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Cytotoxicities and Quantitative Structure Activity Relationships of B13 Sulfonamides in HT-29 and A549 Cells

Lee SK, Park SM, Im C

B13 analogues are being considered as therapeutic agents for cancer cells, since B13 is a ceramide analogue and inhibits ceramidase to promote apoptosis in cancer cells. B13 sulfonamides are assumed...
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A molecular model of a point mutation (Val297Met) in the serine protease domain of protein C

Song KS, Park YS, Choi JR, Kim HK, Park Q

  • KMID: 755027
  • Exp Mol Med.
  • 1999 Mar;31(1):47-51.
A heterozygous GTG to ATG (Val297Met) mutation was detected in a patient with inherited protein C deficiency and deep vein thrombosis. Cosegregation of the mutation with protein C deficiency was observed through...
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Poor Prognostic Implication of ASXL1 Mutations in Korean Patients With Chronic Myelomonocytic Leukemia

Kim HY, Lee KO, Park S, Jang JH, Jung CW, Kim SH, Kim HJ

BACKGROUND: Molecular genetic abnormalities are observed in over 90% of chronic myelomonocytic leukemia (CMML) cases. Recently, several studies have demonstrated the negative prognostic impact of ASXL1 mutations in CMML patients....
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Cytotoxic Activity and Structure Activity Relationship of Ceramide Analogues in Caki-2 and HL-60 Cells

Kim YJ, Kim EA, Sohn UD, Yim CB, Im C

B13, a ceramide analogue, is a ceramidase inhibitor and induces apoptosis to give potent anticancer activity. A series of thiourea B13 analogues was evaluated for their in vitro cytotoxic activities...
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A model for the reaction mechanism of the transglutaminase 3 enzyme

Ahvazi B, Steinert P

  • KMID: 1109310
  • Exp Mol Med.
  • 2003 Aug;35(4):228-242.
Transglutaminase enzymes (TGases) catalyze the calcium dependent formation of an isopeptide bond between protein-bound glutamine and lysine substrates. Previously we have shown that activated TGase 3 acquires two additional calcium...
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Cytotoxicity and Structure-activity Relationships of Naphthyridine Derivatives in Human Cervical Cancer, Leukemia, and Prostate Cancer

Hwang YJ, Chung ML, Sohn UD, Im C

Naphthyridine compounds are important, because they exhibit various biological activities including anticancer, antimicrobial, and anti-inflammatory activity. Some naphthyridines have antimitotic effects or demonstrate anticancer activity by inhibiting topoisomerase II. These...
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Molecular pharmacological interaction of phenylbutazone to human neutrophil elastase

Kang K

  • KMID: 1849847
  • Korean J Physiol Pharmacol.
  • 1998 Jun;2(3):385-393.
Human neutrophil elastase (HNElastase, EC 3.4.21.37), a causative factor of inflammatory diseases, was purified by Ultrogel AcA54 gel filtration and CM-Sephadex ion exchange chromatography. HNElastase was inhibited by phenylbutazone in a concentration dependent...
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Development of semi-empirical model for radiochemical reactions

Lee RJ, Suh HS

A mathematical model, which represents the radio-chemical reactions in water, was developed to study the effect of the radio-chemical products on cell kiling. The five differential equations were solved using...
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WNKs: protein kinases with a unique kinase domain

Huang CL, Cha SK, Wang HR, Xie J, Cobb MH

  • KMID: 1090959
  • Exp Mol Med.
  • 2007 Oct;39(5):565-573.
WNKs (with-no-lysine [K]) are a family of serine-threonine protein kinases with an atypical placement of the catalytic lysine relative to all other protein kinases. The roles of WNK kinases in...
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Identification and Molecular Characterization of Parkin in Clonorchis sinensis

Bai X, Kim TI, Lee JY, Dai F, Hong SJ

Clonorchis sinensis habitating in the bile duct of mammals causes clonorchiasis endemic in East Asian countries. Parkin is a RING-between-RING protein and has E3-ubiquitin ligase activity catalyzing ubiquitination and degradation...
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Non-syndromic hearing loss caused by the dominant cis mutation R75Q with the recessive mutation V37I of the GJB2 (Connexin 26) gene

Kim J, Jung J, Lee MG, Choi JY, Lee KA

GJB2 alleles containing two cis mutations have been rarely found in non-syndromic hearing loss. Herein, we present a Korean patient with non-syndromic hearing loss caused by the R75Q cis mutation...
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Homo-dimerization of RyR1 C-terminus via charged residues in random coils or in an alpha-helix

Lee EH, Allen PD

  • KMID: 1090962
  • Exp Mol Med.
  • 2007 Oct;39(5):594-602.
To investigate the mechanism by which the C-terminus (4,938-5,037) of the ryanodine receptor 1 (RyR1) homo-tetramerizes, forming a functional Ca2+ -release channel, the structural requirements for the tetramerization were studied...
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Molecular characteristics of the inhibition of human neutrophil elastase by nonsteroidal antiinflammatory drugs

Kang K, Bae SJ, Kim WM, Lee DH, Cho US, Lee MS, Lee MH, Nam SI, Kuettner K, Schwartz D

  • KMID: 755079
  • Exp Mol Med.
  • 2000 Sep;32(3):146-154.
Nonsteroidal antiinflammatory drugs(NSAIDs) are known as clinically effective agents for treatment of inflammatory diseases. Inhibition of cyclooxygenase has been thought to be a major facet of the pharmacological mechanism of...
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The N-terminal 1-16 peptide derived in vivo from protein seminal vesicle protein IV modulates alpha-thrombin activity: potential clinical implications

Lepretti M, Costantini S, Ammirato G, Giuberti G, Caraglia M, Facchiano , Metafora S, Stiuso P

We have previously shown that seminal vesicle protein IV (SV-IV) and its 1-70 N-terminal fragment have anti-inflammatory activity and modulate anti-thrombin III (AT) activity. Moreover, mass spectrometry analysis of purified...
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In Vitro and In Vivo Effect of Parathyroid Hormone Analogue (1-14) Containing alpha-amino-iso-butyric Acid Residue (Aib)1,3

Rhee Y, Lee W, Lee EJ, Ma S, Park SY, Lim SK

Firstly, parathyroid hormone (1-14) [PTH (1-14)] analogue containing various alpha-amino-iso-butyric acid residue (Aib) was synthesized by exchanging the 1st and 3rd Ala residues of alpha carbon of PTH (1-14). This...
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Structure-activity relationships of anti-HIV-1 peptides with disulfide linkage between D- and L-cysteine at positions i and i+3, respectively, derived from HIV-1 gp41 C-peptide

Lee MK, Kim HK, Lee TY, Hahm KS, Kim KL

  • KMID: 1105273
  • Exp Mol Med.
  • 2006 Feb;38(1):18-26.
The constrained alpha-helical structure of a C-peptide is useful for enhancing anti-HIV-1 activity. The i and i+3 positions in an alpha-helical structure are located close together, therefore D-Cys (dC) and...
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EF-hand like Region in the N-terminus of Anoctamin 1 Modulates Channel Activity by Ca²⁺ and Voltage

Tak MH, Jang Y, Son WS, Yang YD, Oh U

Anoctamin1 (ANO1) also known as TMEM16A is a transmembrane protein that functions as a Ca²⁺ activated chloride channel. Recently, the structure determination of a fungal Nectria haematococca TMEM16 (nhTMEM16) scramblase...
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Atg3-Mediated Lipidation of Atg8 Is Involved in Encystation of Acanthamoeba

Moon EK, Chung DI, Hong Y, Kong HH

Autophagy is a catabolic process involved in the degradation of a cell's own components for cell growth, development, homeostasis, and the recycling of cellular products. Autophagosome is an essential component...
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Magnolol Inhibits LPS-induced NF-kappaB/Rel Activation by Blocking p38 Kinase in Murine Macrophages

Li MH, Kothandan , Cho SJ, Huong PT, Nan YH, Lee KY, Shin SY, Yea SS, Jeon YJ

This study demonstrates the ability of magnolol, a hydroxylated biphenyl compound isolated from Magnolia officinalis, to inhibit LPS-induced expression of iNOS gene and activation of NF-kappaB/Rel in RAW 264.7 cells....
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Inhibition of Nuclear Receptor Binding SET Domain 2/Multiple Myeloma SET Domain by LEM-06 Implication for Epigenetic Cancer Therapies

di Luccio

BACKGROUND: Multiple myeloma SET domain (MMSET)/nuclear receptor binding SET domain 2 (NSD2) is a lysine histone methyltransferase (HMTase) and bona fide oncoprotein found aberrantly expressed in several cancers, suggesting potential...
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