ArtikelIntegrating Ligands into Nucleic Acid Systemsvon Yang Wang et al. · 15.09.2023 Recent advances of a novel and efficient ligand-oligonucleotide transduction platform functioned through a kinetic control upon the ligand binding are summarized and discussed in this Concept. This new strategy may provide great flexibility to integ...
ArtikelDevelopment of On‐DNA Cyclic Imide Synthesis for DNA Encoded Library Constructionvon Lijun Xue et al. · 15.09.2023 On-DNA synthesis of cyclic imides was developed. The transformation was achieved under mild conditions with high conversions and a broad functional group tolerance, suitable for DEL synthesis. The mechanism study of off-DNA and on-DNA chemical trans...
ArtikelCharacterization of an Unusual α‐Oxoamine Synthase Off‐Loading Domain from a Cyanobacterial Type I Fatty Acid Synthasevon Andrei Ogonkov et al. · 15.09.2023 Fatty acid synthase (FAS) usually releases its products by hydrolysis or transesterification. Here, an α-oxoamine synthase off-loading domain is identified in a cyanobacterial type I FAS. This domain releases the fatty acyl chain by condensing it wi...
ArtikelDesign, Synthesis, and Biological Evaluation of New Urushiol Derivatives as Potent Class I Histone Deacetylase Inhibitorsvon Hao Zhou et al. · 15.09.2023 A novel series of 11 urushiol-based hydroxamic acid histone deacetylase (HDAC) inhibitors was designed, synthesized, and biologically evaluated. Compounds 1, 2, 3, 4, and 5 showed potent HDAC1/2/3/8 inhibitory activity. Western blot analysis validat...
ArtikelApplication of a Synthetic Ferredoxin‐Inspired [4Fe4S]‐Peptide Maquette as the Redox Partner for an [FeFe]‐Hydrogenasevon Andrea Bombana et al. · 15.09.2023 [4Fe4S]-peptide maquettes have been explored as effective models of FeS proteins, but they also hold untapped potential as tools for synthetic biology. Here we demonstrate the application of these maquettes beyond the modelling of electron transfer ...
ArtikelPeptide Amphiphilic Supramolecular Nanogels: Competent Host for Notably Efficient Lipase‐Catalyzed Hydrolysis of Water‐Insoluble Substratesvon Sudeshna Pal et al. · 15.09.2023 Supramolecular self-assembled nanogels in water have been developed from peptide amphiphile hydrogelators. The micro-heterogenous surface of the nanogels was judiciously utilized to catalyze the hydrolysis of water-insoluble substrates like p-nitrop...
ArtikelNordihydroguaiaretic Acid (NDGA) Inhibits CsgA Polymerization, Bacterial Amyloid Biogenesis, and Biofilm Formationvon Joshua A. et al. · 15.09.2023 The natural product nordihydroguaiaretic acid (NDGA) found in the creosote bush is a curlicide. NDGA inhibits in vitro polymerization of the bacterial amyloid protein CsgA and inhibits cellular amyloid biogenesis in E. coli. NDGA's curlicide activit...
ArtikelStable Binding of Full‐Length Chemerin Is Driven by Negative Charges in the CMKLR1 N Terminusvon Kevin Kretschmer et al. · 15.09.2023 The chemerin system is a key player in inflammatory diseases. The N terminus of the receptor CMKLR1 is crucial for high affinity ligand binding. A two-step binding mode is suggested. First, the C terminus binds deep in the transmembrane domain of th...
ArtikelSubstance P‐Derived Extracellular‐Matrix‐Mimicking Peptide Hydrogel as a Cytocompatible Biomaterial Platformvon Nabanita Mukherjee et al. · 15.09.2023 Motivated by the highly conserved C terminus of substance P neuropeptide, we designed and synthesized a novel peptide sequence Fmoc−FFGLMRGD comprising the C-terminal fragment “FFGLM” from substance P with an integrin-interacting RGD motif. This des...
ArtikelSerum‐Based Detection of Liver Pathology Using a Fluorogenic Alkaline Phosphatase Probevon Tijian Zhou et al. · 15.09.2023 We have developed an ALP-activatable NIR fluorescent probe DCM-2F-HP with optimal pKa for the accurate detection of human serum ALP, especially in distinguishing ALP patients from healthy volunteers, as well as assessing the progress of liver diseas...
ArtikelA Fluorescence‐Based Assay for N5‐Carboxyaminoimidazole Ribonucleotide Mutasevon Marcella F. et al. · 15.09.2023 A robust, fluorescence-based assay has been developed that relies on the reaction between the novel istain-fluorecein conjugate and the enzymatically generated compound, AIR. These compounds react non-enzymatically resulting in a highly fluorescent ...
ArtikelTrifunctional Dibromomaleimide Reagents Built Around A Lysine Scaffold Deliver Site‐selective Dual‐modality Antibody Conjugationvon Yanbo Zhao et al. · 15.09.2023 We demonstrate a rapid reduction-bridging-double click sequence to yield dual-modality antibody conjugates using aryl selenols as novel disulfide reducing reagents and trifunctional dibromomaleimides (DBMs) as bridging reagents. This work will provi...
ArtikelSelective and Sustainable Production of Sub‐terminal Hydroxy Fatty Acids by a Self‐Sufficient CYP102 Enzyme from Bacillus Amyloliquefaciensvon Li Zong et al. · 15.09.2023 BAMF0695, a self-sufficient CYP102 enzyme, hydroxylates sub-terminal positions of fatty acids with broad temperature optimum and high thermostability. Mutants of BAMF0695 exhibit very high regioselectivity, generating a single hydroxy fatty acid reg...
ArtikelLipase‐Mediated Conversion of Protecting Group Silyl Ethers: An Unspecific Side Reactionvon Lisa M. et al. · 15.09.2023 Silyl ethers are important protecting groups in organic synthesis and a selective cleavage or formation is highly desirable. The ability of lipases to catalyze the reactions has long been suspected. This study gives experimental and structural evide...
ArtikelFacile Synthesis of Homodimeric Protein Ligandsvon Weijun Gui et al. · 15.09.2023 Bivalent ligands can engage homodimeric protein targets with high affinity due to avidity effects. This study shows that compounds conjugated to a masked formyl acetamide can be coupled efficiently and conveniently through trifluoroacetic acid (TFA)...
ArtikelRNA‐TAG Mediated Protein‐RNA Conjugationvon Ember M. et al. · 15.09.2023 Here we present an enzymatic, covalent, protein-nucleic acid conjugation method. This method precisely links two classes of biological macromolecules using SNAP-tag and RNA-TAG labeling technologies and a bifunctional small molecule probe. We demons...
ArtikelFront Cover: Characterization of an Unusual α‐Oxoamine Synthase Off‐Loading Domain from a Cyanobacterial Type I Fatty Acid Synthase (ChemBioChem 18/2023)von Andrei Ogonkov et al. · 15.09.2023 A new fatty acid synthase off-loading domain. Fatty acid synthase (FAS) usually releases its products by hydrolysis or transesterification. Here, an α-oxoamine synthase off-loading domain is identified in a cyanobacterial type I FAS. This domain rel...
ArtikelThe Evolutionary Pattern of Cocaine and Hyoscyamine Biosynthesis Provides Strategies To Produce Tropane Alkaloidsvon Duchesse‐Lacours Zamar et al. · 15.09.2023 Strategies to increase the availability of tropane alkaloids through metabolic engineering. This article highlights the latest advances in the biosynthetic pathway of cocaine, a tropane alkaloid produced by the Erythroxylaceae family and summarizes ...
ArtikelStimuli‐Responsive Prodrug Chemistries for Cancer Therapyvon Rupa Bargakshatriya et al. · 15.09.2023 The development of Stimuli-responsive prodrugs for controlled release of the drugs to tumour tissues and cells while reducing the exposure of drugs in the blood and healthy cells is a highly challenging task. In this review, the design strategies an...
ArtikelIncreasing the Selectivity of Light‐Active Antimicrobial Agents – Or How To Get a Photosensitizer to the Desired Targetvon Michael Grimmeisen et al. · 15.09.2023 Selective targeting of light-active molecules to pathogens is a very attractive approach in modern drug discovery efforts. In this review, we summarize the current developments and highlights of recent literature dealing with the modification of pho...
ArtikelBiotransamination of Furan‐Based Aldehydes with Isopropylamine: Enzyme Screening and pH Influence
ArtikelModulating the RAGE‐Induced Inflammatory Response: Peptoids as RAGE Antagonistsvon Mihyun Lim et al. · 21.09.2023 Peptoids were designed to mimic receptors for advanced glycation end-products (RAGE) ligand amyloid-β (Aβ) and curtail RAGE inflammatory activation. Here, we reveal the nanomolar binding capability of the peptoid-based mimics to RAGE and demonstrate...
ArtikelRapid On‐Resin N‐Formylation of Peptides as One‐Pot Reactionvon Agon Kokollari et al. · 21.09.2023 Fast but not furious. A rapid on-resin N-formylation protocol for peptides was developed using formic acid, acetic anhydride, pyridine, and DMF. This method is simple in execution and provides near quantitative yield independent of peptide length an...
Artikel[Fe]‐Hydrogenase, Cofactor Biosynthesis and Engineeringvon Francisco J. et al. · 21.09.2023 [Fe]-hydrogenase contains the FeGP cofactor as the prosthetic group for activation of H2. HcgA−G are involved in the biosynthesis of the cofactor. Most of the biosynthesis reactions were elucidated by structure-to-function analysis and in vitro bios...
ArtikelRecent advances in chemical synthesis of structural domains of lipopolysaccharides from the commensal gut‐associated microbiota
ArtikelImproving the Enantioselectivity of CHMO Brevi1 for Asymmetric Synthesis of Podophyllotoxin Precursor
ArtikelAccess to High‐Purity 7mG‐cap RNA in Substantial Quantities by a Convenient All‐Chemical Solid‐Phase Methodvon Mathieu Noël et al. · 20.09.2023 A practical and valuable all-chemical method has been developed to synthesize 5’-7mGppp RNA on solid-support without damaging the 7mG-cap or the RNA during RNA deprotection and release from the support under mild basic conditions. Substantial quanti...
ArtikelTerpenoids as Human Neutrophil Elastase (HNE) Inhibitors: A Comprehensive Review of Natural Anti‐inflammatory Isoprenoidsvon Muhammad Imran et al. · 20.09.2023 The information on the potential therapeutic effects of terpenoids reviewed here should help to guide researchers in the development of safer and more effective drugs derived from natural terpenoid compounds for managing inflammatory problems. Abs...
ArtikelThe conversion of UDP‐Glc to UDP‐Man: In Silico and Biochemical Exploration to Improve the Catalytic Efficiency of CDP‐Tyvelose C2‐Epimerases
ArtikelPhenolic Substitution in Fidaxomicin: A Semisynthetic Approach to Antibiotic Activity Across Species
ArtikelFunctionalized fluorescent organic nanoparticles based AIE enabling effectively targeting cancer cell imaging
ArtikelChemical Probes for Profiling of MALT1 Protease Activityvon Steven H. et al. · 15.09.2023 MALT1 is a cysteine protease and the only human paracaspase. It is implicated in various human diseases. Here, an overview of the currently available molecular tools is given. Furthermore, their application and future possibilities are discussed. We...
ArtikelCurrent State‐of‐the‐Art Toward Chemoenzymatic Synthesis of Polyketide Natural Productsvon Thaddeus Q. et al. · 15.09.2023 Polyketides represent an area of significant interest for drug discovery efforts. Leveraging a combination of chemical synthesis and enzymology, researchers have routinely demonstrated that the best of both strategies are conferred and result in imp...
ArtikelHypoxia Modulates Cellular Endocytic Pathways and Organelles with Enhanced Cell Migration and 3D Cell Invasion von Hema A. et al. · 15.09.2023 Hypoxia in tumors alters cellular processes, affecting cancer cell behavior. Cobalt chloride-induced hypoxia reduced proliferation but increased migration and invasion in cancer cells. Short hypoxia increased galectin3 endocytosis, but prolonged hyp...
Artikel4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteasesvon Jian Yang et al. · 15.09.2023 Rhomboid proteases are serine proteases that reside inside the lipid bilayer of a membrane. They are implicated in several diseases. We here report 4-oxo-β-lactam as a new scaffold for covalent rhomboid inhibitors and activity-based probes. Abstra...
ArtikelExtended Biocatalytic Halogenation Cascades Involving a Single‐Polypeptide Regeneration System for Diffusible FADH2von Nicolai Montua et al. · 15.09.2023 We constructed a bifunctional fusion protein for FADH2 regeneration and successfully coexpressed it with different flavin-dependent halogenases, as well as a dioxygenase that converts 6-chlorotryptophan to 4-Cl-Kynurenine. The figure is a still life...
ArtikelComputation‐Based Design of Salt Bridges in PETase for Enhanced Thermostability and Performance for PET Degradationvon Zhi Qu et al. · 13.09.2023 Amino acid residues with opposite charges were introduced into the flexible region of IsPETase using a computation-based salt bridge design strategy. The mutation sites formed a salt bridge or salt bridge network to improve the thermal stability of ...
ArtikelTerpene Synthases in the Biosynthesis of Drimane‐Type Sesquiterpenes across Diverse Organismsvon Tzu‐Ho Chen et al. · 13.09.2023 Drimane-type sesquiterpenes (DTSs) are bioactive natural products found in various organisms. We review the discovery of DTS synthases and the tailoring enzymes generating the chemical diversity. The catalytic motifs, domain functions and underlying...
ArtikelA Cell‐Free Multi‐enzyme Cascade Reaction for the Synthesis of CDP‐Glycerolvon E. Alberto et al. · 13.09.2023 A multi-enzyme cascade for the cell-free, one-pot synthesis of CDP-glycerol has been developed. Through a design-of-experiments approach, the yield of the cascade was increased from 10 to 89 % with respect to cytidine as a substrate. The final produ...
ArtikelSynthesis and Evaluation of Cereblon‐Recruiting HaloPROTACsvon Britton K. et al. · 13.09.2023 A bifunctional HaloPROTAC ligand was developed to recruit the CRBN E3 ubiquitin ligase to degrade target proteins fused with a HaloTag in the cell. The CRBN-recruiting HaloPROTAC can expand the use of the HaloPROTAC system for screening the degradat...
ArtikelEffects of Replacing a Central Glycine Residue in GLP‐1 on Receptor Affinity and Signaling Profilevon Kyle A. et al. · 13.09.2023 The receptor activated by GLP-1 is a target for drugs that treat type 2 diabetes and obesity. Since glycine has a low α-helix propensity, and Gly22 of GLP-1 does not contact the receptor, we replaced Gly22 with residues that have a higher or lower h...
ArtikelMolecular Highway Patrol for Ribosome Collisionsvon Kaushik Viswanathan et al. · 13.09.2023 Car crashes on highways require responses like rescuing victims, deviating traffic, towing away damaged vehicles, and sometimes even blocking a road. Similarly, during translation, ribosomes can collide into each other with potentially dangerous out...
ArtikelSynthesis of Short Peptides with Perfluoroalkyl Side Chains and Evaluation of Their Cellular Uptake Efficiencyvon Koji Kadota et al. · 13.09.2023 We have synthesized perfluoroalkyl-containing amino acids (RF-AA) and demonstrated that tripeptides composed of the RF-AA have high cellular uptake efficiency. Furthermore, the absolute configuration of RF-AA affected the uptake efficiency due to th...
ArtikelA „Magic Mushroom“ Multi‐Product Sesquiterpene Synthasevon Eike Schäfer et al. · 12.09.2023 Shrooms going terpenoid: The sesquiterpene synthase CubA of the “magic mushroom” Psilocybe cubensis was identified as a multi-functional enzyme producing cubebol, β-copaene, and various other mono-, bi-, and tricyclic sesquiterpenes or -terpenoids. ...
ArtikelGeneration of cannabigerolic acid derivatives and their precursors using the promiscuity of the aromatic prenyltransferase NphB
ArtikelLigand‐Independent Activation of Aryl Hydrocarbon Receptor and Attenuation of Glutamine Levels by Natural Deep Eutectic Solventvon Amina Anaise et al. · 08.09.2023 A natural deep eutectic solvent, CAGE, derived from choline and geranic acid, perturb the metabolome, proteome, and transcriptome of human cell line. Specifically, CAGE upregulated 4-hydroxyphenyllactic acid and indole-3-lactic acid to activate the ...
Artikel[4.3.1]Bicyclic FKBP Ligands Inhibit Legionella Pneumophila Infection by LpMip‐Dependent and LpMip‐Independent Mechanisms von Robin C. et al. · 08.09.2023 In a screening of over 1000 FKBP-inhibitors [4.3.1]-bicyclic sulfonamides turned out to be the preferred binding scaffold for LpMip, a virulence factor of Legionella pneumophila. Although selected [4.3.1]-bicyclic sulfonamides showed anti-infective ...
ArtikelDual‐Responsive Drug‐Delivery System Based on PEG‐Functionalized Pillararenes Containing Disulfide and Amido Bonds for Cancer Theranosticsvon Jiachen Xia et al. · 08.09.2023 A novel drug-delivery system with a dual response to GSH and enzymes is based on the newly designed PEG-functionalized pillararene for efficient and rapid drug release, and cancer therapy. Abstract The construction of a smart drug-delivery system ...
ArtikelGarcinolic Acid Distinguishes Between GACKIX Domains and Modulates Interaction Networksvon Meghan E. et al. · 07.09.2023 Garcinolic acid is a topologically complex natural product derived from Garcinia hanburyi. It engages the KIX domain in the master coactivator CBP/p300 selectively over other closely related motifs and in doing so disrupts CBP/p300 KIX protein-prote...
ArtikelCaulobacter segnis Dioxygenase CsO2: A Practical Biocatalyst for Stilbenoid Ozonolysisvon Valerio De et al. · 07.09.2023 The Caulobacter segnis dioxygenase has been employed for the enzymatic alkene cleavage of several stilbenoids, thus generating the corresponding aldehydes. CsO2-mediated ozonolysis represents a greener, safer, and more selective process with respect...
ArtikelStructural Description of Chiral E‐Tiling DNA Nanotubes with the Chiral Indices (n,m) and Handedness Defined by Microscopic Imagingvon Feiyang Feng et al. · 07.09.2023 The chiral index theory, widely used in carbon nanotubes, has been introduced to describe the chiral structures of E-tiling DNA nanotubes precisely. In particular, we define a general equation of tube curvature with a clear physical picture by modif...
ArtikelBiotechnology in India ‐ An Analysis of Biotechnology Industry Research Assistance Council (BIRAC)‐Supported Projects
ArtikelThe Antimicrobial Properties of PdII− and RuII−pyta Complexes von Annick Niekerk et al. · 05.09.2023 New metalloantibiotics: With the rise and spread of multidrug-resistant fungal pathogens, new drugs are urgently needed. In this work, new ruthenium- and palladium-based compounds with promising antifungal properties are reported. Abstract Infecti...
ArtikelThe Role of Trp79 in β‐Actin on Histidine Methyltransferase SETD3 Catalysisvon Mays S. et al. · 05.09.2023 Second site: A distant Trp79 binding site modulates the histidine methyltransferase SETD3-catalysed methylation of His73 in β-actin. Our findings have implications for the identification of new substrates and chemical probes of biomedically importan...
ArtikelThe Scent of Change: Sustainable Fragrances Through Industrial Biotechnologyvon Freideriki Michailidou · 05.09.2023 This review highlights the role of biotechnology and computational methods in sustainable fragrance production, focusing on fermentation, biocatalysis, and genetic engineering. Abstract Current environmental and safety considerations urge innovati...
ArtikelExploring Photoswitchable Binding Interactions with Small‐Molecule‐ and Peptide‐Based Inhibitors of Trypsinvon Kathryn A. et al. · 04.09.2023 Different for different states: Small-molecule- and peptide-based photoswitchable inhibitors of trypsin were investigated to better understand their binding interactions and hence optimise the difference in biological activity between isomeric state...
ArtikelChemo‐Enzymatic Fluorescence Labeling Of Genomic DNA For Simultaneous Detection Of Global 5‐Methylcytosine And 5‐Hydroxymethylcytosine von Sigal Avraham et al. · 04.09.2023 Dual-color global labelling of 5-hydroxymethylcytosine and umCpG by multi-color fluorescent labelling. We apply an engineered methyltransferase enzyme specific for unmodified CpG to incorporate a modified cofactor that binds to a fluorophore by clic...
ArtikelVariation of Clasper Scent Gland Composition of Heliconius Butterflies from a Biodiversity Hotspot
ArtikelHydrogels with Reversible Crosslinks for Improved Localised Stem Cell Retention: A Reviewvon Ken Princen et al. · 29.08.2023 Tissue repair by administering stem cells retained in adaptable hydrogels. Various promising stem cells for tissue repair are discussed, together with the hydrogels that enclose them and interact well with the tissue. Hydrogel–cell fixation is accom...
ArtikelActivity‐Based Protein Profiling in Methicillin‐Resistant Staphylococcus aureus Reveals the Broad Reactivity of a Carmofur‐Derived Probevon Md Jalal et al. · 29.08.2023 Enzyme targets of activity-based probes built on the anti-neoplastic drug and antimicrobial agent carmofur in methicillin-resistant Staphylococcus aureus (MRSA) have been identified. Chemoproteomic profiling revealed a broad reactivity of the probe ...
ArtikelCuII Pyrazolyl‐Benzimidazole Dinuclear Complexes with Remarkable Antioxidant Activityvon Karim Chkirate et al. · 29.08.2023 The novel dinuclear CuII complex [Cu(NO3)(μ-NO3)(L’)]2 , containing an oxidized ligand, shows remarkable antioxidant properties compared to the original ligand and reference compounds. A mechanism is provided. Abstract Three dinuclear coordination...
ArtikelBacterial J‐Domains with C‐Terminal Tags Contact the Substrate Binding Domain of DnaK and Sequester Chaperone Activityvon Brock Nelson et al. · 29.08.2023 J-proteins are cofactors that assist molecular chaperones in cellular protein folding. We have found that short C-terminal tags added to the N-terminal domains of J-proteins (J-domains) can promote interactions with multiple domains of DnaK, includi...
ArtikelImproved Cytotoxicity and Induced Apoptosis in HeLa Cells by Co‐loading Vitamin E Succinate and Curcumin in Nano‐MIL‐88B‐NH2von Roya Karimi et al. · 29.08.2023 Fe-MIL-88B-NH2 has been co-loaded with α-tocopheryl succinate (TOS) and curcumin (CCM). The incorporation of TOS into the structure of Fe-MIL-88B-NH2 improves cytotoxicity and apoptosis induction in the HeLa cell line. Abstract One of the strategi...
ArtikelEngineering a Formate Dehydrogenase for NADPH Regeneration von Wei Ma et al. · 28.08.2023 This work demonstrated the generative process of a molecularly evolved formate dehydrogenase from Candida dubliniensis (CdFDH). By structure-based semi-rational design, a combinatorial mutant M4 showed dramatically enhanced reactivity toward NADP+. ...
ArtikelQuantitative Analysis of The High‐Yield Hydrolysis of Kelp by Laminarinase and Alginate Lyasevon Taichi E. et al. · 28.08.2023 Laminarin and alginate in kelp are efficiently hydrolyzed by a binary combination of glycoside hydrolase family 55 (SactELam55A, Protein Data Bank 4pf0) and polysaccharide lyase family 18 (CaPL18 A, AlphaFold W7QSR3-F1). 1H-13C NMR spectroscopy show...
ArtikelOn the Role of Temperature in the Depolymerization of PET by FAST‐PETase: An Atomistic Point of View on Possible Active Site Pre‐Organization and Substrate‐Destabilization Effectsvon Carla Orlando et al. · 28.08.2023 The source of improved catalytic efficiency of FAST-PETase, which differs from the wtPETase for five mutations, has been proposed based on molecular dynamics simulations in terms of active site pre-organization and ability to promote substrate desta...
ArtikelA Modular Chemistry Platform for the Development of a Cereblon E3 Ligase‐Based Partial PROTAC Libraryvon Chelsi M. et al. · 22.08.2023 A modular platform for the synthesis of ortho-, meta-, and para-substituted phenyl-connected lenalidomide-derived CRBN E3 ligase ligands and a partial PROTAC library under Suzuki cross-coupling conditions is described. This method allows to systemat...
ArtikelDesign of Cationic Lipids with Acetal Linkers: Conformational Preferences, Hydrolytic Stability, and High Drug‐Loading Abilitiesvon Anand Kumar et al. · 22.08.2023 The design, synthesis, and biophysical characterizations of a library of cationic lipid analogous containing an acetal residue in the linker region (CALs) are presented. These CALs could be conveniently prepared through a trans-acetalization protoco...
Artikelβ‐Carboline Alkaloids Resist the Aggregation and Cytotoxicity of Human Islet Amyloid Polypeptidevon Yanan Wang et al. · 22.08.2023 The β-carboline alkaloids harmine and harmol effectively impede the fibril formation and cytotoxicity of human islet amyloid polypeptide. Both of them change the morphology of peptide aggregates and upregulate the cell viability by reducing peptide ...
ArtikelNucleic‐Acid‐Templated Synthesis of Smart Polymer Vectors for Gene Deliveryvon José García et al. · 22.08.2023 Dynamic covalent polymerization enables translating nucleic acid templates into synthetic precision polymers displaying sensitivity to pH and redox changes. In return, the templated polymers may serve as smart gene delivery vehicles. The overall pro...
ArtikelA Single‐Site Mutation Tunes Fluorescence and Chromophorylation of an Orange Fluorescent Cyanobacteriochrome von Makena K. et al. · 22.08.2023 Phycoerythrobilin (PEB)-binding cyanobacteriochromes are a group of small and bright orange fluorescent proteins that offer new opportunities as biological reporters. Here, protein sequence truncation and single site mutations were used to tune fluo...
ArtikelHeterologous Expression and Partial Characterization of a Putative Opine Dehydrogenase from a Metagenomic Sequence of Desulfohalobium retbaensevon Nevena Kaličanin et al. · 22.08.2023 Gene for putative opine dehydrogenase was identified in Desulfohalobium retbaense and was successfully produced in Escherichia coli. The enzyme was purified and structurally and kinetically characterized. It showed high stability and activity in har...
ArtikelIntegrating Pillar[5]arene and BODIPY for a Supramolecular Nanoplatform To Achieve Synergistic Photodynamic Therapy and Chemotherapyvon Hui Quan et al. · 17.08.2023 Cooperative capability: A novel drug delivery system with synergistic photodynamic therapy and chemotherapy capability was built by integrating pillar[5]arene WP5 and BODIPY BDP-CN to construct nanocarrier to load hypoxia-activated prodrug TPZ. The ...
ArtikelNoncovalent Association Thermodynamics of Turn‐On Fluorescent Probes with Human Serum Albumin: Dual‐Concentration Ratio Methodvon Han‐Yu Chen et al. · 16.08.2023 A dual-concentration ratio method is developed for quantifying the binding affinity of turn-on fluorescent probes (L) and a given protein (P). Only two samples at different [L]0/[protein]0 are required. It is an easy way to greatly reduce the amount...
ArtikelPerfluoro‐tert‐butyl Group‐Derived Capmatinib: Synthesis, Biological Evaluation and Its Application in 19F Magnetic Resonance Imagingvon Xinnan Zhang et al. · 16.08.2023 Fluorine atoms were introduced on Capmatinib to obtain a targeted 19F magnetic resonance imaging (MRI) contrast agent, 9F-CAP, its imaging concentration limit was found to be 25 mM (FLASH sequence). Molecular docking simulation, SPR (KD=40.7 μM), ha...
ArtikelChemical Synthesis of Peptides and Proteins Bearing Base‐Labile Post‐Translational Modifications: Evolution of the Methods in Four Decadesvon Wenjie Ma et al. · 16.08.2023 The S-palmitoylation on Cys residue and O-acetylation on Ser/Thr residues are base-labile post-translational modifications. Their lability to bases and nucleophiles makes them challenging synthetic targets. In this review, we summarized the efforts ...
ArtikelConventional understanding of SARS‐CoV‐2 Mpro and common strategies for developing its inhibitors
Artikel“On‐Off” Switching of Functional Guest Molecules via Exchange of Natural Product Solubilizing Agentsvon Riku Kawasaki et al. · 11.08.2023 Functional guest molecules can be dissolved in water using natural products as host solubilizing agents and transferred between host solubilizing agents. Owing to the different functions of these host-guest complexes, the transfer of guest molecules...
ArtikelTitin UN2A Acts as a Stable, Non‐Polymorphic Scaffold in its Binding to CARPvon Juliane Stehle et al. · 11.08.2023 Long-distance restraints obtained by electron paramagnetic resonance (EPR) spectroscopy revealed that the “unique N2A” (UN2A) domain of the sarcomeric protein titin shows a defined and structured three-helix bundle and preserves this conformation up...
ArtikelPlatinum and Palladium Organometallic Compounds: Disrupting the Ergosterol Pathway in Trypanosoma cruzivon Florencia Mosquillo et al. · 11.08.2023 Pd-dppf-mpo and Pt-dppf-mpo compounds specifically target the ergosterol biosynthesis pathway in Trypanosoma cruzi. These compounds effectively inhibit two key enzymes involved in the pathway, namely lanosterol 14-α demethylase (CYP51) and phosphome...
ArtikelSmall Molecule AIEgens for Illuminating Sub‐Cellular Endoplasmic Reticulum, Mitochondria, and Lysosomes von Jaypalsing Ingle et al. · 11.08.2023 Highly substituted small molecule modular oxazoles having dual intramolecular H-bonding, aggregated in water to instigate aggregation-induced emission (AIE) properties through restriction in motion leading to illuminate sub-cellular ER, mitochondria...
ArtikelTowards Ruthenium(II)‐Rhenium(I) Binuclear Complexes as Photosensitizers for Photodynamic Therapyvon Youchao Wang et al. · 11.08.2023 The preparation of a bimetallic complex, which combines the known photophysical properties of a rhenium(I) tricarbonyl complex and a ruthenium(II) polypyridyl complex and that could act as a PS for PDT, is described. Abstract The search for new me...
ArtikelPrevention of Swelling Phenomenon of Alginate Beads To Improve the Stability and Recyclability of Encapsulated Horse Liver Alcohol Dehydrogenasevon Alice Vetrano et al. · 11.08.2023 We developed a new strategy to avoid alginate bead breakage by inhibiting the loss of calcium ions from the biocatalyst. Several techniques were employed to investigate how the addition of Ca2+ ions to buffer solutions affected their structure. Opti...
ArtikelCo‐Immobilization of a Multi‐Enzyme Cascade: (S)‐Selective Amine Transaminases, l‐Amino Acid Oxidase and Catalasevon Tobias Heinks et al. · 10.08.2023 Co-immobilization of hcLAAO4, hCAT and the (S)-selective ATA from Vibrio fluvialis (ATA-Vfl) resulted in faster reactions and allowed further reduction of the co-substrate amount to 0.1 mol % compared to the soluble enzyme cascade. An engineered ATA...
ArtikelSite‐Specific and Multiple Fluorogenic Metabolic Glycan Labeling and Glycoproteomic Profiling in Live Cellsvon Shwee Khuan et al. · 10.08.2023 We demonstrated a multi-fluorescent MGL strategy combining ZIC-cHILIC StageTip enrichment and subsequent LC–MS/MS analysis for live cell glycan labeling and glycoprotein profiling in a single experiment. This approach enables the simultaneous site-s...
ArtikelTuning the Solution Self‐Assembly of a Peptide‐PEG (Polyethylene Glycol) Conjugate with α‐Cyclodextrinvon Valeria Castelletto et al. · 10.08.2023 The influence of alpha-cyclodextrin (αCD) on the aqueous solution self-assembly of peptide-polymer conjugate YYKLVFF-PEG3K is examined. Cryo-TEM and SAXS show that the conjugate self-assembles into β-sheet fibrils in aqueous solution, but complexati...
ArtikelDNA Nanobarrel‐Based Drug Delivery for Paclitaxel and Doxorubicinvon Jiaoyang Wang et al. · 09.08.2023 A DNA-based paclitaxel (PTX) and doxorubixin (DOX) delivery system was prepared, including Tn-PTX with different length of ssDNA tail (polythymine, Tn) and the DNA origami-based PTX\DOX\MUC-1 aptamer nanobarrel. In addition, the drug release, cytoto...
ArtikelFailure, Success, and Future Direction of Alzheimer Drugs Targeting Amyloid‐β Cascade: Pros and Cons of Chemical and Biological Modalitiesvon JiMin Kim et al. · 09.08.2023 This review paper examines immunotherapeutic and chemical drug candidates for Alzheimer's disease (AD) and suggests a drug discovery strategy to overcome the obstacles in chemical-driven drug discovery. We evaluate the prospects of an alternative ap...
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