoshi*

Org. Biomol. Chem., 2026, 24, 5028-5036

 

Synthesis of meta-substituted phenols and 1-estradiol conjugated analogues of suberoylanilide hydroxamic acid (SAHA)

Chanoknun Boonyaratsewee, Kitiya Rujimongkon, Wannarasmi Ketchart*, Somsak Pianwanit* & Yongsak Sritana-anant*

Org. Biomol. Chem., 2026, 24, 5726-5736

 

Injectable gelatin–PEG hydrogels obtained via cytochrome C-mediated polymerization (Open Access)

Andrea Fumaneri, Edoardo Sisti, Alessandro Ajò, H. Samet Varol, Viola Bertolotti, Luigi Menduti* & Luisa De Cola*

Org. Biomol. Chem., 2026, 24, 6185-6191

Structural controls on catenane co-conformational dynamics: the interplay of ring size, rigidity, and curvature

Yuejia Zhu, Yihe Wang & Ho Yu Au-Yeung*

Org. Biomol. Chem., 2026, 24, 6774-6780

 

BisBF2 pyridoins: a new platform for the design of efficient two-photon absorbers

Patryk Rybczyński, Manuela Grelich-Mucha, Elizaveta F. Petrusevich, Damian Plażuk, Liliana Dobrzańska, Borys Ośmiałowski* & Joanna Olesiak-Bańska*

Org. Chem. Front., 2026, 13, 389-394

mer-Ir(pmp)3 as a strongly photoreducing and stable Ir(C^C)3 photocatalyst for metallaphotoredox catalysis

Máire Griffin & Eli Zysman-Colman*

Org. Chem. Front., 2026, 13, 2707-2718

A polyaromatic dumbbell-based micelle capable of binding large dyes under organic solvent-rich conditions (Open Access)

Lorenzo Catti*, Aguri Sugawara, Kazuki Toyama & Michito Yoshizawa*

Org. Chem. Front., 2026, 13, 3030-3035

Double encapsulation of C60, [6]CPP and Li+@C60 inside a peropyrene-linked, CPP-based double nanohoop (Open Access)

Lei Ye, Yong Yang, Michal Juríček* & Thomas Drewello*

Org. Chem. Front., 2026, 13, 3281-3287

A chiral multibrominated triangular macrocycle for modulating circularly polarized phosphorescence

Yuluo Huang, Jianqiu Li, Ming-Ze Meng, Tuo-Yu Zhou, Xiao-Nian Xue, Huang Wu*, Shanshan Cheng* & Yu Wang*

Org. Chem. Front., 2026, 13, 3923-3933

Intramolecular through-space heavy-atom effect in multiresonant thermally activated delayed fluorescence emitters with [2.2]paracyclophane

Yan Xu, Hassan Hafeez, Wenrui Wang, Ifor D. W. Samuel* & Eli Zysman-Colman*

Org. Chem. Front., 2026, 13, 3934-3943

 

Deep supercooling, crystallisation & dynamically tunable disorder in the simplest geodesic polyarene (Open Access)

Valerio Di Lisio, Mattia Gaboardi, Jay Siegel, Daniele Cangialosi & Felix Fernandez-Alonso*

Org. Chem. Front., 2026, 13, 5612-5621

Solid-state polymerization of thieno[3,4-b]pyrazine derivatives

Vasin Thummasorn, Prapassorn Ongjaroon, Atthapon Saenubol, Taweesak Sudyoadsuk, Vinich Promarak* & Yongsak Sritana-anant*

Org. Chem. Front., Advance Article

 

 

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Editor’s Choice collection: Xiaohua Liu

OBC 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. This month we have a selection of recent OBC articles chosen by our Associate Editor Xiaohua Liu.

 

Meet the Editor

 

Xiaohua Liu obtained her BSc degree from Hubei Normal University (2000), and obtained her MS (2003) and PhD (2006) from Sichuan University. She joined the faculty of Prof. Feng’s group in 2006, and was appointed as an associate professor. In 2010, she was promoted as a full professor. Her current research interests include asymmetric catalysis and chiral drug synthesis.

 

 

Xiaohua’s favourite articles

 

Photo-induced transformation of α-diazocarbonyl compounds into mono-substituted alpha-halogen derivatives
Jinrui Bai, Bin Li, Dan Qi, Zhuoheng Song, Yue Yao & Chao Liu
Org. Biomol. Chem., 2025, 23, 422-426

 

 

“A visible-light driven halogenation reaction of diazo compounds under mild reaction condition is reported. Three new halogenating agents were tolerable, benefiting the efficient introduction of F, Cl and Br-atom.”

 


 

Exploring nickel-catalyzed organochalcogen synthesis via cross-coupling of benzonitrile and alkyl chalcogenols with computational tools
Francisco A. Gómez-Mudarra, Gabriel Aullón & Jesús Jover
Org. Biomol. Chem., 2025, 23, 1673-1682

 

 

“Through DFT calculation and microkinetic modeling, the detailed mechanism of a nickel(0) dcype-catalyzed cross-coupling between benzonitrile and propanethiol to produce new C–S bonds was disclosed, showing the potential usage to predict the construct C–Se and C–Te bonds.”

 


 

 

Formation of complex cyclic compounds via a dehydrogenative Diels–Alder reaction
Zhongwei Xu, Yu Lei, Meng Chang, Ruihua Qiang, Qiong Hu & Yimin Hu
Org. Biomol. Chem., 2025, 23, 9330-9335

 

 

“An unprecedented annulation strategy by trapping DHT for the construction of macrocyclic compounds is reported. The choice of different basic conditions resulted in the formation of distinct types of annulation products, showing the potential application of pentadehydro-Diels–Alder and hexadehydro-Diels–Alder reactions.”


We hope you enjoyed reading these articles. Keep an eye out for more of our Editors’ favourite articles in the future.

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Editor’s Choice collection: Jeroen Dickschat

OBC 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. This month we have a selection of recent OBC articles chosen by our Associate Editor Jeroen Dickschat.

Meet the Editor

Jeroen S. Dickschat studied Chemistry at TU Braunschweig and obtained his PhD under the supervision of Stefan Schulz in 2004, followed by postdoctoral stays with Rolf Müller at Saarland University and with Peter Leadlay at the University of Cambridge (UK). In 2008 he started his independent career at TU Braunschweig, culminating in his habilitation in 2013. In 2014 he accepted an appointment as a Professor of Organic Chemistry and Biochemistry at the University of Bonn. He also holds a honorary Professorship at the NIOO Wageningen (The Netherlands).

His group is interested in the biosynthesis of microbial natural products, with a special focus on the elucidation of the complex reaction mechanisms in their formation.

 

Jeroen’s favourite articles

 

Swermilactones A and B: racemic xanthone–secoiridoid heterodimers from Swertia mileensis
Yao Du, Hao Li, Xiao-Yu Qi, Yuan-Liang Xu, Yan Liu, Xue-Mei Niu, Kai Guo & Sheng-Hong Li
Org. Biomol. Chem., 2025, 23, 3860-3864

 

 

“This research article describes the isolation and structural characterisation of swermilactones A and B from Swertia mileensis. Unlike most natural products, the swermilactones were shown not to be enantiomerically pure, but rather scalemic. The strength of this paper lies in the rigour not only to uncover the scalemic nature of the natural products, but also in giving a sound scientific explanation for their possible biosynthesis.”

 


 

Discovery of a plant-like tridomain bifunctional syn-abieta-7,13-diene synthase in Streptomyces
Caitlin A. McCadden, Diana P. Łomowska-Keehner, Tracy Qu, Jordan Nafie, Tyler A. Alsup & Jeffrey D. Rudolf
Org. Biomol. Chem., 2025, 23, 9845-9850

 

 

“Terpene synthases in bacteria usually exhibit a single so-called alpha-domain or a combination of beta and gamma-domains, while plant terpene synthases usually contain three domains (alpha-beta-gamma). The present paper not only reports about the occurrence of alpha-beta-gamma domain terpene synthases from bacteria, but also about the bioinformatic identification of additional interesting gene fusions, suggesting multifunctional bacterial enzymes to be characterised in future work.”

 


 

Nitrones as directing groups in transition metal-catalysed C–H activation
Barbara Stańska, Anjali Dahiya & Rafał Loska
Org. Biomol. Chem., 2026, 24, 11-37

 

 

“This review highlights the role of nitrones as directing groups in transition metal-catalysed C-H activations. C-H activations continue to be a hot topic, but the non-expert reader may not be aware that nitrones can play important roles in catalytic processes. This review article follows a highly didactic approach and also identifies important open questions such as the development of chiral catalysts for enantioselective reactions.”

 


We hope you enjoyed reading these articles. Keep an eye out for more of our Editors’ favourite articles in the future.

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Editor’s Choice collection: Scott Silverman

OBC 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. This month we have a selection of recent OBC articles chosen by our Associate Editor Scott Silverman.

Meet the Editor

Scott K. Silverman was born in 1972 and raised in Los Angeles, California. He received his BS in chemistry from UCLA in 1991, working with Christopher Foote on photooxygenation mechanisms. He obtained his PhD in chemistry from Caltech in 1997, working with Dennis Dougherty to study high-spin organic polyradicals and molecular neurobiology. After postdoctoral research on RNA biochemistry with Thomas Cech at the University of Colorado at Boulder, he joined the University of Illinois in 2000, where he is currently Professor of Chemistry.

Professor Silverman’s research is in the chemistry and biochemistry of nucleic acids, especially investigations of DNA as an enzyme (DNAzyme, deoxyribozyme).

 

Scott’s favourite articles

 

Facile DNA chemical ligation under mild conditions enabled by 1-cyano-4-(dimethylamino)pyridinium tetrafluoroborate (CDAP)

Hiroki Yamada, Yasuaki Kimura, Hiroshi Abe & Junichiro Yamamoto

Org. Biomol. Chem., 2025, 23, 4866-4872

 

“This paper establishes a new, nonenzymatic approach for DNA ligation. The authors show that CDAP, 1-cyan-4-(dimethylamino)pyridinium tetrafluoroborate, can be used as an alternative to cyanogen bromide (CNBR) to join 3′-OH and 5′-phosphate termini when aligned on a DNA template strand. The CDAP reaction proceeds efficiently, without DNA deglycosylation or other side reactions that are induced by CNBr and can be done on ice. Such findings should have value for joining DNA strands in various contexts.”


 

Viscosity effects on the chemiluminescence emission of 1,2-dioxetanes in water

Maidileyvis Castro Cabello, Palanisamy Kandhan, Peng Tao & Alexander R. Lippert

Org. Biomol. Chem., 2025, 23, 5380-5389

 

“This work explores an interesting physical organic relationship between viscosity and aqueous chemiluminescent emission of 1,2-dioxetanes, noting that chemiluminescence is often the basis for imaging techniques in vivo. The authors used several different models to explain their observations. The findings should be helpful in ongoing design efforts with chemiluminescent compounds.”

 


 

Strategies for the optimisation of troublesome peptide nucleic acid (PNA) sequences

Emma E. Watson

Org. Biomol. Chem., 2025, 23, 9797-9814

 

 

“This review describes many practical aspects of peptide nucleic acids (PNA), focusing on the relationship between PNA sequence and considerations ranging from synthesis to biological uptake, including backbone and nucleobase modifications. As one reviewer mentioned, this article is an excellent launching point for those scientists who wish to get started in PNA research.”

 


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Editor’s Choice collection: Huan Wang

OBC 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. This month we have a selection of recent OBC articles chosen by our Associate Editor Huan Wang.

Meet the Editor

 

Professor Wang graduated from Peking University (2005). He obtained his PhD from University of Maryland at College Park (2010) and conducted post-doctoral research work at University of Illinois at Urbana-Champaign (2010-2014). Huan started at Nanjing University in 2014 and works as a Professor in the Chemistry department.

His research group aims to address problems at the interface of chemistry and biochemistry, including the chemical synthesis and biosynthesis of bioactive peptides, peptide/protein functionalisation and biological functions of non-coding RNAs.

 

Huan’s favourite articles

 

Histidine-bridged cyclic peptide natural products: isolation, biosynthesis and synthetic studies
Pascal M. Engelhardt, Robert Keyzers & Margaret A. Brimble
Org. Biomol. Chem., 2024, 22, 8374-8396

 

 

 

“This timely review synthesises four decades of research on histidine-bridged macrocyclic peptides, highlighting their unusual cross-linking chemistry, diverse biosynthetic origins, and emerging biological activities. By integrating structural, biosynthetic and synthetic perspectives, the article provides a comprehensive resource that will guide future discovery and mechanistic studies of this underexplored class of peptide natural products.”


 

 

Ag(i)-promoted fragment coupling of peptide thioamides
Varsha J. Thombare, Carlie L. Charron & Craig A. Hutton
Org. Biomol. Chem., 2025, 23, 1995-1999

 

 

“This work introduces a conceptually distinct fragment-coupling strategy that leverages Ag(I)-mediated isoimide formation to generate native amide bonds without traditional peptide coupling reagents. The method enables efficient solution- and solid-phase ligations, offering a valuable complement to established NCL-based approaches and showing promise for challenging peptide sequences prone to aspartimide formation.”


 

 

Frog farnesyl pyrophosphate synthases and their role as non-canonical terpene synthases for bisabolane sesquiterpenes
Kexin Yang, Houchao Xu, Miguel Vences, Andolalao Rakotoarison, Stefan Schulz & Jeroen S. Dickschat
Org. Biomol. Chem., 2025, 23, 7940-7945

 

 

“This manuscript reveals that frog FPPS homologs catalyse unexpected cyclisations of (2Z,6E)-FPP to bisabolane-type terpenoids, uncovering a potential alternative function conserved across diverse FPPS enzymes. The finding expands our understanding of terpene biosynthesis in higher animals and raises fundamental questions about enzyme evolution, substrate promiscuity, and physiological relevance of volatile signalling molecules.”


 

We hope you enjoyed reading these articles. Keep an eye out for more of our Editors’ favourite articles in the future.

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Editor’s Choice collection: Cristina Trujillo

OBC 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. This month we have a selection of recent OBC articles chosen by our Associate Editor Cristina Trujillo.

Meet the Editor

 

Dr Cristina Trujillo obtained her Ph.D. in Theoretical and Computational Chemistry in 2008 at the Universidad Autónoma de Madrid. Between 2008-2016 she held several Postdoctoral positions at CSIC, Czech Academy of Sciences and Trinity College Dublin (TCD) before becoming a Research Fellow at TCD from 2016-2018 and subsequently working as an Assistant Lecturer at TU-Dublin. She started her own research group at TCD in 2019 before moving to the University of Manchester in 2022 where she is currently a Lecturer in Computational & Theoretical Chemistry.

Her research interests are focused on the asymmetric catalysis field, with particular emphasis on the application of computational techniques in the design of organocatalysts along with prediction and control of catalytic processes, with a direct impact on the development of products with different applications.

 

Cristina’s favourite articles

 

Friedel-Crafts reactions for biomolecular chemistry

Jun Ohata

Org. Biomol. Chem., 2024, 22, 3544-3558

 

 

“This review delivers a comprehensive perspective on the growing field of Friedel–Crafts reactions in biomolecular chemistry, charting new directions in the selective modification and functionalisation of complex biological molecules. The author highlights the power of Friedel–Crafts processes for creating C–C bonds within challenging biomolecular settings, spotlighting recent advances and experimental strategies that bridge traditional organic methodologies with modern chemical biology. This synthesis of conceptual and practical insights makes the review a compelling read for both organic and bioorganic chemists interested in innovative molecular construction.”

 

 

Exploring nickel-catalyzed organochalcogen synthesis via cross-coupling of benzonitrile and alkyl chalcogenols with computational tools

Francisco A. Gómez-Mudarra, Gabriel Aullón & Jesús Jover

Org. Biomol. Chem., 2025, 23, 1673-1682

 

“This work investigates a distinctive nickel(0)-catalysed cross-coupling between benzonitrile and alkyl chalcogenols to form C–S, C–Se, and C–Te bonds. By outlining a classic oxidative addition–transmetalation–reductive elimination pathway that unusually engages the Ph–CN bond, the study proposes a general mechanistic platform extending beyond thioethers to their heavier chalcogen analogues. Through kinetic analysis and microkinetic simulations, the authors demonstrate that this strategy could expand synthetic access to organochalcogen compounds of biological and materials relevance while maintaining excellent functional group tolerance.”

 

 

Effect of strain and π-acidity on the catalytic efficiency of carbones in carbodiimide hydroboration

Max Schernikau & O. Maduka Ogba

Org. Biomol. Chem., 2025, 23, 9896-9907

 

 

“Using DFT calculations, this paper explores how structural and electronic factors govern the performance of zerovalent carbon-centred organocatalysts (carbones) in the hydroboration of carbodiimides. The authors reveal that cyclic carbodiphosphoranes outperform their acyclic analogues owing to superior substrate activation and more efficient hydride transfer, as mapped by distortion/interaction–activation strain analysis. The study fills key gaps in understanding catalyst design and reactivity, underscoring the growing promise of carbones as versatile organocatalysts for bond-forming transformations.”

 

We hope you enjoyed reading these articles. Keep an eye out for more of our Editors’ favourite articles in the future

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Editor’s Choice collection: Motomu Kanai

OBC 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. This month we have a selection of recent OBC articles chosen by our Associate Editor Motomu Kanai.

Meet the Editor

 

Motomu Kanai received his bachelor degree from the University of Tokyo in 1989 and his PhD from Osaka University in 1995. He then moved to the University of Wisconsin for postdoctoral studies with Professor Laura Kiessling. In 1997, he returned to the University of Tokyo to join Professor Masakatsu Shibasaki’s group as an assistant professor. After being a lecturer (2000-2003) and associate professor (2003-2010), he is now a professor at the University of Tokyo.

His research interests entail design and synthesis of functional (especially, biologically active) molecules.

 

 

Motomu’s favourite articles

 

When transition-metal catalysis meets electrosynthesis: a recent update

Fei Lian, Jiu-Ling Li & Kun Xu

Org. Biomol. Chem., 2024, 22, 4390-4419

 

 

 

“Electrochemistry-driven transition metal catalysis is a rapidly growing area today. Lian, Li and Xu review recent progress in this active field. This review specifically focuses on the first-row transition metal catalysis coupled with electrosynthesis, which offers benefits in terms of sustainability and foreshadows the future of green catalysis.”

 

 

Exploring the catalytic mechanism of the 10–23 DNAzyme: insights from pH–rate profiles

Virginia Parra-Meneses, Victoria Silva-Galleguillos & Marjorie Cepeda-Plaza

Org. Biomol. Chem., 2024, 22, 6833-6840

 

 

“A specific group of DNA molecules, known as DNAzymes, can catalyze chemical reactions, such as the hydrolytic cleavage of RNA. However, the detailed reaction mechanism of DNAzymes is not fully understood, which limits progress. In this paper, Parra-Meneses, Silva-Galleguillos and Cepeda-Plaza provide important insights into the catalytic strategies of RNA-cleaving DNAzymes. This discovery will aid in designing new DNAzymes with therapeutic applications, such as gene silencing.”

 

Total synthesis, stereochemical assignment, and biological evaluation of opantimycin A and analogues thereof

Yoshinosuke Usuki, Ryota Abe, Kazuki Nishiguchi, Tetsuya Satoh, Harumi Aono, Toshihiko Nogawa, Yushi Futamura, Hiroyuki Osada, Izumi Yoshida, Kazuhiro Fujita, Takashi Mishima & Ken-Ichi Fujita

Org. Biomol. Chem., 2024, 22, 8973-8979

 

“An antimalarial natural product, opantimycin A, features a unique structure that includes γ-butyrolactone and dehydro-2-aminobutyric acid motifs. Using the stereodivergent Mukaiyama aldol reaction and Staudinger ligation as key steps, Usuki and coworkers successfully synthesized opantimycin A and its various analogues, enabling the determination of the natural product’s absolute configuration. Some of these analogues exhibit significant biological activities. This study highlights a critical role of natural product synthesis.”

 

We hope you enjoyed reading these articles. Keep an eye out for more of our Editors’ favourite articles in the future.

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Editor’s Choice collection: Kate Jolliffe

OBC 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. This month we have a selection of recent OBC articles chosen by our Associate Editor Kate Jolliffe (University of Sydney). Take a look at which articles she chose and why.

Meet the Editor

Kate Jolliffe received her BSc (Hons) in 1993 and PhD in 1997 from the University of New South Wales. She then held positions at Twente University, University of Nottingham and the Australian National University before taking up an Australian Research Council QEII fellowship at The University of Sydney in 2002. In 2007 she became a Senior lecturer at the same institution and was promoted to Associate Professor in 2008 and to full Professor in 2009. She currently holds the position of Payne-Scott Professor at The University of Sydney.

Her research interests are in the areas of supramolecular, peptide and organic chemistry, with a focus on the design and synthesis of functional molecules, such as molecular sensors capable of detecting anions in biological environments or cyclic peptides for application in biology and medicine.

 

Kate’s favourite articles

Impact of charges on the hybridization kinetics and thermal stability of PNA duplexes

Miguel López-Tena & Nicolas Winssinger

Org. Biomol. Chem., 2024, 22, 5759-5767

 

 

 

“Peptide nucleic acids have a range of potential biomedical applications because they form duplexes with DNA and RNA that are more stable than DNA or RNA homoduplexes. López-Tena and Winssinger analyse how modifications of PNA structure at the γ-position impact hybridisation stability and kinetics, demonstrating that the higher stability of duplexes involving PNA results from slower dissociation kinetics rather than association kinetics (which are also slower relative to a DNA:DNA duplex). This improves our understanding of how to design molecular structures with specific function.”

 

Enhanced binding of methyl alkylammonium cations through preorganization of a water-soluble calix[4]pyrrole

Esteban Valencia & Pablo Ballester

Org. Biomol. Chem., 2024, 22, 5827-5834

 

 

 

“Mimicking nature’s molecular receptors and achieving similar selectivity and affinity is one of the key aims of supramolecular chemists. Valencia and Ballester use extended calix[4]pyrroles to bind biologically relevant methyl trialkylammonium cations with high affinity in water, providing a nice example of how synthetic molecules can be designed to mimic nature.”

 

 

Substituent effects of fluorinated bambusurils on their anion transport

Matúš Chvojka, Vladimír Šindelář & Hennie Valkenier

Org. Biomol. Chem., 2025, Advance Article

 

 

“In another example of supramolecular structure-activity analysis, Chovjka, Šindelář and Valkenier evaluate the anion transport properties of a small library of fluorinated bambusurils. Defining structure-activity relationships of these molecules is key to meeting the multiple criteria for effective ion transport in cells that will be required for application in treating chanellopathies e.g. cystic fibrosis. This paper demonstrates how small structural changes can have a large, and sometimes unanticipated, impact on function.”

 

We hope you enjoyed reading these articles. Keep an eye out for more of our Editors’ favourite articles in the future.

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Editor’s Collection: Meet the authors – Nathalie Busschaert et al.

Meet our researchers:

Elliot Williams

Hassan Gneid

Sarah Marshall

Mario González

Jorgi Mandelbaum

Nathalie Busschaert


Elliot Williams
obtained his BSc in biochemistry from the University of Central Florida. He is currently working towards his PhD at Tulane University. His PhD focuses on the development of hosts for bacterial lipids, in particular anionic lipids such as PG. As such, he was the first author of the paper and performed the majority of the experiments. When not in the lab, he likes to dance, engage in his community, and walk his dog.

Hassan Gneid completed a BSc in chemistry at Damascus University (Syria), in the field of applied chemistry. After a number of years working in industry, he returned to education in 2011 to complete an MPhil degree in chemistry at the University of Southampton (UK) under the supervision of Dr. Martin Grossel. In 2014, he joined the group of Dr. Jonathan Watts to pursue a PhD in chemistry at the University of Southampton (UK) and the RNA Therapeutics Institute (USA). His PhD work revolved around the use of antisense oligonucleotides for the development of novel antibiotics. Hassan joined the Busschaert group in 2020 as a post-doctoral researcher responsible for microbiology studies. His research interests are oligonucleotide therapeutics and antibiotic development.

Sarah Marshall received her B.S. in biology from the Honors College at East Carolina University in 2015. She continued at East Carolina University to receive her M.S. in chemistry under the supervision of Dr. William E. Allen. During her M.S., she focused on the development of fluorescent amino acids and peptide synthesis. Currently, Sarah is a PhD candidate in the Busschaert group at Tulane University, working on various medical and non-medical applications of synthetic transmembrane anion transporters.

Mario González was born in San Juan, Puerto Rico. In 2019, he received his B.S. in Chemistry from the University of Miami. That same year, he joined the Busschaert group at Tulane University as a graduate student working towards a PhD. His current research involves turning commercially available, nonselective sensors selective via liquid-liquid extractions.

Jorgi Mandelbaum graduated from Tulane University with a B.S. (2021) and M.S. (2022) in neuroscience, with undergraduate minors in chemistry and Spanish. During her studies, she performed undergraduate research in the lab of Dr. Nathalie Busschaert, focusing on PG binding. She currently works as Research Scientist II on the Translational Pharmacology team in the Ophthalmology department at Novartis Institutes for BioMedical Research in Cambridge, MA. With her passion for pharmaceutical development, Jorgi is excited to be continuing her research beyond the academic setting in the healthcare industry.

Nathalie Busschaert born in Antwerp, Belgium, completed a BSc in chemistry at the K. U. Leuven, Belgium, and continued studying for an MSc in chemistry at the same university. She then moved to the University to Southampton (UK) in 2010 to undertake a PhD under the supervision of Professor Philip A. Gale, working on the development of synthetic transmembrane anion transporters. In 2015 she joined the group of Andrew Hamilton at the University of Oxford to work as a post-doctoral researcher. In January 2016 she followed prof. Andrew Hamilton to New York University. She is currently working as an assistant professor at Tulane University. Her research interests are ion transport, lipid binding, membrane processes and medicinal applications of supramolecular systems.


What inspired your research in this area?

We are a young research group (established July 2017), and have been looking for a way to carve out our reputation as supramolecular chemists that work towards medical applications. I have been intrigued by the activity of antimicrobial peptides for a long time, due to my interest in biological membranes. Antimicrobial peptides have long been hailed as a solution to the antibiotic resistance crisis, because they target the bacterial membrane and can cause quick bactericidal activity in bacterial cells. However, they have some drawbacks and have not been able to completely live up to their expectation yet. Most antimicrobial peptides are cationic amphiphilic compounds that function by binding to the negatively charged lipids of bacterial membranes, followed by membrane disruption. During my own PhD that focused on the development of small neutral molecules that can transport chloride anions across biological membranes, we often observed binding to the lipid headgroup in molecular dynamics modelling. While binding to the lipid headgroup is detrimental for anion transport, I hypothesized that binding to the headgroup can provide membrane selectivity (e.g., bacterial membranes over human membranes) and can induce membrane perturbations similar to those observed for antimicrobial peptides. From the start of my independent career, my research group therefore started to develop small molecules that can strongly and selectively bind to bacterial lipid headgroups.

What do you personally feel is the most interesting/important outcome of your study?

The most important outcome of our study is that we provided proof-of-principle that small, neutral, structurally simple molecules can selectively bind to lipid headgroups and that this binding event has sufficient impact on membrane permeability to induce antibacterial activity. Even though the reported compounds were our first attempt at binding PG lipids and have not underwent further optimization yet, we have already achieved relatively potent antibiotics with minimum inhibitory concentrations (MIC values) of 12.5 – 25 μM.

What directions are you planning to take with your research in future? What are you going to be working on next?

We are preparing analogs of the PG hosts reported in this paper (https://doi.org/10.1039/D1OB02298A ), as well as the PE hosts that were reported in our previous OBC paper (https://doi.org/10.1039/D1OB00263E). The aim is to improve the antibacterial activity and lipid selectivity, and to elucidate structure-activity relationships that can help other researchers develop hosts for these two important bacterial lipids. In addition, we would like to investigate the effect of physical membrane parameters (such as curvature, and lipid chain length) on the binding of the hosts to the lipid headgroup. Finally, we are working on developing hosts that can bind selectively to other types of biologically relevant lipids.

Read the full article: A supramolecular host for phosphatidylglycerol (PG) lipids with antibacterial activity

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Editor’s Collection: Meet the authors – Luca Gabrielli et al.

Meet our researchers:

Daniele Rosa-Gastaldo

Vytautas Pečiukėnas

Christopher Hunter

Luca Gabrielli

Daniele Rosa-Gastaldo obtained his PhD in Chemistry at the University of Padova in 2020 under the supervision of Prof. Fabrizio Mancin, studying the use of gold nanoparticles as NMR chemosensors. After a postdoctoral experience at the same university in Dr. Gabrielli’s group, he moved to the University of Geneva and joined as a post-doc Prof. Thomas Bürgi’s group, where his research is focused on the properties and applications of atomically precise gold and silver nanoclusters.

Vytautas Pečiukėnas studied Natural Sciences at the University of Cambridge obtaining MSci diploma in 2018. There he carried out his Masters project on informational oligomers in Prof. Hunter’s group under the direct supervision of Dr. Gabrielli. Currently he is a PhD student in Dr. Josep Cornella’s group at the the Max-Planck-Institut für Kohlenforschung in Germany. His research is focused on developing catalytic cross-coupling protocols by employing Bi(III)/(V) redox platform.

Christopher A. Hunter was born in New Zealand and educated at the University of Cambridge, graduating with a PhD in 1989. He was a lecturer at the University of Otago till 1991, when he moved to the University of Sheffield.  He was promoted to a chair in 1997, and in 2014, he took up the Herchel Smith Professorship of Organic Chemistry at the University of Cambridge. In 2008, he was elected a Fellow of the Royal Society, and he is an Honorary Member of the Royal Irish Academy.

Luca Gabrielli obtained his MSc and PhD in Chemistry at the University of Milano-Bicocca with Laura Cipolla, spending part of his PhD at the Ben G. Davis’ group (University of Oxford). After a post-doc experience with Fabrizio Mancin at the University of Padova, he moved to the group of Chris Hunter (University of Cambridge) as an MSCA-IF fellow. In 2019 he moved back to the University of Padova, where is currently an assistant professor. His research interests span from information molecules to kinetically controlled and out of equilibrium systems.


What inspired your research in this area?

The way living systems store information as a sequence of nucleotides, and how this information is copied, transcribed, and translated into a functional molecule, represents the main inspiration of our research. However, these outstanding properties are currently unique to nucleic acids. Synthetic recognition-encoded oligomers have the potential to display similar properties, which would open the way for the directed evolution of function in synthetic polymers.

What do you personally feel is the most interesting/important outcome of your study?

One of the challenges in the realization of synthetic oligomers capable of sequence-selective duplex formation is the competing intramolecular folding interaction between complementary recognition units. Thanks to the modular approach adopted for designing duplex-forming oligoanilines (Chem. Sci., 2020, 11, 561-566), we investigated how variations in the steric bulk around the H-bond acceptor unit and on the backbone structure would affect folding and duplex formation. We observed that using a long rigid linker as the backbone connecting two monomer units successfully prevents 1,2-folding and leads to the formation of a stable mixed-sequence duplex, while increasing the acceptor bulkiness was not effective in preventing the undesired folding.

What directions are you planning to take with your research in future? What are you going to be working on next?

The observation of imine polymerase activity in one of these single-stranded oligomers (Chem. Sci., 2020, 11, 7408-7414) suggested that more interesting analogies between natural biopolymers and the chemistry of synthetic recognition-encoded oligomers will come to light. Hence, our future research will be focused on developing synthetic duplex-forming oligomers able to perform templated synthesis of the complementary sequence molecule, which is the key property that allows to copy, transcript, and translate nucleic acids.

 

Read the full article: Duplex vs. folding: tuning the self-assembly of synthetic recognition-encoded aniline oligomers

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