排序方式: 共有15条查询结果,搜索用时 15 毫秒
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Dr. Cristina Tintori Ilaria Laurenzana Francesco La Rocca Dr. Federico Falchi Prof. Fabio Carraro Alba Ruiz Prof. José A. Esté Miroslava Kissova Dr. Emmanuele Crespan Prof. Giovanni Maga Prof. Mariangela Biava Dr. Chiara Brullo Prof. Silvia Schenone Prof. Maurizio Botta 《ChemMedChem》2013,8(8):1353-1360
Hematopoietic cell kinase (Hck) is a member of the Src family of non‐receptor protein tyrosine kinases. High levels of Hck are associated with drug resistance in chronic myeloid leukemia. Furthermore, Hck activity has been connected with HIV‐1. Herein, structure‐based drug design efforts were aimed at identifying novel Hck inhibitors. First, an in‐house library of pyrazolo[3,4‐d]pyrimidine derivatives, which were previously shown to be dual Abl and c‐Src inhibitors, was analyzed by docking studies within the ATP binding site of Hck to select the best candidates to be tested in a cell‐free assay. Next, the same computational protocol was applied to screen a database of commercially available compounds. As a result, most of the selected compounds were found active against Hck, with Ki values ranging from 0.14 to 18.4 μM , confirming the suitability of the computational approach adopted. Furthermore, selected compounds showed an interesting antiproliferative activity profile against the human leukemia cell line KU‐812, and one compound was found to block HIV‐1 replication at sub‐toxic concentrations. 相似文献
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Cover Feature: Identification of Broad‐Spectrum Dengue/Zika Virus Replication Inhibitors by Functionalization of Quinoline and 2,6‐Diaminopurine Scaffolds (ChemMedChem 14/2018) 下载免费PDF全文
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Arioli F Borrelli S Colombo F Falchi F Filippi I Crespan E Naldini A Scalia G Silvani A Maga G Carraro F Botta M Passarella D 《ChemMedChem》2011,6(11):2009-2018
N‐[2‐Methyl‐5‐(triazol‐1‐yl)phenyl]pyrimidin‐2‐amine derivatives were synthesized and evaluated in vitro for their potential use as inhibitors of Bcr‐Abl. The design is based on the bioisosterism between the 1,2,3‐triazole ring and the amide group. The synthesis involves a copper(I)‐catalyzed azide–alkyne cycloaddition (CuAAC) as the key step, with the exclusive production of anti‐(1,4)‐triazole derivatives. One of the compounds obtained shows general activity similar to that of imatinib; in particular, it was observed to be more effective in decreasing the fundamental function of cdc25A phosphatases in the K‐562 cell line. 相似文献
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Juliana Nunes Lucatto Rosana Aparecida da Silva‐Buzanello Saraspathy Naidoo Terroso Gama de Mendona Tassyana Crespan Lazarotto Jorge Leonardo Sanchez Evandro Bona Deisy Alessandra Drunkler 《International Journal of Dairy Technology》2020,73(1):144-156
Lactobacillus acidophilus or Bifidobacterium animalis subsp. lactis Bb‐12 and green banana pulp were used in order to obtain potentially probiotic and prebiotic yoghurts, which were compared over a 45‐day storage period. Goat milk yoghurts demonstrated probiotic effects up to 45 days of storage. Cow milk yoghurts produced with B. animalis subsp. lactis Bb‐12 showed a probiotic effect reduction during the storage period (1.74 log CFU/g). The type of milk affected the yoghurts’ chemical and physicochemical properties. Sensory acceptance was also affected, where cow milk yoghurts were better accepted than goat milk ones. 相似文献
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Maria Dede Silvia Napolitano Anna Melati Valentina Pirota Giovanni Maga Emmanuele Crespan 《International journal of molecular sciences》2021,22(10)
Ribonucleotides misincorporated in the human genome are the most abundant DNA lesions. The 2′-hydroxyl group makes them prone to spontaneous hydrolysis, potentially resulting in strand breaks. Moreover, their presence may decrease the rate of DNA replication causing replicative fork stalling and collapse. Ribonucleotide removal is initiated by Ribonuclease H2 (RNase H2), the key player in Ribonucleotide Excision Repair (RER). Its absence leads to embryonic lethality in mice, while mutations decreasing its activity cause Aicardi–Goutières syndrome. DNA geometry can be altered by DNA lesions or by peculiar sequences forming secondary structures, like G-quadruplex (G4) and trinucleotide repeats (TNR) hairpins, which significantly differ from canonical B-form. Ribonucleotides pairing to lesioned nucleotides, or incorporated within non-B DNA structures could avoid RNase H2 recognition, potentially contributing to genome instability. In this work, we investigate the ability of RNase H2 to process misincorporated ribonucleotides in a panel of DNA substrates showing different geometrical features. RNase H2 proved to be a flexible enzyme, recognizing as a substrate the majority of the constructs we generated. However, some geometrical features and non-canonical DNA structures severely impaired its activity, suggesting a relevant role of misincorporated ribonucleotides in the physiological instability of specific DNA sequences. 相似文献
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Dr. Maria Grazia Martina Dr. Ilaria Vicenti Dr. Lisa Bauer Dr. Emmanuele Crespan Dr. Enrico Rango Dr. Adele Boccuto Dr. Noemi Olivieri Prof. Matteo Incerti Marleen Zwaagstra Marika Allodi Simona Bertoni Prof. Elena Dreassi Prof. Maurizio Zazzi Prof. Frank J. M. van Kuppeveld Prof. Giovanni Maga Prof. Marco Radi 《ChemMedChem》2021,16(23):3548-3552