Literature DB >> 30540295

Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule.

Qiuye Zhao1, Tianlong Lan, Shang Su, Yu Rao.   

Abstract

Poly (ADP-ribose) polymerase-1 (PARP1) is a major member of the PARP superfamily that is involved in DNA damage signalling and other important cellular processes. Here we report the development of a small molecule targeting PARP1 based on the PROTAC strategy. In the MDA-MB-231 cell line, the representative compound 3 can induce significant PARP1 cleavage and programmed cell death.

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Year:  2019        PMID: 30540295     DOI: 10.1039/c8cc07813k

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN: 1359-7345            Impact factor:   6.222


  27 in total

1.  A MedChem toolbox for cereblon-directed PROTACs.

Authors:  Christian Steinebach; Izidor Sosič; Stefanie Lindner; Aleša Bricelj; Franziska Kohl; Yuen Lam Dora Ng; Marius Monschke; Karl G Wagner; Jan Krönke; Michael Gütschow
Journal:  Medchemcomm       Date:  2019-05-28       Impact factor: 3.597

2.  Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality.

Authors:  Philip P Chamberlain; Laura A D'Agostino; J Michael Ellis; Joshua D Hansen; Mary E Matyskiela; Joseph J McDonald; Jennifer R Riggs; Lawrence G Hamann
Journal:  ACS Med Chem Lett       Date:  2019-11-12       Impact factor: 4.345

3.  Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders.

Authors:  Shang Su; Zimo Yang; Hongying Gao; Haiyan Yang; Songbiao Zhu; Zixuan An; Juanjuan Wang; Qing Li; Sarat Chandarlapaty; Haiteng Deng; Wei Wu; Yu Rao
Journal:  J Med Chem       Date:  2019-08-02       Impact factor: 7.446

4.  The role of Trop2 in prostate cancer: an oncogene, biomarker, and therapeutic target.

Authors:  Michelle Shen; Shiqin Liu; Tanya Stoyanova
Journal:  Am J Clin Exp Urol       Date:  2021-02-15

Review 5.  Targeted protein degradation: elements of PROTAC design.

Authors:  Stacey-Lynn Paiva; Craig M Crews
Journal:  Curr Opin Chem Biol       Date:  2019-04-17       Impact factor: 8.822

6.  Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta.

Authors:  Nan Bai; Sven A Miller; Grigorii V Andrianov; Max Yates; Palani Kirubakaran; John Karanicolas
Journal:  J Chem Inf Model       Date:  2021-02-24       Impact factor: 4.956

Review 7.  Avoid the trap: Targeting PARP1 beyond human malignancy.

Authors:  Chiho Kim; Chuo Chen; Yonghao Yu
Journal:  Cell Chem Biol       Date:  2021-03-02       Impact factor: 8.116

Review 8.  Advancing targeted protein degradation for cancer therapy.

Authors:  Brandon Dale; Meng Cheng; Kwang-Su Park; H Ümit Kaniskan; Yue Xiong; Jian Jin
Journal:  Nat Rev Cancer       Date:  2021-06-15       Impact factor: 60.716

Review 9.  E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points.

Authors:  Aleša Bricelj; Christian Steinebach; Robert Kuchta; Michael Gütschow; Izidor Sosič
Journal:  Front Chem       Date:  2021-07-05       Impact factor: 5.221

Review 10.  Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation.

Authors:  Ming He; Wenxing Lv; Yu Rao
Journal:  Front Cell Dev Biol       Date:  2021-06-22
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