Jun‐Goo Jee
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View article: RA-PR058, a novel ramalin derivative, reduces BACE1 expression and phosphorylation of tau in Alzheimer’s disease mouse models
RA-PR058, a novel ramalin derivative, reduces BACE1 expression and phosphorylation of tau in Alzheimer’s disease mouse models Open
Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder characterized by cognitive decline, anxiety-like behavior, β-amyloid (Aβ) accumulation, and tau hyperphosphorylation. BACE1, the enzyme critical for Aβ production, has…
View article: 1441 The glucocorticoid receptor (GR)-dependent regulations of chronic inflammation and NRF2 as emerging drug targets for cancer therapy
1441 The glucocorticoid receptor (GR)-dependent regulations of chronic inflammation and NRF2 as emerging drug targets for cancer therapy Open
Background Oxidative stress resulting from chronic inflammation in the tumor microenvironment is a major contributing factor to cancer development. Nuclear factor erythroid 2-related factor 2 (NRF2) is a transcription factor that plays a k…
View article: Discovery of Kinase and Carbonic Anhydrase Dual Inhibitors by Machine Learning Classification and Experiments
Discovery of Kinase and Carbonic Anhydrase Dual Inhibitors by Machine Learning Classification and Experiments Open
A multi-target small molecule modulator is advantageous for treating complicated diseases such as cancers. However, the strategy and application for discovering a multi-target modulator have been less reported. This study presents the dual…
View article: Hydroxamic Acid as a Potent Metal-Binding Group for Inhibiting Tyrosinase
Hydroxamic Acid as a Potent Metal-Binding Group for Inhibiting Tyrosinase Open
Tyrosinase, a metalloenzyme containing a dicopper cofactor, plays a central role in synthesizing melanin from tyrosine. Many studies have aimed to identify small-molecule inhibitors of tyrosinase for pharmaceutical, cosmetic, and agricultu…
View article: Repositioning Food and Drug Administration-Approved Drugs for Inhibiting Biliverdin IXβ Reductase B as a Novel Thrombocytopenia Therapeutic Target
Repositioning Food and Drug Administration-Approved Drugs for Inhibiting Biliverdin IXβ Reductase B as a Novel Thrombocytopenia Therapeutic Target Open
Biliverdin IXβ reductase B (BLVRB) has recently been proposed as a novel therapeutic target for thrombocytopenia through its reactive oxygen species (ROS)-associated mechanism. Thus, we aim at repurposing drugs as new inhibitors of BLVRB. …
View article: New Inhibitors of Laccase and Tyrosinase by Examination of Cross-Inhibition between Copper-Containing Enzymes
New Inhibitors of Laccase and Tyrosinase by Examination of Cross-Inhibition between Copper-Containing Enzymes Open
Coppers play crucial roles in the maintenance homeostasis in living species. Approximately 20 enzyme families of eukaryotes and prokaryotes are known to utilize copper atoms for catalytic activities. However, small-molecule inhibitors dire…
View article: Novel Pyridine Bioisostere of Cabozantinib as a Potent c-Met Kinase Inhibitor: Synthesis and Anti-Tumor Activity against Hepatocellular Carcinoma
Novel Pyridine Bioisostere of Cabozantinib as a Potent c-Met Kinase Inhibitor: Synthesis and Anti-Tumor Activity against Hepatocellular Carcinoma Open
Two novel bioisosteres of cabozantinib, 3 and 4, were designed and synthesized. The benzene ring in the center of the cabozantinib structure was replaced by trimethylpyridine (3) and pyridine (4), respectively. Surprisingly, the two compou…
View article: Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy
Structural Deformation of MTX Induced by Nanodrug Conjugation Dictate Intracellular Drug Transport and Drug Efficacy Open
Greater changes in the structural variations of MTX analyzed by nuclear magnetic resonance (NMR) significantly improved the anti-inflammatory drug efficacy of human fibroblast-like synovial cells (FLS) via stable drug release in the extrac…
View article: Synthesis and anti-hepatocellular carcinoma activity of aminopyridinol–sorafenib hybrids
Synthesis and anti-hepatocellular carcinoma activity of aminopyridinol–sorafenib hybrids Open
Sorafenib is recommended as the primary therapeutic drug for patients with hepatocellular carcinoma. To discover a new compound that avoids low response rates and toxic side effects that occur in sorafenib therapy, we designed and synthesi…
View article: Tubulosine selectively inhibits JAK3 signalling by binding to the ATP‐binding site of the kinase of JAK3
Tubulosine selectively inhibits JAK3 signalling by binding to the ATP‐binding site of the kinase of JAK3 Open
Gain‐ or loss‐of‐function mutations in Janus kinase 3 (JAK3) contribute to the pathogenesis of various haematopoietic malignancies and immune disorders, suggesting that aberrant JAK3 signalling is an attractive therapeutic target to treat …
View article: Sulfisoxazole inhibits the secretion of small extracellular vesicles by targeting the endothelin receptor A
Sulfisoxazole inhibits the secretion of small extracellular vesicles by targeting the endothelin receptor A Open
Inhibitors of the secretion of cancer exosomes, which promote cancer progression and metastasis, may not only accelerate exosome biology research but also offer therapeutic benefits for cancer patients. Here we identify sulfisoxazole (SFX)…
View article: 4‐Hydroxynonenal‐induced GPR109A (HCA<sub>2</sub> receptor) activation elicits bipolar responses, G<sub>αi</sub>‐mediated anti‐inflammatory effects and G<sub>βγ</sub>‐mediated cell death
4‐Hydroxynonenal‐induced GPR109A (HCA<sub>2</sub> receptor) activation elicits bipolar responses, G<sub>αi</sub>‐mediated anti‐inflammatory effects and G<sub>βγ</sub>‐mediated cell death Open
Background and Purpose In this study, we examined the possibility that 4‐hydroxynonenal (4‐HNE) acting as a ligand for the HCA 2 receptor (GPR109A) elicits both anti‐inflammatory and cell death responses. Experimental Approach Agonistic ac…
View article: Structural ensemble-based docking simulation and biophysical studies discovered new inhibitors of Hsp90 N-terminal domain
Structural ensemble-based docking simulation and biophysical studies discovered new inhibitors of Hsp90 N-terminal domain Open
View article: Thiopurine Drugs Repositioned as Tyrosinase Inhibitors
Thiopurine Drugs Repositioned as Tyrosinase Inhibitors Open
Drug repositioning is the application of the existing drugs to new uses and has the potential to reduce the time and cost required for the typical drug discovery process. In this study, we repositioned thiopurine drugs used for the treatme…
View article: Interaction between human angiogenin and the p53 TAD2 domain and its implication for inhibitor discovery
Interaction between human angiogenin and the p53 TAD2 domain and its implication for inhibitor discovery Open
Interaction between angiogenin and the p53 TAD2 domain in cancer cells can inhibit the function of the p53 tumor suppressor and promote cell survival. Based on a model structure using NMR and mutational analysis, positively charged 31 RRR …
View article: Antithrombotic properties of JJ1, a potent and novel thrombin inhibitor
Antithrombotic properties of JJ1, a potent and novel thrombin inhibitor Open
View article: Thiopurine Drugs Repositioned as Tyrosinase Inhibitors
Thiopurine Drugs Repositioned as Tyrosinase Inhibitors Open
In this study, we repositioned thiopurine drugs used for the treatment of acute leukaemia as new tyrosinase inhibitors. Tyrosinase catalyses two distinct and successive oxidations in melanin biosynthesis: the conversions of tyrosine to dih…
View article: Ligand-Mediated Folding of the OmpA Periplasmic Domain from Acinetobacter baumannii
Ligand-Mediated Folding of the OmpA Periplasmic Domain from Acinetobacter baumannii Open
View article: Strategy for Determining the Structures of Large Biomolecules using the Torsion Angle Dynamics of CYANA
Strategy for Determining the Structures of Large Biomolecules using the Torsion Angle Dynamics of CYANA Open
With the rapid increase of data on protein-protein interactions, the need for delineating the 3D structures of huge protein complexes has increased. The protocols for determining nuclear magnetic resonance (NMR) structure can be applied to…
View article: Repositioning of Thiourea-Containing Drugs as Tyrosinase Inhibitors
Repositioning of Thiourea-Containing Drugs as Tyrosinase Inhibitors Open
Tyrosinase catalyzes two distinct sequential reactions in melanin biosynthesis: The hydroxylation of tyrosine to dihydroxyphenylalanine (DOPA) and the oxidation of DOPA to dopaquinone. Developing functional modulators of tyrosinase is impo…
View article: Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase
Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase Open
View article: The role of thioredoxin reductase and glutathione reductase in plumbagin-induced, reactive oxygen species-mediated apoptosis in cancer cell lines
The role of thioredoxin reductase and glutathione reductase in plumbagin-induced, reactive oxygen species-mediated apoptosis in cancer cell lines Open
View article: Comparison of NMR structures refined under implicit and explicit solvents
Comparison of NMR structures refined under implicit and explicit solvents Open
Refinements with atomistic molecular dynamics (MD) simulation have contributed to improving the qualities of NMR structures. In most cases, the calculations with atomistic MD simulation for NMR structures employ generalized-Born implicit s…
View article: Bisdemethoxycurcumin Induces Apoptosis in Activated Hepatic Stellate Cells via Cannabinoid Receptor 2
Bisdemethoxycurcumin Induces Apoptosis in Activated Hepatic Stellate Cells via Cannabinoid Receptor 2 Open
Activated Hepatic Stellate Cells (HSCs), major fibrogenic cells in the liver, undergo apoptosis when liver injuries cease, which may contribute to the resolution of fibrosis. Bisdemethoxycurcumin (BDMC) is a natural derivative of curcumin …
View article: Protective effect of butylated hydroxylanisole against hydrogen peroxide-induced apoptosis in primary cultured mouse hepatocytes
Protective effect of butylated hydroxylanisole against hydrogen peroxide-induced apoptosis in primary cultured mouse hepatocytes Open
Butylated hydroxyanisole (BHA) is a synthetic phenolic compound consisting of a mixture of two isomeric organic compounds: 2-tert-butyl-4-hydroxyanisole and 3-tert-butyl-4-hydroxyanisole. We examined the effect of BHA against hydrogen pero…