Literature DB >> 30672063

BMN 673 (talazoparib): A potent PARP inhibitor for triple negative breast cancer with different genetic profile.

Gamze Guney Eskiler1, Gulsah Cecener2, Unal Egeli2, Berrin Tunca2.   

Abstract

The objective of the present study was to elucidate the effect of BMN 673 (talozoparib) on BRCA1 mutant (HCC1937) and wild-type (MDA-MB-231) triple negative breast cancer (TNBC). The in vitro cytotoxicity results indicated that BMN 673 had considerable inhibitory effects on HCC1937 and MDA-MB-231 cell lines by inducing apoptosis, multicaspase activity, G2/M arrest, and altering the expression levels of apoptosis-related genes (P < 0.01). Additionally, BMN 673 indicated no toxicity on MCF-10A control cells until a certain concentration and incubation time. However, BMN 673, a novel and selective poly ADP ribose polymerase inhibitor, was more potent in TNBC cells bearing BRCA1 mutant than those with wild-type BRCA1. In conclusion, our study, for the first time, demonstrated a molecular mechanism of the induction of apoptosis by BMN 673 in TNBC with different genetic profile. However, further investigations regarding the exact molecular mechanisms underlying BMN 673-inducing apoptotic death and gene-cell line associations are required.
© 2019 Wiley Periodicals, Inc.

Entities:  

Keywords:  BMN 673 (talozoparib); BRCA; apoptotic death; triple negative breast cancer

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Year:  2019        PMID: 30672063     DOI: 10.1002/jbt.22286

Source DB:  PubMed          Journal:  J Biochem Mol Toxicol        ISSN: 1095-6670            Impact factor:   3.642


  2 in total

1.  STING agonism reprograms tumor-associated macrophages and overcomes resistance to PARP inhibition in BRCA1-deficient models of breast cancer.

Authors:  Qiwei Wang; Johann S Bergholz; Liya Ding; Ziying Lin; Sheheryar K Kabraji; Melissa E Hughes; Xiadi He; Shaozhen Xie; Tao Jiang; Weihua Wang; Jason J Zoeller; Hye-Jung Kim; Thomas M Roberts; Panagiotis A Konstantinopoulos; Ursula A Matulonis; Deborah A Dillon; Eric P Winer; Nancy U Lin; Jean J Zhao
Journal:  Nat Commun       Date:  2022-05-31       Impact factor: 17.694

2.  The synergistic proapoptotic effect of PARP-1 and HDAC inhibition in cutaneous T-cell lymphoma is mediated via Blimp-1.

Authors:  Oleg Kruglov; Xuesong Wu; Sam T Hwang; Oleg E Akilov
Journal:  Blood Adv       Date:  2020-10-13
  2 in total

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