- Direct interaction, instrumental for signaling processes, between LacCer and Lyn in the lipid rafts of neutrophil-like cells
-
Lactosylceramide [LacCer; β-Gal-(1-4)-β-Glc-(1-1)-Cer] has been shown to contain very long fatty acids that specifically modulate neutrophil properties. The interactions between LacCer and proteins and their role in cell signaling processes were assessed
- Chiricozzi, Elena,Ciampa, Maria Grazia,Brasile, Giuseppina,Compostella, Federica,Prinetti, Alessandro,Nakayama, Hitoshi,Ekyalongo, Roudy C.,Iwabuchi, Kazuhisa,Sonnino, Sandro,Mauri, Laura
-
-
Read Online
- Self-Assembled BolA-like Amphiphilic Peptides as Viral-Mimetic Gene Vectors for Cancer Cell Targeted Gene Delivery
-
In this study, two types of BolA-like amphiphilic peptides with dual ligands comprising a tumor-targeting moiety of RGD sequence and a cell-penetrating moiety of R8 sequence are designed and synthesized as gene vectors. The BolA-structural peptide carriers can self-assemble into spherical nanoparticles with a hydrophilic core and shell, which are similar to the viral capsid and can bind plasmid DNA in an aqueous medium to form viral-mimetic complexes. It is found that the BolA-like dual ligands system exhibits significantly enhanced gene expression in both HeLa and 293T cell lines, as compared with poly(ethylenimine) PEI. These BolA-like amphiphilic peptides are promising in clinical trials of gene therapy.
- Chen, Jing-Xiao,Xu, Xiao-Ding,Yang, Shuo,Yang, Juan,Zhuo, Ren-Xi,Zhang, Xian-Zheng
-
-
Read Online
- Missing Selectivity of Targeted 4β-Phorbol Prodrugs Expected to be Potential Chemotherapeutics
-
Targeting cytotoxic 4β-phorbol esters toward cancer tissue was attempted by conjugating a 4β-pborbol derivative with substrates for the proteases prostate-specific antigen (PSA) and prostate-specific membrane antigen (PSMA) expressed in cancer tissue. The
- Tarvainen, Ilari,Zimmermann, Tomá?,Heinonen, Pia,J?ntti, Maria Helena,Yli-Kauhaluoma, Jari,Talman, Virpi,Franzyk, Henrik,Tuominen, Raimo K.,Christensen, S?ren Br?gger
-
-
Read Online
- A new anti-cancer strategy of damaging mitochondria by pro-apoptotic peptide functionalized gold nanoparticles
-
Gold nanoparticles functionalized with pro-apoptotic peptide (PAP-AuNPs) were fabricated, which were able to lead to programmed cell-death by damaging mitochondria.
- Chen, Wei-Hai,Chen, Jing-Xiao,Cheng, Han,Chen, Chang-Sheng,Yang, Juan,Xu, Xiao-Ding,Wang, Yan,Zhuo, Ren-Xi,Zhang, Xian-Zheng
-
-
Read Online
- A Light-up 1D supramolecular nanoprobe for silver ions based on assembly of pyrene-labeled peptide amphiphiles: Cell-imaging and antimicrobial activity
-
We prepared pyrene-labeled peptide amphiphiles (PAs) consisting of a hydrophobic linear- or branched-alkyl chain (for 1 or 2, respectively) and a hydrophilic histidine-rich peptide of HGGGHGHGGGHG (HG12). Both peptides have a strong tendency to form nanofibrils (NFs) in aqueous media. The resulting histidine-coated NFs show a great binding affinity to Cu2+ as a fluorescence light-off sensor. Interestingly, the emission spectra of the pyrene probe show that the different supramolecular assemblies between 1 and 2 can significantly affect the binding affinity to specific metal ions. In particular, light-up fluorescent Ag+ detection of NFs of 2 through inhibition of photoinduced electron transfer (PET) was observed even at a low concentration of PA solution. As a means to determine the biological responsibility of 2 to Ag+, intracellular detection using the turn-on response was performed. A considerable enhancement of fluorescence in NF-loaded HeLa cells was observed. In addition, the NFs were used as a template scaffold for the production of Ag nanoparticles (AgNPs) with high monodispersity and stability. The NFs decorated with AgNPs are shown to possess highly effective and long-term antibacterial activity against both Gram-negative and -positive bacteria.
- Kim, Inhye,Jeong, Heon-Ho,Kim, Yong-Jae,Lee, Na-Eun,Huh, Kang-Moo,Lee, Chang-Soo,Kim, Geon Hee,Lee, Eunji
-
-
Read Online
- Preparation of enzyme-activated thapsigargin prodrugs by solid-phase synthesis
-
Since cells in solid tumors divide less rapidly than cells in the bone marrow or cells of the immune system, mitotic inhibitors often cause severe side effects when used for treatment of diseases like prostate cancer and breast cancer. One approach to overcome this problem involves attempts at developing drugs based on general cytotoxins, like calicheamicin and thapsigargin, which kill cells at all phases of the cell cycle. However, such toxins can only be used when efficient targeting to the malignant tissue is possible. In the case of thapsigargin, selectivity for tumor-associated cells is achieved by conjugating the drug to a peptide that is only cleaved in the vicinity of tumors to release the cytotoxic drug or an analog with retained activity. Solid-phase synthesis protocols were developed for preparation of three already validated prodrugs of thapsigargin: one prodrug cleavable by human kallikrein 2, one prodrug cleavable by prostate-specific antigen, and one prodrug cleavable by prostate-specific membrane antigen.
- Zimmermann, Tomas,Christensen, S?ren Br?gger,Franzyk, Henrik
-
-
Read Online
- Cell adhesive hydrogels synthesised by copolymerisation of arg-protected Gly-Arg-Gly-Asp-Ser methacrylate monomers and enzymatic deprotection
-
This work reports the synthesis of protected Gly-Arg-Gly-Asp-Ser functionalised hydrogels, which are deprotected (and activated for cell adhesion) by reaction with glutathione-S-transferase. The Royal Society of Chemistry.
- Perlin, Lynne,MacNeil, Sheila,Rimmer, Stephen
-
supporting information; experimental part
p. 5951 - 5953
(2009/05/06)
-
- A new synthesis of lysophosphatidylcholines and related derivatives. Use of p-toluenesulfonate for hydroxyl group protection
-
A new stereoselective synthesis of lysophosphatidylcholines is reported. The synthesis is based upon (1) the use of 3-p-toluenesulfonyl-sn-glycerol to provide the stereocenter for construction of the optically active lysophospholipid molecule, (2) tetrahydropyranylation of the secondary alcohol function to achieve orthogonal protection of the sn-2- and sn-3-glycerol positions, and (3) elaboration of the phosphodiester headgroup using a 2-chloro-1,3,2-dioxaphospholane/trimethylamine sequence. In the course of developing the synthesis it has been discovered that methoxyacetate displacement of the sn-3-p-toluenesulfonate yields a reactive methoxyacetyl ester, which in turn can be selectively cleaved with methanol/tertbutylamine, while the ester group at the sn-1-position remains unaffected. The sequence has been shown to be suitable for preparation of spectroscopically labeled lysophosphatidylcholines. One of these compounds was readily converted to a double-labeled mixed-chain phosphatidylcholine applicable for real-time fluorescence resonance energy transfer (FRET) assay of lipolytic enzymes. In addition, the work led to new synthetic strategies based on chemoselective manipulation of the tosyl group in the presence of other base-labile groups such as FMOC derivatives that are often used for the protection of amino and hydroxyl groups in syntheses.
- Rosseto, Renato,Bibak, Niloufar,DeOcampo, Rosemarie,Shah, Trishul,Gabrielian, Ara,Hajdu, Joseph
-
p. 1691 - 1698
(2007/10/03)
-