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Diphenylpyrazoles as replication protein a inhibitors.

Waterson AG, Kennedy JP, Patrone JD, Pelz NF, Feldkamp MD, Frank AO, Vangamudi B, Souza-Fagundes EM, Rossanese OW, Chazin WJ, Fesik SW
ACS Med Chem Lett 6 140-5 (2015)
Related entries: 4r4c, 4r4i, 4r4q, 4r4t

Cited: 8 times
EuropePMC logo PMID: 25699140

Abstract

Replication Protein A is the primary eukaryotic ssDNA binding protein that has a central role in initiating the cellular response to DNA damage. RPA recruits multiple proteins to sites of DNA damage via the N-terminal domain of the 70 kDa subunit (RPA70N). Here we describe the optimization of a diphenylpyrazole carboxylic acid series of inhibitors of these RPA-protein interactions. We evaluated substituents on the aromatic rings as well as the type and geometry of the linkers used to combine fragments, ultimately leading to submicromolar inhibitors of RPA70N protein-protein interactions.

Articles - 4r4o mentioned but not cited (1)

  1. Diphenylpyrazoles as replication protein a inhibitors. Waterson AG, Kennedy JP, Patrone JD, Pelz NF, Feldkamp MD, Frank AO, Vangamudi B, Souza-Fagundes EM, Rossanese OW, Chazin WJ, Fesik SW. ACS Med Chem Lett 6 140-145 (2015)


Reviews citing this publication (4)

  1. DNA repair targeted therapy: The past or future of cancer treatment? Gavande NS, VanderVere-Carozza PS, Hinshaw HD, Jalal SI, Sears CR, Pawelczak KS, Turchi JJ. Pharmacol Ther 160 65-83 (2016)
  2. Progress in discovery of small-molecule modulators of protein-protein interactions via fragment screening. Magee TV. Bioorg Med Chem Lett 25 2461-2468 (2015)
  3. Recent advancements in the discovery of protein-protein interaction inhibitors of replication protein A. Patrone JD, Waterson AG, Fesik SW. Medchemcomm 8 259-267 (2017)
  4. OB-Folds and Genome Maintenance: Targeting Protein-DNA Interactions for Cancer Therapy. Par S, Vaides S, VanderVere-Carozza PS, Pawelczak KS, Stewart J, Turchi JJ. Cancers (Basel) 13 3346 (2021)

Articles citing this publication (3)



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