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Small molecule inhibitors of DNA-PK for tumor sensitization to anticancer therapy

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11150%2F17%3A10362727" target="_blank" >RIV/00216208:11150/17:10362727 - isvavai.cz</a>

  • Result on the web

    <a href="http://www.jpp.krakow.pl/journal/archive/06_17/pdf/337_06_17_article.pdf" target="_blank" >http://www.jpp.krakow.pl/journal/archive/06_17/pdf/337_06_17_article.pdf</a>

  • DOI - Digital Object Identifier

Alternative languages

  • Result language

    angličtina

  • Original language name

    Small molecule inhibitors of DNA-PK for tumor sensitization to anticancer therapy

  • Original language description

    The most sensitive cell structure - a DNA molecule, is the common target of cancer therapy. DNA damage response (controlled by enzymes from the phosphatidylinositol 3-kinase-related kinases family - PIKK) presents many encouraging targets for improving both conventional cytotoxic anticancer therapy and individualized monotherapy. DNA-dependent protein kinase (DNA-PK) is a member of the PIKK superfamily and plays an important role in the detection and repair of DNA double-strand breaks via the non-homologous end-joining pathway. The ability of cancer cells to repair DNA damage is an important element determining their sensitivity to radio-or chemo-therapy. The overactivation of DNA-PK in cancers can result in resistance to anticancer therapy. The inhibition of DNA-PK is a very promising target in anticancer research. However, the specific DNA-PK inhibitors currently known are limited by poor solubility and high metabolic lability in vivo, leading to a short serum half-life. Construction of new compounds based on existing drugs is the most important strategy to improve drug efficacy, pharmacokinetic parameters and to reduce toxicity. This review will describe small molecule inhibitors and summarize their efficacy in synergizing radio-and chemotherapy in vitro.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10608 - Biochemistry and molecular biology

Result continuities

  • Project

  • Continuities

    S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2017

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Journal of Physiology and Pharmacology

  • ISSN

    0867-5910

  • e-ISSN

  • Volume of the periodical

    68

  • Issue of the periodical within the volume

    3

  • Country of publishing house

    PL - POLAND

  • Number of pages

    8

  • Pages from-to

    337-344

  • UT code for WoS article

    000408565000002

  • EID of the result in the Scopus database

    2-s2.0-85027709278