Radek Pohl

• The Czech Academy of Sciences

Galectins are a family of galactoside‐binding proteins involved in various pathophysiological processes, which makes them attractive targets for drug discovery. The derivatization of d‐galactose at C3 and C1 positions has been shown to increase the affinity of synthetic galectin antagonists. In this study, two small libraries of d‐galactose derivat...

The use of quantum mechanical potentials in protein-ligand affinity prediction is becoming increasingly feasible with growing computational power. To move forward, validation of such potentials on real-world challenges is necessary. To this end, we have collated an extensive set of over a thousand galectin inhibitors with known affinities and docke...

Protein-RNA interactions play important biological roles and hence reactive RNA probes for cross-linking with proteins are important tools in their identification and study. To this end, we designed and synthesized 5′-O-triphosphates bearing a reactive squaramate group attached to position 5 of cytidine or position 7 of 7-deazaadenosine and used th...

DNA modifications on pyrimidine nucleobases play diverse roles in biology such as protection of bacteriophage DNA from enzymatic cleavage, however, their role in the regulation of transcription is underexplored. We have designed and synthesized a series of uracil 2ʹ-deoxyribonucleosides and 5ʹ-O-triphosphates (dNTPs) bearing diverse modifications a...

Linker-Evolved-Group-Optimized-Lipophosphonoxins (LEGO-LPPO) are small synthetic modular peptidomimetics with promising antimicrobial activity. The LEGO-LPPO mechanism of antibacterial action has been determined to be the depolarization and disruption of bacterial membranes. Their modular nature is advantageous for fine tuning their biological prop...

Reactive N‐hydroxy‐9‐azabicyclo[3.3.1]nonane (ABNOH) linked 2′‐deoxyuridine 5′‐O‐mono‐ and triphosphates were synthesized through a CuAAC reaction of ABNOH‐PEG4‐N3 with 5‐ethynyl‐dUMP or ‐dUTP. The modified triphosphate was used as substrate for enzymatic synthesis of modified DNA probes with KOD XL DNA polymerase. The keto‐ABNO radical reacted wit...

We designed and synthesized cytidine 5′-O-triphosphate bearing a reactive squaramate group attached to position 5 of pyrimidine (CESQTP) and used it as substrate for polymerase synthesis of modified RNA. In vitro transcription with T7 RNA polymerase or primer extension using engineered TGK DNA polymerase were used for synthesis of RNA probes bearin...

Inhibition of hypoxanthine–guanine–xanthine phosphoribosyltransferase activity decreases the pool of 6-oxo and 6-amino purine nucleoside monophosphates required for DNA and RNA synthesis, resulting in a reduction in cell growth. Therefore, inhibitors of this enzyme have potential to control infections, caused by Plasmodium falciparum and Plasmodium...

Innovative approaches to controlled nucleobase-modified RNA synthesis are urgently needed to support RNA biology exploration and to synthesize potential RNA therapeutics. Here we present a strategy for enzymatic construction of nucleobase-modified RNA based on primer-dependent engineered thermophilic DNA polymerases – SFM4-3 and TGK. We demonstrate...

The stereoselective reduction of the steroidal 4-ene-3-ketone moiety (enone) affords the 5β-steroid backbone that is a key structural element of biologically important neuroactive steroids. Neurosteroids have been currently studied as novel and potent central nervous system drug-like compounds for the treatment of, e.g., postpartum depression. As a...

Brefeldin A is an important natural product and biochemical tool with cell‐modulating and other diverse biological activities. To explore its chemical space, a generally applicable strategy for total syntheses of naturally occurring (+)‐brefeldin A (BFA), 2‐epi‐BFA, their diastereomers and analogs with varying macrocyclic ring size is reported. The...

Direct N-acylation of 1,2,3-NH-triazoles aimed at obtaining elusive N-acyl-1,2,3-triazoles was investigated. A preference for the formation of thermodynamically favoured N2 isomers was established and an influence of the character of...

A series of 2'-deoxyribonucleoside triphosphates (dNTPs) bearing 2- or 4-linked trans-cyclooctene (TCO) or bicyclononyne (BCN) tethered through a shorter propargylcarbamate or longer triethyleneglycol-based spacer were designed and synthesized. They were found to be good substrates for KOD XL DNA polymerase for primer extension enzymatic synthesis...

We designed and synthesized a series of 2'-deoxyribonucleoside triphosphates (dNTPs) bearing various lipid moieties. Fatty acid- and cholesterol-modified dNTPs proved to be substrates for KOD XL DNA polymerase in primer extension reactions. They were also mutually compatible for simultaneous multiple incorporations into the DNA strand. The methodol...

Direct N-acylation of 1,2,3-NH-triazoles aimed at obtaining elusive N-acyl-1,2,3-triazoles was investigated. A preference for the formation of thermodynamically favoured N2 isomers was established and an influence of the hard/soft character of the electrophile on the regioselectivity of acylation was found. Although N-acylated 1,2,3-triazoles are h...

Nucleosides and 2'-deoxyribonucleoside triphosphates (dNTPs) bearing 3,3'-dimethoxy-2,2'-diphenyl-6-(4-hydroxyphenyl)-bodipy fluorophore attached through a propargyl or propargyl-triethylene glycol linker to position 5 of 2'-deoxycytidine were designed and synthesized. They exerted bright red fluorescence and good sensitivity to viscosity changing...

We designed and synthesized a series of 2’-deoxyribonucleoside triphosphates (dNTPs) bearing various lipid moieties. Fatty acid- and cholesterol-modified dNTPs proved to be substrates for KOD XL DNA polymerase in primer extension reactions. They were also mutually compatible for simultaneous multiple incorporations into the DNA strand. The methodol...

Fully aromatic helicenes are attractive building blocks for the construction of inherently chiral π-conjugated macrocyclic nanocarbons. These hitherto rare molecular architectures are envisaged to exhibit remarkable (chir)optical properties, self-assembly, charge/spin...

The asymmetric synthesis of optically pure and conformationally locked oxabenzo[5]helicenes bearing pyridin-2-yl or isoquinolin-3-yl substituents and their transformation into the corresponding cycloiridated organometallics are described. These helically chiral Cp*IrIII(X)C,N-complexes (X = Cl, I) also contain a configurationally unstable pseudotet...

The alarming rise of bacterial antibiotic resistance requires the development of new compounds. Such compounds, lipophosphonoxins (LPPOs), were previously reported to be active against numerous bacterial species, but serum albumins abolished their activity. Here we describe the synthesis and evaluation of novel antibacterial compounds termed LEGO-L...

Modification of the carbohydrate scaffold is an important theme in drug and vaccine discovery. Therefore, the preparation of novel types of glycomimetics is of interest in synthetic carbohydrate chemistry. In this manuscript, we present an early investigation of the synthesis, structure, and conformational behaviour of (1→1)-Si-disaccharides as a n...

Homologues of natural epigenetic pyrimidine nucleosides and nucleotides were designed and synthesized. They included 5-ethyl-, 5-propyl-, 5-(1-hydroxyethyl)-, 5-(1-hydroxypropyl)- and 5-acetyl- and 5-propionylcytosine and -uracil 2'-deoxyribonucleosides and their corresponding 5'-O-triphosphates (dNXTPs). The epimers of 5-(1-hydroxyethyl)- and 5-(1...

Determining the structure of saccharides in their native environment is crucial to understanding their function and more accurately targeting their utilization. Nuclear magnetic resonance observables such as the nuclear Overhauser effect or spin-spin coupling constants are routinely utilized to study saccharides in their native water environment. H...

5‐(β‐d‐Glucopyranosyloxymethyl)‐2’‐deoxyuridine and ‐cytidine 5’‐O‐triphosphates were prepared and used for polymerase‐mediated (primer extension or PCR) synthesis of DNA containing glucosylated 5‐hydroxymethyluracil (5hmU) or 5‐hydroxymethyluracil (5hmC). The presence of any glucosylated pyrimidines fully protected DNA from cleavage by type II res...

Objective Classical ATP-independent non-shivering thermogenesis enabled by uncoupling protein 1 (UCP1) in brown adipose tissue (BAT) is activated, but not essential for survival, in the cold. It has long been suspected that futile ATP-consuming substrate cycles also contribute to thermogenesis and can partially compensate for the genetic ablation o...

Glyoxal‐linked 2’‐deoxyuridine 5’‐O‐mono‐ and triphosphates were synthesized through a CuAAC click reaction of 4‐azidophenylglyoxal or a Sonogashira reaction of 4‐bromophenylglyoxal with 5‐ethynyl‐dUMP or ‐dUTP. The triphosphates were used as substrates for enzymatic synthesis of modified DNA probes with KOD XL DNA polymerase. The glyoxal‐linked nu...

The conformational changes in a sugar moiety along the hydrolytic pathway are key to understand the mechanism of glycoside hydrolases (GHs) and to design new inhibitors. The two predominant itineraries for mannosidases go via OS2→B2,5→¹S5 and ³S1→³H4→¹C4. For the CAZy family 92, the conformational itinerary was unknown. Published complexes of Bacte...

Pentasubstituted pyrrolidines are ubiquitous constituents of natural products and drugs, however the access options to them especially with respect to absolute and relative stereochemistry are not well developed. We report an asymmetric synthesis of N,2,3,4,5‐pentasubstituted pyrrolidines by oxidative single‐electron transfer‐catalyzed tandem aza‐M...

The conformational changes in a sugar moiety along the hydrolytic pathway are key to understand the mechanism of glycoside hydrolases (GHs) and to design new inhibitors. The two predominant itineraries for mannosidases go via OS2  B2,5  1S5 and 3S  3H4  1C4. For the CAZy family 92, the conformational itinerary was unknown. Published complexes o...

We designed and synthesized nucleosides bearing aminophenyl- or aminonaphthyl-3-methoxychromone fluorophores attached at position 5 of cytosine or thymine and converted them to nucleoside triphosphates. The fluorophores showed solvatochromic fluorescence with strong fluorescence at 433-457 nm in non-polar solvents and very weak fluorescence at 567...

The stereoselective Suzuki–Miyaura cross-coupling of ( Z )-β-enamido triflates is demonstrated. Depending on the nature of the ligand in the palladium catalyst, either retention or inversion of the configuration during the synthesis of β,β-diaryl-substituted enamides is observed. Thus, the method provides synthetic access to both isomers of the tar...

Visions of applying unique helically chiral π-electron systems in diverse areas of chemistry and physics have fuelled the intensifying research aiming at the development of a practical and general methodology for the preparation of functionalised helicenes and their heteroanalogues. [1] Despite the fact, that significant progress has recently been...

Following the conformational pathway of a sugar molecule along its enzymatic hydrolysis is key to understand the mechanism of glycoside hydrolases (GHs) and to design new inhibitors. The expected itineraries for mannosidases go through O S 2  B 2,5  1 S 5 and 3 S 1  3 H 4  1 C 4. For CAZy family 92, the conformational itinerary was puzzling. Pu...

DNA-binding fluorescent probes are useful tools in cell biology for various applications enabling visualisation and quantification of DNA. Herein, we report on HeliDye1 , a novel cationic helicene-like DNA probe, and its versatile usability. HeliDye1 exhibits fluorescence exclusively in the presence of DNA duplexes containing AT base pairs and (con...

DNA-binding fluorescent probes are useful tools in cell biology for various applications enabling visualisation and quantification of DNA. Herein, we report on HeliDye1 , a novel cationic helicene-like DNA probe, and its versatile usability. HeliDye1 exhibits fluorescence exclusively in the presence of DNA duplexes containing AT base pairs and (con...

Linear or branched 1,3‐diketone‐linked thymidine 5′‐O‐mono‐ and triphosphate were synthesized through CuAAC click reaction of diketone‐alkynes with 5‐azidomethyl‐dUMP or ‐dUTP. The triphosphates were good substrates for KOD XL DNA polymerase in primer extension synthesis of modified DNA. The nucleotide bearing linear 3,5‐dioxohexyl group (HDO) effi...

“This work represents another step in the effort to use glycals (1,2‐unsaturated derivatives of carbohydrates) as donor synthons for transition metal‐catalyzed arylation reactions. We have employed a novel 1‐silyl derivative of d‐glucal, which was obtained as a bench‐stable solid and could therefore be used conveniently.” Read more about the story...

DOI: https://doi.org/10.1002/chem.202101994

Access to unprotected (hetero)aryl pseudo‐C‐glucosides via a mild Pd‐catalysed Hiyama cross‐coupling reaction of protecting‐group‐free 1‐diisopropylsilyl‐d‐glucal with various (hetero)aryl halides has been developed. In addition, selected unprotected pseudo‐C‐glucosides were stereoselectively converted into the corresponding α‐ and β‐C‐glucosides,...

Arginine-specific 1,3-diketone-linked reactive nucleotides are reported for the enzymatic construction of DNA probes and cross-linking with peptides and proteins. Abstract Linear or branched 1,3-diketone-linked thymidine 5′-O-mono- and triphosphate were synthesized through CuAAC click reaction of diketone-alkynes with 5-azidomethyl-dUMP or -dUTP....

Phytoglandins from the reaction flask enable their identification in Nature. Hypothetical plant‐based prostaglandin analogs were obtained by a 15‐step asymmetric total synthesis. They were applied as an analytical standard in a detailed LC‐MS/MS study confirming phytoglandin formation in autoxidized linolenic acid and in various edible vegetable oi...

RelA-SpoT Homolog (RSH) enzymes control bacterial physiology through synthesis and degradation of the nucleotide alarmone (p)ppGpp. We recently discovered multiple families of small alarmone synthetase (SAS) RSH acting as toxins of toxin-antitoxin (TA) modules, with the FaRel subfamily of toxSAS abrogating bacterial growth by producing an analog of...

A silyl hydride derivative of d‐glucal was used conveniently as a bench‐stable precursor for the construction of C‐glycosidic bond. After activation by fluoride‐mediated dehydrogenative hydrolysis, an intermediate silanol species was used for Hiyama arylation. Various aryl and heteroaryl C‐glycosides, C‐glycopeptides, as well as both a‐ and b‐isome...

Phytoprostanes (PhytoP) are natural products, which form in plants under oxidative stress conditions from α‐linolenic acid. However, their epimers with relative prostaglandin configuration termed phytoglandins (PhytoG) have never been detected in Nature, likely because of the lack of synthetic reference material. Here, the first asymmetric total sy...

We report a series of 2'-deoxyribonucleoside triphosphates bearing dicarba-nido-undecaborate ([C2B9H11]1-), [3,3'-iron-bis(1,2-dicarbollide)]- (FESAN, [Fe(C2B9H11)2]2-) or [3,3'-cobalt-bis(1,2-dicarbollide)]- (COSAN, [Co(C2B9H11)2]2-) groups prepared either through the Sonogashira cross-coupling or the CuAAC click reaction. The modified dN X TPs we...

RelA-SpoT Homolog (RSH) enzymes control bacterial physiology through synthesis and degradation of the nucleotide alarmone (p)ppGpp. We recently discovered multiple families of Small Alarmone Synthetase (SAS) RSH acting as toxins of toxin-antitoxin (TA) modules, with the FaRel subfamily of toxSAS abrogating bacterial growth by producing an analogue...

DOI https://doi.org/10.1021/jacs.1c02222

Helicobacter pylori (Hp) is a human pathogen that lives in the gastric mucosa of approximately 50% of the world's population causing gastritis, peptic ulcers, and gastric cancer. An increase in resistance to current drugs has sparked the search for new Hp drug targets and therapeutics. One target is the disruption of nucleic acid production, which...

Pyrrolidones are common heterocyclic fragments in various biologically active compounds. Here, a two-step radical-based approach to γ-lactams bearing three to four stereocenters starting from epoxides, N -allylic silylacetamides and TEMPO is reported. The sequence starts with a new tandem nucleophilic substitution/Brook rearrangement/single electro...

Trypanosoma brucei parasites cause Human African Trypanosomiasis and the current drugs for its treatment are often inefficient and toxic. This urges the need to development of new antitrypanosomal agents. We report the synthesis and biological profiling of 3'-deoxy-3'-fluororibonucleosides derived from 7-deazaadenine nucleosides bearing diverse sub...

In analogy to antiviral acyclic nucleoside phosphonates, a series of 5-amino-3-oxo-1,2,4-thiadiazol-3(2H)-ones bearing a 2-phosphonomethoxyethyl (PME) or 3-hydroxy-2-(phosphonomethoxy)propyl (HPMP) group at the position 2 of the heterocyclic moiety has been synthesized. Diisopropyl esters of PME- and HPMP-amines have been converted to the N-substit...

A series of 7-deazaadenine ribonucleosides bearing alkyl, alkenyl, alkynyl, aryl, or hetaryl groups at position 7 as well as their 5′-O-triphosphates and two types of monophosphate prodrugs (phosphoramidates and S-acylthioethanol esters) were prepared and tested for antiviral activity against selected RNA viruses (Dengue, Zika, tick-borne encephali...

Long-chain n-3 polyunsaturated fatty acids (Omega-3) and anti-diabetic drugs thiazolidinediones (TZDs) exhibit additive effects in counteraction of dietary obesity and associated metabolic dysfunctions in mice. The underlying mechanisms need to be clarified. Here, we aimed to learn whether the futile cycle based on the hydrolysis of triacylglycerol...

Multi-orthogonal molecular scaffolds can be applied as core structures of bioactive compounds. Here, we prepared four tri-orthogonal scaffolds based on adamantane or proline skeletons. The scaffolds were used for the solid-phase synthesis of model insulin mimetics bearing two different peptides on the scaffolds. We found that adamantane-derived com...

5-Hydroxymethylcytosine and uracil are epigenetic nucleobases, but their biological roles are still unclear. We present the synthesis of 2-nitrobenzyl photocaged 5-hydroxymethyl-2′-deoxycytidine and uridine 3′-O-phosphoramidites and their use in automated solid-phase synthesis of oligonucleotides (ONs) modified at specific positions. The ONs were u...

A set of modified 2-deoxyribonucleoside triphos-phates (dNTPs) bearing a linear or branched alkane, indole or phenyl group linked through ethynyl or alkyl spacer were synthesized and used as sub-strates for polymerase synthesis of hypermodified DNA by primer extension (PEX). Using the alkyl-linked dNTPs, the polymerase synthesized up to 22-mer full...

Two isomeric sets of 4-substituted pyridopyrrolopyrimidine nucleobases were prepared through nucleophilic substitutions or cross-coupling reactions of 4-chloropyridopyrrolopyrimidines. The corresponding 4-amino-pyridopyrrolopyrimidines were glycosylated with 5-O-tritylribose using the modified Mitsunobu protocol. Several examples of the title heter...

Hemochromatosis (iron overload) encompasses a group of diseases that are characterized by a toxic hyperaccumulation of iron in parenchymal organs. Currently, only few treatments for this disease have been approved; however, all these treatments possess severe side effects. In this study, a paradigm for hemochromatosis maintenance/preventive therapy...

All four isomeric series of novel 4‐substituted pyrido‐fused 7‐deazapurine ribonucleosides possessing the pyridine nitrogen atom at different positions were designed and synthesized. The total synthesis of each isomeric fused heterocycle through multistep heterocyclization was followed by glycosylation and derivatization at position 4 by cross‐coup...

Bis(benzothienyl)ethene sulfones are very interesting molecules for super‐resolution microscopy due to their photoswitching properties. However, functionalization of the ‘classical’ bis(benzothienyl)ethene sulfones with a five‐membered central ring leads to significant decrease of quantum yields of photoconversion of the fluorescent closed form of...

Invited for this month's cover are the synthetic and physical chemistry groups of Paul E. Reyes‐Gutiérrez and Lubomír Pospíšil from the Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, J. Heyrovský Institute of Physical Chemistry of the Czech Academy of Sciences, and Charles University. The cover picture shows azoni...

The Front Cover shows how helquat molecules (shown as solar panels) can be used as organocatalysts in the Povarov reaction. The background combines historical monuments of Prague and the new research centre of the Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, while the yellow plants represent alternative fuels. https:...

The Front Cover shows how helquat molecules (shown as solar panels) can be used as organocatalysts in the Povarov reaction. The background combines historical monuments of Prague and the new research centre of the Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, while the yellow plants represent alternative fuels. More in...

A novel labeled nucleotide exerts very low near‐IR fluorescence in water but lights‐up (up to a 348‐fold increase) after polymerase incorporation to DNA. It can be used to directly visualize enzymatic DNA synthesis in vitro and the labeled DNA probes are also responsive to secondary structure changes or interactions with small molecules or proteins...

Thymidine triphosphate bearing benzylidene‐tetrahydroxanthylium near‐IR fluorophore linked to the 5‐methyl group via triazole was synthesized through the CuAAC reaction and was used for polymerase synthesis of labelled DNA probes. The fluorophore lights up upon incorporation to DNA (up to 348‐times) presumably due to interactions in major groove an...

Fluorescent labelling of nucleic acids is a valuable tool with widespread usage in molecular and cellular biology as well as diagnostics. The team of researchers led by Michal Hocek from IOCB Prague have synthesized a novel thymidine triphosphate substituted with a fluorophore, which only very weakly emits in the near-infrared spectrum. However, af...

A straightforward and scalable method for the synthesis of protected 2-hydroxyglycals is described. The approach is based on the chlorination of carbohydrate-derived hemiacetals, followed by an elimination reaction to establish the glycal moiety. 1,2-dehydrochlorination reactions were studied on a range of glycosyl chlorides to provide suitable rea...

Hot water extract from biomass of heterotrophic mutant green alga Parachlorella kessleri HY1 (Chlorellaceae) was deproteinised, and three polysaccharidic fractions were obtained by preparative chromatography. The low-molecular fraction (1.5 × 104g mol−1) was defined mainly as branched O-2-β-xylo-(1→3)-β-galactofuranan where xylose is partially meth...

Two isomeric series of benzothieno-fused 7-deazapurine (benzo[4',5']thieno[3',2':4,5]- and benzo[4',5']thieno[2',3':4,5]pyrrolo[2,3-d]pyrimidine) ribonucleosides were designed and synthesized. Key steps of the synthesis included the Negishi coupling of zincated dichloropyrimidine with 2- or 3-iodobenzothiophene followed by azidation, thermal or pho...

Helquats (HQs) are structurally linked to helicenes and viologens, and they represent an attractive field of research in chemistry and medicinal chemistry. In the present work they were used as catalysts for the synthesis of 1,2,3,4‐tetrahydroquinolines in good yields by the Povarov reaction. The substrate scope and the capability of different helq...

Merging rearrangement with radical reactions is a largely unexplored field but may hold promise for approaching scaffolds that are inaccessible by other methodology. Here a tandem nucleophilic substitution/Brook rearrangement/single‐electron transfer oxidation/radical oxygenation strategy is presented, through which α,γ‐dioxygenated ε,ζ‐unsaturated...

Tandem anionic oxy‐Cope rearrangement/radical oxygenation reactions provide δ,ϵ‐unsaturated α‐(aminoxy) carbonyl compounds, which serve as convenient precursors to diverse compound classes. Functionalized carbocycles are accessible by very rare all‐carbon 5‐endo‐trig cyclizations, but also common 5‐exo‐trig radical cyclizations, based on the persis...

Achterbahnfahrt zu Cyclopentanen: Neuartige Tandemreaktionen aus anionischer Oxy-Cope-Umlagerung und Radikal- α-Oxygenierung ergeben δ,ϵ-ungesättigte α-(Aminoxy)carbonylverbindungen. Diese Verbindungen sind geeignete Vorstufen für auf dem persistenten Radikaleffekt basierende, sehr seltene 5-endo-trig und andere radikalische Cyclisierungen. Abstra...

Three sets of 7‐deazaadenine and cytosine nucleosides and nucleoside triphosphates bearing either unsubstituted ferrocene, octamethylferrocene and ferrocenecarboxamide linked through an alkyne tether to position 7 or 5, respectively, were designed and synthesized. The modified dNFcXTPs were good substrates for KOD XL DNA polymerase in primer extens...

Cytosine 2'-deoxyribonucleoside dCTBdp and its triphosphate (dCTBdpTP) bearing tetramethylated thiophene-bodipy fluorophore attached at position 5 were designed and synthesized. The green fluorescent nucleoside dCTBdp showed a perfect dependence of fluorescence lifetime on the viscosity. The modified triphosphate dCTBdpTP was substrate to several D...

Substituted ferrocene derivatives with tuned redox potentials were tested as redox labels for electrochemical detection and coding of nucleobases in DNA. The ferrocene‐linked nucleotides were enzymatically incorporated to DNA and analyzed by using capture probes on gold electrodes. Ferrocenecarboxamide and ethynylferrocene were used as tags for ort...

Substituted ferrocene derivatives with tuned redox potentials were tested as redox labels for electrochemical detection and coding of nucleobases in DNA. The ferrocene‐linked nucleotides were enzymatically incorporated to DNA and analyzed by using capture probes on gold electrodes. Ferrocenecarboxamide and ethynylferrocene were used as tags for ort...

Hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT) is a recognized target for antimalarial chemotherapeutics. It synthesises all of the 6-oxopurine nucleoside monophosphates, IMP, GMP and XMP needed by the malarial parasite, Plasmodium falciparum (Pf). PfHGXPRT is also indirectly responsible for the synthesis of the adenosine monophos...

Squaramate‐linked 2′‐deoxycytidine 5′‐O‐triphosphate was synthesized and found to be good substrate for KOD XL DNA polymerase in primer extension or PCR synthesis of modified DNA. The resulting squaramate‐linked DNA reacts with primary amines to form a stable diamide linkage. This reaction was used for bioconjugations of DNA with Cy5 and Lys‐contai...