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Trioxacarcins and analogs: DNA-modifying compounds with potent anti-proliferative effects

The trioxacarcins are a new class of DNA-modifying natural products with potent antiproliferative effects (with subnanmolar IC70 values against lung, mammary, and CNS cancer cell lines). Trioxacarcin A, B, and C were first discovered and isolated…


  • Andrew Myers
  • Jakub Svenda
  • Nicholas Hill
  • Robert Yu
  • Daniel Smaltz
  • Thomas Magauer

Small-molecule macrocycles: Potent and selective Src kinase inhibitors

Macrocyclic compounds have unique properties that allow them to cover regions of chemical space not addressed by other small-molecule structural classes. By performing an in vitro selection screen of a broad untargeted DNA-encoded library of 13,824…


  • David Liu
  • Ralph Kleiner

Small molecule inhibitors of Ebola virus entry

Background: Human cells that are susceptible to infection by pathogenic viruses express surface membrane proteins that mediate attachment and membrane fusion activity of virus glycoproteins. There are strong structural and functional similarities…


  • Dennis Kasper
  • Kyungae Lee
  • Tao Ren
  • James Cunningham
  • Kartik Chandran

Synthesis of compounds with peptide characteristics

Although peptides have shown some promise in clinical trials as therapeutic agents, its success has largely been limited by several factors, including rapid degradation by peptidases, poor cell permeability, and a lack of binding specificity…


  • Gregory Verdine
  • Milan Chytil
  • Mary Didiuk
  • Tiffany Gierasch

Inhibitors of protein-processivity factor

Harvard investigators have discovered that Pol interacts with a processivity factor at a site that is distinct from sites of normal interaction between known Pol family members and other cellular factors. Unlike most protein-protein interactions,…


  • Donald Coen
  • James Hogle
  • Harmon Zuccola
  • Kristie Bridges
  • Carl Elkin
  • Scott Lokey

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