• Proceedings of the PSK Conference
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• 2002.10a
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• pp.342.2-342.2
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• 2002

The ${\beta}$-turn has been implicated as an important conformation for biological recognition of peptides or proteins. Benzodiazepine classes have been known as one of the non peptide ${\beta}$-turn mimic scaffolds. We have developed an efficient approach for the synthesis and derivatization of a scaffold of hydroxytetrahydrodizepinone class in order to screen compound library in various protein targets for new lead generations as well as for structure activity relationships of the scaffold. (omitted)

• BMB Reports
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• v.42 no.11
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• pp.743-746
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• 2009

L-ascorbic acid (Vitamin C) and peptide are both useful compounds for collagen biosynthesis in cosmeceuticals (cosmetic and pharmaceutical fields). The instability of these compounds, however, limit their application in these industries. In this report, we describe the development of a novel compound, Stabilized Ascorbyl Pentapeptide (SAP), which physically is much more stable than L-ascorbic acid in water. The inhibitory effects of this SAP compound on tyrosinase and melanin synthesis is comparable to that of L-ascorbic acid. Importantly, the SAP compound displays no cytotoxicity at a high concentration (5 mM). The ability of SAP to promote collagen biosynthesis is greater than that of L-ascorbic acid or the KTTKS peptide alone. Considering the in vitro stability and functional effects, our data strongly suggest that the SAP compound is a good candidate not only as a cosmetic ingredient, but also as a wound healing agent.

• Journal of Microbiology and Biotechnology
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• v.8 no.1
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• pp.34-41
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• 1998

A method was developed for the controlled expression of an antimicrobial peptide magainin in Escherichia coli. A series of concatemeric magainin genes was constructed with a gene amplification vector, and fused to the 3'end of malE gene encoding the affinity ligand, E. coli maltose-binding protein (MBP). The construct directed the synthesis of the fusion protein with the magainin polypeptide fused to the C-terminus of MBP. The fusion protein was expressed in a tightly regulatable expression system which was under the control of an invertible promoter. The MBP-fused magainin monomer was expressed efficiently. However, the expression level of the MBP-fused magainin in E. coli decreased with the increasing size of multimers possibly because of the transcription and translation inhibition by the multimeric peptides. After purification using an amylose affinity column, the fusion protein was digested by factor Xa at a specific cleavage site between the monomers. The recombinant magainin had an antimicrobial activity identical to that of synthetic magainin. This experiment shows that a biologically active, antimicrobial peptide magainin can be produced by fusing to MBP, along with a promoter inversion vector system.

• Korean Journal of Agricultural Science
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• v.41 no.3
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• pp.237-243
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• 2014

Human Glucagon like peptide-1 (GLP-1) is an incretin hormone that promotes secretion of insulin. In order to eliminate the formation of the soluble aggregate, Ala19 in GLP-1 was substituted with Thr, resulting in a GLP-1 mutant GLP-1A19T. The gene synthesis of GLP-1A19T and the fusion of 6-lysine tagged ubiquitin gene were accomplished by using the overlap extension polymerase chain reaction. The ubiquitin fused GLP-1A19T (K6UbGLP-1A19T) is expressed as form of inclusion body with little formation of the soluble aggregation in recombinant E. coli. In order to produce K6UbGLP-1A19T in large amounts, fed-batch fermentation was carried out in a pH-stat feeding strategy. Maximum dry cell weight of 87.7 g/L and 20.4% of specific K6UbGLP-1A19T content were obtained. Solid-phase refolding using a cation exchanger was carried out to renature K6UbGLP-1A19T. The refolded K6UbGLP-1A19T aggregated little and was released GLP-1A19T by on-column cleavage with ubiquitin-specific protease-1. The molecular mass of GLP-1A19T showed an accurate agreement with its theoretical molecular mass.

• Biomolecules & Therapeutics
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• v.20 no.3
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• pp.245-255
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• 2012

Amyloid-${\beta}$ peptide ($A{\beta}$) is still best known as a molecule to cause Alzheimer's disease (AD) through accumulation and deposition within the frontal cortex and hippocampus in the brain. Thus, strategies on developing AD drugs have been focused on the reduction of $A{\beta}$ in the brain. Since accumulation of $A{\beta}$ depends on the rate of its synthesis and clearance, the metabolic pathway of $A{\beta}$ in the brain and the whole body should be carefully explored for AD research. Although the synthetic pathway of $A{\beta}$ is equally important, we summarize primarily the clearance pathway in this paper because the former has been extensively reviewed in previous studies. The clearance of $A{\beta}$ from the brain is accomplished by several mechanisms which include non-enzymatic and enzymatic pathways. Nonenzymatic pathway includes interstitial fluid drainage, uptake by microglial phagocytosis, and transport across the blood vessel walls into the circulation. Multiple $A{\beta}$-degrading enzymes (ADE) implicated in the clearance process have been identified, which include neprilysin, insulin-degrading enzyme, matrix metalloproteinase-9, glutamate carboxypeptidase II and others. A series of studies on $A{\beta}$ clearance mechanism provide new insight into the pathogenesis of AD at the molecular level and suggest a new target for the development of novel therapeutics.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.28 no.3
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• pp.7-39
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• 2002

The extensive variation in human cutaneous pigmentation is mainly due to differences in the rate of melanin synthesis by epidermal melanocytes, the relative amounts of eumelanin and pheomelanin synthesized, and the manner and rate of transfer of melanosomes from melanocytes to keratinocytes. Pigmentation is a complex trait that is regulated genetically and environmentally. One gene that has been receiving a lot of attention is the gene for the melanocortin 1 receptor The extensive polymorphism of this gene in human populations suggests its significance in the diversity of pigmentation. Exposure to solar ultraviolet radiation (UV) results in increased synthesis of a variety of growth factors, cytokines and hormones, and in modulation of their receptors in the epidermis. Knowledge about the regulation of pigmentation has led to strategies for clinical treatment of hyperpigmented skin lesions. Three main strategies are: 1) the use of chemicals that interfere with the melanin synthetic pathway, 2) the design of peptides or peptide-mimetics based on the structure of hormones that regulate eumelanin synthesis, and 3) the use of agents that reduce melanosome transfer from melanocytes to keratinocytes. All three strategies are expected to induce hypopigmentation, by inhibiting total melanin synthesis, eumelanin production, or the epidermal melanin unit, respectively.

• Journal of the Korean Chemical Society
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• v.38 no.6
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• pp.449-455
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• 1994

In order to obtain the basic data for synthetic studies of bioactive peptide using enzyme, Kyotorphin(analgesic peptide) derivative was synthesized from Ac-Tyr-OH and $Arg-NH_2$ by $\alpha-chymotrysin$ in two phase system(organic phase and aqueous phase). In effect of organic solvent on Kyotorphin derivative synthesis from Ac-Tyr-OH(10 mM) and $Arg-NH_2$ (20 mM), the synthesis in ethyl acetate system of organic solvents was higher than those in other organic solvents (n-butanol, n-hexane, dichloromethane and chloroform). The optimal conditions for the synthesis are as follows: enzyme conc., 10 ${\mu}M;$ reaction pH, 7.0; reaction temp., $35^{\circ}C$ ; the ratio of organic phase volume/aqueous phase volume $(\alpha)$, 15. Under the optimal conditions, the yield was 70.2%, and the reaction achieved to equilibrium after 24 hrs.

• Polymer Science and Technology
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• v.23 no.3
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• pp.282-288
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• 2012

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.168.3-169
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• 2000

• Archives of Pharmacal Research
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• v.23 no.3
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• pp.211-221
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• 2000

L-3-Deoxymimosine-containing decapeptides were prepared for the development of protein tyrosine kinase (PTK) inhibitors. During the preparation of peptides, several side products were formed. identification and determination of major peptides generated were reported.