ChemInform Abstract: Advances in Automatic, Manual and Microwave‐Assisted Solid‐Phase Peptide Synthesis

Sabatino, Giuseppina; Papini, Anna Maria

doi:10.1002/chin.200911263

Cited by 25 publications

(30 citation statements)

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“…Peptides were synthesized as one polypeptide with TAT 47-57 carrier in the following order: N-terminus-TAT-spacer (Gly-Gly) -cargo (corresponding to regions 108,109, 110, 111, 112 or 113)-C-terminus. The C-termini of the peptides were modified to C(O)-NH2 using Rink Amide AM resin to increase stability (Sabatino and Papini, 2008). Peptides were analyzed by analytical reverse-phase high-pressure liquid chromatography (RP-HPLC) (Shimadzu, MD, USA) and matrix-assisted laser desorption/ionization (MALDI) mass spectrometry (MS) and purified by preparative RP-HPLC (Shimadzu, MD, USA).…”

Section: Peptide Synthesismentioning

confidence: 99%

Novel Drp1 inhibitor diminishes aberrant mitochondrial fission and neurotoxicity

Qvit

et al. 2012

Journal of Cell Science

344

409

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SummaryExcessive mitochondrial fission is associated with the pathology of a number of neurodegenerative diseases. Therefore, inhibitors of aberrant mitochondrial fission could provide important research tools in addition to potential leads for drug development. Using a rational approach, we designed a novel and selective peptide inhibitor, P110, of excessive mitochondrial fission. P110 inhibits Drp1 enzyme activity and blocks Drp1/Fis1 interaction in vitro and in cultured neurons, whereas it has no effect on the interaction between Drp1 and other mitochondrial adaptors, as demonstrated by co-immunoprecipitation. Furthermore, using a model of Parkinson's disease (PD) in culture, we demonstrated that P110 is neuroprotective by inhibiting mitochondrial fragmentation and reactive oxygen species (ROS) production and subsequently improving mitochondrial membrane potential and mitochondrial integrity. P110 increased neuronal cell viability by reducing apoptosis and autophagic cell death, and reduced neurite loss of primary dopaminergic neurons in this PD cell culture model. We also found that P110 treatment appears to have minimal effects on mitochondrial fission and cell viability under basal conditions. Finally, P110 required the presence of Drp1 to inhibit mitochondrial fission under oxidative stress conditions. Taken together, our findings suggest that P110, as a selective peptide inhibitor of Drp1, might be useful for the treatment of diseases in which excessive mitochondrial fission and mitochondrial dysfunction occur.

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Section: Peptide Synthesismentioning

confidence: 99%

Novel Drp1 inhibitor diminishes aberrant mitochondrial fission and neurotoxicity

Qvit

et al. 2012

Journal of Cell Science

344

409

View full text Add to dashboard Cite

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“…Structurally, the collagen-mimetic peptides contain repeat units of the amino acid triad Gly-Pro-Hyp (GPO). For these studies, we prepared homo-trimeric collagen-mimetic peptides containing the cleavage site for MMP-9 employing a microwave-assisted, solid-phase peptide synthesizer (37). The peptides have the general structure of CH 3 (CH 2 ) 16 CONH-GPQGIAGQR(GPO) n GG-COOH, where the MMP-9 cleavage site is the peptide bond connecting Gly and Ile.…”

Section: Resultsmentioning

confidence: 99%

Release of Liposomal Contents by Cell-Secreted Matrix Metalloproteinase-9

et al. 2009

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Liposomes have been widely used as a drug delivery vehicle and currently, more than 10 liposomal formulations are approved by the Food and Drug Administration for clinical use. However, upon targeting, the release of the liposome-encapsulated contents is usually slow. We have recently demonstrated that contents from appropriately-formulated liposomes can be rapidly released by the cancer-associated enzyme matrix metalloproteinase-9 (MMP-9). Herein, we report our detailed studies to optimize the liposomal formulations. By properly selecting the lipopeptide, the major lipid component and their relative amounts, we demonstrate that the contents are rapidly released in the presence of cancer-associated levels of recombinant human MMP-9. We observed that the degree of lipid mismatch between the lipopepides and the major lipid component profoundly affects the release profiles from the liposomes. By utilizing the optimized liposomal formulations, we also demonstrate that cancer cells (HT-29) which secrete low levels of MMP-9 failed to release significant amount of the liposomal contents. Metastatic cancer cells (MCF7) secreting high levels of the enzyme rapidly release the encapsulated contents from the liposomes.

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“…Cecropin is known for exhibiting strong antimicrobial activities, especially against Gram-positive bacteria (4,11). Cecropin D was chemically synthesized by standard Merrifield solid-phase peptide synthesis (14,17), purified by reversephase high-performance liquid chromatography (RP-HPLC), and controlled by electrospray ionization mass spectrometry (ESI-MS) (see Fig. S1A and B in the supplemental material).…”

Section: Vol 77 2011mentioning

confidence: 99%