Haigen Fu
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View article: Asymmetric Conjugate Hydrocyanation of <i>α</i> , <i>β</i> ‐Unsaturated Aldehydes Catalyzed by Engineered 2‐Deoxy‐D‐ribose‐5‐phosphate Aldolase
Asymmetric Conjugate Hydrocyanation of <i>α</i> , <i>β</i> ‐Unsaturated Aldehydes Catalyzed by Engineered 2‐Deoxy‐D‐ribose‐5‐phosphate Aldolase Open
The enantioselective conjugate hydrocyanation of α , β ‐unsaturated aldehydes remains a long‐standing challenge in synthetic chemistry. Here, we report the redesign of 2‐deoxy‐D‐ribose‐5‐phosphate aldolase (DERA) into an efficient biocatal…
View article: Biocatalytic Atroposelective Synthesis of Axially Chiral Styrenes via Dynamic Kinetic Resolution
Biocatalytic Atroposelective Synthesis of Axially Chiral Styrenes via Dynamic Kinetic Resolution Open
Enzymatic synthesis of atropisomers has recently attracted considerable research attention, with most studies focusing on axially chiral biaryls. We report a less explored atroposelective dynamic kinetic resolution (DKR) of nonbiaryl styre…
View article: From Ground-State to Excited-State Activation Modes: Flavin-Dependent “Ene”-Reductases Catalyzed Non-natural Radical Reactions
From Ground-State to Excited-State Activation Modes: Flavin-Dependent “Ene”-Reductases Catalyzed Non-natural Radical Reactions Open
Enzymes are desired catalysts for chemical synthesis, because they can be engineered to provide unparalleled levels of efficiency and selectivity. Yet, despite the astonishing array of reactions catalyzed by natural enzymes, many reactivit…
View article: Photobiocatalytic Strategies for Organic Synthesis
Photobiocatalytic Strategies for Organic Synthesis Open
Biocatalysis has revolutionized chemical synthesis, providing sustainable methods for preparing various organic molecules. In enzyme-mediated organic synthesis, most reactions involve molecules operating from their ground states. Over the …
View article: CCDC 2218380: Experimental Crystal Structure Determination
CCDC 2218380: 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 2218381: Experimental Crystal Structure Determination
CCDC 2218381: 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 2218382: Experimental Crystal Structure Determination
CCDC 2218382: 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 2218379: Experimental Crystal Structure Determination
CCDC 2218379: 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: Asymmetric <i>C</i> -Alkylation of Nitroalkanes <i>via</i> Enzymatic Photoredox Catalysis
Asymmetric <i>C</i> -Alkylation of Nitroalkanes <i>via</i> Enzymatic Photoredox Catalysis Open
Tertiary nitroalkanes and the corresponding α-tertiary amines represent important motifs in bioactive molecules and natural products. The C-alkylation of secondary nitroalkanes with electrophiles is a straightforward strategy for construct…
View article: Asymmetric C-Alkylation of Nitroalkanes via Enzymatic Photoredox Catalysis
Asymmetric C-Alkylation of Nitroalkanes via Enzymatic Photoredox Catalysis Open
Tertiary nitroalkanes and the corresponding α-tertiary amines represent important motifs in bioactive molecules and natural prod-ucts. The C-alkylation of secondary nitroalkanes with electrophiles is a straightforward strategy for construc…
View article: An Asymmetric sp3–sp3 Cross-Electrophile Coupling Using Biocatalysis
An Asymmetric sp3–sp3 Cross-Electrophile Coupling Using Biocatalysis Open
The catalytic asymmetric construction of Csp3–Csp3 bonds remains one of the foremost challenges in organic synthesis. Metal-catalyzed cross-electrophile couplings have emerged as a powerful tool for C–C bond formation. However, these catal…
View article: Ground-State Electron Transfer as an Initiation Mechanism for Biocatalytic C–C Bond Forming Reactions
Ground-State Electron Transfer as an Initiation Mechanism for Biocatalytic C–C Bond Forming Reactions Open
The development of non-natural reaction mechanisms is an attractive strategy for expanding the synthetic capabilities of substrate promiscuous enzymes. Here, we report an "ene"-reductase catalyzed asymmetric hydroalkylation of olefins usin…
View article: Ground-State Electron Transfer as an Initiation Mechanism for Asymmetric Hydroalkylations in Radical Biocatalysis
Ground-State Electron Transfer as an Initiation Mechanism for Asymmetric Hydroalkylations in Radical Biocatalysis Open
Stereoselective bond-forming reactions are essential tools in modern organic synthesis. However, catalytic strategies for controlling the stereochemical outcome of radical-mediated C–C bond formation remain underdeveloped. Here, we report …
View article: Ground-State Electron Transfer as an Initiation Mechanism for Asymmetric Hydroalkylations in Radical Biocatalysis
Ground-State Electron Transfer as an Initiation Mechanism for Asymmetric Hydroalkylations in Radical Biocatalysis Open
Stereoselective bond-forming reactions are essential tools in modern organic synthesis. However, catalytic strategies for controlling the stereochemical outcome of radical-mediated C–C bond formation remain underdeveloped. Here, we report …
View article: Activation modes in biocatalytic radical cyclization reactions
Activation modes in biocatalytic radical cyclization reactions Open
Radical cyclizations are essential reactions in the biosynthesis of secondary metabolites and the chemical synthesis of societally valuable molecules. In this review, we highlight the general mechanisms utilized in biocatalytic radical cyc…
View article: Structural Aspects of Photopharmacology: Insight into the Binding of Photoswitchable and Photocaged Inhibitors to the Glutamate Transporter Homologue
Structural Aspects of Photopharmacology: Insight into the Binding of Photoswitchable and Photocaged Inhibitors to the Glutamate Transporter Homologue Open
Photopharmacology addresses the challenge of drug selectivity and side effects through creation of photoresponsive molecules activated with light with high spatiotemporal precision. This is achieved through incorporation of molecular photo…
View article: Aminocarboxylic acids related to aspergillomarasmine A (AMA) and ethylenediamine-<i>N</i>,<i>N</i>′-disuccinic acid (EDDS) are strong zinc-binders and inhibitors of the metallo-beta-lactamase NDM-1
Aminocarboxylic acids related to aspergillomarasmine A (AMA) and ethylenediamine-<i>N</i>,<i>N</i>′-disuccinic acid (EDDS) are strong zinc-binders and inhibitors of the metallo-beta-lactamase NDM-1 Open
Aminocarboxylic acid analogues of aspergillomarasmine A (AMA) and ethylenediamine-N,N′-disuccinic acid (EDDS) were preparedviaa robust chemoenzymatic approach. These compounds display potent inhibition of the bacterial resistance enzyme ND…
View article: Engineered C–N Lyase: Enantioselective Synthesis of Chiral Synthons for Artificial Dipeptide Sweeteners
Engineered C–N Lyase: Enantioselective Synthesis of Chiral Synthons for Artificial Dipeptide Sweeteners Open
Aspartic acid derivatives with branched N‐alkyl or N‐arylalkyl substituents are valuable precursors to artificial dipeptide sweeteners such as neotame and advantame. The development of a biocatalyst to synthesize these compounds in a singl…
View article: Engineered C–N Lyase: Enantioselective Synthesis of Chiral Synthons for Artificial Dipeptide Sweeteners
Engineered C–N Lyase: Enantioselective Synthesis of Chiral Synthons for Artificial Dipeptide Sweeteners Open
Aspartic acid derivatives with branched N‐alkyl or N‐arylalkyl substituents are valuable precursors to artificial dipeptide sweeteners such as neotame and advantame. The development of a biocatalyst to synthesize these compounds in a singl…
View article: Biocatalytic asymmetric synthesis of unnatural amino acids using C-N lyases
Biocatalytic asymmetric synthesis of unnatural amino acids using C-N lyases Open
Optically pure functionalized aspartic acid derivatives are highly valuable as core structures in pharmaceuticals, nutraceuticals, and agrochemicals. Despite their broad applications, the direct asymmetric synthesis of functionalized aspar…
View article: <scp>SLC</scp> 1A3 contributes to L‐asparaginase resistance in solid tumors
<span>SLC</span> 1A3 contributes to L‐asparaginase resistance in solid tumors Open
L-asparaginase (ASNase) serves as an effective drug for adolescent acute lymphoblastic leukemia. However, many clinical trials indicated severe ASNase toxicity in patients with solid tumors, with resistant mechanisms not well understood. H…
View article: Biocatalytic Asymmetric Synthesis of <i>N</i>-Aryl-Functionalized Amino Acids and Substituted Pyrazolidinones
Biocatalytic Asymmetric Synthesis of <i>N</i>-Aryl-Functionalized Amino Acids and Substituted Pyrazolidinones Open
N-arylated α-amino acids and pyrazolidin-3-ones are widely being used as chiral building blocks for pharmaceuticals and agrochemicals. Here we report a biocatalytic route for the asymmetric synthesis of various N-arylated aspartic acids ap…
View article: Biocatalytic Enantioselective Hydroaminations for Production of <i>N</i>‐Cycloalkyl‐Substituted L‐Aspartic Acids Using Two C−N Lyases
Biocatalytic Enantioselective Hydroaminations for Production of <i>N</i>‐Cycloalkyl‐Substituted L‐Aspartic Acids Using Two C−N Lyases Open
N ‐cycloalkyl‐substituted amino acids have wide‐ranging applications in pharma‐ and nutraceutical fields. Here we report the asymmetric synthesis of various N ‐cycloalkyl‐substituted l ‐aspartic acids using ethylenediamine‐ N,N′ ‐disuccini…
View article: Synthesis and Biological Evaluation of Quinoline Derivatives as a Novel Class of Broad-Spectrum Antibacterial Agents
Synthesis and Biological Evaluation of Quinoline Derivatives as a Novel Class of Broad-Spectrum Antibacterial Agents Open
Nineteen new quinoline derivatives were prepared via the Mannich reaction and evaluated for their antibacterial activities against both Gram-positive (G+) and Gram-negative (G−) bacteria, taking compound 1 as the lead. Among the target com…
View article: Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors
Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors Open
Aspartate (Asp) derivatives are privileged compounds for investigating the roles governed by excitatory amino acid transporters (EAATs) in glutamatergic neurotransmission. Here, we report the synthesis of various Asp derivatives with (cycl…
View article: Glutamate Transporter Inhibitors with Photo‐Controlled Activity
Glutamate Transporter Inhibitors with Photo‐Controlled Activity Open
Glutamate is an important signaling molecule in the nervous system and its extracellular levels are regulated by amino acid transporters. Studies on the role of glutamate transport have benefitted from the development of small molecule inh…