Explanipedia

The XNA alphabet Open

John C. Chaput, Martin Egli, Piet Herdewijn · 2025

Inspired by nature, chemists have spent the last 50 years systematically designing and synthesizing a vast array of sugar-modified nucleic acids, so-called xenonucleic acids (XNAs), collectively forming what we now describe as the XNA alph…

Subnanomolar MAS-related G protein-coupled receptor-X2/B2 antagonists with efficacy in human mast cells and disease models Open

Ghazl Al Hamwi, Mohamad Wessam Alnouri, Sven Verdonck, Piotr Leonczak, Shaswati Chaki , et al. · 2025

Synthesis of Xylo‐nucleoside H‐Phosphinates and Insights into Their Conformational Preferences Within a Chimeric Duplex Open

Yuqing Xu, Sten Reynders, Frédérick Coosemans, Piet Herdewijn, Elisabetta Groaz , et al. · 2025

An efficient method for the synthesis of xylo‐nucleoside H ‐phosphinate building blocks containing both pyrimidine and purine nucleobases is reported. A DNA‐phoXyloNA‐DNA chimeric sequence containing a central 2′‐5′‐phosphonomethoxy‐linked…

Tuning i-motif folding and stability with acyclic phosphonate-linked (ZNA) cytidine residues Open

Marlies Derden, Sten Reynders, Jérôme Rihon, Xinlu Li, Frédérick Coosemans , et al. · 2025

ZNA residues are accommodated within an i-motif core without disrupting C:H + C base pairing but inducing measurable changes in loop dynamics.

Design, Synthesis and Application of Aggregation-Induced Emission Bifunctional Fluorescence Probe Open

Kai Yan, Shihao Wang, Zichen Yang, Sheng Liu, Dayong Gu , et al. · 2025

Structural insights into a DNA polymerase reading the xeno nucleic acid HNA Open

Cédric Gutfreund, Karin Betz, Mikhail Abramov, Frédérick Coosemans, Philipp Holliger , et al. · 2024

Xeno nucleic acids (XNAs) are unnatural analogues of the natural nucleic acids in which the canonical ribose or deoxyribose rings are replaced with alternative sugars, congener structures or even open-ring configurations. The expanding rep…

Correction to “Synthesis of a 3′-Fluoro-3′-deoxytetrose Adenine Phosphonate” Open

Swarup De, Steven De Jonghe, Piet Herdewijn · 2024

3-nitropyridine analogues as novel microtubule-targeting agents Open

Jean Herman, Els Vanstreels, Dorothée Bardiot, A.E. Prota, Natacha Gaillard , et al. · 2024

Microtubule-targeting agents are an important class of anti-cancer drugs; their full potential is however not realized because of significant myelotoxicity and neurotoxicity. We here report 3-nitropyridine analogues as a novel group of mic…

Rational design of a bacterial import system for new-to-nature molecules Open

Emilio Rodríguez-Robles, David Müller, Tilmann Künzl, Suren J. Nemat, M. Edelmann , et al. · 2024

Integration of novel compounds into biological processes holds significant potential for modifying or expanding existing cellular functions. However, the cellular uptake of these compounds is often hindered by selectively permeable membran…

Impact of Single Acyclic Phosphonate Nucleotide (ZNA) Modifications on DNA Duplex Stability Open

Xinlu Li, Elisabetta Groaz, Piet Herdewijn, Eveline Lescrinier · 2024

An acyclic phosphonate‐linked nucleic acid backbone (ZNA) demonstrated the capability to support duplex formation and propagate genetic information in vivo, unveiling its potential for evolution into a synthetic genetic system (XNA). To de…

Degraders in epigenetic therapy: PROTACs and beyond Open

Xing‐Jie Dai, Shi‐Kun Ji, Meng‐Jie Fu, Gao-Zhi Liu, Huimin Liu , et al. · 2024

Epigenetics refers to the reversible process through which changes in gene expression occur without changing the nucleotide sequence of DNA. The process is currently gaining prominence as a pivotal objective in the treatment of cancers and…

Unlocking the synthetic approaches and clinical application of approved small-molecule drugs for gastrointestinal cancer treatment: A comprehensive exploration Open

Xiaojing Li, Peng Nie, Piet Herdewijn, Jiangang Sun · 2023

Synthetic approaches and application of clinically approved small-molecule drugs to treat hepatitis Open

Zhen-Xi Niu, Peng Nie, Piet Herdewijn, Yatao Wang · 2023

Synthesis and clinical application of small-molecule inhibitors of Janus kinase Open

Jingyi Zhang, Jinfeng Sun, Peng Nie, Piet Herdewijn, Yatao Wang · 2023

Conformational Morphing by a DNA Analogue Featuring 7-Deazapurines and 5-Halogenpyrimidines and the Origins of Adenine-Tract Geometry Open

Pradeep S. Pallan, Terry P. Lybrand, Eriks Rozners, Mikhail Abramov, Guy Schepers , et al. · 2023

Several efforts are currently directed at the creation and cellular implementation of alternative genetic systems composed of pairing components that are orthogonal to the natural dA/dT and dG/dC base pairs. In an alternative approach, Wat…

Modulation of the tetrameric I-motif folding of C-rich Tetrahymena telomeric sequences by hexitol nucleic acid (HNA) modifications Open

Michele Ghezzo, Luca Grigoletto, Riccardo Rigo, Piet Herdewijn, Elisabetta Groaz , et al. · 2023

Characterization of an HNA aptamer suggests a non-canonical G-quadruplex motif Open

Peter Schofield, Alexander I. Taylor, Jérôme Rihon, Cristian David Peña Martinez, Sacha Zinn , et al. · 2023

Nucleic acids not only form the basis of heredity, but are increasingly a source of novel nano-structures, -devices and drugs. This has spurred the development of chemically modified alternatives (xeno nucleic acids (XNAs)) comprising chem…

Controlled E. coli Aggregation Mediated by DNA and XNA Hybridization Open

Cécile Gasse, Puneet Srivastava, Guy Schepers, Joachim Jose, Marcel Hollenstein , et al. · 2023

Chemical cell surface modification is a fast‐growing field of research, due to its enormous potential in tissue engineering, cell‐based immunotherapy, and regenerative medicine. However, engineering of bacterial tissues by chemical cell su…

Synthesis, antiviral activity, and computational study of β-d-xylofuranosyl nucleoside phosphonates Open

Yuqing Xu, Elisabetta Groaz, Jérôme Rihon, Piet Herdewijn, Eveline Lescrinier · 2023

Synthesis and anti-SARS-CoV-2 evaluation of lipid prodrugs of β-D-N4-hydroxycytidine (NHC) and a 3′-fluoro-substituted analogue of NHC Open

Zhaohui Wen, Mengmeng Wang, Lingyun Li, Piet Herdewijn, Robert Snoeck , et al. · 2023

CRISPR-Cas9 recognition of enzymatically synthesized base-modified nucleic acids Open

Hui Yang, Elena Eremeeva, Mikhail Abramov, Maarten Jacquemyn, Elisabetta Groaz , et al. · 2023

An enzymatic method has been successfully established enabling the generation of partially base-modified RNA (previously named RZA) constructs, in which all G residues were replaced by isomorphic fluorescent thienoguanosine (thG) analogs, …

A microbiological system for screening the interference of XNA monomers with DNA and RNA metabolism Open

Aude Blanchard, Mikhail Abramov, Camille Hassan, Philippe Marlière, Piet Herdewijn , et al. · 2023

Impact of xenobiotic nucleoside triphosphates on E. coli nucleic acids synthesis.

Synthesis and anticancer evaluation of acetylated-lysine conjugated gemcitabine prodrugs Open

Mengmeng Wang, Kunyu Qu, Peipei Zhao, Xin Yin, Yiwei Meng , et al. · 2023

We report a series of acetylated lysine conjugated gemcitabine prodrugs that exhibit highly selective tumor cell growth inhibition and enhanced metabolic stability.

Synthesis of Novel 2,2'-Anhydro-L-threosylpyrimidine Phosphonates Open

Chuantao Zhu, Song Wang, Yifan Zhao, Piet Herdewijn, Feng‐Wu Liu · 2023

A series of L-threoylnucleoside phosphonates were synthesized via a nine-step procedure firstly.When the L-threoylpyrimidine nucleoside phosphonate was treated by diethylaminosulphur trifluoride (DAST), all the tried pyrimidine L-threosyln…

Identification of Polyphenol Derivatives as Novel SARS-CoV-2 and DENV Non-Nucleoside RdRp Inhibitors Open

Shenghua Gao, Letian Song, Hongtao Xu, Antonios Fikatas, Merel Oeyen , et al. · 2022

The Coronavirus Disease 2019 (COVID-19) and dengue fever (DF) pandemics both remain to be significant public health concerns in the foreseeable future. Anti-SARS-CoV-2 drugs and vaccines are both indispensable to eliminate the epidemic sit…

Amino-acyl tXNA as inhibitors or amino acid donors in peptide synthesis Open

Lauriane Rietmeyer, I. Li de la Sierra-Gallay, Guy Schepers, Delphine Dorchêne, Laura Iannazzo , et al. · 2022

Xenobiotic nucleic acids (XNAs) offer tremendous potential for synthetic biology, biotechnology, and molecular medicine but their ability to mimic nucleic acids still needs to be explored. Here, to study the ability of XNA oligonucleotides…

O -2-Alkylated Cytosine Acyclic Nucleoside Phosphonamidate Prodrugs Display Pan-Genotype Antiviral Activity against African Swine Fever Virus Open

Leah Goulding, Eleonóra Kiss, Robert Vrancken, Nesya Goris, Min Luo , et al. · 2022

African swine fever virus is a highly contagious hemorrhagic viral disease. Since its transcontinental spread to Georgia in 2007, ASFV has continued to spread across the globe into countries previously without infection.

A two-residue nascent-strand steric gate controls synthesis of 2′-O-methyl- and 2′-O-(2-methoxyethyl)-RNA Open

Niklas Freund, Alexander I. Taylor, Sebastian Arangundy‐Franklin, Nithya Subramanian, Sew‐Yeu Peak‐Chew , et al. · 2022

Crystallographic analysis of engineered polymerases synthesizing phosphonomethylthreosyl nucleic acid Open

Mohammad Hajjar, Nicholas Chim, Chao Liu, Piet Herdewijn, John C. Chaput · 2022

Xeno-nucleic acids (XNAs) are synthetic genetic polymers with backbone structures composed of non-ribose or non-deoxyribose sugars. Phosphonomethylthreosyl nucleic acid (pTNA), a type of XNA that does not base pair with DNA or RNA, has bee…

Cryo-EM structures of wild-type and E138K/M184I mutant HIV-1 RT/DNA complexed with inhibitors doravirine and rilpivirine Open

Abhimanyu K. Singh, Brent De Wijngaert, Marc Bijnens, Kris Uyttersprot, Hoai Viet Nguyen , et al. · 2022

Structures trapping a variety of functional and conformational states of HIV-1 reverse transcriptase (RT) have been determined by X-ray crystallography. These structures have played important roles in explaining the mechanisms of catalysis…

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