Synthesis, purification and initial structural characterization of octarellin, a de novo polypeptide modelled on the alpha/beta-barrel proteins; ; Martial, Joseph ![]() in Protein Engineering (1990), 3(4), 259-66 We have attempted to construct an artificial polypeptide that folds like the eight-stranded parallel beta-barrel structures. Our approach consists of repeating eight times a unit peptide designed to adopt ... [more ▼] We have attempted to construct an artificial polypeptide that folds like the eight-stranded parallel beta-barrel structures. Our approach consists of repeating eight times a unit peptide designed to adopt a 'beta-strand/alpha-helix' pattern. A first 'test' sequence for this structural unit was deduced from a series of parameters defined after an analysis of three natural alpha/beta-barrel proteins and including principally the lengths of the secondary structure elements, the alpha/beta packing and the fitting on average Garnier profiles. The gene encoding this structural unit was synthesized, cloned and expressed in Escherichia coli either as a monomer or as direct repeats of 2-12 units. Preliminary structural characterization of the 7-, 8- and 9-fold unit polypeptides by circular dichroism measurements indicates the presence of the predicted amount of alpha-helix in the three proteins. Further analysis by urea-gradient gel electrophoresis demonstrates that, in the conditions tested, only the 8-fold unit polypeptide forms a compact structure through a cooperative and rapid two-state folding transition involving long-range molecular interactions. [less ▲] Detailed reference viewed: 13 (2 ULg) Synthesis, purification and kinetic properties of fluorescein-labelled penicillinsLakaye, Bernard ; Damblon, Christian ; et alin Biochemical Journal (1994), 300 Detailed reference viewed: 8 (1 ULg) Synthesis, quality control and in vivo evaluation of [I-123] rhTIMP-2, a potential tumour-imaging agent; ; et al in Journal of Labelled Compounds & Radiopharmaceuticals (2005), 48(5), 387-396 Matrix metalloproteinases (MMPs) are enzymes involved in the turnover of the extracellular matrix. Their overexpression in tumours may provide a target for diagnostic imaging by using labelled MMP ... [more ▼] Matrix metalloproteinases (MMPs) are enzymes involved in the turnover of the extracellular matrix. Their overexpression in tumours may provide a target for diagnostic imaging by using labelled MMP inhibitors. MMPs are inhibited by endogenous tissue inhibitors of metalloproteinases (TIMPs). The enhanced production of MT1-MMP, located on the surface of cells within or in the direct vicinity of the tumour, and the high affinity interaction between TIMP-2 and MT1-MMP suggested that TIMP-2 could be a potential agent for non-invasive monitoring of cancer MMP levels, diagnosis of primary and secondary tumours and tumour response to MMP inhibitor therapy. There is also evidence that I-125-rhTIMP-2 internalizes, which is an important feature for its possible use as a radiotherapeuticum if labelled with I-131. Labelling of rhTIMP-2 was performed using the iodogen method resulting in a radiochemical yield of 51.1 +/- 11.8% (n = 5) and a radiochemical purity of > 98%. The trichloroacetic acid (TCA) precipitability of I-123 rhTIMP-2 was 95.2%. SDS-PAGE confirmed the correct size (21 kDa) of the purified I-123 rhTIMP-2 without degradation. HPLC showed one radioactive peak with a retention time corresponding to the nonlabelled rhTIMP-2. In vivo biodistribution showed no long-term accumulation in organs and the possibility to accumulate in the tumour. These results show the potential of I-123 rhTIMP-2 as tumour-imaging agent. Copyright (c) 2005 John Wiley [less ▲] Detailed reference viewed: 5 (1 ULg) Synthesis, radiosynthesis, in vitro and preliminary in vivo evaluation of biphenyl carboxylic and hydroxamic matrix metalloproteinase (MMP) inhibitors as potential tumor imaging agents.; ; et al in Applied Radiation & Isotopes (2005), 62(6), 903-13 Excess matrix degradation is one of the hallmarks of cancer and is an important factor in the process of tumor progression. It is implicated in invasion, metastasis, growth, angiogenesis and migration ... [more ▼] Excess matrix degradation is one of the hallmarks of cancer and is an important factor in the process of tumor progression. It is implicated in invasion, metastasis, growth, angiogenesis and migration. Many characteristics of matrix metalloproteinases (MMPs) make them attractive therapeutic and diagnostic targets. MMP expression is upregulated at the tumor site, with localization of activity in the tumor or the surrounding stroma, providing a target for medical imaging techniques. Radioiodinated carboxylic and hydroxamic MMP inhibitors 2-(4′-[123I] iodo-biphenyl-4-sulfonylamino)-3-methyl-butyric acid (9) and 2-(4′-[123I] iodo-biphenyl-4-sulfonylamino)-3-methyl-butyramide (11), their unlabelled standards and precursors were synthesized. Radioiodination was conducted by electrophilic aromatic substitution of the tributylstannyl precursors and resulted in radiochemical yields of 70±5% (n=6) and 60±5% (n=4), respectively. In vitro zymography and enzyme assays showed for both hydroxamic acid and carboxylic acid compounds a good inhibition activity and a high selectivity for MMP-2. In vivo biodistribution in NMRI mice showed no long-term accumulation in organs and the possibility to accumulate in the tumor in a later phase of this study. [less ▲] Detailed reference viewed: 6 (2 ULg) Synthesis: tension-type headache mechanisms; Schoenen, Jean ![]() in Olesen, J.; Tfelt-Hansen, P.; Welch, K. M. A. (Eds.) The Headaches (1999) Detailed reference viewed: 7 (0 ULg) Synthetic and mechanistic advances in the cobalt-mediated radical polymerization of N-vinyl amidesDebuigne, Antoine ; Hurtgen, Marie ; Liu, Ji et alConference (2012, May 28) see the pdf file Detailed reference viewed: 9 (3 ULg) Synthetic and mechanistic inputs of photochemistry into the bisacetylacetonatocobalt- mediated radical polymerization of n-butyl acrylate and vinyl acetateDetrembleur, Christophe ; ; et alin Polymer Chemistry (2012), 3(7), 1856-1866 The input of photochemistry to the Co(acac)2 mediated radical polymerization (CMRP) of n-butyl acrylate and vinyl acetate is investigated for the first time. Upon UV irradiation, photoinitiators are able ... [more ▼] The input of photochemistry to the Co(acac)2 mediated radical polymerization (CMRP) of n-butyl acrylate and vinyl acetate is investigated for the first time. Upon UV irradiation, photoinitiators are able to initiate the n-butyl acrylate polymerization that remains controlled up to very high molar masses (>4 × 106 g mol−1) with low polydispersities. The photoinitiator as well as the irradiation time must be appropriately chosen to reach acceptable initiator efficiencies while maintaining an optimal control over the polymerization. Laser flash photolysis experiments were then carried out to evidence the addition of alkyl and phosphonyl radicals onto Co(acac)2 and to determine the rate constants (kdeact) of these addition reactions that were still lacking. Finally, both kinetics of polymerization and spin-trapping experiments have evidenced that the C–Co bond at the extremity of the dormant polymer chains can be easily photocleaved. UV irradiation can therefore be considered as an additional lever for tuning the reactivity of the CMRP process mediated by Co(acac)2. [less ▲] Detailed reference viewed: 26 (7 ULg) Synthetic and mechanistic insights in cobalt mediated radical polymerization (CMRP) of vinyl acetate and acrylonitrileDebuigne, Antoine ; ; Jérôme, Robert et alConference (2008, July 03) Detailed reference viewed: 4 (1 ULg) Synthetic aperture co-phasing and co-alignment using an external reference sourceRoose, Stéphane ; ; Lecat, Jean-Hervé et alin Proceedings of ICSO 2006 (2006, June 27) A breadboard set-up has demonstrated a concept of co-phasing and co-alignment based on an external reference source for synthetic aperture telescopes applications. These types of systems can be extremely ... [more ▼] A breadboard set-up has demonstrated a concept of co-phasing and co-alignment based on an external reference source for synthetic aperture telescopes applications. These types of systems can be extremely valuable in order to perform coarse re-alignment of synthetic aperture telescope, following thermo-elastic deformation and deployment effects in space flight environments. [less ▲] Detailed reference viewed: 14 (0 ULg) Synthetic biomedical polymersGrandfils, Christian ; Dubois, Philippe ; et alPoster (1991, November 28) Detailed reference viewed: 2 (0 ULg) Synthetic Biomedical Polymers (Part B); ; et al Poster (1991, May 31) Detailed reference viewed: 2 (0 ULg) Synthetic Biomedical Polymers : Part B. a. Their formulation as dispersed systems for the controlled delivery of bioactive peptides and proteins b. Developement of a biodegradable implant by microspheres aggregation; ; et al Poster (1991, January 16) Detailed reference viewed: 1 (0 ULg) Synthetic holography: Signal synthesis with binary diffractive structuresRoose, Stéphane ![]() Doctoral thesis (1995) Detailed reference viewed: 5 (0 ULg) Synthetic model peptides for apolipoproteins. I. Design and properties of synthetic model peptides for the amphipathic helices of the plasma apolipoproteins.Brasseur, Robert ; ; et alin Biochimica et Biophysica Acta (1993), 1170(1), 1-7 Amphipathic helical peptides are the lipid-binding motives of the plasma apolipoproteins, and synthetic peptide analogs have been used to unravel the mechanism of lipid association within this class of ... [more ▼] Amphipathic helical peptides are the lipid-binding motives of the plasma apolipoproteins, and synthetic peptide analogs have been used to unravel the mechanism of lipid association within this class of proteins. Hydrophobic interactions between the apolar amino acid residues belonging to the hydrophobic face of the amphipathic helices and the lipids are the major driving forces in the peptide-lipid association to form discoidal complexes. Ionic interactions and salt bridge formation between contiguous peptide chains in the complex can, however, contribute to the overall stability of the lipid-protein particle. This was studied by designing peptide analogs to the helical repeats of the apolipoproteins with variable degrees of salt bridge formation between adjacent peptide chains. The most stable conformation for pairs of synthetic peptides was calculated by energy minimisation together with the energy of interaction between peptides. The sequence of the peptides was derived from that of the 18A peptide synthesized by Segrest et al., and the theoretical calculations confirmed that ionic interactions between residues close to each other, along the edge of two adjacent anti-parallel peptides, can significantly contribute towards the stability of a peptide-phospholipid complex. [less ▲] Detailed reference viewed: 10 (0 ULg) Synthetic model peptides for apolipoproteins. II. Characterization of the discoidal complexes generated between phospholipids and synthetic model peptides for apolipoproteins.; ; et al in Biochimica et Biophysica Acta (1993), 1170(1), 8-16 The structure, composition and physico-chemical properties of complexes generated between phospholipids and synthetic model peptides for the amphipathic helices of the plasma apolipoproteins were studied ... [more ▼] The structure, composition and physico-chemical properties of complexes generated between phospholipids and synthetic model peptides for the amphipathic helices of the plasma apolipoproteins were studied. The sequences of the peptides were derived from that of the 18A peptide and designed to either enhance or decrease ionic interactions between pairs of peptides, as described in the accompanying paper. Complexes were prepared with dimyristoylphosphatidylcholine (DMPC), dipalmitoylphosphatidylcholine (DPPC), or with DPPC and cholesterol, and isolated on a Superose 6HR column. Association kinetics for the DMPC-peptides complexes were followed by measuring the turbidity as a function of the temperature. The diameters of the DPPC-peptide complexes, measured by gradient gel electrophoresis (GGE), were about 120 A. Fluorescence polarization measurements after labeling with diphenyl hexatriene (DPH) yielded transition temperatures of, respectively, 40.6, 41.5 and 41.8 degrees C for the DPPC/18AM1-, DPPC/18AM4- and DPPC/18A-peptide complexes. These values were confirmed by differential scanning calorimetry. Circular dichroism and infrared spectroscopy revealed that the peptides adopt an alpha-helical structure in solution and this percentage increased from 30-40% in the free peptides up to 50-60% in the complexes. Attenuated total reflection (ATR) infrared measurements of the complexes indicated that the peptides are oriented parallel to the acyl chains of the phospholipid bilayer. Denaturation of the peptides and of the peptide-lipid complexes was monitored by Trp fluorescence under addition of increasing amounts of GdmCl. The mid-points of the denaturation curves lie at, respectively, 0.05, 0.25 and 0.35 M GdmCl for the 18AM4, 18A and 18AM1 peptide and are shifted towards higher GdmCl concentrations after peptide-lipid binding. GdmCl denaturation decreased the alpha-helical content of the peptides and of the complexes, as monitored by circular dichroism measurement. The helix to random coil structure transition occurred at, respectively, 2.1, 2.2, and 2.0 M GdmCl for 18A, 18AM1 and 18AM4, compared to 5.1, 5.0, and 5.3 M in the corresponding complexes. These data suggest altogether that the structural properties, the mode of lipid-protein association and the stability of the phospholipid-peptide complexes are similar to those of native plasma apolipoproteins. The 18A and 18AM4 peptides which contain charged residues along the edge of the helix, leading to salt bridge formation between peptides were shown to mimic the amphipathic helices of the plasma apolipoproteins. [less ▲] Detailed reference viewed: 10 (0 ULg) Synthetic peptide inhibitors of transpeptidation by the exocellular DD-carboxypeptidase-transpeptidase from Actinomadura R39; Frère, Jean-Marie ; Ghuysen, Jean-Marie ![]() in FEBS Letters (1981), 123(1), 75-78 Detailed reference viewed: 6 (0 ULg) Synthetic Peptides Approach To Identification Of Epitopes On Bovine Leukemia-Virus Envelope Glycoprotein-Gp51Portetelle, Daniel ; ; et alin Virology (1989), 169(1), Detailed reference viewed: 6 (1 ULg) Synthetic pulsational line profile variations; ; et al in Astrophysics & Space Science (2010), 329 We have produced simulated time series of high resolution spectroscopy for sdBs. We present the first results of testing classical mode identification techniques. Here, in particular, we analyse the ... [more ▼] We have produced simulated time series of high resolution spectroscopy for sdBs. We present the first results of testing classical mode identification techniques. Here, in particular, we analyse the behaviour of individual spectral lines and discuss the results and applicability of the moment method. [less ▲] Detailed reference viewed: 3 (0 ULg) Synthetic, structural, magnetic, and Mossbauer spectral study of {Fe[HC(3,5-Me(2)pz)(3)](2)}I-2 and its spin-state crossover behavior; ; et al in European Journal Of Inorganic Chemistry (2002), (5), 1190-1197 The complex {Fe[HC(3,5-Me(2)pz)(3)](2)}I-2 (1) has been prepared from the reaction of FeI2 and HC(3,5-Me(2)pz)(3) (pz = pyrazolyl ring) in a 1:2 ratio. The complex is high-spin in both the solid state and ... [more ▼] The complex {Fe[HC(3,5-Me(2)pz)(3)](2)}I-2 (1) has been prepared from the reaction of FeI2 and HC(3,5-Me(2)pz)(3) (pz = pyrazolyl ring) in a 1:2 ratio. The complex is high-spin in both the solid state and in solution at ambient temperature, In the solid state, magnetic susceptibility and Mossbauer spectral studies indicate that samples of the complex that have been crystallized and dried change completely from high-spin to low-spin upon cooling below 195 K, with a substantial two-step thermal hysteresis in the transition, The spin-crossover properties of I are sample dependent: powder samples do not change to low-spin at low temperatures. Two crystalline forms of I have been identified by X-ray crystallography, one form containing no solvent of crystallization and the other containing solvent, In both, there is only one iron site, with average Fe-N bond lengths of 2.18 and 2.17 Angstrom, values that confirm that the complex is high-spin. Single crystals of the nonsolvated form shatter at low temperatures whereas single crystals of the solvated form can be cooled to 110 K with no loss of crystallinity and remain fully high spin at this temperature, Crystallographic information: nonsolvated form is triclinic, P (1) over bar, a = 8,8062(2) Angstrom, b = 10.3549(2) Angstrom, c = 11.3549(2) Angstrom, a = 104.0768(10), beta = 110.2473(10)degrees, gamma = 92.6385(11)degrees, Z = 1; solvated form is monoclinic P2(1)/c, a 10.3214(5) Angstrom, b = 12.7753(7) Angstrom, c = 20.1995(11) Angstrom, alpha = 90degrees, beta = 97.5380(10)degrees, gamma = 90degrees, Z = 2. [less ▲] Detailed reference viewed: 4 (0 ULg) |
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