• Journal of Integrative Natural Science
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• v.7 no.3
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• pp.159-165
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• 2014

Pyrazole, hydroxyimino, aldehyde and isoxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against Phospholipases $A_2$ enzyme. This enzymes has implicated as potential targets for anti-inflammatory drug design. co-crystal structure (PDB ID: 1POE) of $PLA_2$ deposited in Protein Data Bank has been retrieved for docking analysis. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• Journal of Environmental Health Sciences
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• v.30 no.5 s.81
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• pp.374-377
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• 2004

Dual actions are the most recently used delivery system in drug study. Dual-action agents are unique chemical entities comprised of two different type of antibacterial compounds covalently linked together in a single molecule in such a way that both components are able to exert their bactericidal properties. Crosslinked sulfadiazine-sulfanilamide such as antibiotics is synthesized by synthetic handle with glutaraldehyde. As a result, New synthetic antibacterial agent exhibited the broad antibacterial activities against Gram(+) and Gram(-) of 4 strains and a long durability supposing that the stomach and blood.

• Archives of Pharmacal Research
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• v.27 no.9
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• pp.978-983
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• 2004

The effects of glycyrrhizic acid (GLZ) on protein binding of diltiazem, verapamil, and nifedipine were investigated. Protein binding studies (human serum, human serum albumin (HSA) and (X1-acid glycoprotein (AAG)) were conducted using the equilibrium dialysis method with and without addition of GLZ. The binding parameters, such as the number of moles of bound drug per mole of protein, the number of binding sites per protein molecule, and the association con-stant, were estimated using the Scatchard plot. The serum binding of nifedipine, verapamil, and diltiazem was displaced with addition of GLZ, and the decreases of Ks for serum were observed. GLZ decreased the association constants of three drugs for HSA and AAG, while the binding capacity remained similar with addition of GLZ. Although the characteristics of interaction were not clear, GLZ seemed to mainly affect HSA binding of nifedipine rather than AAG binding, while GLZ seemed to affect both AAG- and HSA-bindings of verapamil and dilt-iazem resulting in a serum binding displacement.

• Journal of Integrative Natural Science
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• v.8 no.3
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• pp.204-208
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• 2015

Pyrazole, ${\beta}$-lactam, salicidine, pyren and oxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against COX-2 enzyme. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.8
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• pp.3561-3568
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• 2012

The calcium sensing receptor (CaSR) is a member of the largest family of cell surface receptors, the G protein-coupled receptors involved in calcium homeostasis. The role of the CaSR in neoplasia appears to be homeostatic; loss of normal CaSR-induced response to extracellular calcium is observed in cancers of the colon and ovary, while increased release of PTHrP is observed in cancers of the breast, prostate and Leydig cells. Currently CaSR can be considered as a molecule that can either promote or prevent tumor growth depending on the type of cancer. Therefore, recognition of the multifaceted role of CaSR in gliomas and other malignant tumors in general is fundamental to elucidating the mechanisms of tumor progression and the development of novel therapeutic agents. Emphasis should be placed on development of drug-targeting methods to modulate CaSR activity in cancer cells.

• BMB Reports
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• v.43 no.11
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• pp.711-719
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• 2010

Kinomics is an emerging and promising approach for deciphering kinomes. Chemical kinomics is a discipline of chemical genomics that is also referred to as "chemogenomics", which is derived from chemistry and biology. Chemical kinomics has become a powerful approach to decipher complicated phosphorylation-based cellular signaling networks with the aid of small molecules that modulate kinase functions. Moreover, chemical kinomics has played a pivotal role in the field of kinase drug discovery as it enables identification of new molecular targets of small molecule kinase modulators and/or exploitation of novel functions of known kinases and has also provided novel chemical entities as hit/lead compounds. In this short review, contemporary chemical kinomics technologies such as activity-based protein profiling, T7 kinasetagged phages, kinobeads, three-hybrid systems, fluorescenttagged kinase binding assays, and chemical genomic profiling are discussed along with a novel allosteric Bcr-Abl kinase inhibitor (GNF-2/GNF-5) as a successful application of chemical kinomics approaches.

• Journal of the Korean Applied Science and Technology
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• v.17 no.4
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• pp.267-272
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• 2000

Dual-actions are the most recently used delivery system in drug study. Dual-action agents are unique chemical entities comprised of two different type of antibacterial compounds covalently linked together in a single molecule in such a way that both components are able to exert their bactericidal properties. Crosslinked sulfadiazine-sulfanilamide such as antibiotics is synthesized by synthetic handle with glutaraldehyde. As a result, New synthetic antibacterial agent exhibited the broad antibacterial activities against gram(+) and gram(-) of 4 strains and a long durability supposing that the stomach and blood.

• Biomolecules & Therapeutics
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• v.20 no.1
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• pp.19-26
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• 2012

There are many cyclic peptides with diverse biological activities, such as antibacterial activity, immunosuppressive activity, and anti-tumor activity, and so on. Encouraged by natural cyclic peptides with biological activity, efforts have been made to develop cyclic peptides with both genetic and synthetic methods. The genetic methods include phage display, intein-based cyclic peptides, and mRNA display. The synthetic methods involve individual synthesis, parallel synthesis, as well as split-and-pool synthesis. Recent development of cyclic peptide library based on split-and-pool synthesis allows on-bead screening, in-solution screening, and microarray screening of cyclic peptides for biological activity. Cyclic peptides will be useful as receptor agonist/antagonist, RNA binding molecule, enzyme inhibitor and so on, and more cyclic peptides will emerge as therapeutic agents and biochemical tools.

• Archives of Pharmacal Research
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• v.19 no.3
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• pp.248-250
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• 1996

In conclusion, a series of N-Cbz-.alpha.-amono-glutarimides (1a-f), combining common structures such as N-CO-C-N and cyclic imide in a single molecule, were prepared from the (R)- or (S)-N-Cbz-glutamic acid and evaluated for their anticonvulsant activities in MES and PTZ tests in order to develope new and broad spectrum anticonvulsant. In this study, N-Cbz-.alpha.-aminoglutarimides (1) except ac and af, showed significant anticonvulsant activity in both MES and PTZ tests enough to be recommended as promising new anticonvulsant drug candidates. Now we are continuing to investigate further anticonvulsant test (quantification)for these compounds and synthesize their analogues in order to develop more active anticonvulsant and define the structure activity relationship more precisely.

• Proceedings of the Korean Vacuum Society Conference
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• 2013.08a
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• pp.87-87
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• 2013

The interface between nanomaterials and biosystems is emerging as one of the broadest and most dynamic areas of science and technology, bringing together biology, chemistry, physics and many areas of engineering, biomedicine. The combination of these diverse areas of research promised to yield revolutionary advances in healthcare, medicine, and life science. For example, the creation of new and powerful nanosensors that enable direct, sensitive, and rapid analysis of biological and chemical species can advance the diagnosis and treatment of disease, discovery and screening of new drug molecules. Nanowire based sensors are emerging as a powerful and general platform for ultrasensitive and multiplex detection of biological and chemical species. Here, we present the studies about noble metal nanowire sensors that can be used for sensitive detection of a wide-range of biological and chemical species including nucleic acids, proteins, and toxic metal ions. Moreover, the optical and electrochemical applications of noble metal nanowires are introduced. Noble metal nanowires are successfully used as plasmonic antennas and nanoelectrodes, thereby provide a pathway for a single molecule sensor, in vivo neural recording, and molecular injection and detection in a single living cell.