A5075143500- Synthetic Organic Chemistry Methods
- Asymmetric Synthesis and Catalysis
- Advanced Synthetic Organic Chemistry
- Chemical Synthesis and Analysis
- Ion Channels and Receptors
- Chemical synthesis and alkaloids
- Microbial Natural Products and Biosynthesis
- Inflammatory mediators and NSAID effects
- Natural product bioactivities and synthesis
- Bioactive Compounds and Antitumor Agents
- Cancer, Hypoxia, and Metabolism
- Carbohydrate Chemistry and Synthesis
- Synthesis and Biological Evaluation
- Biological Activity of Diterpenoids and Biflavonoids
- Heat shock proteins research
- Cytokine Signaling Pathways and Interactions
- Eicosanoids and Hypertension Pharmacology
- Marine Sponges and Natural Products
- Traditional and Medicinal Uses of Annonaceae
- Retinal Diseases and Treatments
- Phytochemicals and Antioxidant Activities
- Alkaloids: synthesis and pharmacology
- Oxidative Organic Chemistry Reactions
- Computational Drug Discovery Methods
- Radiopharmaceutical Chemistry and Applications
CHA University
2017-2025
National Cancer Center
2023
Seoul National University
2012-2021
Yonsei University
2004-2021
Seoul National University Hospital
2019-2021
Dankook University
2021
Korea University of Science and Technology
2021
Gangnam Severance Hospital
2021
Dongguk University
2021
Korea Research Institute of Chemical Technology
2021
Capsaicin, a pungent ingredient of hot peppers, causes excitation small sensory neurons, and thereby produces severe pain. A nonselective cation channel activated by capsaicin has been identified in neurons cDNA encoding the cloned recently. However, an endogenous activator receptor not yet found. In this study, we show that several products lipoxygenases directly activate capsaicin-activated isolated membrane patches neurons. Among them, 12- 15-( S )-hydroperoxyeicosatetraenoic acids, 5-...
BackgroundThe molecular chaperone heat shock protein 90 (Hsp90) participates in preserving the expression and activity of various oncoproteins, including hypoxia-inducible factor 1α (HIF-1α) Akt. Deguelin is a rotenoid with antitumor activities. We investigated whether activities deguelin involve functional inhibition Hsp90.
Deguelin exhibits potent apoptotic and antiangiogenic activities in a variety of transformed cells cancer cells. also tumor suppressive effects xenograft models for many human cancers. Our initial studies confirmed that deguelin disrupts ATP binding to HSP90 consequently induces destabilization its client proteins such as HIF-1α. Interestingly, fluorescence probe assay revealed analogues do not compete with the N-terminus HSP90, unlike most inhibitors. To determine key parts contribute...
Blood–brain barrier (BBB) breakdown and inflammation are critical events in ischemic stroke, contributing to aggravated brain damage. The BBB mainly consists of microvascular endothelial cells sealed by tight junctions protect the from blood-borne substances. Thus, maintenance integrity may be a potential target for neuroprotection. Sac-1004, pseudo-sugar derivative cholesterol, enhances stabilization cortical actin ring. Here, we report on protective effects Sac-1004 cerebral...
Isosteric replacement of the phenolic hydroxyl group in potent vanilloid receptor (VR1) agonists with alkylsulfonamido provides a series compounds which are effective antagonists to action capsaicin on rat VR1 heterologously expressed Chinese hamster ovary (CHO) cells. In particular, compound 61, N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N'-[3-fluoro-4-(methylsulfonylamino)benzyl]thiourea was full antagonist against capsaicin, displayed Ki value 7.8 nM (compared 520 for capsazepine and...
Circadian rhythms, biological oscillations with a period of about 24 h, are maintained by genetically determined innate time-keeping system called the molecular circadian clockwork. Despite physiological and clinical importance clock, development small molecule modulators that directly target core clock machinery has only been recently initiated. In present study, we aimed to identify novel influencing feedback loop applying our two-step cell-based screening strategy based on E-box-mediated...
Eye diseases characterized by excessive angiogenesis such as wet age-related macular degeneration, proliferative diabetic retinopathy, and retinopathy of prematurity are major causes blindness. Cremastranone is an antiangiogenic, naturally occurring homoisoflavanone with efficacy in retinal choroidal neovascularization models antiproliferative selectivity for endothelial cells over other cell types. We undertook a cell-based structure-activity relationship study to develop more potent...
The vanilloid receptor VR1 has attracted great interest as a sensory transducer for capsaicin, protons, and heat, therapeutic target. Here we characterize two novel antagonists, KJM429 [<i>N</i>-(4-<i>tert</i>-butylbenzyl)-<i>N</i>′-[4-(methylsulfonylamino)benzyl]thiourea] JYL1421 [<i>N</i>-(4-<i>tert</i>-butylbenzyl)-<i>N</i>′-[3-fluoro-4-(methylsulfonylamino)benzyl]thiourea], with enhanced activity compared capsazepine on rat expressed in Chinese hamster ovary (CHO) cells. JYL1421, the...
Using the approach of ligand-based drug design, we discovered a novel series 4,6-disubstituted 2-aminopyrimidines as RAGE inhibitors. In transgenic mouse models AD, one 4,6-bis(4-chlorophenyl)pyrimidine analogs, 59, significantly lowered concentration toxic soluble Aβ in brain and improved cognitive function. SPR analysis confirmed direct binding 59 with RAGE, which should contribute to its biological activities via inhibition RAGE–Aβ interaction. We also predicted mode analogs V-domain...
To examine the pro-resolving effects of taurine chloramine (TauCl).TauCl injected into peritoneum mice enhanced resolution zymosan A-induced peritonitis. Furthermore, when macrophages obtained from peritoneal exudates were treated with TauCl, their efferocytic ability was elevated. In murine macrophage-like RAW264.7 cells exposed to proportion engulfing apoptotic neutrophils also increased. these expression heme oxygenase-1 (HO-1) elevated along increased nuclear translocation factor...
The Hsp90 facilitates proper folding of signaling proteins associated with cancer progression, gaining attention as a target for therapeutic intervention. natural rotenoid deguelin was identified an inhibitor, but concerns about neurotoxicity have limited prospects clinical development. In this study, we report progress on analogues that address limitation, focusing the novel analogue SH-1242 candidate to broadly human lung cells, including those are chemoresistant or harboring KRAS...
The clinical benefit of current anticancer regimens for lung cancer therapy is still limited due to moderate efficacy, drug resistance, and recurrence. Therefore, the development effective drugs first-line optimal second-line treatment necessary. Because 90-kDa molecular chaperone heat shock protein (Hsp90) contributes maturation numerous mutated or overexpressed oncogenic proteins, targeting Hsp90 may offer an therapy. Here, we investigated antitumor activities toxicity a novel...
Abstract Dynamic communication between hepatocytes and the environment is critical in hepatocellular carcinoma (HCC) development. Clinical immunotherapy against HCC currently unsatisfactory needs more systemic considerations, including identification of new biomarkers immune checkpoints. Transmembrane 4 L six family member 5 (TM4SF5) known to promote HCC, but it remains unclear how cancerous avoid surveillance whether avoidance can be blocked. We investigated TM4SF5-mediated hepatic...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSubstituent effects on the Claisen rearrangement. The accelerating effect of a 6-donor substituentDennis P. Curran and Young Ger SuhCite this: J. Am. Chem. Soc. 1984, 106, 17, 5002–5004Publication Date (Print):August 1, 1984Publication History Published online1 May 2002Published inissue 1 August 1984https://pubs.acs.org/doi/10.1021/ja00329a061https://doi.org/10.1021/ja00329a061research-articleACS PublicationsRequest reuse permissionsArticle...
Abstract The natural compound deguelin has promising preventive and therapeutic activity against diverse cancers by directly binding to heat shock protein-90 thus suppressing its function. Potential side effects of over a certain dose, however, could be substantial obstacle clinical use. To develop derivative(s) with reduced potential effects, we synthesized five analogues (SH-02, SH-03, SH-09, SH-14, SH-15) compared them the parent each other for structural biochemical features; solubility;...
// Vijayendra Agrawal 1 , Sony Maharjan Kyeojin Kim 2 Nam-Jung 3 Jimin Son Keunho Lee Hyun-Jung Choi Seung-Sik Rho Sunjoo Ahn 4 Moo-Ho Won 5 Sang-Jun Ha Gou Young Koh 6 Young-Myeong 7 Young-Ger Suh and Young-Guen Kwon Department of Biochemistry, College Life Science Biotechnology, Yonsei University, Seoul 120-749, Republic Korea, Pharmacy, National 599 Gwanak-ro, Gwanak-gu, 151-742, Kyung Hee 130-701, Korea Research Institute Chemical Technology (KRICT), 141 Gajeong-ro, Yuseong-gu, Daejeon...
Circadian rhythms, biological oscillations with a period of about 24 h, are maintained by an innate genetically determined time-keeping system called the molecular circadian clockwork. Despite physiological and clinical importance clock, development small molecule modulators targeting core clock machinery has only recently been initiated. BMAL1, gene, is controlled ROR/REV-ERB-response element (RORE)-dependent mechanism, which plays important role in stabilizing clock. Therefore, we aimed to...