A5001295371- Cancer, Hypoxia, and Metabolism
- Antimicrobial Peptides and Activities
- Monoclonal and Polyclonal Antibodies Research
- Cancer-related Molecular Pathways
- Immunotherapy and Immune Responses
- HIV Research and Treatment
- RNA Interference and Gene Delivery
- Hepatitis B Virus Studies
- Advanced biosensing and bioanalysis techniques
- RNA modifications and cancer
- Nanoparticle-Based Drug Delivery
- Hepatitis C virus research
- Biochemical and Structural Characterization
- Mitochondrial Function and Pathology
- HIV/AIDS drug development and treatment
- 3D Printing in Biomedical Research
- Protein purification and stability
- Advanced Biosensing Techniques and Applications
- RNA and protein synthesis mechanisms
- Ubiquitin and proteasome pathways
- Cancer Research and Treatments
- Glycosylation and Glycoproteins Research
- Epigenetics and DNA Methylation
- Virology and Viral Diseases
- High Altitude and Hypoxia
Sungkyunkwan University
2023
Korea Research Institute of Bioscience and Biotechnology
2010-2019
Korea University of Science and Technology
2012-2019
Government of the Republic of Korea
2015
Daejeon University
2015
Korea Institute of Science and Technology
1991
Hypoxia inducible factor (HIF) is regulated by dual pathways involving oxygen-dependent prolyl and asparaginyl hydroxylation of its α-subunits. Prolyl at two sites within a central degradation domain promotes association HIF-α with the von Hippel-Lindau ubiquitin E3 ligase destruction ubiquitin-proteasome pathways. Asparaginyl blocks recruitment p300/CBP co-activators to C-terminal activation in HIF-α. These hydroxylations are catalyzed members Fe(II) 2-oxoglutarate (2-OG) oxygenase family....
Abstract Hypoxia-inducible factor (HIF)-1 plays a key role in tumor promotion by inducing ∼60 genes required for adaptation to hypoxia; thus, it is viewed as target cancer therapy. For this reason, YC-1, which down-regulates HIF-1α and HIF-2α at the post-translational level, being developed novel anticancer drug. We here found that YC-1 acts manner inhibit HIF-1. In Gal4 reporter system, not degraded was significantly inactivate COOH-terminal transactivation domain (CAD) of HIF-1α, whereas...
The hypoxia inducible factor (HIF) system is central to the signaling of low oxygen (hypoxia) in animals. levels HIF-α isoforms are regulated an oxygen-dependent manner by activity HIF prolyl-hydroxylases (PHD or EGLN enzymes), which Fe(II) and 2-oxoglutarate (2OG) dependent oxygenases. Here, we describe biochemical, crystallographic, cellular profiling, animal studies on PHD inhibitors including selectivity using a representative set human 2OG We identify suitable probe compounds for use...
The antimicrobial peptide, lactoferricin, is generated upon the gastric pepsin cleavage of lactoferrin and has many basic hydrophobic amino acid residues essential for its biological activity. To investigate structure‐antimicrobial activity relationships, acid‐rich region bovine lactoferricin (BLFC), RRWQWRMKKLG, was selected. Using chemically synthesized BLFC substituted peptides, activities peptides were tested by determining minimal inhibitory concentration (MIC) Escherichia coli Bacillus...
The hybrid peptide (CA-ME) derived from cecropin A(1-8) and melittin (1-12) has potent antibacterial antimalarial activities. Because the N-terminal sequence 1-12 of magainin 2 is similar to melittin(1-12), CA-MA with CA(1-8) MA(1-12) their analogues were designed synthesized. Antitumor activities these peptides evaluated using three small cell lung cancer lines. Greater antitumor activity was observed when residues 16, 18 19 hydrophobic (Leu or Val), basic (Lys) (Lys), respectively. IC50...
The interplay among hypoxia-inducible factor 1-alpha (HIF-1α), p53 and human orthologue of murine double minute 2 (Hdm2) has been introduced as a key event in tumor promotion angiogenesis. Recently, nutlin-3, small-molecule antagonist Hdm2, was demonstrated to inhibit the HIF-1-mediated vascular endothelial growth production Yet, mechanism by which nutlin-3 inhibits HIF-1 is an open question. We here addressed mode-of-action with respect HIF-1α–p53–Hdm2 interplay. effect on HIF-1α function...
Hypoxia inducible factor 1α (HIF-1α), an essential transcriptional factor, is negatively regulated by two different types of oxygen and Fe(2+) -dependent HIF hydroxylases, proline hydroxylase (PHD) inhibiting (FIH), under normoxia. Iron chelators have therefore been used for inducing HIF-1α expression the hydroxylases. In this study, iron displayed differential effects PHD FIH in cells depending on their specificity membrane permeability rather than vitro potencies. The strict -chelator...
This work demonstrates successful delivery of a gene to EGFR-overexpressed cancer cells by using rationally designed branched GE11 peptide as targeting ligand.
Fc-specific antibody binding proteins (FcBPs) with the minimal domain of protein G are widely used for immobilization well-oriented antibodies onto solid surfaces, but noncovalently bound to FcBPs unstable in sera containing large amounts antibodies. Here we report novel photoactivatable photomethionine (pMet) expressed E. coli, which induce photo-cross-linking upon UV irradiation. Unfortunately, pMet did not support expression native coli system, and therefore also developed an engineered...
Hypoxia and inflammation often develop concurrently in numerous diseases, both hypoxia‐inducible factor (HIF)‐1α nuclear factor‐kappaB (NF‐κB) are key transcription factors of stress response genes. An NF‐κB inhibitor, inhibitor NF‐κBα (IκBα), was found to interact with inhibiting HIF (FIH) be hydroxylated by FIH. However, FIH did not functionally regulate IκBα, the consequence FIH–IκBα interaction thus remains uncertain. In present study, we tested possibility that IκBα regulates binding...
Inhibition of the hypoxia-inducible factor (HIF) prolyl hydroxylases (PHD or EGLN enzymes) is interest for treatment anemia and ischemia-related diseases. Most PHD inhibitors work by binding to single ferrous ion competing with 2-oxoglutarate (2OG) co-substrate at active site. Non-specific iron chelators also inhibit PHDs, both in vitro cells. We report identification dual action inhibitors, which bind site induce a second Following analysis small-molecule complexes application...
Abstract In order to obtain peptides having improved antimicrobial activity with low hemolytic effect, a hybrid peptide (CA‐MA) composed from cecropin A (1‐8) and magainin 2(1‐12), its analogues amino acid substitutions were designed synthesized. The activities against bacterial cells human red blood analyzed for each peptide. Secondary structures of the in aqueous solution, 50% trifluoroethanol, sodium dodecylsulfate micelles estimated using circular dichroism spectroscopy. increase...
The factor-inhibiting hypoxia-inducible factor (FIH) hydroxylates the asparagine 803 (Asn803) residue of 1alpha (HIF-1alpha), and modification abrogates transcriptional activity HIF-1alpha. Because FIH is more active on HIF-1alpha than prolyl hydroxylase domain proteins under hypoxic conditions, its inhibitors have potential to be developed as anti-ischemic drugs targeting normal cells stressed by hypoxia. In this study, authors first monoclonal antibody, SHN-HIF1alpha, specifically Asn803...
Thanatin, a 21-residue peptide, is an inducible insect peptide with broad range of activity against bacteria and fungi. It has C-terminal disulfide loop, like the frog skin secretion antimicrobial peptides brevinin family. In this study, we tried to find effect number amino acids between bond. Thanatin showed stronger antibacterial Gram negative than other mutants, except Th1; whereas, mutant deletion had higher positive thanatin. An increase in acid(s) using alanine residue decreased all...
Abstract In order to design synthetic peptides with potent antifungal activity but low cytotoxic under physiological conditions, several analogues of the previously reported cecropin A (CA)‐melittin (ME) hybrid peptide, CA(1‐8)‐ME(1‐12), were synthesized. These designed by analysis α‐helical wheel diagram CA(1‐8)‐ME(1‐12). Antifungal activities measured growth inhibition yeast Trichosporon beigelii and hemolytic assay human red blood cells, respectively. Substitution Thr for Lys at position...
Total kidney volume (TKV) measurement is crucial for selecting treatment candidates in autosomal dominant polycystic disease (ADPKD). We developed and investigated the performance of fully-automated 3D-volumetry model applied it to software as a service (SaaS) clinical support on tolvaptan prescription ADPKD patients.Computed tomography scans patients taken between January 2000 June 2022 were acquired from seven institutions. The quality images was manually reviewed advance. dataset split...