• 제목/요약/키워드: Covalent

검색결과 367건 처리시간 0.022초

Conductance Study on the Characteristics of Solution Containing Crown Ethers and Univalent Cation Perchlorates

  • Lee, Shim-Sung;Park, Sung-Oh;Jung, Jong-Hwa;Lee, Bu-Yong;Kim, Si-Joong
    • Bulletin of the Korean Chemical Society
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    • 제11권4호
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    • pp.276-281
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    • 1990
  • The equivalent conductance of univalent cation (potassium, silver, thallium and ammonium) perchlorates in methanol containing 18-membered crown ethers, 18-crown-6 (18C6) and 1,10-dithia-18-crown-6 (DT18C6) were measured at different temperatures. The equivalent conductances of ammonium perchlorate were increased by increasing content of DT18C6 exceptionally, due to more favorable solvations than complexations. From the equivalent conductance changes, the formation constants for 1:1 compmlexes have been determined, and the values of enthalpy and entropy changes have been calculated. The complexations of 18C6 and DT18C6 with the univalent cations under investigation are all exothermic and the ${\Delta}$S values are all negative and no considerable differences around 50 J/ (k mol). The selectivity order of 18C6 is $K^+ > Tl^+ > Ag^+ > NH_4^+$, while that of DT18C6 is $Ag^+ > Tl^+ > NH_4^+ > K^+$. By sulfur substitutions in 18C6 result in significant decrease in stability, but the stability of $Ag^+$-DT18C6 complex are $10^4$ times larger than those of $K^+$. This increase of stabilities for $Ag^+$-DT18C6 complex are primary due to the result of favorable exothermic heat of reaction between the polarizable soft cation and soft sulfur centers. In NMR experiment, the stepwise additions of cation perchlorates into crown ether solutions induced two major spectral changes. First, the resonance all shift down field and the cation induced shifts were linear up to 1:1 cation/crown ratio, above which no further changes were observed. On the basis of these results, it could be concluded that 1:1 complex is formed. Second, the magnitudes of cation induced shifts were different each other in same ligand. By addition of silver ion to the solution of DT18C6, the largest shift of proton peak near the sulfur atom was observed. These effects are also arisen from the results of covalent bonding between "soft-soft" interactions.

Chronicles of EGFR Tyrosine Kinase Inhibitors: Targeting EGFR C797S Containing Triple Mutations

  • Duggirala, Krishna Babu;Lee, Yujin;Lee, Kwangho
    • Biomolecules & Therapeutics
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    • 제30권1호
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    • pp.19-27
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    • 2022
  • Epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase widely expressed in many cancers such as non-small cell lung cancer (NSCLC), pancreatic cancer, breast cancer, and head and neck cancer. Mutations such as L858R in exon 21, exon 19 truncation (Del19), exon 20 insertions, and others are responsible for aberrant activation of EGFR in NSCLC. First-generation EGFR tyrosine kinase inhibitors (TKIs) such as gefitinib and erlotinib have clinical benefits for EGFR-sensitive (L858R and Del19) NSCLC patients. However, after 10-12 months of treatment with these inhibitors, a secondary T790M mutation at the gatekeeper position in the kinase domain of EGFR was identified, which limited the clinical benefits. Second-generation EGFR irreversible inhibitors (afatinib and dacomitinib) were developed to overcome this T790M mutation. However, their lack of selectivity toward wild-type EGFR compromised their clinical benefits due to serious adverse events. Recently developed third-generation irreversible EGFR TKIs (osimertinib and lazertinib) are selective toward driving mutations and the T790M mutation, while sparing wild-type EGFR activity. The latest studies have concluded that their efficacy was also compromised by additional acquired mutations, including C797S, the key residue cysteine that forms covalent bonds with irreversible inhibitors. Because second- and third-generation EGFR TKIs are irreversible inhibitors, they are not effective against C797S containing EGFR triple mutations (Del19/T790M/C797S and L858R/T790M/C797S). Therefore, there is an urgent unmet medical need to develop next-generation EGFR TKIs that selectively inhibit EGFR triple mutations via a non-irreversible mechanism.

Role of modifiers on the structural, mechanical, optical and radiation protection attributes of Eu3+ incorporated multi constituent glasses

  • Poojha, M.K. Komal;Marimuthu, K.;Teresa, P. Evangelin;Almousa, Nouf;Sayyed, M.I.
    • Nuclear Engineering and Technology
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    • 제54권10호
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    • pp.3841-3848
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    • 2022
  • The effect of modifiers on the optical features and radiation defying ability of the Eu3+ ions doped multi constituent glasses was examined. XRD has established the amorphous nature of the specimen. The presence of various functional/fundamental groups in the present glasses was analyzed through FTIR spectra. The physical, structural and elastic traits of the glasses were explored. The variation in the structural compactness of the glass structure according to the incorporated modifier was enlightened to describe their suitability for a better shielding media. For the examined glasses, the metallization criterion value varied in the range 0.613-0.692, indicating the non-metallic character of the glasses with possible nonlinear optical applications. The computed elastic moduli expose the Li-containing glass (BTLi:Eu) to be tightly packed and rigid, which is a requirement for a better shielding channel. Furthermore, the optical bandgap and the Urbach energy values are calculated based on the optical absorption spectra. The evaluated bonding parameters revealed the nature of the fabricated glasses covalent. In addition, we investigated the radiation attenuation attributes of the prepared Eu3+ ions doped multi constituent glasses using Phy-X software. We determined the linear attenuation coefficient (LAC) and reported the influence of the five oxides Li2O3, CaO, BaO, SrO, and ZnO on the LAC values. The LAC varied between 0.433 and 0.549 cm-1 at 0.284 MeV. The 39B2O3-25TeO2-15Li2O3-10Na2O-10K2O-1Eu2O3 glass has a much smaller LAC than the other glasses.

탄소나노튜브 대면적 어셈블리를 통한 고감도-고선택성 과산화수소 센서 개발 (Highly sensitive and selective enzymatic detection for hydrogen peroxide using a non-destructively assembled single-walled carbon nanotube film)

  • 이동욱;안희호;서병관;이승우
    • 센서학회지
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    • 제30권4호
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    • pp.229-235
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    • 2021
  • This study presents a simple approach for the assembly of a free-standing conductive electronic nanofilm of single-walled carbon nanotubes (SWNTs) suitable for enzymatic electrochemical biosensors. A large-scale SWNT electronic film was successfully produced by the dialysis of p-Terphenyl-4,4''-dithiol (TPDT)-treated SWNTs. Furthermore, Horseradish peroxidase (HRP) was immobilized on the TPDT-SWNT electronic film, and the enzymatic detection of hydrogen peroxide (H2O2) was demonstrated without mediators. The detection of H2O2 in the negative potential range (-0.4 V vs. Ag/AgCl) was achieved by direct electron transfer of heme-based enzymes that were immobilized on the TPDT-SWNT electronic film. The SWNT-based biosensor exhibited a wide detection range of H2O2 from 10 µM to 10 mM. The HRP-doped SWNT electronic film achieved a high sensitivity of 342 ㎛A/mM·cm2 and excellent selectivity against a variety of redox-active interfering substances, such as ascorbic acid, uric acid, and acetaminophen.

분리유청단백질-이눌린 유래 마이야르 공액체의 기능적 특성 연구 (Functional Properties of Maillard Conjugates Made from Whey Protein Isolate and Inulin)

  • 김연우;이세희;이원재
    • Journal of Dairy Science and Biotechnology
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    • 제40권4호
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    • pp.143-150
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    • 2022
  • 본 연구에서는 분리유청단백질과 이눌린을 이용하여 마이야르 공액체를 성공적으로 제조하였다. 제조된 마이야르 공액체의 제조공정요인인 pH와 열처리 온도는 마이야르 공액체의 기능적 특성(유화특성, 표면특성, 항산화특성)에 영향을 미치는 핵심 제조공정임을 알 수 있었으며, 상대적으로 마이야르 반응이 활발한 pH 8.4와 열처리 온도 70℃에서 마이야르 공액체의 기능적 특성이 향상되었음을 확인하였다.

Development of Hydrophobically Modified Casein Derivative-Based Delivery System for Docosahexaenoic Acids by an Acid-Induced Gelation

  • Ho-Kyung Ha;Dan-Bi Woo;Mee-Ryung Lee;Won-Jae Lee
    • 한국축산식품학회지
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    • 제43권2호
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    • pp.220-231
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    • 2023
  • Although omega-3 fatty acids including docosahexaenoic acid (DHA) contain various health-promoting effects, their poor aqueous solubility and stability make them difficult to be induced in dairy foods. The aims of this research were to manufacture casein derivative-based delivery system using acid-induced gelation method with glucono-σ-lactone and to investigate the effects of production variables, such as pH and charged amount of linoleic acid, on the physicochemical properties of delivery systems and oxidative stability of DHA during storage in model milk. Covalent modification with linoleic acid resulted in the production of casein derivatives with varying degrees of modification. As pH was reduced from 5.0 to 4.8 and the charged amount of linoleic acid was increased from 0% to 30%, an increase in particle size of casein derivative-based delivery systems was observed. The encapsulation efficiency of DHA was increased with decreased pH and increased charged amount of linoleic acid. The use of delivery system for DHA resulted in a decrease in the development of primary and secondary oxidation products. An increase in the degree of modification of casein derivatives with linoleic acid resulted in a decrease in the formation of primary and secondary oxidation products than of free DHA indicating that delivery systems could enhance the oxidative stability of DHA during storage in model milk. In conclusions, casein derivatives can be an effective delivery system for DHA and charged amount of linoleic acid played a key role determining the physicochemical characteristics of delivery system and oxidative stability of DHA.

Recent progress of enzyme cleavable linker in antibody-drug conjugates: sulfatase and phosphatase

  • Sushil K. Dwivedi;Abhinav Bhise;Rajkumar Subramani;Jeongsoo Yoo
    • 대한방사성의약품학회지
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    • 제7권1호
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    • pp.33-40
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    • 2021
  • Recently, antibody-drug conjugates (ADCs) are used to deliver efficient cytotoxic payloads selectively in cancer cells. In the designing of an ADC, the antibody is connected to a toxic payload via a covalent linker, which helps to solubilizes the typical hydrophobic payload as well as stabilizes the linkage over circulation. The development of the linkers for the antibody drug conjugate is still in demand. Initially, the acid, disulfide, and cathepsin-sensitive ADCs attracted considerable attention for the delivery of a potent cytotoxic payload but suffer from instability in human and mouse plasma with a short half-life. In addition, It also suffer from a solubility issue that induces aggregation, which is the major problem in their development. ADCs associated with sulfatase and phosphatase cleavable linker are highly soluble due to the anionic nature of sulfate and phosphate groups. The ADCs also showed high stability in human and mouse plasma. Therefore, to overcome these limitations, sulfatase and phosphatase cleavable linkers were developed. This review focuses on the recently reported advantages of sulfatase and phosphatase cleavable linkers for ADCs.

Laccase Immobilization on Copper-Magnetic Nanoparticles for Efficient Bisphenol Degradation

  • Sanjay K. S. Patel;Vipin C. Kalia;Jung-Kul Lee
    • Journal of Microbiology and Biotechnology
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    • 제33권1호
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    • pp.127-134
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    • 2023
  • Laccase activity is influenced by copper (Cu) as an inducer. In this study, laccase was immobilized on Cu and Cu-magnetic (Cu/Fe2O4) nanoparticles (NPs) to improve enzyme stability and potential applications. The Cu/Fe2O4 NPs functionally activated by 3-aminopropyltriethoxysilane and glutaraldehyde exhibited an immobilization yield and relative activity (RA) of 93.1 and 140%, respectively. Under optimized conditions, Cu/Fe2O4 NPs showed high loading of laccase up to 285 mg/g of support and maximum RA of 140% at a pH 5.0 after 24 h of incubation (4℃). Immobilized laccase, as Cu/Fe2O4-laccase, had a higher optimum pH (4.0) and temperature (45℃) than those of a free enzyme. The pH and temperature profiles were significantly improved through immobilization. Cu/Fe2O4-laccase exhibited 25-fold higher thermal stability at 65℃ and retained residual activity of 91.8% after 10 cycles of reuse. The degradation of bisphenols was 3.9-fold higher with Cu/Fe2O4-laccase than that with the free enzyme. To the best of our knowledge, Rhus vernicifera laccase immobilization on Cu or Cu/Fe2O4 NPs has not yet been reported. This investigation revealed that laccase immobilization on Cu/Fe2O4 NPs is desirable for efficient enzyme loading and high relative activity, with remarkable bisphenol A degradation potential.

수분 수착 MOF를 이용한 건조한 지역의 대기 중 워터하베스팅 기술의 최근 동향 (Recent Advances on MOF-assisted Atmospheric Water Harvesting at Dry Regions)

  • 이근호;송우철
    • 멤브레인
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    • 제34권1호
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    • pp.30-37
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    • 2024
  • 전 세계적인 물 부족을 해결하기 위한 유망한 방법으로 수착제를 이용하여 공기 중에서 물을 수확하는 기술은 수자원이 부족한 지역에서 식수를 전달할 수 있는 큰 잠재력을 보여주고 있음. 본 총설에서는 대기 중 물을 수확하기 위한 수착제로 금속유기골격구조(MOF)를 사용하는 최근 연구에 대해 소개함. 제올라이트나 실리카 기반 물질과 같은 다른 수착제 물질에 비해, MOF는 상대습도 10% 부근에서 물 수착 곡선의 변곡점을 보이는 특성 덕분에 건조한 사막지역에서 물을 수확하기에 적합한 특성을 가지고 있음. 이러한 특성으로 말미암아 최근 MOF를 이용하여 물을 수확할 수 있는 실용적인 물 수확 장치를 개발하기 위한 연구가 활발히 진행되고 있음. 이 기술은 전 세계 어느 곳에서나 지리 환경적 영향을 받지 않고 대기 중의 물에 접근할 수 있기 때문에, 미래 지속가능한 수자원 확보 기술 측면에서 새로운 패러다임을 제시할 것으로 기대됨.

후생유전학 (Epigenetics)과 DNA methylation의 이해 (UNDERSTANDING OF EPIGENETICS AND DNA METHYLATION)

  • 오정환;권용대;윤병욱;최병준
    • Maxillofacial Plastic and Reconstructive Surgery
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    • 제30권3호
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    • pp.302-309
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    • 2008
  • DNA 메틸화는 histone modification과 함께 DNA의 염기서열이 유지되면서 유전기능이 변화되고 자손까지 전달 될 수 있는 후생 유전의 중요한 한 부분이다. DNA 메틸화는 크로마틴의 구조를 변경시키는 과정을 통하여 유전자와 repetitive sequence의 표현을 억제시킬 수 있다. DNA 메틸화는 X-불활성화, 유전체 각인, 유전자 발현조절, 암 생성 등에 중요한 역할을 하는 것으로 밝혀졌고, DNA 메틸화 표지자 (DNA methylation marker)들은 종양의 진단과 치료에 대한 반응을 예측하는 지표로 활용되고 있다. 지금까지 많은 연구 성과에도 불구하고 DNA메틸화, 메틸화에 의한 gene silencing, DNA 메틸화의 표적부위 등에 대한 명확한 기전이 아직도 밝혀지지 않고 있어 향후 더 많은 기초적 연구가 필요할 것이다. 최근에는 후생 유전적 변화는 가역적이기 때문에 종양억제유전자를 억압하는 후생 유전적 변화를 제거한다면 그 종양억제유전자를 다시 활성화시킬 수 있다는 개념의 후생유전 치료법 연구로 DNA 메틸화 억제제와 histone deacetyaltion에 관여하는 HDAC의 억제제들이 항암제로서 개발되어 사용되고 있는데 향후 더 많은 약제 개발과 임상적 연구가 진행되어야 할 것이다.