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View article: Phosphorus fluoride exchange chemistry: An emerging strategy for covalent drug discovery
Phosphorus fluoride exchange chemistry: An emerging strategy for covalent drug discovery Open
As a next-generation click chemistry platform, Phosphorus Fluoride Exchange (PFEx) involves the substitution of P(V)–F bonds with nucleophiles to form stable P(V)–O and P(V)–N linkages. Aryl phosphoramidofluoridates, key PFEx substrates, e…
View article: Identification of Covalent Cyclic Peptide Inhibitors Targeting Protein-Protein Interactions Using Phage Display
Identification of Covalent Cyclic Peptide Inhibitors Targeting Protein-Protein Interactions Using Phage Display Open
Peptide macrocycles are promising therapeutics for a variety of disease indications due to their overall metabolic stability and potential to make highly selective binding interactions with targets. Recent advances in covalent macrocycle p…
View article: Arginine Accelerates Sulfur Fluoride Exchange and Phosphorus Fluoride Exchange Reactions between Proteins
Arginine Accelerates Sulfur Fluoride Exchange and Phosphorus Fluoride Exchange Reactions between Proteins Open
Sulfur fluoride exchange (SuFEx) and phosphorus fluoride exchange (PFEx) click chemistries are advancing research across multiple disciplines. By genetically incorporating latent bioreactive unnatural amino acids (Uaas), these chemistries …
View article: Arginine Accelerates Sulfur Fluoride Exchange and Phosphorus Fluoride Exchange Reactions between Proteins
Arginine Accelerates Sulfur Fluoride Exchange and Phosphorus Fluoride Exchange Reactions between Proteins Open
Sulfur fluoride exchange (SuFEx) and phosphorus fluoride exchange (PFEx) click chemistries are advancing research across multiple disciplines. By genetically incorporating latent bioreactive unnatural amino acids (Uaas), these chemistries …
View article: Genetically enabling phosphorus fluoride exchange click chemistry in proteins
Genetically enabling phosphorus fluoride exchange click chemistry in proteins Open
Phosphorus Fluoride Exchange (PFEx), recently debuted in small molecules, represents the forefront of click chemistry. To explore PFEx's potential in biological settings, we developed amino acids PFY and PFK featuring phosphoramidofluorida…
View article: Covalent Proteins as Targeted Radionuclide Therapies Enhance Antitumor Effects
Covalent Proteins as Targeted Radionuclide Therapies Enhance Antitumor Effects Open
Molecularly targeted radionuclide therapies (TRTs) struggle with balancing efficacy and safety, as current strategies to increase tumor absorption often alter drug pharmacokinetics to prolong circulation and normal tissue irradiation. Here…
View article: The proximity-enabled sulfur fluoride exchange reaction in the protein context
The proximity-enabled sulfur fluoride exchange reaction in the protein context Open
Proximity-enabled SuFEx reaction between interacting proteins was found to follow a two-step mechanism. Kinetics and essential properties were thoroughly studied for SuFEx applications in protein cross-linking and covalent biotherapeutics.
View article: Restoring and Enhancing the Potency of Existing Antibiotics against Drug-Resistant Gram-Negative Bacteria through the Development of Potent Small-Molecule Adjuvants
Restoring and Enhancing the Potency of Existing Antibiotics against Drug-Resistant Gram-Negative Bacteria through the Development of Potent Small-Molecule Adjuvants Open
The rapid and persistent emergence of drug-resistant bacteria poses a looming public health crisis. The possible task of developing new sets of antibiotics to replenish the existing ones is daunting to say the least. Searching for adjuvant…
View article: Titelbild: Prodrugs of Persulfide and Sulfide: Is There a Pharmacological Difference between the Two in the Context of Rapid Exchanges among Various Sulfur Species In Vivo<i>?</i> (Angew. Chem. 20/2022)
Titelbild: Prodrugs of Persulfide and Sulfide: Is There a Pharmacological Difference between the Two in the Context of Rapid Exchanges among Various Sulfur Species In Vivo<i>?</i> (Angew. Chem. 20/2022) Open
Eine Serie von Schwefel-Prodrugs (verkapselte reaktive Schwefelspezies), die reinen Schwefelwasserstoff (H2S) und Persulfidwasserstoff (H2S2) freisetzen können, wurde von Bowen Ke et al. in ihrer Zuschrift (e202201668) verwendet, um die ph…
View article: Developing Chemical Tools for Probing Biological Problems: From Prodrugs of Various Sulfur Species to Bacterial Sensitizers for Combination-Therapy
Developing Chemical Tools for Probing Biological Problems: From Prodrugs of Various Sulfur Species to Bacterial Sensitizers for Combination-Therapy Open
Chemical probes are important tools in examining biological mechanisms and potential therapeutics. Along the direction of studying sulfur signaling, perthiol species (RSnH, nò2) and hydrogen polysulfides (H2Sn, nò2) play essential roles in…
View article: Accelerating PERx Reaction Enables Covalent Nanobodies for Potent Neutralization of SARS-Cov-2 and Variants
Accelerating PERx Reaction Enables Covalent Nanobodies for Potent Neutralization of SARS-Cov-2 and Variants Open
The long-lasting COVID-19 pandemic and increasing SARS-CoV-2 variants demand effective drugs for prophylactics and treatment. Protein-based biologics offer high specificity yet their noncovalent interactions often lead to drug dissociation…
View article: A Genetically Encoded Fluorosulfonyloxybenzoyl-<scp>l</scp>-lysine for Expansive Covalent Bonding of Proteins via SuFEx Chemistry
A Genetically Encoded Fluorosulfonyloxybenzoyl-<span>l</span>-lysine for Expansive Covalent Bonding of Proteins via SuFEx Chemistry Open
Genetically introducing novel chemical bonds into proteins provides innovative avenues for biochemical research, protein engineering, and biotherapeutic applications. Recently, latent bioreactive unnatural amino acids (Uaas) have been inco…
View article: Novel Hydrogen Sulfide (H2S)-Releasing BW-HS-101 and Its Non-H2S Releasing Derivative in Modulation of Microscopic and Molecular Parameters of Gastric Mucosal Barrier
Novel Hydrogen Sulfide (H2S)-Releasing BW-HS-101 and Its Non-H2S Releasing Derivative in Modulation of Microscopic and Molecular Parameters of Gastric Mucosal Barrier Open
Hydrogen sulfide (H2S) is an endogenously produced molecule with anti-inflammatory and cytoprotective properties. We aimed to investigate for the first time if a novel, esterase-sensitive H2S-prodrug, BW-HS-101 with the ability to release …
View article: Making smart drugs smarter: The importance of linker chemistry in targeted drug delivery
Making smart drugs smarter: The importance of linker chemistry in targeted drug delivery Open
Smart drugs, such as antibody‐drug conjugates, for targeted therapy rely on the ability to deliver a warhead to the desired location and to achieve activation at the same site. Thus, designing a smart drug often requires proper linker chem…
View article: Issue Information ‐ TOC
Issue Information ‐ TOC Open
The journal publishes timely critical reviews of topics related to medicinal research, broadly defined, to which the authors have made significant contributions.Appropriate topics include, but are not limited to, the underlying pathophysio…
View article: Innentitelbild: Esterase‐Sensitive Prodrugs with Tunable Release Rates and Direct Generation of Hydrogen Sulfide (Angew. Chem. 14/2016)
Innentitelbild: Esterase‐Sensitive Prodrugs with Tunable Release Rates and Direct Generation of Hydrogen Sulfide (Angew. Chem. 14/2016) Open
Eine Serie von Thiosäuren wurde zu Schwefelwasserstoff-Prodrugs entwickelt, die B. Wang et al. in ihrer Zuschrift auf S. 4590 ff. vorstellen. Die H2S-Freisetzung beruht auf einer Esterase-vermittelten Spaltung, die eine Hydroxygruppe als a…
View article: Comparative analysis of Cu (I)‐catalyzed alkyne‐azide cycloaddition (CuAAC) and strain‐promoted alkyne‐azide cycloaddition (SPAAC) in <i>O</i>‐GlcNAc proteomics
Comparative analysis of Cu (I)‐catalyzed alkyne‐azide cycloaddition (CuAAC) and strain‐promoted alkyne‐azide cycloaddition (SPAAC) in <i>O</i>‐GlcNAc proteomics Open
O ‐linked β‐ N ‐acetylglucosamine ( O ‐GlcNAc) is emerging as an essential protein post‐translational modification in a range of organisms. It is involved in various cellular processes such as nutrient sensing, protein degradation, gene ex…
View article: CCDC 1409473: Experimental Crystal Structure Determination
CCDC 1409473: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1409474: Experimental Crystal Structure Determination
CCDC 1409474: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …