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

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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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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Type

J_imp - 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

Project

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Continuities

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

Publication year

2017

Confidentiality

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

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