PARP Inhibitors for Cancer Therapy
A special issue of Cancers (ISSN 2072-6694). This special issue belongs to the section "Cancer Therapy".
Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 11637
Special Issue Editor
Interests: Epigenetics in normal development and pathogenesis; chromatin regulation; role of poly(ADP-ribose) metabolism in transcription regulation and oncogenesis; PARP-1 inhibitors in oncology; Drosophila and mammalian model organisms
Special Issue Information
Dear Colleagues,
During the past few years, the poly(ADP-ribose) polymerase 1 (PARP1) protein has become a very popular target for anti-cancer treatment. PARP1 is a constitutive component of chromatin, crucial for both DNA repair and transcription (D’Amours et al., 1999; Satoh and Lindahl 1992; and Tulin et al., 2003). PARP1 takes an active part in the DNA repair process by binding to breaks in DNA and catalyzing the transfer of ADP-ribose from NAD to the glutamic acids of protein-acceptors and the polymerization of ADP-ribose into long chains (pADPr) (D’Amours et al., 1999). Many nuclear proteins—such as histones, transcription factors, and PARP1 itself (D’Amours et al., 1999)—are acceptors of pADPr in vivo and in vitro. The activation of the PARP1 protein in chromatin in response to developmental and environmental stress is known to mediate changes in chromatin and stimulate transcription (Kim et al., 2004; Petesch and Lis 2008; and Tulin and Spradling 2003). Although the PARP1 protein is abundant in the nucleus, its localization in chromatin is not uniform and is restricted to the promoters of a specific subset of genes (Krishnakumar et al., 2008; and Tulin et al., 2002). PARP1 has been of interest since a publication in Nature described the protein’s inhibition as having synthetic lethality in BRCA-2 deficient tumor cells (Bryant et al., 2005). Several lines of evidence indicate that PARP1 deregulation is involved in the onset of malignancy. Inhibitors of PARP1 are known to obstruct tumor development. The anticancer action of PARP-1 inhibitors is generally attributed to their role in preventing PARP1-driven DNA repair in tumorigenic cells, eventually leading to cell death. In the past 40 years, many PARP1 inhibitors have been identified, and their effectiveness has been shown in the treatment of aggressive and non-responsive tumors, such as triple-negative breast cancer (-BRCA, –HER, and -PR) (Curtin 2005). This Special Issue of the open access journal “Cancers” is focused on most recent advances in “PARP Inhibitors for Cancer Therapy”.
Prof. Dr. Alexei Tulin
Guest Editor
Manuscript Submission Information
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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Cancers is an international peer-reviewed open access semimonthly journal published by MDPI.
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Keywords
- PARP-1
- PARG
- PARP-1 inhibitors
- PARP-1 roles in cancer
- poly(ADP-ribose)
- cancer models
