Some pseudo-peptide analogs of thiol proteinase inhibitors were synthesized by a conventional solution method. Among them, Suc-Ala-Val-Val-Ala-psi-(CH2-NH)-Ala-pNA (peptide 1) and Suc-Ala-Val-Val-psi-(CH2-NH)-Ala-Ala-pNA (peptide 2) showed a stronger inhibitory activity compared with parent peptide such as Suc-Ala-Val-Val-Ala-Ala-pNA. In particular, peptide 2 was about 10-fold as active as the parent peptide (IC50 = 8 microM). Inserting psi-(CH2-NH) possibly makes the inhibitor less susceptible to papain and, as a result, produces more potent inhibition.
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http://dx.doi.org/10.1248/cpb.47.423 | DOI Listing |
Biochem Biophys Res Commun
November 2021
Graduate School of Life and Environmental Sciences, University of Tsukuba, Tsukuba, 305-8572, Japan. Electronic address:
Peptide nucleic acid (PNA), an artificial DNA analog, comprises a purine or pyrimidine base and a pseudo-peptide backbone instead of deoxyribose-phosphate. PNA has been found to have stronger adhesion and higher stability in binding to its complementary DNA than deoxyribose-phosphate. Thus, it could serve as an agent for gene modulation, demonstrating potential in antisense therapy, molecular diagnostics, and nanotechnology.
View Article and Find Full Text PDFMethods Mol Biol
March 2021
Department of Chemistry, Life Sciences and Environmental Sustainability, Parma University, Parma, Italy.
The importance of peptide nucleic acids (PNAs) for alteration of gene expression is nowadays firmly established. PNAs are characterized by a pseudo-peptide backbone composed of N-(2-aminoethyl)glycine units and have been found to be excellent candidates for antisense and antigene therapies. Recently, PNAs have been demonstrated to alter the action of microRNAs and thus can be considered very important tools for miRNA therapeutics.
View Article and Find Full Text PDFQ J Nucl Med Mol Imaging
December 2020
Division of Oncology, Department of Internal Medicine, Medical University of Graz, Graz, Austria.
In recent years, the introduction of theranostic twins for specific diagnosis and treatment in patients with neuroendocrine tumors became a nuclear medicine success story. Cu/F labeled prostate specific membrane antigen (PSMA) for molecular imaging with PET-CT and peptide radioligand therapy with Lu labeled PSMA inhibitors will favorably become the next theranostic twins in nuclear medicine history. Ga/ Cu/F PSMA PET/CT detects metastatic prostate cancer with high diagnostic sensitivity and specificity.
View Article and Find Full Text PDFBioorg Med Chem
February 2020
Department of Pharmacy and Pharmaceutical Sciences, "A. Moro" University of Bari, Bari, Italy. Electronic address:
Matrix metalloproteinases (MMPs) are a large family of zinc-dependent endoproteases known to exert multiple regulatory roles in tumor progression and invasiveness. This encouraged over the years the approach of MMP, and particularly MMP-2, targeting for anticancer treatment. Early generations of MMP inhibitors, based on aspecific zinc binding groups (ZBGs) assembled on (pseudo)peptide scaffolds, have been discontinued due to the clinical emergence of toxicity and further drawbacks, giving the way to inhibitors with alternative zinc-chelator moieties or not binding the catalytic zinc ion.
View Article and Find Full Text PDFNanomedicine
August 2019
Institute for Diagnostic and Interventional Radiology, Jena University Hospital-Friedrich Schiller University Jena, Jena, Germany. Electronic address:
In this paper we show that conjugation of magnetic nanoparticles (MNPs) with Gemcitabine and/or NucAnt (N6L) fostered their internalization into pancreatic tumor cells and that the coupling procedure did not alter the cytotoxic potential of the drugs. By treating tumor cells (BxPC3 and PANC-1) with the conjugated MNPs and magnetic hyperthermia (43 °C, 60 min), cell death was observed. The two pancreatic tumor cell lines showed different reactions against the combined therapy according to their intrinsic sensitivity against Gemcitabine (cell death, ROS production, ability to activate ERK 1/2 and JNK).
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