• Title/Summary/Keyword: Protein drug

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Potentiometric Sensor for the Determination of Dibucaine in Pharmaceutical Preparations and Electrochemical Study of the Drug with BSA

  • Ensafi, Ali A.;Allafchian, A.R.
    • Bulletin of the Korean Chemical Society
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    • v.32 no.8
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    • pp.2722-2726
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    • 2011
  • Plasticized poly(vinyl chloride), PVCs, with different membrane compositions tested for use in the construction of an ion-selective sensor for the determination dibucaine. A prepared membrane with dioctyl phthalate-PVC and ion-pair of N-(1-naphthyl)ethylenediamine dihydrochloride-tetraphenyl borate had a good potential to acts as a potentiometric sensor for the analysis of dibucaine. A linear relationship was obtained between potential and logC varying between $1.0{\times}10^{-6}$ and $1.0{\times}10^{-2}$ M dibucaine with a good repeatability and reproducibility. The sensor was applied for the determination of the drug in pharmaceuticals and biological fluids such as plasma and urine samples with satisfactory results. The drug electrode has also been used to study the interaction of bovine serum albumin (BSA) with dibucaine. The saturated quantities of dibucaine binding were 13.04, 5.30 and 9.70 mol/mol in 0.01, 0.02 and 0.1% of protein, respectively.

The Structure-Based Three-Dimensional Pharmacophore Models for Arabidopsis thaliana HPPD inhibitors as Herbicide

  • Cho, Jae Eun;Kim, Jun Tae;Kim, Eunae;Ko, Young Kwan;Kang, Nam Sook
    • Bulletin of the Korean Chemical Society
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    • v.34 no.10
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    • pp.2909-2914
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    • 2013
  • p-Hydroxyphenylpyruvate dioxygenase (HPPD) is a potent herbicide target that is in current use. In this study, we developed a predictive pharmacophore model that uses known HPPD inhibitors based on a theoretically constructed HPPD homology model. The pharmacophore model derived from the three-dimensional (3D) structure of a target protein provides helpful information for analyzing protein-ligand interactions, leading to further improvement of the ligand binding affinity.

Drug-drug Interactions between Psychotropic Agents and Other Drugs in Physically Ill Patients - Experience of Consultation-liason in Korea University Hospital - (내외과계 환자의 정신과 약물치료에서 약물-약물 상호작용 - 고려대학교 부속병원의 자문조정의 경험을 통하여 -)

  • Lee, Min Soo;Lee, Heon-Jeong
    • Korean Journal of Biological Psychiatry
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    • v.6 no.1
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    • pp.49-66
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    • 1999
  • Polypharmacotherapy, both psychotropic and nonpsychotropic, is widespread in various situations including psychiatric hospitals and general hospitals. As the clinical practice of using more than one drug at a time increase, the clinician is faced with ever-increasing number of potential drug interactions. Although many interactions have little clinical significances, some may interfere with treatment or even be life-threatening. The objective of this review is evaluation for drug-drug interactions often encountered in psychiatric consultation. Drug interactions can be grouped into two principal subdivisions : pharmacokinetic and pharmacodynamic. These subgroups serve to focus attention on possible sites of interaction as a drug moves from the site of administration and absorption to its site of action. Pharmacokinetic processes are those that include transport to and from the receptor site and consist of absorption, distribution on body tissue, plasma protein binding, metabolism, and excretion. Pharmacodynamic interactions occur at biologically active sites. In psychiatric consultation, these two subdivisions of drug interactions between psychotropic drugs and other drugs are likely to happen. We gathered informations of the drugs used in physically ill patients who are consulted to psychiatric department in Korea University Hospital. And we reviewed the related literatures about the drug-drug interactions between psychotropic drugs and other drugs.

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Recent advances in utilization of photochemical internalization (PCI) for efficient nano carrier mediated drug delivery

  • Park, Wooram;Park, Sin-Jung;Lee, Jun;Na, Kun
    • Biomaterials and Biomechanics in Bioengineering
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    • v.2 no.1
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    • pp.1-13
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    • 2015
  • Despite recent progresses in nanoparticle-based drug delivery systems, there are still many unsolved limitations. Most of all, a major obstacle in current nanoparticle-based drug carrier is the lack of sufficient drug delivery into target cells due to various biological barriers, such as: extracellular matrix, endolysosomal barrier, and drug-resistance associated proteins. To circumvent these limitations, several research groups have utilized photochemical internalization (PCI), an extension of photodynamic therapy (PDT), in design of innovative and efficient nano-carriers drug delivery. This review presents an overview of a recent research on utilization of PCI in various fields including: anti-cancer therapy, protein delivery, and tissue engineering.

Characterization of alginate/carboxymethyl scleroglucan hydrogels as a delivery system for protein drug

  • Lee, Chang-Moon;Park, Jeong-Eun;Kim, Dong-Woon;Rhee, Joon-Haeng;Kim, Gwang-Yun;Lee, Ki-Young
    • 한국생물공학회:학술대회논문집
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    • 2005.04a
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    • pp.580-583
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    • 2005
  • The aim of this study was to prepare a hydrogels composed of alginate blended with a carboxymethyl scleroglucan (CMSC) and evaluate the feasibility of the hydrogels as a drug delivery system for a protein. The main advantage of the alginate/CMSC hydrogels is to improve a restricted drug release from alginate hydrogels. The CMSC was chemically synthesized with chloroacetic acid and confirmed using a FT-IR. The alginate/CMSC hydrogels were prepared at distinct compositions by crosslinking with calcium ions. The swelling ratios of these hydrogels increased significantly with increasing the content of CMSC. At pH 7.4, the swelling ratios of the hydrogels increased remarkably as compared to those at pH 1.2. In ovalbumin (OVA) release test, the amount of OVA released from the hydrogels showed higher as compared to those released at pH 1.2. In addition, the release of OVA was improved with increasing the content of CMSC. Thus, the alginate/CMSC hydrogels may be used as a potential system for oral delivery of protein drugs.

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Structure-Based Virtual Screening of Protein Tyrosine Phosphatase Inhibitors: Significance, Challenges, and Solutions

  • Reddy, Rallabandi Harikrishna;Kim, Hackyoung;Cha, Seungbin;Lee, Bongsoo;Kim, Young Jun
    • Journal of Microbiology and Biotechnology
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    • v.27 no.5
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    • pp.878-895
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    • 2017
  • Phosphorylation, a critical mechanism in biological systems, is estimated to be indispensable for about 30% of key biological activities, such as cell cycle progression, migration, and division. It is synergistically balanced by kinases and phosphatases, and any deviation from this balance leads to disease conditions. Pathway or biological activity-based abnormalities in phosphorylation and the type of involved phosphatase influence the outcome, and cause diverse diseases ranging from diabetes, rheumatoid arthritis, and numerous cancers. Protein tyrosine phosphatases (PTPs) are of prime importance in the process of dephosphorylation and catalyze several biological functions. Abnormal PTP activities are reported to result in several human diseases. Consequently, there is an increased demand for potential PTP inhibitory small molecules. Several strategies in structure-based drug designing techniques for potential inhibitory small molecules of PTPs have been explored along with traditional drug designing methods in order to overcome the hurdles in PTP inhibitor discovery. In this review, we discuss druggable PTPs and structure-based virtual screening efforts for successful PTP inhibitor design.

Mechanisms involved in adenosine pharmacological preconditioning-induced cardioprotection

  • Singh, Lovedeep;Kulshrestha, Ritu;Singh, Nirmal;Jaggi, Amteshwar Singh
    • The Korean Journal of Physiology and Pharmacology
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    • v.22 no.3
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    • pp.225-234
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    • 2018
  • Adenosine is a naturally occurring breakdown product of adenosine triphosphate and plays an important role in different physiological and pathological conditions. Adenosine also serves as an important trigger in ischemic and remote preconditioning and its release may impart cardioprotection. Exogenous administration of adenosine in the form of adenosine preconditioning may also protect heart from ischemia-reperfusion injury. Endogenous release of adenosine during ischemic/remote preconditioning or exogenous adenosine during pharmacological preconditioning activates adenosine receptors to activate plethora of mechanisms, which either independently or in association with one another may confer cardioprotection during ischemia-reperfusion injury. These mechanisms include activation of $K_{ATP}$ channels, an increase in the levels of antioxidant enzymes, functional interaction with opioid receptors; increase in nitric oxide production; decrease in inflammation; activation of transient receptor potential vanilloid (TRPV) channels; activation of kinases such as protein kinase B (Akt), protein kinase C, tyrosine kinase, mitogen activated protein (MAP) kinases such as ERK 1/2, p38 MAP kinases and MAP kinase kinase (MEK 1) MMP. The present review discusses the role and mechanisms involved in adenosine preconditioning-induced cardioprotection.

Development and Applications of Proteomics Technology (Proteomics 기술의 개발 및 응용)

  • 이지원;이은규
    • KSBB Journal
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    • v.16 no.2
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    • pp.99-106
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    • 2001
  • Proteomics research includes identification and quantitation of single protein and/or protein complex, profiling of protein expression changes in response to biological perturbations, characterization of protein functions and interactions, and elucidation the linkage between proteins and diseases. In this review paper, recent developments in the basic technologies involved in the proteomics research such as 2-dimensional PAGE and mass spectrometry are discussed. Also, the application areas of proteomics technology such as protein expression mapping and cell map proteomics are introduced with the focus on new drug development.

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Proteomics in Drug Discovery

  • Mathews, W. Rodney
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.73-73
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    • 2002
  • The study of the protein complement of the genome, or proteome, represents an important new avenue for drug discovery. Proteomics research aims to quantify and characterize all of the expressed proteins in a biological system, and to determine the effect of various perturbations of the system on the expressed proteins. (omitted)

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In Vitro Infectivity Assessment by Drug Susceptibility Comparison of Recombinant Leishmania major Expressing Enhanced Green Fluorescent Protein or EGFP-Luciferase Fused Genes with Wild-Type Parasite

  • Sadeghi, Somayeh;Seyed, Negar;Etemadzadeh, Mohammad-Hossein;Abediankenari, Saeid;Rafati, Sima;Taheri, Tahereh
    • Parasites, Hosts and Diseases
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    • v.53 no.4
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    • pp.385-394
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    • 2015
  • Leishmaniasis is a worldwide uncontrolled parasitic disease due to the lack of effective drug and vaccine. To speed up effective drug development, we need powerful methods to rapidly assess drug effectiveness against the intracellular form of Leishmania in high throughput assays. Reporter gene technology has proven to be an excellent tool for drug screening in vitro. The effects of reporter proteins on parasite infectivity should be identified both in vitro and in vivo. In this research, we initially compared the infectivity rate of recombinant Leishmania major expressing stably enhanced green fluorescent protein (EGFP) alone or EGFP-luciferase (EGFP-LUC) with the wild-type strain. Next, we evaluated the sensitivity of these parasites to amphotericin B (AmB) as a standard drug in 2 parasitic phases, promastigote and amastigote. This comparison was made by MTT and nitric oxide (NO) assay and by quantifying the specific signals derived from reporter genes like EGFP intensity and luciferase activity. To study the amastigote form, both B10R and THP-1 macrophage cell lines were infected in the stationary phase and were exposed to AmB at different time points. Our results clearly revealed that the 3 parasite lines had similar in vitro infectivity rates with comparable parasite-induced levels of NO following interferon-${\gamma}$/lipopolysaccharide induction. Based on our results we proposed the more reporter gene, the faster and more sensitive evaluation of the drug efficiency.