FEN1

Blacksmith Medicines To Highlight Preclinical Oncology Data Demonstrating a Potent and Selective FEN1 Inhibitor Has Synergy with Multiple DDR Drug Classes at AACR Annual Meeting 2024

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Mercredi, avril 10, 2024
DNA replication, PARP1, Olaparib, PARG, CRISPR, PARP, HR, IC50, ADME, DNA, Chromatin, PDD, San Diego Convention Center, FEN1, DNA repair, DDR, EC50, Blacksmith, Niraparib, Erosion (morphology), AACR, ATR, Drug discovery, USP1, SAN, Pharmaceutical industry

"Using our metalloenzyme fragment-based drug discovery approach, we have identified a highly potent and selective inhibitor of FEN1 having synergies with multiple DDR drug classes that include inhibitors of PARP, PARG, USP1, and ATR."

Key Points: 
  • "Using our metalloenzyme fragment-based drug discovery approach, we have identified a highly potent and selective inhibitor of FEN1 having synergies with multiple DDR drug classes that include inhibitors of PARP, PARG, USP1, and ATR."
  • The Blacksmith fragment-based drug discovery platform identified a novel metal-binding pharmacophore that binds to the two magnesium ions in the FEN1 active site.
  • Further elaboration using fragment growth strategies resulted in highly potent and selective inhibitors.
  • Title: "Small molecule inhibitor of FEN1 nuclease utilizing a novel metal binding pharmacophore synergizes with inhibitors of USP1, PARP, PARG and ATR"

Blacksmith Medicines Announces Upcoming Presentation at AACR Annual Meeting 2024

Retrieved on: 
Mercredi, mars 6, 2024
SAN, PARG, San Diego Convention Center, Blacksmith, FEN1, USP1, AACR, ATR, PARP, Pharmaceutical industry

SAN DIEGO, March 6, 2024 /PRNewswire/ -- Blacksmith Medicines, Inc. (Blacksmith), a leading biopharma dedicated to discovering and developing medicines targeting metalloenzymes, today announced the company will present data on its oncology program targeting flap endonuclease 1 (FEN1), a structure-specific metallonuclease that cleaves 5' DNA flaps during replication and repair, at the American Association for Cancer Research (AACR) Annual Meeting 2024, taking place April 5-10 at the San Diego Convention Center, San Diego CA.

Key Points: 
  • SAN DIEGO, March 6, 2024 /PRNewswire/ -- Blacksmith Medicines, Inc. (Blacksmith), a leading biopharma dedicated to discovering and developing medicines targeting metalloenzymes, today announced the company will present data on its oncology program targeting flap endonuclease 1 (FEN1), a structure-specific metallonuclease that cleaves 5' DNA flaps during replication and repair, at the American Association for Cancer Research (AACR) Annual Meeting 2024, taking place April 5-10 at the San Diego Convention Center, San Diego CA.
  • Details of the poster presentation are as follows:
    Title: "Small molecule inhibitor of FEN1 nuclease utilizing a novel metal binding pharmacophore synergizes with inhibitors of USP1, PARP, PARG and ATR"