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View article: Synthesis of 1,3-Thiazine and 1,4-Thiazepine Derivatives via Cycloadditions and Ring Expansion
Synthesis of 1,3-Thiazine and 1,4-Thiazepine Derivatives via Cycloadditions and Ring Expansion Open
Non-cephem drugs with 1,3-thiazine-derived rings are very rare, although a number of bioactive 1,3-thiazine derivatives are known. Similarly, 1,4-thiazepine-derived drugs are rare, but many 1,4-thiazepine derivatives show interesting biolo…
View article: Synthesis and Docking Studies of Novel Spiro[5,8-methanoquinazoline-2,3′-indoline]-2′,4-dione Derivatives
Synthesis and Docking Studies of Novel Spiro[5,8-methanoquinazoline-2,3′-indoline]-2′,4-dione Derivatives Open
In this study, a set of spiro[5,8-methanoquinazoline-2,3′-indoline]-2′,4-dione derivatives 3a–p were synthesized starting from unsubstituted and N-methyl-substituted diendo- and diexo-2-aminonorbornene carboxamides, as well as various subs…
View article: Target‐Templated Construction of Functional Proteomimetics Using Photo‐Foldamer Libraries
Target‐Templated Construction of Functional Proteomimetics Using Photo‐Foldamer Libraries Open
Current methods for proteomimetic engineering rely on structure‐based design. Here we describe a design strategy that allows the construction of proteomimetics against challenging targets without a priori characterization of the target sur…
View article: Target‐Templated Construction of Functional Proteomimetics Using Photo‐Foldamer Libraries
Target‐Templated Construction of Functional Proteomimetics Using Photo‐Foldamer Libraries Open
Current methods for proteomimetic engineering rely on structure‐based design. Here we describe a design strategy that allows the construction of proteomimetics against challenging targets without a priori characterization of the target sur…
View article: As<sup>III</sup> Selectively Induces a Disorder-to-Order Transition in the Metalloid Binding Region of the AfArsR Protein
As<sup>III</sup> Selectively Induces a Disorder-to-Order Transition in the Metalloid Binding Region of the AfArsR Protein Open
Arsenic is highly toxic and a significant threat to human health, but certain bacteria have developed defense mechanisms initiated by AsIII binding to AsIII-sensing proteins of the ArsR family. The transcriptional regulator AfArsR responds…
View article: Light-Fueled Primitive Replication and Selection in Biomimetic Chemical Systems
Light-Fueled Primitive Replication and Selection in Biomimetic Chemical Systems Open
The concept of chemically evolvable replicators is central to abiogenesis. Chemical evolvability requires three essential components: energy-harvesting mechanisms for nonequilibrium dissipation, kinetically asymmetric replication and decom…
View article: Structural Adaptation of the Single-Stranded DNA-Binding Protein C-Terminal to DNA Metabolizing Partners Guides Inhibitor Design
Structural Adaptation of the Single-Stranded DNA-Binding Protein C-Terminal to DNA Metabolizing Partners Guides Inhibitor Design Open
Single-stranded DNA-binding protein (SSB) is a bacterial interaction hub and an appealing target for antimicrobial therapy. Understanding the structural adaptation of the disordered SSB C-terminus (SSB-Ct) to DNA metabolizing enzymes (e.g.…
View article: Structural adaptation of the single-stranded DNA-binding protein C-terminal to DNA metabolizing partners guides in-hibitor design
Structural adaptation of the single-stranded DNA-binding protein C-terminal to DNA metabolizing partners guides in-hibitor design Open
Fluorescence anisotropy metadata and polarization values Isotermal titration calorimetry raw files (protein-ligand and background titrations) Input files for PRALINE calculation in FASTA format CSV file containing the SSB sequences in SMIL…
View article: Structural adaptation of the single-stranded DNA-binding protein C-terminal to DNA metabolizing partners guides in-hibitor design
Structural adaptation of the single-stranded DNA-binding protein C-terminal to DNA metabolizing partners guides in-hibitor design Open
Fluorescence anisotropy metadata and polarization values Isotermal titration calorimetry raw files (protein-ligand and background titrations) Input files for PRALINE calculation in FASTA format CSV file containing the SSB sequences in SMIL…
View article: Light-fuelled primitive replication and selection in evolvable biomimetic chemical networks
Light-fuelled primitive replication and selection in evolvable biomimetic chemical networks Open
The concept of chemically evolvable replicators is central to abiogenesis. Evolvability requires three essential components: energy harvesting mechanisms for non-equilibrium dissipation, kinetically asymmetric decomposition pathways, and t…
View article: Light-fuelled dissipative replication and selection in evolvable biomimetic chemical networks
Light-fuelled dissipative replication and selection in evolvable biomimetic chemical networks Open
The concept of chemically evolvable replicators is central to abiogenesis. Evolvability requires three essential components: energy harvesting mechanisms for non-equilibrium dissipation, effective decomposition pathways and transfer of str…
View article: Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks
Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks Open
Evolvability of chemical replicator systems requires non-equilibrium energy dissipation, effective decomposition pathways and transfer of structural information in the autocatalytic cycles. We engineered a chemical network with peptidic fo…
View article: Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks
Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks Open
Evolvability of chemical replicator systems requires non-equilibrium energy dissipation, effective decomposition pathways and transfer of structural information in the autocatalytic cycles. We engineered a chemical network with peptidic fo…
View article: Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks
Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks Open
Evolvability of the chemical replicator systems requires non-equilibrium energy dissipation, effective death pathways and transfer of structural information in the autocatalytic cycles. We engineered a chemical network with peptidic foldam…
View article: Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks
Light-Fuelled Dissipative Replication and Selection in Adaptive Biomimetic Chemical Networks Open
Evolvability of the chemical replicator systems requires non-equilibrium energy dissipation, effective death pathways and transfer of structural information in the autocatalytic cycles. We engineered a chemical network with peptidic foldam…
View article: Proteomimetic surface fragments distinguish targets by function
Proteomimetic surface fragments distinguish targets by function Open
Foldameric local surface mimetics (LSMs) detect spots at protein surfaces and are promising building blocks in a fragment-centric design of xenobiotic structures and protein–protein interaction inhibitors.
View article: Lewis Acid-Catalyzed Diastereoselective Synthesis of Multisubstituted <i>N</i>-Acylaziridine-2-carboxamides from 2<i>H</i>-Azirines via Joullié–Ugi Three-Component Reaction
Lewis Acid-Catalyzed Diastereoselective Synthesis of Multisubstituted <i>N</i>-Acylaziridine-2-carboxamides from 2<i>H</i>-Azirines via Joullié–Ugi Three-Component Reaction Open
A ZnCl2-catalyzed diastereoselective Joullié-Ugi three-component reaction from 2 H-azirines, isocyanides, and carboxylic acids was established. The protocol allows the preparation of highly and diversely functionalized N-acylaziridine-2-ca…
View article: Anti-inflammatory Activity of <i>Melampyrum barbatum</i> and Isolation of Iridoid and Flavonoid Compounds
Anti-inflammatory Activity of <i>Melampyrum barbatum</i> and Isolation of Iridoid and Flavonoid Compounds Open
Melampyrum barbatum Waldst. & Kit. ex Willd. (Scrophulariaceae) has been used in traditional medicine for the treatment of rheumatic complaints and different skin diseases. In the course of our study the anti-inflammatory activity of the a…
View article: Peripheral cyclic β-amino acids balance the stability and edge-protection of β-sandwiches
Peripheral cyclic β-amino acids balance the stability and edge-protection of β-sandwiches Open
cis-2-Aminocyclohexanecarboxylic acid replacements at the edges of β-sandwiches reduce β-sheet propensities just enough to prevent aggregation but still maintain a compact structure.
View article: De Novo Modular Development of a Foldameric Protein–Protein Interaction Inhibitor for Separate Hot Spots: A Dynamic Covalent Assembly Approach
De Novo Modular Development of a Foldameric Protein–Protein Interaction Inhibitor for Separate Hot Spots: A Dynamic Covalent Assembly Approach Open
Protein–protein interactions stabilized by multiple separate hot spots are highly challenging targets for synthetic scaffolds. Surface‐mimetic foldamers bearing multiple recognition segments are promising candidate inhibitors. In this work…
View article: Competitive inhibition of TRPV1–calmodulin interaction by vanilloids
Competitive inhibition of TRPV1–calmodulin interaction by vanilloids Open
There is enormous interest toward vanilloid agonists of the pain receptor TRPV1 in analgesic therapy, but the mechanisms of their sensory neuron‐blocking effects at high or repeated doses are still a matter of debate. Our results have demo…