• 제목/요약/키워드: Hydrophobic Structure

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Solution Structure of Water-soluble Mutant of Crambin and Implication for Protein Solubility

  • Kang, Su-Jin;Lim, Jong-Soo;Lee, Bong-Jin;Ahn, Hee-Chul
    • Bulletin of the Korean Chemical Society
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    • 제32권5호
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    • pp.1640-1644
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    • 2011
  • Water-soluble mutant of intrinsically insoluble protein, crambin, was produced by mutagenesis based on the sequence analysis with homologous proteins. Thr1, Phe13, and Lys33 of crambin were substituted for Lys, Tyr, and Lys, respectively. The resultant mutant was soluble in aqueous buffer as well as in dodecylphosphocholine (DPC) micelle solution. The $^1H-^{15}N$ spectrum of the mutant crambin showed spectral similarity to that of the wild-type protein except for local regions proximal to the sites of mutation. Solution structure of water-soluble mutant crambin was determined in aqueous buffer by NMR spectroscopy. The structure was almost identical to the wild-type structure determined in non-aqueous solvent. Subtle difference in structure was very local and related to the change of the intra- and inter-protein hydrophobic interaction of crambin. The structural details for the enhanced solubility of crambin in aqueous solvent by the mutation were provided and discussed.

불화계 양친매성 폴리아크릴아마이드의 합성과 용액거동 (Synthesis and Solution Properties of Fluorinated Amphiphilic Polyacrylamide)

  • Zhao, Fangyuan;Du, Kai;Yi, Zhuo;Du, Chao;Fang, Zhao;Mao, Bingquan
    • 폴리머
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    • 제39권3호
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    • pp.403-411
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    • 2015
  • A series of hydrophobically associating fluorinated amphiphilic polyacrylamide copolymers with remarkably high heat resistance and salt tolerance were synthesized by free radical micellar copolymerization, using acrylamide (AM) and sodium 2-acrylamido-tetradecane sulfonate ($AMC_{14}S$) as amphiphilic monomers, and 2-(perfluorooctyl) ethyl acrylate (PFHEA) as hydrophobic monomer. The structure of the terpolymer was characterized by FTIR, $^1H$ NMR and $^{19}F$ NMR. The solution properties of the terpolymers were investigated in details, and the results showed that the terpolymer solution had strong intermolecular hydrophobic association as the concentration exceeded the critical association concentration 1.5 g/L. The terpolymer solution possessed high surface activity, viscoelasticity, excellent heat resistance, salt tolerance and shearing resistance. The viscosity retention rate of copolymer solution was as high as 59.9% under the condition of fresh wastewater, $85^{\circ}C$ and a 60-days aging test.

Transparent and Superhydrophobic Films Prepared by Polydimethylsiloxane-Coated Silica nanoparticles

  • Park, Eun Ji;Sim, Jong Ki;Jeong, Myung-Geun;Kim, Young Dok;Lim, Dong Chan
    • 한국진공학회:학술대회논문집
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    • 한국진공학회 2013년도 제44회 동계 정기학술대회 초록집
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    • pp.218-218
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    • 2013
  • We report a simple and cost-effective method to fabricate transparent superhydrophobic surface on various substrates. The surface was fabricated by coating hydrophobic PDMS (polydimethylsiloxane) film on the silica nanoparticle and subsequent fixing of the hydrophobic silica nanoparticles onto substrates. The water contact angle for the prepared surface was determined to be over $150^{\circ}$, whichindicates that the surface is highly repellent to water. The hierarchical structure and roughness of the surface were examined by scanning electron microscopy (SEM) and atomic force microscopy (AFM). Additionally, transparency of the prepared surface was measured with UV-VIS spectrometer. The transmittance of the superhydrophobic surface was ~80%, which is lower than that without PDMS-coated silica by only 5 to 10%. It is also notable that the superhydrophobic surface fully recovers its original transmittance after self-cleaning process. Also the PDMS coating is stable under a wide range of pH conditions, UV radiation and salinity conditions, which is essential for the practical use. Moreover, our fabrication method is applicable in large scale production.

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Influence of the Hydrophobic Amino Acids in the N- and C-Terminal Regions of Pleurocidin on Antifungal Activity

  • Lee, June-Young;Lee, Dong-Gun
    • Journal of Microbiology and Biotechnology
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    • 제20권8호
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    • pp.1192-1195
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    • 2010
  • To investigate the influence of the N- or C-terminal regions of pleurocidin (Ple) peptide on antifungal activity, four analogs partially truncated in the N- or C-terminal regions were designed and synthesized. Circular dichroism (CD) spectroscopy demonstrated that all the analogs maintained an alpha-helical structure. The antifungal susceptibility testing also showed that the analogs exhibited antifungal activities against human fungal pathogens, without hemolytic effects against human erythrocytes. The result further indicated that the analogs had discrepant antifungal activities [Ple>Ple (1-22)>Ple (4-25)>Ple (1- 19)>Ple (7-25)] and that N-terminal deletion affected the activities much more than C-terminal deletion. Hydrophobicity [Ple>Ple (1-22)>Ple (4-25)>Ple (1-19)> Ple (7-25)] was thought to have been one of the consistent factors that influenced these activity patterns, rather than the other primary factors like the helicity [Ple>Ple (4-25) >Ple (1-22)>Ple (1-19)>Ple (7-25)] or the net charge [Ple=Ple (4-25)=Ple (7-25)>Ple (1-22)=Ple (1-19)] of the peptides. In conclusion, the hydrophobic amino acids in the N-terminal region of Ple is more crucial for antifungal activity than those in the C-terminal region.

PAMAM Dendrimers Augment Inhibitory Effects of Curcumin on Cancer Cell Proliferation: Possible Inhibition of Telomerase

  • Mollazade, Mahdie;Nejati-Koshki, Kazem;Akbarzadeh, Abolfazl;Zarghami, Nosratollah;Nasiri, Marzieh;Jahanban-Esfahlan, Rana;Alibakhshi, Abbas
    • Asian Pacific Journal of Cancer Prevention
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    • 제14권11호
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    • pp.6925-6928
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    • 2013
  • Background: Despite numerous useful anticancer properties of curcumin, its utility is limited due to its hydrophobic structure. In this study, we investigated the comparative antiproliferative effect of PAMAM encapsulating curcumin with naked curcumin on the T47D breast cancer cell line. Materials and Methods: Cytotoxic effects of PAMAM dendrimers encapsulating curcumin and curcumin alone were investigated by MTT assay. After treating cells with different concentrations of both curcumin alone and curcumin encapsulated for 24h, telomerase activity was determined by TRAP assay. Results: While PAMAM dendrimers encapsulating curcumin had no cytotoxicity on cancer cells, they decreased the $IC_{50}$ for proliferation and also increased the inhibitory effect on telomerase activity. Conclusions: Considering the non-toxicity in addition to effectiveness for enhancing curcumin anticancer properties, dendrimers could be considered good therapeutic vehicles for this hydrophobic agent.

3D Quantitative and Qualitative Structure-Activity Relationships of the δ -Opioid Receptor Antagonists

  • Chun, Sun;Lee, Jee-Young;Ro, Seong-Gu;Jeong, Ki-Woong;Kim, Yang-Mee;Yoon, Chang-Ju
    • Bulletin of the Korean Chemical Society
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    • 제29권3호
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    • pp.656-662
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    • 2008
  • Antagonists of the d -opioid receptor are effective in overcoming resistance against analgesic drugs such as morphine. To identify novel antagonists of the d -opioid receptor that display high potency and low resistance, we performed 3D-QSAR analysis using chemical feature-based pharmacophore models. Chemical features for d -opioid receptor antagonists were generated using quantitative (Catalyst/HypoGen) and qualitative (Catalyst/HipHop) approaches. For HypoGen analysis, we collected 16 peptide and 16 non-peptide antagonists as the training set. The best-fit pharmacophore hypotheses of the two antagonist models comprised identical features, including a hydrophobic aromatic (HAR), a hydrophobic (HY), and a positive ionizable (PI) function. The training set of the HipHop model was constructed with three launched opioid drugs. The best hypothesis from HipHop included four features: an HAR, an HY, a hydrogen bond donor (HBD), and a PI function. Based on these results, we confirm that HY, HAR and PI features are essential for effective antagonism of the d -opioid receptor, and determine the appropriate pharmacophore to design such antagonists.

제올라이트 복합 분리막의 합성 및 특성화(I): ZSM-5계 제올라이트의 합성 (Synthesis and Characterization of Zeolite Composite Membranes (I):Synthesis of ZSM-5 Type Zeolites)

  • 현상훈;김준학;송재권
    • 한국세라믹학회지
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    • 제33권9호
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    • pp.1064-1072
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    • 1996
  • The synthetic conditions and characteristics of ZSM-5 type zeolites (ZSM-5/silicalite) for the preparation of the zeolite composite membranes for gas separation were investigated. ZSM-5 zeolites could be synthesized by the hydrothermal treatment of the mixture of colloidal silica sol aluminum nitrate sodium hydroxide and TPABr at a temperature range of 150-17$0^{\circ}C$ in the autoclave. Silicalties were done from the solution of water glass water and TPABr. Their crystalline structures transformed from orthorhombic to monoclinic from and their pore structures of three-dimensional channels were opened as TPABr filling channels was burned off at the calcination temperature of 50$0^{\circ}C$. The specific surface area of the calcined zeolite was about 360 m3/g and its surface property was hydrophobic. Crystal sizes of ZSM-5 and silicalite were 0.5-1.0${\mu}{\textrm}{m}$ and 8-10${\mu}{\textrm}{m}$ respectively having no change due to the calcination. In particular the shape and the size of the ZSM-5 type zeolite were sensitively varied with silica sources and concentrations of reaction solutions/sols.

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고분자전해질 막을 위한 나프탈렌 단위를 포함하는 디 및 트리 블록공중합체의 합성 및 특성분석 (Synthesis and Characterization of Di and Triblock Copolymers Containing a Naphthalene Unit for Polymer Electrolyte Membranes)

  • 김애란
    • 한국수소및신에너지학회논문집
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    • 제27권6호
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    • pp.660-669
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    • 2016
  • A fluorinated-sulfonated, hydrophobic-hydrophilic copolymer was planed subsequently synthesized using typical nucleophilic substitution polycondensation reaction. A novel AB and ABA (or BAB) block copolymers were synthesized using sBCPSBP (sulfonated 4,4'-bis[4-chlorophenyl)sulfonyl]-1,1'-biphenyl), DHN (1,5-dihydroxynaphthalene), DFBP (decafluorobiphenyl) and HFIP (4,4'-hexafluoroisopropylidenediphenol). All block copolymers were easily cast and made into clear films. The structure and synthesized copolymers and corresponding membranes were analyzed using GPC (gel permeation chromatography), $^1H$-NMR ($^1H$ nuclear magnetic resonance) and FT-IR (Fourier transform infrared). TGA (Thermogravimetric analysis) and DSC (differential scanning calorimetry) analysis showed that the prepared membranes were thermally stable, so that elevated temperature fuel cell operation would be possible. Hydrophobic/hydrophilic phase separation and clear ionic aggregate block morpology was confirmed in both triblock and diblock copolymer in AFM (atomic force microscopy), which may be highly related to their proton transport ability. A sulfonated BAB triblock copolymer membrane with an ion-exchange capacity (IEC) of 0.6 meq/g has a maximum ion conductivity of 40.3 mS/cm at $90^{\circ}C$ and 100% relative humidity.

The nonconserved N-terminus of protein phosphatases 1 influences its active site

  • Xie, XiuJie;Huang, Wei;Xue, ChengZhe;Wei, Qun
    • BMB Reports
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    • 제41권12호
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    • pp.881-885
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    • 2008
  • Protein phosphatase 1 consists of a secondary structure arrangement, conserved in the serine/threonine protein phosphatase gene family, flanked by nonconserved N-terminal and C-terminal domains. The deletion mutant of PP1 with the 8 nonconserved N-terminal residues removed was designated PP1-(9-330). PP1-(9-330) had a higher activity and affinity than PP1 when assayed against four different substrates, and it also demonstrated a 6-fold higher sensitivity to the inhibitor okadaic acid. This suggested that the N-terminal domain suppresed the activity of PP1 and interfered with its inhibition by okadaic acid. The ANS fluorescence intensity of PP1-(9-330) was greater than that of PP1, which implies that the hydrophobic groove running from active site in the truncated PP1 was more hydrophobic than in PP1. Our findings provide evidence that the nonconserved N-terminus of PP1 functions as an important regulatory domain that influences the active site and its pertinent properties.

Design, Syntheses, and Conformational Study of Angiogenesis Inhibitors

  • 박경수;백동하;임동열;박상돈;김민영;박영선;김양미
    • Bulletin of the Korean Chemical Society
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    • 제22권9호
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    • pp.984-988
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    • 2001
  • Since anti-angiogenesis could lead to the suppression of tumor growth, angiogenesis inhibitors have received particular attention for their therapeutic potential. In this study, two angiogenic inhibitors using the bioactive sequence from the kring le 5, AK1(KLYDY), AK2(KLWDF) were designed and synthesized. We have investigated their solution structures using NMR spectroscopy and their activities as angiogenesis inhibitors. AK2 has an intramolecular hydrogen bon d between the side chain amino proton of Lys1 and the carboxyl oxygen of Asp4 with a N ${\cdot}{\cdot}{\cdot}$O distance of $3.27\AA$, while AK1 shows more flexible structures than AK2. Indole ring in Trp is much bigger than the phenyl ring in Tyr and may have good face-to-edge interaction enforcing more rigid and constrained conformational features of AK2. Because of this relatively stable structure, Trp3 in AK2 may have better hydrophobic interaction with Phe5 than Tyr3 in AK1 if two adjacent aromatic groups are located in hydrophobic pocket of receptor. Since AK2 shows the similar anti-angiogenic activities to AK1, we are also able to confirm that the activity of AK1 is irrelevant to the Tyr phosphorylation. More rigid drug with higher activities can be provided by the mimetic approaches. For the further development of the angiogenesis inhibitors, these conformational studies on our lead peptides will be helpful in design of peptidomimetics.