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
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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
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology
Result continuities
Project
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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
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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