• Bulletin of the Korean Chemical Society
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• 제15권8호
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• pp.680-684
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• 1994

Pilocarpine analogs were prepared by empoying a radical cyclization reaction as a key step for the five-membered ring formation.

• Bulletin of the Korean Chemical Society
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• 제35권5호
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• pp.1365-1374
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• 2014

Thirteen analogs of tridecapeptide ${\alpha}$-factor (WHWLQLKPGQPMY) of Saccharomyces cerevisiae with C- or N-terminal Trp extension and isosteric replacement by Aib at position 8 and 11, Trp at position 13, D-Ala at position 9, and Orn and Glu at position 6 were synthesized and assayed for their biological activity. Receptor binding assay was carried out using our newly developed spectrophotometric method with detector peptide 14. C- or N-terminal extended analogs, ${\alpha}$-factor-$[Trp]_n$ (n =1-5) 1-5 and $[N-Trp]_1$-${\alpha}$-factor 6, were all less active than native ${\alpha}$-factor and gradual decreases in both activity and receptor affinity were observed with greater Trp extension. Trp-substituted analog at position 13, $[Trp^{13}]{\alpha}$-factor 7, exhibited about 2-fold reductions in both activity and receptor affinity. Aib-substituted analogs, $[Aib^8]{\alpha}$-factor 8 and $[Aib^{11}]{\alpha}$-factor 9, showed 5- to 10-fold reduction in activity as well as 3-fold reduction in receptor affinity compared to native ${\alpha}$-factor. $[Orn^6]{\alpha}$-factor 10 demonstrated strong potency with a 7.0-fold increase in halo activity as well as 1.8-fold increase in receptor affinity compared to native ${\alpha}$-factor. For two double substituted analogs, [$Glu^6,{\small{D}}-Ala^9$]${\alpha}$-factor 12 showed the slightly decreased potency in halo activity compared to analog 10, whereas [$Orn^6,{\small{D}}-Ala^9$]${\alpha}$-factor 11 exhibited 15-fold higher halo activity as well as nearly 3-fold higher receptor affinity compared to native ${\alpha}$-factor.

• 한국미생물·생명공학회지
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• 제40권4호
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• pp.409-413
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• 2012

인돌리시딘(indolicidin)은 소의 호중구(bovine neutrophils)로 부터 분리된 13개의 아미노산 잔기로 이루어 지고, 트립토판(tryptophan)을 많이 함유한 항균 펩타이드(antimicrobial peptide)이다. 인돌리시딘은 강력한 항균활성과 더불어 mammalian cells에 대해 독성을 나타낸다. 본 연구에서는 인돌리시딘 보다 서열이 짧으며, 보다 증가된 원핵세포 선택성(박테리아세포에 대해 독성을 나타내지만 mammalian cells에 대해서는 독성을 나타내지 않음을 의미함)을 지닌 새로운 짧은 항균 펩타아드를 개발하기 위해, 몇 종의 인돌리시딘 유사체 펩타이드를 설계하고 합성하였다. 결과적으로, 인돌리시딘 보다 서열이 짧으며(10개의 아미노산 잔기로 이루어짐), 증가된 원핵세포선택성을 지닌 4종의 새로운 펩타이드(SI, SI-PA, SI-WF 및 SI-WL)를 개발하였다. 본 연구를 통하여 가장 높은 원핵세포선택성을 나타내는 인돌리시딘 유사체 펩타이드 SI의 항균활성에는 중앙부위에 위치하는 소수성 및 방향족 아미노산이 중요하며, 2군데의 프로린(proline) 잔기는 중요하지 않다는 것을 알았다. 인돌리시딘과 유사체 펩타이드에 대한 원핵세포 선택성은 SI>SI-PA>SI-WF>SI-WL>ID>SI-WA의 순서 이였다. 따라서, 본 연구에서 설계되고 합성한 4종의 인돌리시딘 유사체 펩타이드(SI, SI-PA, SI-WF 및 SI-WL)는 박테리아 감염의 치료제로서 개발될 수 있을 것이다.

• 한국과학교육학회지
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• 제19권4호
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• pp.645-652
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• 1999

비유물의 개수, 출처 및 제시 순서가 중학생들의 과학 개념 회상 및 응용에 미치는 효과를 조사하였다. 비유물의 개수(1개/2개)와 출처(일상/과학)에 따라 네 종류의 학습 교재를 제작하여 예비 연구를 통해 수정하였다. 수업 처치 이전에 장의존성/독립성 검사를 실시하여 구획 변인으로 사용하였다. 88명의 중학생들에게 네 가지 유형의 학습 교재를 무선 배포하여 읽게 한 직후 과학 개념 회상 및 응용 검사를 실시하고, 4주 후에 개념의 파지 검사를 실시하였다. 비유물의 개수, 출처 및 제시 순서가 과학 개념 회상 및 응용에 미치는 주효과는 없었다. 파지 개념 응용 검사에서 학습자의 장의존성/독립성에 따라 비유물의 개수 및 비유물의 제시 순서가 과학 개념 회상 및 응용에 미치는 상호작용 효과가 나타났다. 즉, 장독립적인 학습자는 비유물을 한 개 사용하였을 때보다 두 개 사용하였을 때 더 높았고, 비유물을 두 개 사용할 경우 장의존적 학습자는 과학 일상 비유물의 순서보다 일상-과학 비유물의 순서로 제시했을 때 더 높았다.

• Bulletin of the Korean Chemical Society
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• 제31권4호
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• pp.874-880
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• 2010

A series of 13- and 14-membered cyclic enkephalin analogs based on the moderately $\mu$ selective prototype compound Tyr-C[D-$A_2bu$-Gly-Phe-Leu] 8a were synthesized to investigate the structure-activity relationship. The modifications of sequence were mainly focused on two positions 3 and 5, critical for the selective recognition for $\mu$ and $\delta$ opioid receptors. The substitution of hydrophobic $Leu^5$ with hydrophilic $Asp^5$ derivatives led to Tyr-C[D-$A_2bu$-Gly-Phe-Asp(N-Me)] 7 and Tyr-C[D-Glu-Phe-gPhe-rAsp(O-Me)] 5, the peptides with a large affinity losses at both $\mu$ and $\delta$ receptors. The substitution of $Phe^3$ with $Gly^3$ led to Tyr-C[D-Glu-Gly-gPhe-rLeu] 3 and Tyr-C[D-Glu-Gly-gPhe-D-rLeu] 4, the peptides with large affinity losses at $\mu$ receptors, indicating the critical role of phenyl ring of $Phe^3$ for $\mu$ receptor affinities. One atom reduction of the ring size from 14-membered analogs Tyr-C[D-Glu-Phe-gPhe-(L and D)-rLeu] 6a, 6b to 13-membered analogs Tyr-C[D-Asp-Phe-gPhe-(L and D)-rLeu] 1, 2 reduced the affinity at both $\mu$ and $\delta$ receptors, but increased the potency in the nociceptive assay, indicating the ring constrain is attributed to high nociceptive potency of the analogs. For the influence of D- or L-chirality of $Leu^5$ on the receptor selectivity, regardless of chirality and ring size, all cyclic diastereomers displayed marked $\mu$ selectivity with low potencies at the $\delta$ receptor. The retro-inverso analogs display similar or more active at $\mu$ receptor, but less active at $\delta$ receptor than the parent analogs.

• Journal of Microbiology and Biotechnology
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• 제31권1호
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• pp.144-153
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• 2021

Organophosphorus nerve agents (OPNAs), including both G- and V-type nerve agents such as sarin, soman, tabun and VX, are extremely neurotoxic organophosphorus compounds. Catalytic bioscavengers capable of hydrolyzing OPNAs are under development because of the low protective effects and adverse side effects of chemical antidotes to OPNA poisoning. However, these bioscavengers have certain limitations for practical application, including low catalytic activity and narrow specificity. In this study, we generated a fusion-hybrid form of engineered recombinant human paraoxonase 1 (rePON1) and bacterial organophosphorus hydrolase (OPH), referred to as GV-hybrids, using a flexible linker to develop more promising catalytic bioscavengers against a broad range of OPNAs. These GV-hybrids were able to synergistically hydrolyze both G-type OPNA analogs (paraoxon: 1.7 ~ 193.7-fold, p-nitrophenyl diphenyl phosphate (PNPDPP): 2.3 ~ 33.0-fold and diisopropyl fluorophosphates (DFP): 1.4 ~ 22.8-fold) and V-type OPNA analogs (demeton-S-methyl (DSM): 1.9 ~ 34.6-fold and malathion: 1.1 ~ 4.2-fold above) better than their individual enzyme forms. Among the GV-hybrid clones, the GV7 clone showed remarkable improvements in the catalytic activity toward both G-type OPNA analogs (kcat/Km (106 M-1 min-1): 59.8 ± 0.06 (paraoxon), 5.2 ± 0.02 (PNPDPP) and 47.0 ± 6.0 (DFP)) and V-type OPNA analogs (kcat/Km (M-1 min-1): 504.3 ± 48.5 (DSM) and 1324.0 ± 47.5 (malathion)). In conclusion, we developed GV-hybrid forms of rePON1 and bacterial OPH mutants as effective and suitable catalytic bioscavengers to hydrolyze a broad range of OPNA analogs.

• 대한치과보철학회지
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• 제40권3호
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• pp.287-295
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• 2002

Statement of Problem. Endodontically treated teeth frequently required posts and cores to provide retention and resistance form for crowns. In spite of excellent mechanical properties of metal post and core, its metallic color can be detected through all ceramic restorations occasionally. To solve esthetic problems of metal post and core zirconia post system has been introduced recently. Purpose. The purpose of this study was to examine the fracture strength and mode of resin root analogs restored with zirconia, gold and titanium posts with resin, ceramic and metal cores after cementation with metal crowns. Materials and methods. To avoid the morphological variations of natural teeth, 40 root analogs were fabricated with composite resin. Forty resin root analogs were randomly assigned to four groups according to post and core materials: Group A: cast gold post and core and complete cast crowns, as control. Group B: titanium posts (Parapost, Coltent/Whaledent Inc., NJ, USA) and composite resin cores. Group C: zirconia posts (Cosmopost, Ivoclar AG, Schaan/Liechtenstein) and composite resin cores Group D: zirconia posts and heat-pressed ceramic cores (IPS Empress Cosmo Ingots, Ivoclar AG) After thermocycling ($5^{\circ}C{\sim}55^{\circ}C$, 30 sec.), cyclic loading was applied at 3mm below the incisal edge on the palatal surfaces at an angle of 135 degree to the long axis (2Hz, 50N, 50000cycles). Fracture strength was measured by universal testing machine (Instron, High Wycombe, UK) and fracture pattern of restored resin root analogs was also evaluated. Results and conclusion. Within the limitations of this study following results were drawn. 1. Resin root analogs restored with zirconia posts and composite resins demonstrated lowest fracture strength among tested groups. 2. There was no significant difference in the fracture strength between zirconia posts and heat pressed glass ceramic cores and cast gold posts and cores 3. The fracture strength of resin root analogs restored with titanium posts and composite resin cores was lower than that of gold posts and cores. 4. The deep oblique fracture lines were dominantly observed in root analogs restored with cast gold post and core and zirconia post and heat-pressed ceramic core groups.

• Archives of Pharmacal Research
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• 제24권1호
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• pp.39-43
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• 2001

4'-Bromoacetophenone analogs, which are able to generate monophenyl radicals capable of hydrogen atom abstraction, were investigated as possible photoinducible DNA cleaving agents. The potential of 4'-Bromoacetophenone as a possible new DNA cleaver is explored. Pyrrolecarboxatmid conjugated 4'-Bromoacetophenone, in particular, DNA cleaving activity and sequence-selectivity on the contiguous AT base pair sites.

• Archives of Pharmacal Research
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• 제20권2호
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• pp.197-199
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• 1997

In conclusion, benzotriazole analogs prepared in this research showed strong possibility to be photochemically activated DNA cleaving agents. Electrophilic groups such as haloacetoxy groups on the alkyl chain of benzotriazole analogs promote the DNA cleaving ability. Synthesis of 1-(2-Naphthoyl) Benzotriazoles.

• Bulletin of the Korean Chemical Society
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• 제25권8호
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• pp.1269-1272
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• 2004