Prolynx LLC

Shaun Fontaine

Daniel V Santi

Brian R Hearn

Gary W Ashley

Eric L Schneider

Provided herein are releasable conjugates of inhibitors of DNA damage response suitable for use as therapeutic agents in the treatment of disease.

Conjugated inhibitors of DNA damage response

Provided are β-eliminative linkers suitable for the conjugation of small molecule, peptide, and protein and compounds comprising the linkers.

Conjugation linkers

Conjugates of topoisomerase I inhibitors linked to a macromolecule through a linkage that undergo beta elimination in situ in combination with one or more of an assessed defect in DNA damage response (DDR) in a subject bearing cancer, a cell cycle checkpoint inhibitor and/or a DDR inhibitor provides improved outcomes for cancer-bearing subjects.

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Concord, CA, United States of America

Shaun Fontaine