N-Descyclopropanecarbaldehyde Olaparib

Background Introduction

N-Descyclopropanecarbaldehyde Olaparib is a designed ligand that combines a modified Olaparib moiety—an established poly(ADP-ribose) polymerase (PARP) inhibitor—with an aldehyde group suitable for further conjugation. This advanced chemical building block is widely used in the synthesis of PROTACs (Proteolysis Targeting Chimeras) and other targeted protein degradation modalities. Olaparib-based ligands are valued for their ability to precisely engage PARP proteins, making them ideal handles for engineering next-generation therapeutics.

Mechanism

The mechanism of N-Descyclopropanecarbaldehyde Olaparib lies in its bifunctional properties. As a ligand, the Olaparib derivative retains high binding affinity for PARP, ensuring effective target engagement. The descyclopropanecarbaldehyde functionality enables efficient conjugation to a linker, which can be attached to an E3 ligase ligand, creating a complete PROTAC molecule. When used in a PROTAC construct, this conjugate brings PARP proteins in close proximity to an E3 ubiquitin ligase, leading to ubiquitination and subsequent proteasomal degradation of PARP. This process harnesses the cell's own protein quality control pathways to selectively degrade disease-relevant proteins.

Applications

N-Descyclopropanecarbaldehyde Olaparib is most commonly applied in the field of drug discovery and chemical biology for the development of PARP-targeting PROTACs. It is a powerful tool for researchers designing novel protein degraders to study PARP function, dissect resistance mechanisms in cancer, and create innovative therapeutics for oncology and beyond. Additionally, this conjugate serves as a versatile intermediate in synthesizing bifunctional molecules, facilitating the exploration of new E3 ligase-PARP pairings, and supporting the advancement of precision protein degradation technologies.

• Features a strategic ligand structure ideal for targeted PARP degradation in PROTAC research.
• Versatile functional group enables robust linker attachment, streamlining synthesis of custom PROTAC molecules.