Copper‐CX‐5461: A novel liposomal formulation for a small molecule rRNA synthesis inhibitor
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Controlled Release"
DOI: 10.1016/j.jconrel.2018.07.025
Abstract: ABSTRACT CX‐5461 is currently in Phase I/II clinical trials for advanced hematologic malignancies and triple negative or BRCA‐deficient breast cancer. The compound is currently administered to patients intravenously (i.v.) at low pH (3.5) due to… read more here.
Keywords: novel; copper; formulation; copper 5461 ... See more keywords
PCAF-Mediated Histone Acetylation Promotes Replication Fork Degradation by MRE11 and EXO1 in BRCA-Deficient Cells.
Sign Up to like & getrecommendations! Published in 2020 at "Molecular cell"
DOI: 10.1016/j.molcel.2020.08.018
Abstract: Stabilization of stalled replication forks is a prominent mechanism of PARP (Poly(ADP-ribose) Polymerase) inhibitor (PARPi) resistance in BRCA-deficient tumors. Epigenetic mechanisms of replication fork stability are emerging but remain poorly understood. Here, we report the… read more here.
Keywords: mre11 exo1; deficient cells; deficient; fork ... See more keywords
The function of RAD52 N-terminal domain is essential for viability of BRCA-deficient cells
Sign Up to like & getrecommendations! Published in 2020 at "Nucleic Acids Research"
DOI: 10.1093/nar/gkaa1145
Abstract: Abstract RAD52 is a member of the homologous recombination pathway that is important for survival of BRCA-deficient cells. Inhibition of RAD52 leads to lethality in BRCA-deficient cells. However, the exact mechanism of how RAD52 contributes… read more here.
Keywords: deficient cells; brca deficient; viability brca; deficient ... See more keywords
Abstract A107: Development of polymerase theta inhibitors for precision medicine in BRCA-deficient cancers
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.targ-17-a107
Abstract: DNA polymerase theta (Polq) is important for the proliferation of BRCA-deficient cancer cells, but is dispensable for normal cell growth. Thus, Polq is widely considered to be an important new drug target for BRCA-deficient cancers,… read more here.
Keywords: medicine; brca deficient; polymerase theta; deficient cancers ... See more keywords
Abstract B39: Small Molecule Disruption of RAD52 Rings as a Mechanism for Precision Medicine in BRCA Deficient Cancers
Sign Up to like & getrecommendations! Published in 2017 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1538-8514.synthleth-b39
Abstract: Suppression of RAD52 causes synthetic lethality in BRCA deficient cells. Yet pharmacological inhibition of RAD52, which binds single-strand DNA (ssDNA) and lacks enzymatic activity, has not been demonstrated. Here, we identify the small molecule 6-hydroxy-dopa… read more here.
Keywords: rad52; medicine; brca deficient; small molecule ... See more keywords
The PRIMPOL Protein Shields Replication Forks in BRCA-Deficient Cells.
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DOI: 10.1158/2159-8290.cd-rw2019-168
Abstract: PRIMPOL shields replication forks after multiple rounds of cisplatin in BRCA-deficient cancer cells. read more here.
Keywords: shields replication; replication forks; primpol protein; protein shields ... See more keywords
In Silico Investigation of the Molecular Mechanism of PARP1 Inhibition for the Treatment of BRCA-Deficient Cancers
Sign Up to like & getrecommendations! Published in 2023 at "Molecules"
DOI: 10.3390/molecules28041829
Abstract: The protein PARP1, which plays a crucial role in DNA repair processes, is an attractive target for cancer therapy, especially for BRCA-deficient cancers. To overcome the acquired drug resistance of PARP1, PARP1 G-quadruplex (G4) identified… read more here.
Keywords: parp1 parp1; brca deficient; deficient cancers; parp1 ... See more keywords