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Journal of Environmental Pathology, Toxicology and Oncology

Publication de 4  numéros par an

ISSN Imprimer: 0731-8898

ISSN En ligne: 2162-6537

The Impact Factor measures the average number of citations received in a particular year by papers published in the journal during the two preceding years. 2017 Journal Citation Reports (Clarivate Analytics, 2018) IF: 2.4 To calculate the five year Impact Factor, citations are counted in 2017 to the previous five years and divided by the source items published in the previous five years. 2017 Journal Citation Reports (Clarivate Analytics, 2018) 5-Year IF: 2.8 The Immediacy Index is the average number of times an article is cited in the year it is published. The journal Immediacy Index indicates how quickly articles in a journal are cited. Immediacy Index: 0.5 The Eigenfactor score, developed by Jevin West and Carl Bergstrom at the University of Washington, is a rating of the total importance of a scientific journal. Journals are rated according to the number of incoming citations, with citations from highly ranked journals weighted to make a larger contribution to the eigenfactor than those from poorly ranked journals. Eigenfactor: 0.00049 The Journal Citation Indicator (JCI) is a single measurement of the field-normalized citation impact of journals in the Web of Science Core Collection across disciplines. The key words here are that the metric is normalized and cross-disciplinary. JCI: 0.59 SJR: 0.429 SNIP: 0.507 CiteScore™:: 3.9 H-Index: 49

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Inhibition of the p53 Y220C Mutant by 1-Hydroxy-2- Methylanthraquinone Derivatives: A Novel Strategy for Cancer Therapy

Volume 35, Numéro 4, 2016, pp. 355-364
DOI: 10.1615/JEnvironPatholToxicolOncol.2016012256
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RÉSUMÉ

Y220C, a substitution mutation in p53, causes major structural changes in the protein and is known to form a new protein cavity. This cavity is reckoned to accommodate small drug candidates that may play a key role in cancer treatment. Present study was aimed at determining a drug candidate that could inhibit the mutant p53 based on structural drug rationale. Docking of mutated p53 was performed to determine the drug of choice from the derivatives of 1-hydroxy-2- methylanthraquinone exhibiting anti-cancer properties. The cavity had been tested for identification of an accurate position vector for molecular docking studies using structure based drug design. The docked structure was validated using discovery studio 3.5. The best choice of two molecules were obtained by docking in specific solvent for 6 nanoseconds at a temperature of 310 K. Out of a library of compounds, acetamido-2-carboxy-4-dimethylamino-2- hydroxybenzophenone satisfied the ADMET and was found to be a potential target for mutant p53. This ligand binds at the active site of the protein. Results of present study offer a rationale of the lead ligands that can rescue oncogenic p53 by targeting the mutation site. Therefore, it is suggestive that small molecules may serve as an effective and novel anti-cancer drug.

CITÉ PAR
  1. Li Yang, Wang Zhuoyi, Chen Yuchen, Petersen Robert B., Zheng Ling, Huang Kun, Salvation of the fallen angel: Reactivating mutant p53, British Journal of Pharmacology, 176, 7, 2019. Crossref

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