Search results for "HeLa"
showing 10 items of 738 documents
Synthesis of Enantiopure ω-(4-Fluorophenyl)-6,11-Methylene Lipoxin B4 Methyl Ester
2021
AbstractThe synthesis of Lipoxin B4 analogues (LXB4) to gain access to stabilized inflammation-resolving compounds is an active field of research. Focusing on variation and stabilization of the conjugated E,Z,E,E C6–C13 tetraene moiety of natural LXB4, a methylene bridge introduced between C6 and C11 suppresses any Z/E isomerization of the C8–C9 olefin. Furthermore, rapid ω-oxidation (C20) should be avoided by replacing the C18–C20 segment by an aromatic moiety. Optically active C1–C12 building blocks were accessed from methyl cycloheptatriene-1-carboxylate (C6–C11, C21) and glutaryl chloride (C1–C5) as described earlier. The ω-segment was generated via a five-step sequence starting from 4-…
The giant spectrin βV couples the molecular motors to phototransduction and Usher syndrome type I proteins along their trafficking route.
2013
International audience; Mutations in the myosin VIIa gene cause Usher syndrome type IB (USH1B), characterized by deaf-blindness. A delay of opsin trafficking has been observed in the retinal photoreceptor cells of myosin VIIa-deficient mice. We identified spectrin bV, the mammalian b-heavy spectrin, as a myosin VIIa-and rhodopsin-interacting partner in photoreceptor cells. Spectrin bV displays a polarized distribution from the Golgi apparatus to the base of the outer segment, which, unlike that of other b spectrins, matches the trafficking route of opsin and other phototransduction proteins. Formation of spectrin bV-rhodopsin complex could be detected in the differentiating photoreceptors a…
A promising camptothecin derivative: Semisynthesis, antitumor activity and intestinal permeability.
2014
Oral administration of camptothecin (Cm) derivatives and other antitumoral agents is being actively developed in order to improve the quality of life of patients with cancer. Though several lipophilic derivatives of CPT have shown interesting oral bioavailability in preclinical and clinical studies, only Topotecan has been approved for this route of administration. Semisynthesis, antitumor activity, biological inhibition mechanism, and in situ intestinal permeability of 9, 10-[1,3]-Dioxinocamptothecin (CDiox), an unexplored CPT derivative, have been studied in this paper. The hexacyclic analog was as effective as Topotecan and CPT in different tumor cell lines, showing an expected similar a…
Synthesis of rigid ethynyl-bridged polytopic picolinate ligands for MOF applications
2015
Abstract Segmented homopolytopic ligands that consist of a rigid central arylene platform, ethynylene spacers, and terminal chelating picolinate subunits have been synthesized in good yields in a two-step procedure involving a Sonogashira-type cross coupling reaction between the ester methyl 5-bromopyridine-2-carboxylate and several arylacetylenes, followed by hydrolysis of the resulting methyl picolinates. A similar strategy has been employed for the preparation of heteroditopic ligands containing picolinate and a second non-chelating pyridine or benzoate unit. The compounds are potential candidates for organic linkers in metal–organic frameworks (MOFs).
Amino acids requirements of measles virus in HeLa cells.
1973
A low plating efficiency for measles virus was obtained when arginine, threonine and isoleucine were omitted from Eagle's basal medium and a stimulatory effect on the plaque production was produced by increasing the concentration up to 0.5 mm of arginine and glutamine. However, of all amino acids in Eagle's basal medium, only methionine was found to be essential for the synthesis of infectious progeny virus. Omission of any one of the other amino acids from the culture medium permitted limited virus production, but none whatever could be detected in the absence of mediummethionine. Moreover, when methionine was restored to infected cultures after 24 hours of deprivation, release of virus be…
Cytotoxic Action of Serratia marcescens Hemolysin on Human Epithelial Cells
1999
ABSTRACT Incubation of human epithelial cells with nanomolar concentrations of chromatographically purified Serratia marcescens hemolysin (ShlA) caused irreversible vacuolation and subsequent lysis of the cells. Vacuolation differed from vacuole formation by Helicobacter pylori VacA. Sublytic doses of ShlA led to a reversible depletion of intracellular ATP. Restoration to the initial ATP level was presumably due to the repair of the toxin damage and was inhibited by cycloheximide. Pores formed in epithelial cells and fibroblasts without disruption of the plasma membrane, and the pores appeared to be considerably smaller than those observed in artificial lipid membranes and in erythrocytes a…
In Vitro Evaluation of the Squaramide-Conjugated Fibroblast Activation Protein Inhibitor-Based Agents AAZTA5.SA.FAPi and DOTA.SA.FAPi
2021
Recently, the first squaramide-(SA) containing FAP inhibitor-derived radiotracers were introduced. DATA5m.SA.FAPi and DOTA.SA.FAPi with their non-radioactive complexes showed high affinity and selectivity for FAP. After a successful preclinical study with [68Ga]Ga-DOTA.SA.FAPi, the first patient studies were realized for both compounds. Here, we present a new squaramide-containing compound targeting FAP, based on the AAZTA5 chelator 1,4-bis-(carboxylmethyl)-6-[bis-(carboxymethyl)-amino-6-pentanoic-acid]-perhydro-1,4-diazepine. For this molecule (AAZTA5.SA.FAPi), complexation with radionuclides such as gallium-68, scandium-44, and lutetium-177 was investigated, and the in vitro properties of…
Multi-Functional Nanogels for Tumor Targeting and Redox-Sensitive Drug and siRNA Delivery
2016
(1) Background: A new family of nanosystems able to discern between normal and tumor cells and to release a therapeutic agent in controlled way were synthetized by e-beam irradiation. This technique permits to obtain biocompatible, sterile, carboxyl-functionalized polyvinylpyrrolidone (PVP-co-acrylic acid) nanogels (NGs); (2) Methods: Here, we performed a targeting strategy based on the recognition of over-expressed proteins on tumor cells, like the folate receptor. The selective targeting was demonstrated by co-culture studies and flow cytometry analysis, using folate conjugated NGs. Moreover, nanoparticles were conjugated to a chemotherapeutic drug or to a pro-apoptotic siRNA through a gl…
P(HPMA)-block-P(LA) copolymers in paclitaxel formulations: Polylactide stereochemistry controls micellization, cellular uptake kinetics, intracellula…
2012
In order to explore the influence of polymer microstructure and stereochemistry in biological settings, the synthesis, micellization, cellular fate and the use in paclitaxel formulations of poly(N-(2-hydroxypropyl)-methacrylamide)-block-poly(L-lactide) (P(HPMA)-block-P(LLA)) and poly(N-(2-hydroxypropyl)-methacrylamide)-block-poly(DL-lactide) block copolymers (P(HPMA)-block-P(DLLA)) were studied. To this end, P(HPMA)-block-P(lactide) block copolymers and their fluorescently labeled analogues were synthesized. The polymers exhibited molecular weights M-n around 20,000 g/mol with dispersities (D=M-w/M-n) below 1.3. In addition, the solution conformation of this new type of partially degradable…
Palaeomagnetic results from the late Precambrian Chela Group of southwest Angola
1992
Abstract Palaeomagnetic results from fourteen sites (56 samples) in the late Precambrian Chela Group of southwest Angola are reported. After alternating field demagnetization eight of the sites have mean directions closely grouped around D = 123°, I = −44 1 2 ° ; the dispersion of these directions increases substantially after tectonic corrections suggesting magnetic overprinting. Intensive thermal demagnetization proved more effective than alternating field demagnetization in resolving magnetic components. After removal of viscous components, samples from five sites (Group I) show a single component, similar to that observed after alternating field demagnetization. At four more sites (Grou…