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Discovery of a small-molecule inhibitor that traps Polθ on DNA and synergizes with PARP inhibitors.
Nat Commun. 2024 Apr 5;15(1):2862. doi: 10.1038/s41467-024-46593-1.
Nat Commun. 2024.
PMID: 38580648
Free PMC article.
PARG is essential for Polθ-mediated DNA end-joining by removing repressive poly-ADP-ribose marks.
Vekariya U, Minakhin L, Chandramouly G, Tyagi M, Kent T, Sullivan-Reed K, Atkins J, Ralph D, Nieborowska-Skorska M, Kukuyan AM, Tang HY, Pomerantz RT, Skorski T.
Vekariya U, et al.
Nat Commun. 2024 Jul 11;15(1):5822. doi: 10.1038/s41467-024-50158-7.
Nat Commun. 2024.
PMID: 38987289
Free PMC article.
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Structural basis for a Polθ helicase small-molecule inhibitor revealed by cryo-EM.
Ito F, Li Z, Minakhin L, Chandramouly G, Tyagi M, Betsch R, Krais JJ, Taberi B, Vekariya U, Calbert M, Skorski T, Johnson N, Chen XS, Pomerantz RT.
Ito F, et al.
Nat Commun. 2024 Aug 14;15(1):7003. doi: 10.1038/s41467-024-51351-4.
Nat Commun. 2024.
PMID: 39143110
Free PMC article.
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Structural Basis for Polθ-Helicase DNA Binding and Microhomology-Mediated End-Joining.
Ito F, Li Z, Minakhin L, Khant HA, Pomerantz RT, Chen XS.
Ito F, et al.
bioRxiv [Preprint]. 2024 Jun 7:2024.06.07.597860. doi: 10.1101/2024.06.07.597860.
bioRxiv. 2024.
PMID: 38895274
Free PMC article.
Preprint.
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